Novel natural system with technical lubricating effect

Abstract

The present invention relates to systems with emergent properties, in particular suitable for use as lubricants, for example for the manufacture of tablets and capsules, and as technical aids for the operation of processing machines for the preparation of said materials, and provides novel natural systems with lubricating action, suitable for use as lubricants, 100% of natural origin, compositions containing them, their uses and methods of preparation. In particular, the present invention provides novel natural systems with lubricating activity, suitable for use as lubricants, 100% consisting of products of natural origin, not chemically synthesized, consisting of powders of seeds-containing fruits or seeds, wherein said fruits or seeds are characterized by the presence of fatty acids, optionally in combination with natural gums, to replace the common chemical origin powder lubricants.

Description

Technical Field

[0001] This invention relates to systems with emergent properties, particularly systems suitable for use as lubricants, for example, in the manufacture of tablets and capsules, and as technical aids for the operation of processing machines used to prepare said materials. It provides novel natural systems of 100% natural origin with lubricating activity (suitable for use as lubricants), compositions comprising them, uses of said lubricants, and methods of preparation. Specifically, the invention provides novel natural systems of lubricating activity (suitable for use as lubricants) composed of 100% naturally sourced (not chemically synthesized) products consisting of powders of seeds or fruits containing seeds, wherein said fruits or seeds are characterized by the presence of fatty acids, optionally combined with natural gums, to replace commonly used chemically sourced powdered lubricants. Background Technology

[0002] Lubricants are substances that prevent the powder to be compressed from adhering to the surface of the punch die, reduce friction, and facilitate the ejection of tablets from the die. These raw materials can be used directly in the mixture and / or outside the formulation (technical adjuvants) to obtain compliant tablets or capsules.

[0003] The lubricating effect and effectiveness of a lubricant (whether used as an additive, a technical aid, or both) can be evaluated, for example, by monitoring the tablet release force detected throughout the compression process.

[0004] Furthermore, the fundamental properties of powders (particle size and distribution or particle size and specific surface area) and their derived properties (bulk density and flowability) play an important role in obtaining compliant solid pharmaceutical forms.

[0005] In conventional manufacturing processes for tablets and capsules of plant-derived products, chemically derived stearates are typically added to lubricate the mixture. Alternatively, stearates are intended as a technical aid for the operation of processing machinery, in which case they are added externally, leaving traces of the aid on the product surface.

[0006] Magnesium stearate is one of the most widely used lubricants in the world, obtained by reacting magnesium chloride or magnesium oxide with stearic acid in a high-temperature aqueous environment. Prolonged mixing time results in the formation of a lamellar layer that masks the active ingredients, effectively isolating them and delaying their bioavailability.

[0007] Therefore, there is a need to provide mixtures of stearates that can avoid the use of chemically derived stearates as formulation ingredients and as technical aids in conventional manufacturing processes for capsules and tablets of naturally derived products, thereby obtaining 100% natural products.

[0008] Document JP2007320856 describes a lubricant utilizing the properties of fats and oils present in plant raw materials (particularly soybeans), document US2020 / 170936 describes a rice husk-based lubricant, and document KR2020 / 0009128 describes a cocoa powder-based lubricant. The types and amounts of plant fats that must be present in the lubricants to provide technical effects comparable to magnesium stearate are not reported in the literature. Although some tablet lubricants composed of natural substances (e.g., seed derivatives and / or fats from certain plants) have begun to be described in the prior art, it appears that there is no lubricant technically comparable to magnesium stearate composed of 100% natural ingredients. Attached Figure Description

[0009] Figure 1 A target curve for release force [N] was used to define the range of values ​​attributable to the release force required to ensure the tablet's release from the punch (Experimental 4, Example Section). Given a standard powder mixture (also known as a standard mixture) consisting of microcrystalline cellulose and calcium carbonate or limestone powder in a 4:1 weight ratio, performance tests were conducted using a composition containing said mixture and 1% magnesium stearate (w / w of the composition) at different mixing times, and the release force of the tablets was evaluated. The mixing time was correlated with the obtained release force to construct the target curve. Figure 1 The measurements performed allowed for the determination of the range of extrusion forces applied by magnesium stearate, which could be used as a reference for comparative testing. In particular, two parameters were determined: the mixing time at which the mixture obtained the lowest demolding force value, equal to 5', and the mixing time at which the mixture obtained the highest demolding force value, equal to 30'.

[0010] Based on the quality of the resulting tablets, the effective release force is considered to be in the range of 0.05 to 0.50 N.

[0011] Figure 2 Comparison of release forces of different seed-containing fruit powders (Experimental 5, Examples).

[0012] Compression tests were conducted using compositions consisting of a standard mixture according to this specification, with the addition of seed-containing fruit powders of caraway, fennel, and cumin, each fruit powder present in a percentage relative to the total weight of the composition such that the amount of fatty acids contained therein is approximately equivalent to the amount of fatty acids present in 1% magnesium stearate in the same formulation, calculated according to the desired percentage of fatty acids in Table 1 of the specification. Specifically, demolding force was evaluated in compositions containing fruit powders composed of seeds (achenes) of fennel, caraway, and cumin, and the standard mixture described above (microcrystalline cellulose and calcium carbonate in a weight ratio of 4:1). Results were obtained using the compositions (standard mixture and seed-containing fruit powders) with the following weight percentages: fruit powder containing fennel seeds 4.21% relative to the total weight of the composition, fruit powder containing caraway seeds 3.75% relative to the total weight of the composition, and fruit powder containing caraway seeds 3.91% relative to the total weight of the composition, using the same optimal mixing time as magnesium stearate, equal to 5 minutes.

[0013] The release force of the tablets was then analyzed and compared with parameters obtained from the compression of a standard mixture (composed of microcrystalline cellulose and calcium carbonate or limestone powder in a 4:1 weight ratio, relative to the total weight of the formulation (standard mixture + stearate), which also contained 1% magnesium stearate by weight) and the maximum experimental push force of other products, with a generally accepted value corresponding to 0.5 N. The control was obtained from... Figure 1 The compositions described herein are indicated by mixing times of 5 and 30 minutes.

[0014] All pressing tests were conducted using the same operating parameters. Although the demolding force measured in all tests was less than 0.5 N, according to Figure 1 The measured values ​​of magnesium stearate tended to the upper limit set in the study (i.e., 0.5N).

[0015] Figure 3Release force of mixtures comprising seed and / or fruit powder and gum arabic (also known as gum arabic) (Experimental Part 6 Examples). A system consisting of powdered gum arabic in a 7:1 ratio and seeded fruit powders of fennel, caraway, and cumin, or a mixture of said seeded fruit powders, was premixed. The resulting mixture was added to the above-described standard mixture at a content of 32.34% (4.21% of seeded fruit powders of fennel, caraway, and cumin in a 1:1:1 ratio) and 28.13% gum arabic relative to the total weight of the resulting composition (standard mixture + mixture of seeded fruit powder and gum arabic). The release force values ​​obtained compared to the control (standard mixture and 1% by weight of magnesium stearate) and the above-described composition comprising a single seeded fruit in powder form (4.21% fennel, 3.75% caraway, and 3.91% cumin) are reported below. Under the same operating conditions, the composition consisting of a standard mixture, gum arabic, and several types of seeded fruit (fennel, caraway, or cumin) powders produced a lower release force value compared to a composition consisting of a standard mixture and a single type of seeded fruit (fennel, caraway, or cumin) powder, and also compared to a composition consisting of a standard mixture and magnesium stearate.

[0016] Figure 3 The precise values ​​obtained from the experiments shown are displayed in Table 4 of Experiment 6.

[0017] Figure 4 Distribution curves obtained by sieving (Experiment 7, Example 1). A mixture of gum arabic and fruit powder containing fennel seeds in a 5:1 ratio was granulated with water and sieved using a vibrating sieve. Particle size analysis of the obtained particles was performed, and the results are shown below. Figure 4 As shown in Table 8, the characteristics of the particle properties are represented.

[0018] Figure 5 Comparison of release forces (Experiment 7, Example Section).

