Powder for slow release of active ingredient on teeth
By forming a coating containing organic compounds and porous materials on the tooth surface and using a powder spraying device to achieve slow release of active ingredients, the problems of short contact time and poor stability in existing technologies are solved, thus improving the chemical reaction effect of tooth treatment.
Patent Information
- Application Number
- CN202480054211.5
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2023-08-16
- Filing Date
- 2024-08-16
- Publication Date
- 2026-03-27
AI Technical Summary
In existing tooth treatment methods, the contact time of active ingredients on the tooth surface is short, resulting in insignificant chemical reaction effects. Furthermore, the aqueous environment and fluid flow make it difficult for chemical substances to be fixed, affecting the treatment outcome.
Using powder containing organic compounds and porous materials, a coating is formed on the tooth surface through a powder spraying device. The active ingredients are adsorbed in the pores and slowly released, and the kinetic energy of the powder is used to melt the powder to form a coating that is not easy to remove.
It achieves slow release of active ingredients on the tooth surface, ensuring sufficient contact time and stability, improving the effectiveness of chemical reactions, and is suitable for supragingival and subgingival treatments.
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Abstract
Description
[0001] This invention relates to powders for use in treating tooth surfaces with a powder spraying device, the powders being capable of slowly releasing an active component onto the teeth. The invention also relates to coatings on tooth surfaces that can be obtained by applying the powder.
[0002] Professional dental preventative care is an important, regular treatment that helps maintain oral health because it removes biofilm and tartar that patients cannot remove during their routine home dental care. Professional dental preventative care includes powder spray cleaning or air polishing, which is particularly effective because it allows access to and cleaning of all tooth surfaces and the spaces between teeth, implants, brackets, and orthodontic appliances.
[0003] In powder spraying cleaning, a powder spraying device is used, in which powder is sprayed onto the tooth surface along with a gaseous carrier medium (usually air), allowing for effective cleaning. Alternatively, or as an alternative to a gaseous carrier medium, a liquid carrier medium, such as water, can be used. Powder spraying is performed using a powder spraying device and is particularly effective because it does not require repetitive movements. Furthermore, it is faster than other cleaning methods and requires relatively little training to learn correctly.
[0004] Because of the product's convenient and direct contact with the tooth surface, the clean teeth achieved after powder spray cleaning have the potential to enhance effects such as fluoride treatment or remineralization. However, other chemical treatments typically require longer contact times to allow for chemical reactions to occur. Examples of these additional chemical treatments include fluoride treatment to improve enamel's acid resistance, remineralization to repair the tooth's exterior, antibacterial treatments to slow biofilm recolonization, or healing aids utilizing anti-inflammatory ingredients or bone growth factors.
[0005] For supragingival treatments such as fluoride, creams or varnishes that can be deposited on teeth are available. EP 2 455 064A1 discloses polymer-filled sheets for subgingival treatments, such as Periochip. DE 10 114244 A1 describes thick gels, such as Ligosan, for subgingival antibacterial retention.
[0006] However, all of these methods have their limitations. For supragingival deposits, the contact time is often too short to achieve a true chemical effect. Typically, at least several hours of contact time will be required. However, patients are often unwilling to spend 20 minutes or longer in the dental chair for the chemical reaction to begin. Furthermore, the aqueous environment of the oral cavity rapidly dissolves and removes all water-soluble compounds. For subgingival additives, the presence of bodily fluid flow allows all chemicals not fixed within the periodontal pockets to be expelled. However, fixing the active ingredient in the presence of a fairly thick support material also hinders soft tissue reattachment. Additionally, a higher product concentration is required.
[0007] During the development of this invention, it was discovered that powders containing organic compounds with a melting point preferably <165°C can form a coating on the tooth surface when applied by a powder spraying device. This coating may contain active ingredients or active components. However, further research has shown that most active ingredients are released too quickly.
[0008] Therefore, one object of the present invention is to provide a protective system for tooth surfaces that overcomes the above problems, the protective system being easy to apply and allowing the active ingredients to be slowly delivered to the tooth surface.
[0009] This objective is achieved according to the invention by a powder for use in treating tooth surfaces with a powder spraying device according to claim 1. This objective is also achieved by a coating according to claim 13. Preferred embodiments of the invention depend on the dependent claims and the following description.