[0019] The obtained release force values ​​are reported compared to those obtained for the control group as defined above. The "gum-fennel" pre-granulation system shows a similar performance to... Figure 3 The composition varies in different proportions. The pre-granules consist of 2% by weight of fruit powder containing anise seeds and 10% by weight of gum arabic, totaling 12% by weight in the composition containing the granules and the standard mixture. The figure shows that this system allows for the production of tablets without the need for the addition or external addition of magnesium stearate to the formulation. Furthermore, the amount added to the mixture by the processing system is... Figure 3 The amount used in the composition is much lower, thus indicating that even less than Figure 3 The amounts of gum arabic and seed-containing fruit powder tested in the middle were also sufficient.

[0020] Figure 4 The release force of the preparticles described in the paper was also compared with that of the fraction with the same amount of 355 μm particle size.

[0021] Pre-particles and their fractions have comparable lubrication properties.

[0022] Figure 6 Global plot of release forces (Experiment 6, Examples, Table 5). All release force values ​​for the compositions described in Table 5 are reported. The plot shows a completely unexpected synergistic effect in compositions with natural lubrication systems consisting of mixtures of different seed-containing fruit powders, and in compositions with natural lubrication systems consisting of gum arabic and one or more seed-containing fruit powders, with the latter being even more effective.

[0023] In this specification, the term "ICCarr index" refers to a dimensionless physical quantity that characterizes the compressibility and formability of powder or granular materials.

[0024] In this specification, the term "IHHausner index" refers to the ratio between the density of the powder after pressing and its initial density. This parameter can be used to evaluate the flowability of powders or powder mixtures.

[0025] The term "bulk density" in this specification refers to the powder density taking into account both the space between and within particles.

[0026] In this specification, the term "tap density" refers to the density value after filling. The terms "Dv10," "Dv50," "Dv90," and "SPAN" refer to:

[0027] -Dv10: The particle size distribution value for 10% of the volume is lower than the indicated value.

[0028] -Dv50: 50% of the volume has a particle size distribution value below the indicated value. Average distribution volume value.

[0029] -Dv90: 90% of the volume has a particle size distribution value below the indicated value.

[0030] -SPAN: Use the following formula get.

[0031] The value corresponding to 1 corresponds to a Gaussian distribution.

[0032] The term "granulation" refers to the process of converting a substance or material into granules for final use or further processing.

[0033] The term "pressing" refers to the production process aimed at obtaining tablets mechanically.

[0034] The term "release force" refers to an experimental parameter, expressed in [N], that allows for the measurement of tablet adhesion to the punch. For the purposes of this specification, an acceptable maximum release force is considered to be equal to 0.5 N; exceeding this value will result in the observation of friction-related technical problems such as tablet adhesion to the machine punch, sticking, and descaling. The value of the release force is an indicator of the effectiveness of the lubrication system used; in particular, a good lubricant can reduce the release force value to below 0.1 N. The term "system with emergent properties" in this specification refers to a system exhibiting emergent behavior, in this case, a mixture or composition, i.e., the individual reagents constituting the mixture produce more complex behavior when operated in a given environment because they are in the form of a system. These properties are not easily predicted in themselves and represent the subsequent evolutionary level of the system. Complex emergent behavior is not a property of the individual entities; in fact, to obtain the observed emergent behavior, the entire system must be implemented.

[0035] In this invention, 100% natural means that a substance defined as 100% natural contains no components obtained from chemical synthesis, but only components of natural origin, particularly products derived from plants. The term "active ingredient" in this specification refers to a substance having specific biological activity, including all substances that exert specific activity in formulations, such as having therapeutic or preventative effects.

[0036] In this specification, the standard mixture of powders, also known as the standard mixture, is a mixture consisting of microcrystalline cellulose and calcium carbonate or limestone powder in a weight ratio of 4:1, and a lubricant or system (the variable content of which depends on the type of lubricant).

[0037] In this specification, the term "physiologically active system" refers to a system whose components interact structurally and functionally to determine emergent properties. The described system is physiologically active because it is able to interact with the organism through multi-level mechanisms without artificially altering a single and specific function. In this specification, the term "natural raw material in powder form" refers to natural raw materials (e.g., seeds, seed-containing fruits, fruits) that have been dried and pulverized by a grinding process.

[0038] In this specification, the term "relative humidity" refers to the ratio of the density of vapor contained in a substance to the density of saturated vapor at the substance's temperature. It is an indicator of the amount of water vapor contained in a substance.

[0039] In this specification, the term "formulation preparation" refers to a mixture of an active ingredient and optional excipients, colorants, flavoring agents, and carriers, used to prepare a product in capsule or tablet form. Those skilled in the art will readily identify a formulation preparation, and it is any formulation that typically uses magnesium stearate as a lubricant.

[0040] A fruit containing seeds refers to the whole fruit, and therefore includes the seeds contained within it. Summary of the Invention

[0041] In order to create products made entirely of natural substances and therefore not chemically synthesized, the authors of this invention sought to identify natural systems with lubricating technical activity, thus suitable for use as lubricants in tablet and capsule manufacturing processes and for machinery used in such manufacturing, wherein such systems exhibit different technical effects, for example, in terms of effectiveness, relative to the roles played by their individual components. To obtain a lubricant composed of 100% natural substances and possessing effectiveness comparable to magnesium stearate, the inventors have verified the lubricating properties of various seed-containing fruit powders or seed powders containing fatty acids with similar chain lengths to magnesium stearate in tablet or capsule manufacturing, and evaluated the lubricating activity of these powders compared to magnesium stearate. Grinding seed-containing fruits or seeds allows these materials to be converted into powder and efficiently mixed into a 100% natural product formulation. Furthermore, the grinding process allows lipid components to be exposed, which can effectively interact with the powder or particles of the product's active ingredients, thereby achieving effective lubrication.

[0042] This efficient contact allows the resulting mixture to be converted into capsules and / or tablets, ensuring the functionality of the technology used for these conversions, thereby avoiding the use of chemically derived stearates as formulation ingredients and technical aids in conventional manufacturing processes for capsules and tablets of naturally derived products, thus allowing for the acquisition of 100% natural products.

[0043] Furthermore, the authors of this invention have unexpectedly discovered that natural gums, such as gum arabic, even when used as the sole lubricant or as a component of a lubricant, also have a lubricating effect in the preparation of tablets and capsules.

[0044] like Figure 2 As shown, due to the effectiveness of magnesium stearate in lubrication, from Figure 1 The optimal mixing time obtained from the curves showed a release force value below 0.1 N, while the seed-containing fruit powder showed a release force value close to the maximum acceptable release force limit for the purposes of this invention at the same mixing time considered optimally controlled at t min. Although all individual seed-containing fruit powders or seed powders tested provided “acceptable” lubricating activity, the excellent release force value observed with magnesium stearate could not be obtained.

[0045] Surprisingly, the authors found that appropriate mixtures of seed-containing fruit powders or seed powders exhibit a synergistic effect and provide a system with emergent properties, in which lubricating activity is unexpectedly significantly superior to that of a single powder, and this effectiveness is even greater when one or more seed-containing fruit powders are mixed with plant gums / powders, providing a 100% natural lubricating system (suitable for use as a lubricant), even better than magnesium stearate. Furthermore, the authors of this invention unexpectedly found that the same plant gums themselves can provide effective lubricating activity in the manufacture of capsules and tablets. In other words, the authors of this invention unexpectedly found that the combination of plant gums with specific seed-containing fruit powders or seed powders, or optionally with different seed-containing fruit or seed powders combined with plant gums (also referred to herein as natural gums), provides a system with emergent properties of excellent lubricating properties, comparable to (if not inferior to) those exhibited by one of the most common and effective synthetic chemical lubricants used in the manufacture of tablets and capsules (i.e., magnesium stearate) under its optimal use conditions (i.e., a mixing time of 5 minutes) (see...). Figure 6 ).

[0046] Therefore, the system of the present invention, presented herein in the form of a mixture or composition, provides an excellent lubricant suitable for manufacturing 100% natural formulations.

[0047] Therefore, the object of the present invention is as follows: - a mixture consisting of one or more seed-bearing fruit or seed species in powder form and natural gum powder, or a mixture consisting of seeds in powder form of at least three different species, wherein the seed-bearing fruit or seed of each of said species contains C in powder form greater than 45% w / w relative to the total fatty acid percentage. 16 -C 18 Fatty acids and fatty acids with a percentage of at least 21% w / w.

[0048] The species containing seeds are cumin, caraway, and fennel;

[0049] - A composition comprising the mixture of the present invention as the sole lubricant;

[0050] - The use of the mixture of the present invention as a lubricant in the preparation of tablets, capsules, and solid compositions;

[0051] - The use of natural gums as lubricants in the preparation of tablets, capsules, and solid compositions.

[0052] - A method for manufacturing capsules, tablets, or solid compositions, comprising the step of mixing the mixture of the present invention with a suitable formulation preparation, wherein the mixture is the only lubricant used in the method;

[0053] - A method for manufacturing capsules, tablets, or solid compositions, comprising the following steps:

[0054] i) Prepare one or more seed-containing fruit or seed species and / or natural gums in powder form, wherein the seed-containing fruit or seed of each said species in powder form contains C40% or more C40% relative to the total fatty acid percentage of greater than 45% w / w. 16 -C 18 Fatty acids and fatty acids in a percentage of at least 21% w / w, wherein the species are cumin and / or caraway and / or fennel;

[0055] ii) Mix one or more of the seed-containing fruits or seeds in powder form and / or the natural gum with a suitable formulation for 2 to 30 minutes, preferably 5 to 15 minutes, or even more preferably 5 minutes;

[0056] iii) Press or package the product obtained in step ii).

[0057] The components used in steps i) and ii) constitute the only lubricant used in the method.

[0058] - Capsules, tablets, or solid compositions that can be obtained by the method described.

[0059] Further advantages and / or embodiments of the invention will become apparent from the following detailed description. Detailed Implementation

[0060] The authors of this invention have unexpectedly discovered that the combination of plant gum and powders of seed-containing fruits or seeds; or the combination of different powders of seed-containing fruits or seeds, provides a system with emergent properties of excellent lubrication properties, which are comparable to those exhibited by one of the most common chemically synthesized lubricants used in the manufacture of tablets and capsules (i.e., magnesium stearate) under its optimal use conditions.

[0061] Therefore, the object of the present invention is to provide a mixture comprising, but not limited to, powdered seed-bearing fruits or seeds of one or more species and powdered natural gum, or a mixture of powdered seed-bearing fruits or seeds of at least three different species, wherein each seed-bearing fruit or powdered seed of said species contains C40% (w / w) greater than 45% (w / w) of total fatty acids. 16 -C 18 Fatty acids and fatty acids at a percentage of at least 21% w / w, wherein the species containing the fruit or powdered seeds are cumin, caraway, and fennel. As can be seen from Table 1 in the Examples section of this specification, the C present in the seed powder... 16 -C18 The fatty acids are primarily oleic acid and linoleic acid. According to the invention, the species are preferably characterized in that their dried fruits contain orthodox seeds, i.e., seeds that can resist long periods (years) of non-germination and remain viable.

[0062] Fennel fruit, also known as fennel (Foeniculi fructus), consists of mericarps, sometimes called "double achenes," but more commonly, it consists of single, small achenes ("achenes"), 3-12 mm long and 2-4 mm wide, yellowish-green to yellowish-brown in color. Fragments of the style are usually located at the upper part of the style base. Each achene has 5 straight, prominent ridges, especially well-developed at the fused joint. It has a strong pungent aroma and a slightly spicy fragrance. The mother plant of fennel fruit is fennel (Foeniculum vulgare), belonging to the Apiaceae family. Caraway fruit, also known as parsley fruit (Carvi fructus), consists of mericarps from the original double achenes. It is 3-6 mm long and about 1 mm thick, grayish-brown, often slightly sickle-shaped, pointed at both ends, and hairless. The back is slightly convex, with three straight, fine, prominent, and distinct ridges; on the fused surface, the edges are slightly arched, with two ridges. The style and its rounded base are usually still present at the top. It has an aromatic and spicy flavor. The mother plant of the caraway fruit is Caramelium carvi, which belongs to the Apiaceae family.

[0063] The fruit of cumin consists of straight-elliptical and linear achenes, 5-6 mm long, yellowish-brown, containing one seed. The seed is aromatic, with a characteristic bitterness and a strong sweetness. The parent plant of cumin fruit is *Cuminum cyminum* or *Cuminum odorum*, belonging to the Apiaceae family (or Umbelliferae family). In one embodiment, the particle size distribution value of the powdered fruit or seeds of the species, containing seeds, is calculated as Dv50 as 15 μm to 500 μm, preferably 150 μm to 350 μm. The Dv50 parameter, like the Dv10 and Dv90 parameters, is an index of particle size distribution, measured in μm, representing the average volume diameter of dust particles. Values ​​10, 50, and 90 represent 10%, 50%, and 90% of the analyzed particles below the corresponding μm value, respectively, and can be obtained using a laser diffractometer. Examples of laser diffractometer experiments are given in the Examples section of this specification.

[0064] In one embodiment, the specific surface area of ​​the seed-bearing fruit or powdered seed of the species is 25 m². 2 / kg to 600m 2 / kg, preferably 25m 2 / Kg to 70m 2 / Kg.

[0065] In one embodiment, the powdered form of the seed-containing fruit species or seeds is represented as The SPAN value is between 1.5 and 3.

[0066] SPAN is an index that correlates D90, D10, and D50 using the formula described above. A value of 1 corresponds to a perfect Gaussian distribution, and a higher value indicates a greater polydispersity of the distribution.

[0067] In one embodiment, the weight ratio of the powdered seed-bearing fruit or seeds of the species to the powdered natural gum is 1:1 to 1:8, preferably 1:5 to 1:7. To provide a non-limiting example of an embodiment of the invention, the weight ratio of the powdered seed-bearing fruit species or seeds to the natural gum powder is 1:7 in formulations that do not require a granulation step in their preparation, and 1:5 in formulations that require a granulation step in their preparation.

[0068] Granulation is a technical process in which powder particles (understood as particulate matter) are adhered to each other to form particles with a larger diameter, called granules. This process is commonly used in the pharmaceutical industry to prepare granules, which will be used directly or subsequently processed to prepare other drug forms, such as capsules or tablets.

[0069] In a preferred embodiment, the natural gum is gum arabic and / or gum arabic. Gum arabic is a natural gum, also known as arabic resin, because it is extracted from two Saharan acacia species (Acacia senegal and Acacia seyal). Like almost all plant-derived gums and resins, it is produced by plants through a natural “gluing” process that is spontaneously activated to heal wounds (wounds) to their surface integrity. Chemically, gum arabic is a mixture of calcium, magnesium, and potassium salts of arabic acid. Hydrolysis releases the constituent monosaccharides, namely L-arabinose, D-galactose, L-rhamnose, and D-glucuronic acid. At the molecular level, it consists of glycoproteins and oligosaccharides. Its applications are very wide-ranging due to its edibility, viscosity, ability to prevent sugar crystallization, and emulsification of fats. Its main uses include as a natural additive in the food industry, as an excipient and component in the pharmaceutical industry, as a film-forming and fixing agent in cosmetics, and as an egg tempera adhesive in glues and coatings. Coral resin is a gum-like secretion that occurs naturally or after cutting from the trunks and branches of some plants in the genus *Sterculia* (especially *Sterculia urens*). These plants are native to the highlands of India and Pakistan, although some resin-producing species also grow in Africa. Coral resin obtained from *Sterculia scaphigera* (a species found in Vietnam) is extracted from the fruit through maceration.

[0070] From a chemical perspective, *Aralia elata* gum is a complex polysaccharide with a high molecular weight, composed of galactose, rhamnose, and glucuronic acid. It is poorly soluble in water and swells rapidly upon contact with water, increasing in volume significantly beyond its initial size. This property explains its diverse applications in industrial and health fields. It is widely used as a thickener / stabilizer in the food (E416) and cosmetic industries, as well as an adhesive, and as a bulking laxative for treating constipation. For this purpose, it can also be used in combination with sulfates or magnesium oxide. In a further embodiment, the natural gum powder has a Dv50 value in the range of 60 μm to 70 μm and a specific surface area of ​​100 m². 2 / Kg to 150m 2 Within the range of / Kg, preferably 137m 2 / kg, and the SPAN value is in the range of 1 to 1.8, preferably 1.75.