[0010] One embodiment of the present invention relates to a powder for use in treating a tooth surface with a powder spraying device, wherein the powder comprises:
[0011] (a) An organic compound in powder form, wherein the organic compound has a melting point of 35°C to 170°C and a solubility of <10 g / l in water at 25°C;
[0012] (b) A material in powder form having pores, said material comprising pores with a diameter <50 nm, wherein the average particle size d of the material is... 50 <50 μm; and
[0013] (c) Active components adsorbed in the pores of the material.
[0014] Unexpectedly, it was found that when the powder according to the invention is applied to the tooth surface using a powder atomizing device, a coating is formed on the tooth surface that protects the tooth and provides a slow release of active ingredients to the tooth surface. When the powder according to the invention is atomized onto the surface along with an airflow, i.e., when the powder is used in a powder atomizing device typically used for cleaning tooth surfaces, the powder adheres to the tooth surface, thereby forming a coating. Not bound by this interpretation, it is thought that due to the kinetic energy transferred to the powder, the powder undergoes a melting process upon collision with the tooth surface, forming a coating on the tooth surface (kinetic melting). The small average particle size of the material (d...) 50 The thickness (<50 μm) ensures that the material is not abrasive, preventing the coating from being removed. The active ingredient is not in the structure of the organic compound forming the coating (which has been found to cause excessively rapid release), but rather adsorbed within the pores of the material, ensuring slow release.
[0015] One advantage of the powder according to the invention is that it produces a coating in the correct location on the tooth surface when used in conventional powder spraying devices. The powder comprises an organic compound, a porous material, and an active ingredient adsorbed in the pores of said material. The active ingredient or active component is, for example, a pharmaceutically active compound or active pharmaceutical ingredient, meaning a therapeutically effective amount of a pharmaceutically active compound or active pharmaceutical ingredient.
[0016] In the context of this invention, the term "treating a tooth surface" means "applied to a tooth surface." Treating or applying to a tooth surface is a typical use of powder atomizing devices, where powder is sprayed onto the tooth surface along with a carrier medium such as air. In a preferred embodiment of the invention, the powder used in treating a tooth surface with a powder atomizing device is the same powder used in coating a tooth surface with a powder atomizing device. This treatment is preferably a therapeutic treatment, and the use of powder in the treatment is preferably a therapeutic use.
[0017] Slow release allows the active ingredient, preferably a pharmaceutically active compound, a tooth fluoride agent, or a tooth remineralizer, to remain on the tooth surface long enough to act on the tooth surface or to deliver the active ingredient directly from the coating to the tooth surface, i.e., to the correct location. Adsorption within the pores of the material, including the porous structure, and incorporation into the coating, ensure the slow release of the active ingredient. For example, adsorption within the pores of the material can be achieved by adding a solution of the active ingredient in a solvent to the porous material and then evaporating the solvent.
[0018] The powder according to the invention is easily applied using conventional powder spraying devices, especially after dental cleaning, and the same powder spraying device can be used for cleaning and subsequently for applying the powder according to the invention to the cleaned tooth surface. Only the powder is changed.
[0019] In a preferred embodiment of the invention, based on the total weight of the powder, the powder used for treating the tooth surface with a powder spraying device contains ≥30% by weight, more preferably ≥50% by weight, even more preferably ≥60% by weight, and most preferably ≥70% by weight of an organic compound having a melting point of 35°C to 170°C and a solubility of <10 g / L in water at 25°C.
[0020] In a preferred embodiment of the invention, based on the total weight of the powder, the powder used for treating the tooth surface with a powder spraying device comprises ≤40% by weight, more preferably ≤30% by weight, even more preferably ≤20% by weight, and most preferably ≤15% by weight of a porous powder material.
[0021] According to a preferred embodiment of the invention, the powder contains 0.01% to 20% by weight of an active compound or active ingredient, based on the total weight of the powder. More preferably, the powder contains 0.05% to 15% by weight, even more preferably 0.1% to 10% by weight, and most preferably 0.1% to 5% by weight of an active ingredient, based on the total weight of the powder.
[0022] Within the meaning of this invention, it should be understood that the total amount of the components of the powder given in wt% (weight %) is 100%. One example is a powder comprising: 50 wt% organic compound, 40 wt% porous material, 7 wt% active ingredient and 3 wt% other components such as flow aids, flavoring agents, etc.