[0071] In a preferred embodiment, the powdered form of the at least three species of seed-containing fruits or mixtures of different seeds consists of fruit powder containing cumin seeds, fruit powder containing caraway seeds, and fruit powder containing fennel seeds, or may consist of powders of the aforementioned seeds.

[0072] In a further embodiment, the weight ratio of the fruit powder containing cumin seeds, the fruit powder containing caraway seeds, and the fruit powder containing fennel seeds is 1:1:1 to 1:1:3, preferably 1:1:1.

[0073] The same applies when using the powdered seeds described above. In any embodiment according to the present invention, the mixture comprises the following:

[0074] -Powdered caraway fruit containing seeds and powdered gum arabic, in a weight ratio of 1:1 to 1:8, preferably 1:5 to 1:7; and / or

[0075] - Powdered fennel containing seeds and powdered gum arabic, in a weight ratio of 1:1 to 1:8, preferably 1:5 to 1:7; and / or

[0076] - Powdered cumin seeds and powdered gum arabic in a weight ratio of 1:1 to 1:8, preferably 1:5 to 1:7.

[0077] In a preferred embodiment, the mixture comprises caraway, fennel and cumin seeds and gum arabic powder in a weight ratio of 1:1:1, with each component weighing from 1:1 to 1:8, preferably from 1:5 to 1:7.

[0078] The same applies when using the powdered form of the aforementioned seeds. Therefore, another object of the present invention is a lubricant for tableting, which comprises the mixture of the invention as defined in this specification and the claims.

[0079] Characterization of the basic properties of the powders used in this invention shows that fruit powder containing seeds and magnesium stearate exhibit significantly different values ​​in terms of specific surface area and Dv50, but at the same time, characterization of indirect properties, such as flowability index (IC) and compressibility index (IH), shows values ​​comparable to (if not lower than) those obtained with magnesium stearate.

[0080] Another object of the invention is represented by a composition comprising a mixture as defined according to the previously described embodiments, wherein the composition is a tablet, capsule, or solid composition, and wherein the mixture is the only lubricant contained in the composition. A non-limiting example of a tablet according to any embodiment of the invention is...

[0081] Plain tablets or coated tablets (sugar-coated pills): swallow directly;

[0082] Tablets: Do not swallow directly, but dissolve in the mouth;

[0083] Chewable tablets: Chew before swallowing;

[0084] Sublingual tablets: absorbed through the tongue mucosa (e.g., nitroglycerin);

[0085] Soluble tablets: These are tablets that are to be dissolved in water. They are usually effervescent to facilitate dissolution or improve flavor.

[0086] Sterile tablets used for the preparation of injectable solutions;

[0087] Sterile dressings for subcutaneous implants;

[0088] Tablets used as vaginal suppositories have almost completely replaced gelatin suppositories;

[0089] Tablets used to prepare solutions for external or diagnostic purposes (pregnancy tests, denture sterilizers, etc.);

[0090] Tooth ingot.

[0091] Furthermore, the tablets according to the invention can be coated tablets, and the coating can also be a coating for controlled release.

[0092] In one embodiment, the mixture of powdered fruit containing seeds or powdered seeds is present in the composition at a content of 1% to 35% w / w, preferably 3% to 4.5% in a mixture without natural gum, and preferably 12% to 33% in a mixture containing natural gum.

[0093] According to one embodiment, the composition is a pharmaceutical, cosmetic, nutritional composition, medical device, food supplement, or food. In embodiments where the composition is a pharmaceutical composition, the composition comprises at least one natural active complex system (e.g., one or more plant extracts or fractions thereof) or one or more pharmacologically or physiologically active ingredients, and other pharmaceutical-grade powdered natural raw materials or one or more pharmaceutically acceptable excipients and / or carriers, preferably of natural origin (e.g., plant extracts or derivatives). The excipients and / or pharmaceutically acceptable carriers are known to those skilled in the art. In this invention, a medical device corresponds to any class of medical devices as described in Regulation 745 / 2017 of EEC Directive 93 / 42 on Medical Devices (which also includes substances and not just the term "device" in a mechanical sense).

[0094] As mentioned above, the composition may also be in food form, such as food for special medical purposes, food supplement, or any form permitted by the regulations of the country where the composition is produced.

[0095] In one embodiment, the composition is in the form of capsules, tablets, powders, granules, or solid compositions (e.g., solid toothpaste). The use of the mixtures defined in the embodiments of this specification as lubricants in the preparation of tablets, capsules, powders, granules, or solid compositions (e.g., solid toothpaste) is also an object of this invention.

[0096] Another object of the present invention is to use natural gums, preferably gum arabic or gum arabic, as a lubricant in the preparation of tablets, capsules, and solid compositions.

[0097] In one embodiment, the natural gum is present in the range of 1% to 35% by weight of the tablet, capsule, or solid composition.

[0098] In another embodiment, the natural rubber powder has a Dv50 value in the range of 60 μm to 70 μm and a specific surface area of ​​100 m². 2 / Kg to 150m 2 Within the range of / Kg, preferably 137m 2 / kg, and the SPAN value is in the range of 1 to 1.8, preferably 1.75. In summary, the present invention also relates to pharmaceuticals, cosmetics, nutritional products, medical devices, food supplements, and foods comprising capsules, tablets, or solid compositions comprising, as the sole lubricant, the lubrication system of the present invention according to any embodiment described herein.

[0099] In one embodiment, the mixture is contained in a product in the form of tablets, capsules, or solid compositions (e.g., solid toothpaste), and thus serves only as an internal lubricant. However, it can also be used again as the sole lubricant for lubricating machines suitable for preparing the product form, and thus can be used as an external lubricant. Lubricating a machine using the mixture of the present invention can be done by spraying it through a nozzle. Therefore, for the purposes of the present invention and for the aforementioned uses, the powder can be appropriately micronized to obtain a particle size suitable for the desired use. Therefore, the present invention also aims at a method for manufacturing capsules, tablets, or solid compositions, comprising the step of mixing the mixture as defined in this specification and claims with a suitable formulation preparation (i.e., with other substances or ingredients that must be present in the capsules, tablets, or compositions), wherein the sole lubricant is the mixture. The present invention also relates to a method for manufacturing capsules, tablets, or solid compositions, comprising the following steps:

[0100] i) Prepare one or more seed-containing fruit or seed species and / or natural gums in powder form, wherein the seed-containing fruit or seed of each said species in powder form contains more than 45% w / w C relative to total fatty acids. 16 -C18 Fatty acids and fatty acids with a percentage of at least 21% w / w;

[0101] ii) Mix the seed-containing fruit or seeds of one or more species in powder form and / or the natural gum with a suitable formulation preparation for 2 to 30 minutes, preferably 5 to 15 minutes, more preferably 5 minutes;

[0102] iii) Press or package the product obtained in step ii).

[0103] The components used in steps i) and ii) constitute the only lubricant used in the method.

[0104] Optionally, the above method may include, between steps i) and ii), a further step of granulating the one or more powdered forms of seed-containing fruits or seed species and / or the natural gum.

[0105] The present invention also relates to a method for manufacturing capsules, tablets, or solid compositions as described above, wherein step ii) is replaced by the following steps:

[0106] iia) Granulation of the formulation with natural gum;

[0107] (iib) The granules obtained in step ii) are mixed with the one or more powdered seed-containing fruit or seed species prepared in step i) until a homogeneous mixture is obtained, for a duration of 2 to 30 minutes, preferably 5 to 15 minutes, or even more preferably 5 minutes. In one embodiment, the granules obtained in step iia) are dried until a relative humidity between 23% and 26% is reached, and then mixed in step iib). The granulation, pressing or encapsulation, and mixing steps of the method subject to the present invention are performed according to techniques known in the prior art.

[0108] According to this specification, a formulation preparation is any preparation used to prepare tablets, capsules, or solid compositions as described anywhere in this specification, without the addition of a lubricant. In other words, it corresponds to a preparation intended for a capsule, tablet, or solid product manufacturing process, to which a person skilled in the art would typically add magnesium stearate as a lubricant, or other lubricants commonly used in pharmaceuticals, nutritional products, cosmetics, and food, to prepare a product that must be compressed or packaged using industrial machinery typically used for this purpose. Therefore, a person skilled in the art can understand the general definition of a formulation preparation / preparation because they know which preparations are suitable for conversion into tablets, capsules, or solid products after the appropriate addition of a lubricant.

[0109] Examples of such preparations are mixtures of powders and / or granules, which, in addition to pharmaceutical substances (e.g., one or more active ingredients), nutritional products, food, and cosmetics, may also contain one or more of the following:

[0110] Diluents: They increase the mass of the tablets, thereby achieving a sufficient volume suitable for processing;

[0111] Adsorbents: These are used to aggregate particles. In addition, solvents (water or alcohol) or other syrup solutions or viscous substances (pectin, methylcellulose, carboxymethylcellulose, gelatin, etc.) that act as binders through evaporation are also used.

[0112] Gliding agents: These agents insert themselves between the particles of the powder or granules to which they are added, filling irregular cavities present on their surface; thus, the shape of the powder or granules becomes more regular and friction is reduced;

[0113] Disintegrants: They shorten the time it takes for tablets to depolymerize.

[0114] In the method of the present invention, instead of using common lubricants such as Ca, Mg, Al stearates, octadecyl alcohol, stearyl alcohol, cetyl alcohol, palmitic acid, alcohols, starch, PEG, talc, only mixtures or systems in the form of natural gums having emergent lubricating properties as described herein are used.

[0115] Granulation is a technique that increases particle size through agglomeration and is one of the most important unit operations in the production of drug forms such as tablets and capsules. During granulation, small or coarse particles are transformed into large aggregates called granules.

[0116] This technology can be carried out in two ways: dry granulation and wet granulation. In both processes, particle formation is achieved by generating binding forces between powder particles. Dry granulation uses mechanical pressing (tableting) or compaction (rolling) to promote the agglomeration of powder particles, while wet granulation involves using liquid granulation (binder / solvent) to promote agglomeration by adhering and forming wet agglomerates.

[0117] Classic granulation techniques include the use of cylindrical compactors or segmented kneaders, as well as zeta or sigma arms or even vibrating and rotary granulators. Now, other newer techniques have been added, such as: pneumatic granulation, reverse wet granulation, steam granulation, water-activated dry granulation, thermally bonded granulation, melt granulation, cryogenic granulation, and foam granulation. Furthermore, for wet granulation, the granulator used plays a crucial role in particle formation during the process, and they can be categorized into three types: low-speed, high-speed, and fluidized bed. Low-speed granulators can be kneaders equipped with arms or vibrating or rotary granulators. On the other hand, high-speed granulators basically consist of a cylindrical container sealed with a lid, with a stirring paddle (impeller) at the bottom. Inside the container is a crusher (cutting blade), composed of rotating blades, whose task is to break up excessively large clumps, and a sprayer / atomizer for adding a binder solution, which can simply be water or a temporary solution. Fluidized bed granulation is performed using an apparatus that mixes, wets, and dries a powder bed fluidized by air in a single process. In this apparatus, an airflow passes upwards through the powder agglomerates to be granulated, maintaining them in a turbulent suspension state, i.e., “fluidization.” A binder solution is sprayed directly countercurrently onto the suspended agglomerates to induce particle aggregation, thereby forming granules. At some stage of the process, the air is heated to the desired temperature, so this type of apparatus can also complete the drying process of solid agglomerates in a single step. Because the suspended material has a very large surface area to be dried, the drying is actually carried out at very low temperatures. In a preferred embodiment, the lubricant of the invention, i.e., a mixture of seed-containing fruits or seeds and / or natural gums of one or more species disclosed herein and defined in the claims, is used in the above method in an amount such that its total content is from 1% to 35% by weight relative to the capsule, tablet, or solid composition.

[0118] As described above, according to the present invention, the lubricant is the only lubricant contained in the capsule, tablet or solid composition.

[0119] The object of the present invention is also obviously to obtain capsules, tablets or solid compositions by any of the embodiments described herein. As can be seen from the experimental data reported in the figures and described in the Examples section, the presence of the granulation step allows for a reduction in the amount of lubricating mixture in the formulation, reducing the content of a 1:7 anise-gum system of 32.34% to a 1:5 granulated anise-gum system of 12%.

[0120] In any part of this specification and claims, the term "comprising / including" may be replaced by the term "consisting of".

[0121] The following examples are provided to better illustrate the methods disclosed in this specification. These examples should not in any way be considered as limiting the foregoing specification and the appended claims.

[0122] Example

[0123] The powders used in the examples provided below were characterized in terms of nutritional properties, direct and indirect properties, and compared with magnesium stearate.

[0124] The following is the composition of the powder in terms of its fat content, which is known to have lubricating properties:

[0125] Experiment 1:

[0126] To investigate the presence of fatty acids with lubricating properties, samples of magnesium stearate, as well as powdered seeds of anise, cumin, and caraway, were sent to an external laboratory for complete nutritional composition analysis. Specifically, fatty acids were analyzed using GC / FID. The percentage of residual water was obtained by gravimetric analysis. The results showed that the fatty acids present in the seeded fruit powders differed from those present in magnesium stearate, but the major fatty acids had the same chain length.

[0127] Table 1: Reference nutritional analysis of seed-containing fruits compared to magnesium stearate.

[0128]

[0129] To evaluate the content of seed-containing fruit powder to be added to the mixture for pressing tests, C was compared. 16 -C 18 Percentage of chain fatty acids.

[0130] Considering the amount of fatty acids contained in 1% magnesium stearate, it is estimated that a variable percentage of seed-containing fruit powder between 1% and 5% should be used.

[0131] Experiment 2:

[0132] The seed-containing fruit powder was characterized in terms of bulk density, tap density, and relative humidity (%). The obtained density values ​​were used to calculate the relative flowability and compressibility index.

[0133] Table 2: Representation of Indirect Attributes

[0134] Angle of repose IC IH Bulk density Tap density % relative humidity magnesium stearate 1.55 16.42 1.2 0.35 0.448 2.63 loose, very fine powder of cumin seeds 29.41 11.86 1.13 0.43 0.489 8.34 Caraway seed powder 35.15 11.28 1.13 0.38 0.427 7.08 Loose, very fine powder of fennel seeds 30.96 10.42 1.12 0.35 0.391 6.26

[0135] Data analysis shows that this type of powder is characterized by flowability index (IC) and compressibility (IH) comparable to those obtained for magnesium stearate (if not lower).

[0136] Experiment 3:

[0137] The particle volume distribution of the powder in solid form was determined using a Mastersizer 3000 laser diffractometer (Malvin, UK). Approximately 5–7 g of dried powder was analyzed using the following parameters: background measurement duration: 10 s, sample measurement duration: 19.56 s, lower limit of occlusion: 0.10%, upper limit of occlusion: 15%, air pressure: 2 bar, hopper gap: 2.50 mm.

[0138] All analyses retained the parameters used for comparison of the obtained outputs; these parameters were automatically calculated using Mastersizer software v3.81.

[0139] - The median diameter volume Dv50 is the diameter that is above and below the 50% distribution (relative to the 50th percentile diameter).

[0140] - The relative difference between two average particle size measurements should not exceed 5%, and the curves from the two measurements should be identical.

[0141] -Dv90, 90% of the distribution volume is below this value.

[0142] -Dv10, 10% of the distribution volume is below this value.

[0143] - The span is the distribution width based on the 10th, 50th, and 90th percentiles.

[0144] Fruits containing seeds:

[0145] Based on the data comparison, the specific surface area and average particle distribution of the tested powder are different from those of magnesium stearate.

[0146] Table 3: Representation of basic attributes

[0147] Specific surface area [m² / kg] span DV50[μm] Caraway 53.07 2.694 181 cumin 31.89 2.016 282 fennel 57.65 2.797 197 magnesium stearate 600 2.279 15

[0148] Experiment 4:

[0149] The range of values ​​attributable to the release force that ensures the tablet is ejected from the punch is defined.