[0023] Organic compounds according to the present invention are understood to be compounds containing one or more carbon atoms (especially carbon skeletons).
[0024] In a preferred embodiment of the invention, the organic compound in the powder used for treating tooth surfaces with a powder spraying device has a melting point of 35°C to 165°C, more preferably 37°C to 162°C, even more preferably 40°C to 158°C, and most preferably 42°C to 156°C. The low melting point results in an advantageous coating due to the promotion of kinetic melting. The solubility of the organic compound in water at 25°C is preferably <5 g / L, more preferably <2 g / L, and most preferably <1 g / L. The solubility in water refers to distilled water (pH approximately 7.0). Limited solubility in water enhances the stability of the coating in the aqueous environment of the oral cavity.
[0025] In the course of this invention, it was discovered that the organic compounds in the powder according to the invention are preferably selected from fatty acids, fatty alcohols, sterols, hydroxylated aromatic compounds, and mixtures thereof. Where possible, the fatty acids, fatty alcohols, sterols, and hydroxylated aromatic compounds may be optionally substituted and / or (partially) saturated.
[0026] The fatty acid is preferably a carboxylic acid having 10 to 24 carbon atoms, more preferably 12 to 22 carbon atoms, and even more preferably tridecanoic acid, pentadecanoic acid, palmitic acid, heptadecanoic acid, stearic acid, arachidic acid, and mixtures thereof. The most preferred fatty acids are palmitic acid, stearic acid, arachidic acid, and mixtures thereof.
[0027] The fatty alcohol is preferably an alcohol having 10 to 24 carbon atoms, more preferably 12 to 22 carbon atoms, and even more preferably stearyl alcohol or lauryl alcohol.
[0028] The sterols are preferably selected from cholesterol, β-sitosterol, campesterol, stigmasterol, ergosterol, brassosterol, and mixtures thereof. More preferably, the sterols are cholesterol and / or β-sitosterol.
[0029] The hydroxylated aromatic compound is preferably hydroxybenzene or hydroxytoluene, more preferably butylated hydroxytoluene (BHT) or butylated hydroxyanisole (BHA). Butylated hydroxytoluene (BHT) is the most preferred hydroxylated aromatic compound.
[0030] The advantage of using the above organic compounds as powders for forming coatings or deposits is that the organic compounds form a layer on the surface. The pores of the substrate (teeth) are not blocked, so the exchange between the tooth surface and the environment is not significantly altered. Furthermore, bodily functions such as tissue attachment are not hindered. Additionally, the diffusion of fluids within the medium can be used to fine-tune the delivery of active ingredients.
[0031] The powder according to the invention is deposited on the tooth surface due to the kinetic energy transferred to the powder by air. Deposition can be made on the gingiva, either in the enamel or exposed dentin, for example using a standard EMS airflow nozzle, or subgingivally, for example using an EMS PERIOFLOW subgingival nozzle. In a preferred embodiment of the invention, the powder, along with a gaseous carrier medium, particularly air, is sprayed toward the tooth surface using a powder spraying device. The powder is sprayed toward the tooth surface along with the air. The air may contain water, preferably less than 10 mL / min, particularly less than 5 mL / min. In a preferred embodiment, the powder spraying device is used without water.
[0032] The use of the present invention in treating tooth surfaces with a powder spraying device means spraying powder onto the tooth surface using a conventional powder spraying device. The powder then forms a coating on the tooth surface.
[0033] In the context of this invention, d 50 The value (average particle size) is the percentage of particles by volume that are smaller than d. 50 The value and 50% of the particles by volume are greater than d 50The value of the particle size. This also applies to d. 90 Values, of which 90% are less than d in terms of volume. 90 The d-value according to the invention is determined by dry dispersion using laser diffraction (Malvern Mastersizer 2000, equipped with a Scirocco dry dispersion apparatus, operating at 1.5 bar).
[0034] The average particle size d of the material 50 <50 μm, preferably <20 μm, more preferably <10 μm. d 90 Preferably <120 μm, more preferably <100 μm, and even more preferably <80 μm.