[0150] Given a standard powder mixture suitable for this purpose (79% microcrystalline cellulose, 20% calcium carbonate, 1% magnesium stearate), performance tests were conducted at different mixing times.

[0151] Then assess the tablet's release force.

[0152] The mixing time was correlated with the obtained demolding force to construct the target curve. Figure 1Time exceeding 30 minutes is considered useless because it leads to overmixing of the mixture, negatively impacting the bioavailability of APS present in the formulation. Furthermore, for the purposes of this invention, the maximum release force is considered to be equal to 0.50 N; exceeding this value will cause the tableting machine to begin producing tablets that adhere to the punch, resulting in ineligible tablets.

[0153] Therefore, the effective release force range is considered to be 0.05 to 0.50 N.

[0154] Experiment 5:

[0155] Development of mixtures containing a single seed as a lubricant

[0156] Given a standard mixture, the following compression test was performed using fruit powders containing caraway, fennel, and cumin seeds (individually), with the same percentage content of fatty acids as in 1% magnesium stearate in the same formulation.

[0157] The demolding force of the tablets was then analyzed and compared with parameters obtained by pressing a base mixture containing 1% magnesium stearate, and with the maximum experimental demolding force of other products. All pressing tests were performed using the same operating parameters, such as... Figure 2 As shown.

[0158] Based on the data obtained, we can infer that:

[0159] - Indirect indicators describing the rheological behavior of a raw powder are related to the ability of a mixture to contain a single raw material.

[0160] Surprisingly, when using the raw materials studied, the particle volume distribution value (dv50) and specific surface area did not appear to be related to the success of the pressing test.

[0161] Although the pushing force measured in all tests was less than 0.5 N, the values ​​tended towards the upper limit set in the study. In conclusion, the use of fruit powder containing individual seeds appears to have a lubricating effect, but it is not entirely effective; therefore, it may be advantageous to study systems that allow for optimization of this lubrication effect.

[0162] Experiment 6:

[0163] Development of blends containing a mixture of seeds and gum

[0164] In order to find functional synergy, gum arabic was studied.

[0165] Gum arabic is a 100% natural raw material obtained from the exudate of the acacia tree. Its adhesive and hyperdisintegration properties are known in the literature, but its lubricating properties have never been studied.

[0166] The purpose of the test was to investigate the possible synergistic effect of gum arabic and fruit seed powder on lubrication properties.

[0167] The mixture consisting of gum arabic and seed powder in a 7:1 ratio is premixed and added to the standard mixture. Figure 3 The demolding force values ​​obtained are shown compared to the blank and the mixture containing a single seed.

[0168] Table 4: Demolding force obtained during a mixing time of 5 minutes in the pressing test.

[0169] The "control" values ​​represent the demolding forces of the standard mixture composition and magnesium stearate according to Table 5 at two different mixing times, in column 3 (mixing for 5 minutes) and column 7 (mixing for 30 minutes).

[0170] For experimental testing, the optimal mixing time for magnesium stearate is 5 minutes.

[0171] mixture Demolding force [N] Caraway 0.417 cumin 0.467 fennel 0.415 Mix control for 5 minutes 0.040 1% Gum Arabic 0.26 10% Gum Arabic 0.28 30% Gum Arabic 0.27 Mix the control for 30 minutes 0.430 Cumin / Caraway / Fennel Mixture 0.13 Gum Arabic / Fennel Blend 0.01 Gum Arabic / Cumin Mixture 0.01 Gum arabic / Caraway mixture 0.01 Gum arabic / cumin-caraway-fennel blend 0.01 Maximum acceptable value 0.50

[0172] With other components present in the mixture and operating conditions being the same, the pusher force value produced by the system consisting of gum arabic and fruit powder containing seeds was lower than that produced by fruit powder containing individual seeds and magnesium stearate alone, as tested.

[0173] Table 5: Detailed description of the experiments conducted and the data obtained using different combinations.

[0174] The table shows release force data obtained using: mixtures of standard powders themselves (microcrystalline cellulose and calcium carbonate in a 4:1 ratio), or mixtures of standard powders to which magnesium stearate has been added, or various seed-containing fruit powders (caraway, fennel, cumin), or gum arabic, or systems in powder or granular form with the emergent properties of the present invention (mixtures of different seed-containing fruit powders or mixtures of gum arabic with one or more seed-containing fruit powders). It is evident from the table how mixing at least three different seed-containing fruit powders or at least one seed-containing fruit powder with gum arabic can have a synergistic effect, thereby providing a 100% natural lubrication system. The combination of gum arabic with at least one seed-containing fruit powder is particularly noteworthy.

[0175] Pol.Imp. represents extremely fine powder.

[0176] The particles in the table are those described in Experiment 7.

[0177] TQ represents the original state.

[0178] Table 5

[0179]

[0180] In the graph, the data displayed in columns 3 and 7 above represent the 5-minute and 30-minute controls, respectively.

[0181] Experiment 7:

[0182] Development of a technically processed system containing mixtures of seeds, fruits, and gums.

[0183] A 5:1 mixture of gum arabic and fennel seed powder was granulated with water and then sieved through a vibrating screen.

[0184] Granulation (especially fluidized bed granulation) is carried out in a device that mixes, wets, and dries a powder bed fluidized by air in one process. In this device, an airflow is passed upwards through the powder agglomerates to be granulated, maintaining them in a turbulent, suspended state – a process defined as “fluidization.” A binder solution is sprayed directly countercurrently onto the suspended powder agglomerates, thus determining particle aggregation and granulation. At some stage of the process, the air is heated to the desired temperature, allowing the device to also perform the drying process of the solid powder agglomerates in a single step. Because the suspended material has a very large surface area to be dried, the drying is actually carried out at very low temperatures. Granules obtained using this technique, consisting of gum arabic and fennel seeds in a 5:1 ratio, are added to a standard mixture and then pressed.

[0185] The amounts of raw materials and adhesive solution (water) used are shown in Table 6 and are calculated based on the container volume.

[0186] Table 6

[0187] <![CDATA[Batch size (50％) 12 liters]]> Total amount to be granulated 2100 Amount of ultrafine powder to be granulated 420 Amount of gum arabic to be granulated 1680 Recommended water volume 1365

[0188] Table 7 below shows the range of experimental parameters used to obtain the particle in question:

[0189] Table 7

[0190]

[0191] variable Granulation stage Drying stage Nozzle diameter 1.2 Atomization rate (g / ml) 9 to 11 Spray pressure (lubricating air pressure) 1-0.8 Inlet temperature 66-45 80-35 <![CDATA[Inlet air flow rate (m 3 / hr)]]> 65-80 95-90 Inlet air humidity (g / kg) 6.7-6.5 6.7-6.6 Exhaust humidity 14-13.4 16.8-6.7 Pump speed % 20-30 Filtration pressure 264-363 190-517 Product pressure 694-892 801-1054 Total Time 1 hour 40 minutes 60 minutes Total amount of solution sprayed 1143 Product temperature 40.7-24.9 25.4-61.3-38.1

[0192] The obtained particles were analyzed for particle size using a Mastersizer 3000 laser diffractometer (see previous experiments), and the results were as follows: Figure 4 The results are shown. The particles themselves and most of the sieved fraction (355 μm) were also characterized in terms of specific surface area, SPAN, and Dv50, and the results showed no significant differences.

[0193] Table 8: Characterization of the basic properties of particles and their components.

[0194] <![CDATA[Specific surface area [m 2 / kg]]]> SPAN <![CDATA[D V 50[μm]]]> As is 35.95 1.818 207 355μm 34.93 1.612 214

[0195] Both were evaluated in compression tests.

[0196] Compared to the values ​​obtained for blank samples, the obtained demolding force values ​​are as follows: Figure 5 As shown.

[0197] In fact, the same "gum-seed-containing fruit powder" system with a different ratio than the ungranulated mixture (7:1) in point 3 allows for the production of tablets without the addition of magnesium stearate, either in or external to the formulation. Furthermore, the amount of processing system added to the mixture is far less than... Figure 3 The amounts used in the mixtures shown are from 32% to 12%.

[0198] Option 1. A method for preparing capsules or tablets containing seed and / or gum powder.

[0199]

[0200] Fruit powder containing seeds and powdered natural gums can optionally be pre-granulated.

[0201] Option 2. A method for preparing capsules or tablets containing seed powder and natural gum.

[0202]

[0203] Scheme 3. A method for preparing charcoal tablets containing magnesium stearate.

[0204]

[0205] Charcoal and maltodextrin are granulated using a fluidized bed granulator, which performs nucleation and drying steps (as described above).

[0206] The granulated product is mixed with magnesium stearate and then pressed to form a finished product with some residual moisture, which is removed by secondary fluidized bed drying.

[0207] Option 4. A method for preparing charcoal tablets without the addition of synthetic stearates.

[0208]

[0209] The charcoal, maltodextrin and gum are mixed and granulated at low speed for 15 minutes using a granulator, and then dried in an oven.

[0210] The resulting granules are mixed with fruit powder containing fennel seeds and then pressed to form a finished product with some residual moisture. The residual moisture is then removed by secondary drying in an oven.

[0211] Example of preparation of charcoal tablets without the addition of synthetic stearates:

[0212] - Crush fennel seeds;

[0213] - Perform aqueous granulation of 70% charcoal with 10% rubber and 17.6% maltodextrin for 15 minutes;

[0214] -Dry the particles until the relative humidity reaches between 23% and 26%;

[0215] - Mix the dried granules with 2.4% anise seed powder until a homogeneous mixture is obtained, for 5 to 10 minutes.

[0216] -suppress;

[0217] - Final drying of the tablets.

[0218] Table 9. Composition of charcoal tablets with and without added synthetic stearate

[0219] Material Old formula New formula charcoal 70% + / - 5% p / p 69.72% + / - 5% p / p Maltodextrin 29.5% + / - 5% p / p 17.51% + / - 5% p / p magnesium stearate 0.5% p / p gum arabic 10.38% p / p Fennel seed powder 2.39% p / p

Claims

1. A tableting lubricant, said lubricant comprising a mixture, said mixture: a. Composed of one or more powdered forms of seed-containing fruit or seeds of a species and natural gum powder; or b. Composed of a mixture of seed-containing fruits or seeds in powder form from three different species described. The powdered fruit or seeds of each of the said species contain at least 21% w / w fatty acids and contain more than 45% w / w C relative to the total fatty acids. 16 -C 18 fatty acid, The species mentioned are cumin, caraway, and fennel, and Based on the mixture b. it consists of a mixture of seed-containing fruits or seeds in powder form of three different species, wherein the weight ratio of the seed-containing fruit or seed powders of cumin, caraway and fennel is 1:1:1 to 1:1:3; Based on the mixture a, which consists of one or more powdered fruits or seeds of the species containing seeds and the natural gum powder, wherein the natural gum is gum arabic, the mixture comprises the following: - Caraway in powder form contains the fruit or seeds of the seed and gum arabic powder in a weight ratio of 1:1 to 1:8; and / or - Anise in powder form contains the fruit or seeds of the seed and gum arabic powder in a weight ratio of 1:1 to 1:8; and / or - Cumin in powder form, consisting of seeded fruit or seeds and gum arabic powder, in a weight ratio of 1:1 to 1:8; and / or The powder of seeds or seeds of caraway, fennel and cumin, and powdered gum arabic in a weight ratio of 1:1:1 to 1:1:3, and in a weight ratio of 1:1 to 1:

8.

2. The lubricant according to claim 1, wherein the mixture b is composed of a mixture of seeded fruits or seeds in powder form of three different species, wherein the weight ratio of the seeded fruits or seeds of cumin, caraway, and fennel is 1:1:

1.

3. The lubricant according to claim 1, comprising the following components: - Caraway in powder form contains the fruit or seeds of the seed and gum arabic powder in a weight ratio of 1:5 to 1:7; and / or - Anise in powder form contains the fruit or seeds of the seed and gum arabic powder in a weight ratio of 1:5 to 1:7; and / or - Cumin in powder form, consisting of the fruit or seeds of the seed and gum arabic powder, in a weight ratio of 1:5 to 1:

7.

4. The lubricant according to claim 1, comprising the following components: The powder of seeds or seeds of caraway, fennel and cumin, and powdered gum arabic in a weight ratio of 1:1:1, and in a weight ratio of 1:5 to 1:

7.

5. The lubricant according to any one of claims 1 to 4, wherein the particle size distribution value of the seed-containing fruit or seed powder is calculated as Dv50 to be from 15 μm to 500 μm.

6. The lubricant according to claim 5, wherein the particle size distribution value of the seed-containing fruit or seed powder is calculated as Dv50 to be from 150 μm to 350 μm.

7. The lubricant according to any one of claims 1 to 4, wherein the specific surface area of ​​the seed-containing fruit or seed powder is 25 m². 2 / Kg to 600 m 2 / Kg.

8. The lubricant according to claim 7, wherein the specific surface area of ​​the seed-containing fruit or seed powder is 25 m². 2 / Kg to 70 m 2 / Kg.

9. The lubricant according to any one of claims 1 to 4, wherein the seed-containing fruit or seed powder is represented as The SPAN value is between 1.5 and 3.

10. The lubricant according to any one of claims 1 to 4, wherein the natural gum powder has a Dv50 value in the range of 60 μm to 70 μm and a specific surface area of ​​100 m². 2 / Kg to 150 m 2 Within the range of / Kg, and with a SPAN value between 1 and 1.

8.

11. The lubricant according to claim 10, wherein the specific surface area is 137 m². 2 / Kg.

12. The lubricant of claim 10, wherein the SPAN value is 1.

75.

13. A solid composition comprising, as the sole lubricant, any one of claims 1 to 12.

14. The solid composition according to claim 13, wherein the lubricant according to any one of claims 1 to 12 is present in an amount of 1% to 35% w / w.

15. The solid composition according to claim 14, wherein the lubricant according to any one of claims 1 to 12 is present in an amount of 3% to 4.5% w / w.

16. The solid composition according to any one of claims 13 to 15, wherein the solid composition comprises ingredients having 100% natural origin.

17. A tablet comprising the lubricant according to any one of claims 1 to 12 as the sole lubricant.

18. The tablet according to claim 17, wherein the lubricant according to any one of claims 1 to 12 is present in an amount of 1% to 35% w / w.

19. The tablet according to claim 17, wherein the lubricant according to any one of claims 1 to 12 is present in an amount of 3% to 4.5% w / w.

20. The tablet according to any one of claims 17 to 19, wherein the tablet comprises an ingredient having a 100% natural origin.

21. A capsule comprising the lubricant according to any one of claims 1 to 12 as the sole lubricant.

22. The capsule of claim 21, wherein the lubricant of any one of claims 1 to 12 is present in an amount of 1% to 35% w / w.

23. The capsule of claim 21, wherein the lubricant of any one of claims 1 to 12 is present in an amount of 3% to 4.5% w / w.

24. The capsule according to any one of claims 21 to 23, wherein the capsule comprises an ingredient having a 100% natural origin.

25. A pharmaceutical, cosmetic, nutritional product, or food supplement, comprising a solid composition as defined in any one of claims 13 to 16.

26. A pharmaceutical, cosmetic, nutritional product, or food supplement, comprising a tablet as defined in any one of claims 17 to 20.

27. A drug, cosmetic, nutritional product, or food supplement, comprising a capsule as defined in any one of claims 21 to 24.

28. A food product comprising a solid composition as defined in any one of claims 13 to 16.

29. A food product comprising tablets as defined in any one of claims 17 to 20.

30. A food product comprising a capsule as defined in any one of claims 21 to 24.

31. Use of the lubricant according to any one of claims 1 to 12 in the preparation of a solid composition.

32. The use according to claim 31, wherein the lubricant is the only lubricant contained in the product in the form of a solid composition; and / or the lubricant is used to lubricate a machine suitable for preparing the product in the form of the solid composition.