[0035] The porous powdered material according to the present invention is preferably a porous material. The porous material according to the present invention is understood to be a material having pores. This means that the porous powdered material can also be referred to as a porous material in powder form. Such a porous powdered material includes pores with a diameter <50 nm, preferably <50 nm and >2 nm. Such a material can also be referred to as a mesoporous material. According to the present invention, the porous powdered material preferably includes pores with a diameter <20 nm, more preferably <10 nm. In both cases, the pores are more preferably >2 nm. In a preferred embodiment of the present invention, the porous powdered material is silica and / or zeolite.
[0036] The pore size or pore diameter and cumulative pore volume of the material were measured by nitrogen absorption according to the Barrett-Joyner-Halenda method (BJH method) of the BET method (ISO 9277:2010). The results of this BJH method are pore volume and cumulative pore volume (i.e., pore size distribution) in relation to pore diameter. See also EP Barret, LG Joyner, PH Halenda, J. Am.Chem. Soc. 73 (1951) 373; JC Groen, LAA Peffer, J. Perez-Ramirez, Microporous Mesoporous Mater. 60 (2003) 1; SJ Gregg, KSW Sing, “Adsorption, Surface Area and Porosity”, 2nd ed., Academic Press, London, 1982.
[0037] In a preferred embodiment of the invention, 90% of the cumulative pore volume of the powdered material with pores comes from pores with a diameter of <20 nm, more preferably <15 nm, and most preferably <8 nm.
[0038] According to the present invention, the active ingredient (active compound) having an effect on teeth or on the human or animal body can preferably be a pharmaceutically active compound, a tooth fluoride agent, or a tooth remineralizer. Therefore, the present invention allows for the creation of a smart delivery system for an active ingredient (e.g., a pharmaceutically active compound) that is placed on the tooth surface and releases the active ingredient.
[0039] The active ingredients according to the present invention are preferably selected from anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, bone growth factors, tooth fluoride agents, and tooth remineralizing agents. Anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, and bone growth factors are understood as pharmaceutically active compounds or pharmaceutically active ingredients. The powder may contain one or more active ingredients, for example, one, two, three, four, or five. The powder may also contain one or more organic compounds and / or one or more porous materials, for example, one, two, three, four, or five.
[0040] The powder according to the invention refers to a substance in the form of small particles. The average particle size (d) of the powder according to the invention (i.e., a powder generally comprising particles of organic compounds and materials) 50 The particle size is preferably from 0.5 μm to 500 μm, more preferably from 1 μm to 300 μm, even more preferably from 2 μm to 200 μm, and most preferably from 5 μm to 100 μm. The particle size can be adapted to the application area. For example, for treating subgingival tooth surfaces, a smaller average particle size is preferred, particularly from about 0.5 μm to 50 μm, more preferably from 1 μm to 30 μm. For treating supragingival tooth surfaces, a larger average particle size can be used, preferably from 0.5 μm to 200 μm, more preferably from 2 μm to 100 μm.
[0041] In another preferred embodiment of the invention, the powder further comprises a flow aid, a bleaching agent, and / or a flavoring agent. Based on the total weight of the powder, the total amount of these additional substances is preferably from 0.2% to 5% by weight, more preferably from 0.5% to 2% by weight.
[0042] The flow aid is preferably selected from silica (silica, especially amorphous silica), aluminum silicate, and / or aluminum hydroxide. Silica is more preferred, particularly in an amount of 0.2% to 3% by weight, and most preferably 0.5% to 2% by weight, based on the total weight of the powder.
[0043] Preferred bleaching agents are peroxides, such as magnesium peroxide, calcium peroxide, or zinc peroxide; persulfates, such as sodium persulfate, potassium persulfate, or ammonium persulfate; or perborates.
[0044] In a preferred embodiment of the invention, the powder comprises less than 10% by weight of abrasive powder (abrasive powder spray cleaning powder), more preferably less than 5% by weight, even more preferably less than 2% by weight, and particularly less than 1% by weight of abrasive powder, each based on the total weight of the powder.
[0045] According to the present invention, abrasive powder or abrasive jet cleaning powder refers to powder used in a powder spraying device for cleaning tooth surfaces. The abrasive powder or abrasive jet cleaning powder is preferably sodium bicarbonate, calcium carbonate, aluminum hydroxide, sugar alcohol, amino acids, sugar, cyclodextrin, or a mixture thereof. Therefore, based on the total weight of the powder, the powder according to the present invention preferably contains less than 10% by weight, more preferably less than 5% by weight, even more preferably less than 2% by weight, and most preferably less than 1% by weight of sodium bicarbonate, calcium carbonate, aluminum hydroxide, sugar alcohol, amino acids, sugar, cyclodextrin, or a mixture thereof. The sugar alcohol is preferably erythritol, and the amino acid is preferably glycine. The sugar is preferably trehalose or tagatose. Therefore, it is preferred that, based on the total weight of the powder, the powder according to the present invention contains less than 10% by weight, more preferably less than 5% by weight, even more preferably less than 2% by weight, and most preferably less than 1% by weight of sodium bicarbonate, calcium carbonate, aluminum hydroxide, erythritol, glycine, trehalose, tagatose, cyclodextrin, or a mixture thereof.
[0046] In another preferred embodiment of the invention, based on the total weight of the powder, the powder contains less than 10% by weight, preferably less than 5% by weight, more preferably less than 2% by weight, and most preferably less than 1% by weight of one or more compounds, said one or more compounds having a melting point >170°C, more preferably >165°C, and most preferably >160°C, and / or having a solubility in water at 25°C >10 g / L, preferably >5 g / L, more preferably >2 g / L, and most preferably >1 g / L.
[0047] The powder according to the invention comprises an active ingredient (active component). According to the invention, an active ingredient is understood to be an active ingredient that generally has an effect on teeth or on the human or animal body. Preferred active ingredients according to the invention are pharmaceutically active compounds, tooth fluoride agents, or tooth remineralizing agents; more preferably, anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, bone growth factors, tooth fluoride agents, and tooth remineralizing agents (tooth repair agents).
[0048] The anti-inflammatory agent according to the present invention is preferably selected from acetylclofenac, acemetidine, acetaminophen, acetylsalicylic acid, alclofenac, amineprofen, α-bisabolol, amantadine, bromofenac, benzene Profen, benpiridone, permoprofen, bromosalicylic acid, buccal, butylbenzyl hydroxy acid, butylpropionate diphenylhydrazine, butebufen, carbofen, guimethicone, cyclochloroindica acid, chlorpheniramine maleate, diclofenac sodium, diflunisal, ditazol, enfenamic acid Acid), ε-acetaminophen, bendazac, etodoxacin, etofenamic acid, biphenylacetic acid, fenbufen, fenclofen, benzoinsalic acid, fennoprofen, fentimic acid, fepradiol, flufenamic acid, flunorprofen, flurbiprofen, gentianic acid, glucosinolate, ethylene glycol salicylate, isobutyric acid, ibuprofen, isobutyroxen, indomethacin, indoprofen, triphenylazole acid, isocolic acid, isoxic acid, ketoprofen, ketoprofen, lornoxicam, Lonazola, lorazoxic acid, cloprofen, meclofenamic acid, meloxicam, mesalazine, mexaazinic acid, mupirocin, mupirocin, naproxen, nifluoxetine Acids, oxalacil, oxasilor, oxamexin, oxaprazine, oxacrine, hydroxyphenylbutazone, renitoline, persamide, pelisozazole, phenyl salicylate, pyrazole acid, piroxicam, piroxicam, piroxicam, pranoprofen, propionic acid, propionic acid, acetylsalicylic acid, salicylic acid, salicylamide O-acetic acid, salicylsulfonic acid, sulfasalazine, sulindac, sulofen, succinate, tannic acid ester, tenoxicam, terfenadine, thiamethoxam, thiamethoxam, tenoridone, tofenamic acid, tometetin, Tropesin, simmoprofen, zaltoprofen, zilutone, and zolenic acid.
[0049] Antimicrobial agents are preferably selected from sulfonamides, phenols, quaternary ammonium salts, and hexadecylpyridine chloride. (CPC), chlorhexidine and its salts. Preferred antibacterial agents include penicillin, cephalosporins, tetracycline, doxycycline, chloramphenicol, and erythromycin.
[0050] The preferred bone growth factor is Emdogain. ® (Enamel matrix derivatives), BMP (bone morphogenetic protein), or calcium phosphate. The fluorinating agent can be any fluoride-containing or fluoride-delivering compound, such as fluoride salts, like sodium fluoride or aminofluorides. The remineralizing agent is preferably selected from bioglass, nano-hydroxyapatite, amorphous hydroxyapatite, and calcium phosphate.