33. Use of the lubricant according to any one of claims 1 to 12 in tablet preparation.

34. The use according to claim 33, wherein the lubricant is the only lubricant contained in the tablet form product; and / or the lubricant is used to lubricate a machine suitable for preparing the tablet form product.

35. Use of the lubricant according to any one of claims 1 to 12 in the preparation of capsules.

36. The use according to claim 35, wherein the lubricant is the only lubricant contained in the product in capsule form; and / or the lubricant is used to lubricate a machine suitable for preparing the product in capsule form.

37. A method for manufacturing a solid composition, comprising the step of mixing a mixture as defined in any one of claims 1 to 12 with a formulation preparation, wherein the only lubricant used in the method is the mixture.

38. A method for manufacturing tablets, comprising the step of mixing a mixture as defined in any one of claims 1 to 12 with a formulation preparation, wherein the only lubricant used in the method is the mixture.

39. A method for manufacturing capsules, comprising the step of mixing a mixture as defined in any one of claims 1 to 12 with a formulation preparation, wherein the only lubricant used in the method is the mixture.

40. A method for manufacturing a solid composition, comprising the following steps: i) Prepare a mixture of seed-bearing fruits or seeds of three different species in powder form; or a mixture of seed-bearing fruits or seeds of one or more of the species in powder form and natural gum powder, wherein the seed-bearing fruits or seeds of each of the species in powder form contain at least 21% w / w fatty acids and contain C4% ... 16 -C 18 Fatty acids, wherein the species mentioned are cumin, caraway, and fennel, and Based on the preparation of a mixture of seed-containing fruits or seeds in powder form of three different species, wherein the weight ratio of cumin, caraway and fennel is 1:1:1 to 1:1:3; Based on the preparation of one or more powdered forms of the species containing seeds, or a mixture of seeds and natural gum powder, wherein the natural gum is gum arabic, wherein... - Caraway seeds in powder form, with a weight ratio of fruit or seeds containing seeds to gum arabic powder of 1:1 to 1:8; and / or - Anise in powder form, containing the seeds or fruit, and gum arabic powder, in a weight ratio of 1:1 to 1:8; and / or - The weight ratio of cumin seeds or fruit containing seeds to gum arabic powder in powder form is 1:1 to 1:8; and / or The weight ratio of caraway, fennel and cumin seed-containing fruit or seed powder and powdered gum arabic is 1:1:1 to 1:1:3 and 1:1 to 1:

8. ii) Mix the mixture with the formulation preparation for 2 to 30 minutes; iii) Press or package the product obtained in step ii). The components used in steps i) and ii) constitute the only lubricant used in the method.

41. A method for manufacturing tablets, comprising the following steps: i) Prepare a mixture of seed-bearing fruits or seeds of three different species in powder form; or a mixture of seed-bearing fruits or seeds of one or more of the species in powder form and natural gum powder, wherein the seed-bearing fruits or seeds of each of the species in powder form contain at least 21% w / w fatty acids and contain C4% ... 16 -C 18 Fatty acids, wherein the species mentioned are cumin, caraway, and fennel, and Based on the preparation of a mixture of seed-containing fruits or seeds in powder form of three different species, wherein the weight ratio of cumin, caraway and fennel is 1:1:1 to 1:1:3; Based on the preparation of one or more powdered forms of the species containing seeds, or a mixture of seeds and natural gum powder, wherein the natural gum is gum arabic, wherein... - Caraway seeds in powder form, with a weight ratio of fruit or seeds containing seeds to gum arabic powder of 1:1 to 1:8; and / or - Anise in powder form, containing the seeds or fruit, and gum arabic powder, in a weight ratio of 1:1 to 1:8; and / or - The weight ratio of cumin seeds or fruit containing seeds to gum arabic powder in powder form is 1:1 to 1:8; and / or The weight ratio of caraway, fennel and cumin seed-containing fruit or seed powder and powdered gum arabic is 1:1:1 to 1:1:3 and 1:1 to 1:

8. ii) Mix the mixture with the formulation preparation for 2 to 30 minutes; iii) Press or package the product obtained in step ii). The components used in steps i) and ii) constitute the only lubricant used in the method.

42. A method for manufacturing capsules, comprising the following steps: i) Prepare a mixture of seed-bearing fruits or seeds of three different species in powder form; or a mixture of seed-bearing fruits or seeds of one or more of the species in powder form and natural gum powder, wherein the seed-bearing fruits or seeds of each of the species in powder form contain at least 21% w / w fatty acids and contain C4% ... 16 -C 18 Fatty acids, wherein the species mentioned are cumin, caraway, and fennel, and Based on the preparation of a mixture of seed-containing fruits or seeds in powder form of three different species, wherein the weight ratio of cumin, caraway and fennel is 1:1:1 to 1:1:3; Based on the preparation of one or more powdered forms of the species containing seeds, or a mixture of seeds and natural gum powder, wherein the natural gum is gum arabic, wherein... - Caraway seeds in powder form, with a weight ratio of fruit or seeds containing seeds to gum arabic powder of 1:1 to 1:8; and / or - Anise in powder form, containing the seeds or fruit, and gum arabic powder, in a weight ratio of 1:1 to 1:8; and / or - The weight ratio of cumin seeds or fruit containing seeds to gum arabic powder in powder form is 1:1 to 1:8; and / or The weight ratio of caraway, fennel and cumin seed-containing fruit or seed powder and powdered gum arabic is 1:1:1 to 1:1:3 and 1:1 to 1:

8. ii) Mix the mixture with the formulation preparation for 2 to 30 minutes; iii) Press or package the product obtained in step ii). The components used in steps i) and ii) constitute the only lubricant used in the method.

43. The method according to any one of claims 40 to 42, wherein the cumin, caraway and fennel are prepared in a weight ratio of 1:1:1 based on the preparation of a mixture of seed-containing fruits or seeds in powder form of three different species.

44. The method according to any one of claims 40 to 42, step ii) comprises: Mix the mixture with the formulation preparation for 5 to 15 minutes.

45. The method according to any one of claims 40 to 42, step ii) comprises: Mix the mixture with the formulation preparation for 5 minutes.

46. ​​The method according to any one of claims 40 to 42, wherein the step of granulating the mixture is included between steps i) and ii).

47. The method according to any one of claims 40 to 42, wherein step ii) is replaced by the following steps: iia) Granulation of the formulation with natural gum; iib) The granules obtained in step iia) are mixed with one or more powdered forms of the species prepared in step i) containing seeds, until a homogeneous mixture is obtained, for a period of 2 to 30 minutes.

48. The method according to any one of claims 40 to 42, wherein step ii) is replaced by the following steps: iia) Granulation of the formulation with natural gum; iib) The granules obtained in step iia) are mixed with one or more powdered forms of the species prepared in step i) containing seeds, until a homogeneous mixture is obtained, for a period of 5 to 15 minutes.

49. The method according to any one of claims 40 to 42, wherein step ii) is replaced by the following steps: iia) Granulation of the formulation with natural gum; iib) The granules obtained in step iia) are mixed with one or more powdered forms of the species prepared in step i) containing seeds, until a homogeneous mixture is obtained, for a period of 5 minutes.

50. The method of claim 47, wherein the particles obtained in step iia) are dried until a relative humidity between 23% and 26% is achieved, and then mixed in step iib).

51. The method of claim 46, wherein the granulation is dry granulation, wet granulation, steam granulation, thermal bonding granulation, melt granulation, freeze granulation, or foam granulation.

52. The method according to claim 51, wherein the dry granulation includes dry pneumatic granulation and moisture-activated dry granulation; and the wet granulation includes reverse wet granulation.

53. The method of claim 40, wherein the mixture is present in a total content of 1% to 35% by weight relative to the solid composition.

54. The method of claim 41, wherein the mixture is present in a total content of 1% to 35% by weight relative to the tablet.

55. The method of claim 42, wherein the mixture is present in a total content of 1% to 35% by weight relative to the capsule.

56. A solid composition obtainable by the method according to any one of claims 40, 43 to 53.

57. A tablet obtainable by the method according to any one of claims 41, 43 to 52, 54.

58. Capsules obtainable by the method according to any one of claims 42, 43 to 52, 55.

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