[0051] Preferably, the powder according to the invention for use in treating tooth surfaces with a powder spraying device consists of the described components.
[0052] Preferably, a coating on the tooth surface is obtained when the powder jetting device is used in a typical process also used for cleaning teeth with a powder jetting device, and the deposition efficiency of the powder according to the invention, measured in percentage (defined as the mass of powder adhering to the surface divided by the mass of powder jetted toward the surface) is ≥1%, more preferably ≥3%, or even more preferably ≥5%.
[0053] Surprisingly, fatty acids, hydroxyl-substituted aromatic compounds, and sterols were found to be particularly effective in terms of deposition efficiency, defined as the amount of powder adhering to the surface relative to the amount of powder delivered from the device. The deposition efficiency of fatty acids, sterols, and hydroxyl-substituted aromatic compounds was ten times that of PLGA used in the prior art (poly(lactic acid-copolymer-glycolic acid)).
[0054] According to the embodiments, one reason for this improved efficiency is considered to be the melting point of fatty acids, sterols, and hydroxyl-substituted aromatic compounds, since the melting point of PLGA is typically between about 170°C and 200°C, depending on the ratio of lactic acid to glycolic acid in the PLGA (95:5, with a melting point of about 173°C, and 10:90, with a melting point of about 200°C). However, powders with melting points below 165°C according to the invention produce a more effective coating and thus a more efficient powder deposition when used in powder spraying devices for treating tooth surfaces.
[0055] For drug delivery, powders can contain active ingredients such as anti-inflammatory agents (e.g., aspirin) and bone growth factors (e.g., BMP, Emdogain). ® Additives include calcium phosphate, antimicrobial agents (e.g., CPC, chlorhexidine, antibiotics), fluorinating agents (sodium fluoride, amino-fluoride, etc.), dental restorative agents (nano-hydroxyapatite, amorphous hydroxyapatite, calcium phosphate), or desensitizing agents (arginine, potassium chloride). The concentration of additives is typically from 0.1% to 30% by weight, based on the total weight of the powder.
[0056] The powder used for treating tooth surfaces with a powder jetting device is preferably a therapeutic powder used for treating tooth surfaces with a powder jetting device.
[0057] The present invention also relates to a coating that can be obtained by applying powder according to the invention to a surface, preferably to a tooth surface, using a powder spraying device. The average thickness of the coating is preferably <100 μm, more preferably <50 μm, and most preferably <20 μm.
[0058] The above-mentioned coating thickness is the average thickness, which is determined by calculating the arithmetic mean of 3 to 5 thickness measurements. The thickness is determined by optical measurement (e.g., 3D microscopy) of the step height between the uncoated and coated surfaces (Keyence, VH-6000).
[0059] The present invention also relates to the use of the powder according to the invention in treating or applying powder to the tooth surface. The present invention further relates to the use of the powder according to the invention in a powder spraying device. This use includes powder spraying, wherein the powder according to the invention is sprayed onto the tooth surface together with a gaseous carrier medium, particularly air, using a powder spraying device.
[0060] The present invention also relates to a method for forming a coating on a tooth surface by applying a powder according to the invention onto the tooth surface using a powder spraying device. The present invention further relates to a coating on a tooth surface obtainable by applying a powder according to the invention onto the tooth surface using a powder spraying device.
[0061] The following embodiments provide preferred embodiments of the invention and further illustrate the invention.
[0062] Example
[0063] The carrier used is called MESOPOROSIL ® Mesoporous silica. The powder has an average pore size (d) of 4 nm as measured by the BJH method. 50 ) and 0.3 cm 3 g -1 The pore volume.
[0064] Mix 50 mg of chlorhexidine diacetate (CAS 206986-79-0, ref C6143, SIGMA-Aldrich) with 50 mg of mesoporosil ® Mix with 2.5 mL of a water-ethanol mixture containing 70% ethanol. Stir the mixture for 24 hours to ensure deep penetration of the active ingredient into the pores.
[0065] After this contact time, the solid contents were centrifuged twice at 6000 rpm for 10 minutes each time. The supernatant was then replaced first with a fresh 70% water-ethanol mixture, followed by demineralized water. The residue was then filtered, washed with demineralized water, and dried in an oven at 40°C for 24 hours.
[0066] Then 20 mg of loaded MESOPOROSIL was added to 180 mg (10% by weight) of milled cholesterol powder (d 50 =20 micrometers). Stir the mixture magnetically in a beaker for 30 minutes to ensure uniform distribution.
[0067] The 200 mg powder was then poured into a HANDY 3.0 PERIO (ref: FT-221, EMS Switzerland). The HANDY was operated using only dry air at an inlet static pressure of 3 bar. The powder was sprayed onto a glass plate (75 mm × 25 mm, VWR, 631-1553) with rapid sweeping over a period of 20 seconds to cover the maximum surface area. The nozzle-to-plate distance was 3 mm. The non-sticky powder on the glass was then removed with 3 bar compressed air.
[0068] The glass plate was then placed in 15 mL of artificial saliva (Ringer's solution, Merk, 1.15525.0001), and aliquots were taken periodically and measured using standard HPLC methods to determine the concentration of the active ingredient in the solution.
[0069] The following are typical release curves showing the percentage of released active material relative to the total active material added to the initial mixture.
[0070]
Claims
1. A powder for use in the treatment of a dental surface with a powder jet device, characterized in that, The powder comprises: (a) an organic compound in powder form, wherein the organic compound has a melting point of 35°C to 170°C and a solubility in water at 25°C of < 10 g / l; (b) a material in powder form having pores, the material comprising pores with a pore diameter < 50 nm, wherein the average particle size d 50 < 50 μm; and (c) an active ingredient adsorbed in the pores of the material.
2. The powder according to claim 1, characterized in that, The material comprises pores with a pore diameter of < 20 nm.
3. The powder according to claim 1 or 2, characterized in that, The average particle size d of the material 50 < 20 μm, preferably < 10 μm.
4. The powder according to any one of the preceding claims, characterized in that, 90% of the cumulative pore volume of the material is from pores with a pore diameter of < 20 nm, preferably < 15 nm.
5. The powder according to any one of the preceding claims, characterized in that, The organic compound has a melting point of 35°C to 160°C and / or the organic compound has a solubility in water at 25°C of < 5 g / l.
6. The powder according to any one of the preceding claims, characterized in that, The organic compound is selected from the group consisting of fatty acids, fatty alcohols, sterols, hydroxy-substituted aromatic compounds and mixtures thereof.
7. The powder according to claim 6, characterized in that, The fatty acid is selected from the group consisting of tridecanoic acid, pentadecanoic acid, palmitic acid, heptadecanoic acid, stearic acid, arachidic acid and mixtures thereof, and / or the fatty alcohol is selected from the group consisting of stearyl alcohol and lauryl alcohol, and / or the sterol is selected from the group consisting of cholesterol, beta-sitosterol and mixtures thereof, and / or the hydroxy-substituted aromatic compound is selected from the group consisting of butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA) and mixtures thereof.
8. The powder according to any one of the preceding claims, characterized in that, The powder comprises: (a) ≥ 60 wt.-% of the organic compound based on the total weight of the powder, and / or (b) ≤ 30 wt.-% of the material having pores in powder form based on the total weight of the powder, and / or (c) 0.1 wt.-% to 10 wt.-% of the active ingredient based on the total weight of the powder.
9. The powder according to any one of the preceding claims, characterized in that, The material is silica and / or a zeolite.
10. The powder according to any one of the preceding claims, characterized in that, The active ingredient is selected from the group consisting of pharmaceutically active compounds, dental fluoridating agents, dental remineralizing agents and mixtures thereof, preferably from the group consisting of anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, bone growth factors, dental fluoridating agents, dental remineralizing agents and mixtures thereof.
11. The powder according to any one of the preceding claims, characterized in that, The powder comprises less than 5 wt.-% of a compound selected from the group consisting of sodium bicarbonate, calcium carbonate, aluminum hydroxide, sugar alcohols, amino acids, sugars, cyclodextrins and mixtures thereof.
12. The powder according to any one of the preceding claims, characterized in that, The use in the treatment of a dental surface with a powder jetting device is the use in the coating of a dental surface with a powder jetting device.
13. A coating on a dental surface obtainable by applying a powder according to any of the preceding claims to a dental surface with a powder jetting device.
Citation Information
Patent Citations
antibiotic / antibiotics preparation with delayed release of active ingredient
DE10114244A1
Device for treating a periodontal disease
EP2455064A1