Powder for the gradual release of active ingredients to teeth

Abstract

The present invention relates to a powder for use in tooth surface treatment using a powder jet device, wherein the powder comprises (a) an organic compound in powder form having a melting point of 35°C-170°C and a solubility of less than 10 g / L in water at 25°C, and (b) a porous material in powder form, comprising pores with a pore diameter of less than 50 nm and an average particle size d 50 The present invention relates to a powder comprising (c) a material having a pore size of less than 50 μm, and an active ingredient absorbed into the pores of the material.

Description

[Technical Field]

[0001] The present invention relates to a powder for use in tooth surface treatment using a powder jet device that enables the sustained release of active ingredients to the tooth. The present invention further relates to a coating on the tooth surface obtained by applying the powder. [Background technology]

[0002] Professional dental preventive care is an important regular procedure that helps maintain oral hygiene because it removes biofilm and tartar that patients cannot remove during their daily home dental care. Professional dental preventive care, including powder jet cleaning or air polishing, is particularly effective because it allows for cleaning of all tooth surfaces and interdental spaces, as well as implants, brackets, and instruments. Professional dental preventive care is an important procedure that helps maintain oral hygiene because it removes biofilm and tartar that patients cannot remove during their daily home dental care.

[0003] In the powder jet cleaning process, a powder jet device is used, in which powder is sprayed onto the tooth surface along with a gaseous carrier medium (usually air), enabling efficient cleaning of the teeth. In addition to, or instead of, a liquid carrier medium (e.g., water) may be used. Powder jet cleaning is performed using a powder jet device. Furthermore, powder jet cleaning is particularly effective because it does not require repetitive movements. Moreover, it is faster and requires relatively little training to master compared to other cleaning methods.

[0004] The clean teeth obtained after powder jet cleaning present an opportunity to enhance the effects of, for example, tooth fluoride treatment or remineralization, as the product easily comes into direct contact with the tooth surface. However, additional chemical treatments generally require longer contact times to induce chemical reactions. Examples of these additional chemical treatments include tooth fluoride treatment to improve the acid resistance of enamel, tooth remineralization to repair the outer portion of the tooth, antibacterial treatment to delay the recolonization of biofilm, or healing aids using anti-inflammatory components or bone growth factors.

[0005] For supragingival treatments such as fluoride treatment, creams or varnishes that can be deposited on the tooth are available. Patent Document 1 discloses polymer filling sheets such as Periochip for subgingival treatments. Patent Document 2 describes, for example, thick gels such as Ligosan for maintaining antibacterial properties in the subgingival region.

[0006] However, all these methods have limitations. For supragingival deposition, the contact time is often too short to achieve the desired chemical effect. Generally, a contact time of at least several hours may be necessary. However, patients usually do not want to remain on the dental chair for more than 20 minutes to initiate a chemical reaction. Furthermore, the aqueous environment of the mouth rapidly dissolves and removes all water-soluble compounds. For subgingival additives, there is a flow of bodily fluids that drains all chemicals that are not fixed within the pocket. However, fixing the active ingredients in the presence of a sufficiently thick support material also creates a barrier to soft tissue reattachment. Moreover, higher product concentrations are required.

[0007] In developing this invention, it was found that powders containing organic compounds with a melting point preferably below 165°C can form a coating on tooth surfaces when applied by a powder jet device. This coating may contain an active ingredient or active component. However, further investigation has shown that most active ingredients are released very quickly. [Prior art documents] [Patent Documents]

[0008] [Patent Document 1] European Patent Application Publication No. 2455064 [Patent Document 2] German Patent Application Publication No. 10114244 [Overview of the Initiative] [Problems that the invention aims to solve]

[0009] Therefore, the object of the present invention is to provide a tooth surface protection system that overcomes the above-mentioned problems, which is easily applicable and allows for gradual delivery of active ingredients to the tooth surface. [Means for solving the problem]

[0010] This objective is achieved, according to the present invention, by a powder for use in tooth surface treatment using the powder jet device described in claim 1. This objective is also achieved by a coating described in claim 13. Preferred embodiments of the present invention are according to the dependent claims and the following description. [Modes for carrying out the invention]

[0011] One embodiment of the present invention relates to a powder for use in tooth surface treatment using a powder jet device, wherein the powder is (a) an organic compound in powder form having a melting point of 35°C-170°C and a solubility of less than 10 g / L in water at 25°C, (b) A material in the form of a porous powder, comprising pores with a diameter of less than 50 nm and with an average particle size d 50 Materials with a thickness of less than 50 μm, (c) The active ingredient absorbed into the pores of the material.

[0012] Surprisingly, it has been found that when the powder according to the present invention is applied to a tooth surface using a powder jet device, it provides a coating on the tooth surface that protects the tooth and provides a sustained release of the active ingredient to the tooth surface. When the powder according to the present invention is ejected onto a surface with an airflow, i.e., when the powder is used in a powder jet device commonly used to clean tooth surfaces, the powder adheres to the tooth surface and forms a coating. Although not limited to this description, it is thought that the kinetic energy delivered to the powder causes it to undergo a melting process at the point of impact with the tooth surface, forming a coating on the tooth surface (kinetic melting). 50 The small average particle size of the material, less than 50 μm, ensures that the material is not abrasive so that the coating is not removed. The active ingredient is not present in the structure of the organic compound forming the coating (in which case release is known to be very rapid), but is absorbed into the pores of the material, thereby ensuring sustained release.

[0013] One advantage of the powder according to the present invention is that, when used in conventional powder jet devices, the coating is delivered to the correct position on the tooth surface. The powder comprises an organic compound, a porous material, and an active ingredient absorbed into the pores of the material. The active ingredient or active component may be, for example, a pharmaceutically active compound, i.e., a component, which means a therapeutically effective amount of the pharmaceutically active compound, i.e., a component.

[0014] The term "treating tooth surface(s)" means, in the context of the present invention, "applying to tooth surface(s)". Treatment of the tooth surface, i.e., application to the tooth surface, is a typical use of a powder jet device, in which case the powder is ejected onto the tooth surface together with a carrier medium (e.g., air). In a preferred embodiment of the present invention, the powder for use in treating tooth surfaces using a powder jet device is the same powder as that for use in coating tooth surfaces using a powder jet device. The treatment is preferably a therapeutic treatment, and the use of the powder in the treatment is preferably a therapeutic use in the treatment.

[0015] By means of controlled release, an active ingredient, preferably a pharmaceutically active compound, a dental fluoridating agent or a dental remineralizing agent, can act on the tooth surface or remain on the tooth surface long enough to deliver the active ingredient directly from this coating to the tooth surface (i.e., to the correct position). The controlled release of the active ingredient is ensured by absorption into the pores of the pore-containing material and incorporation into the coating. Absorption into the pores of the material can be achieved, for example, by adding a solution of the active ingredient in a solvent to the porous material and evaporating the solvent.

[0016] The powder according to the present invention can be easily applied using a conventional powder jet device, especially after tooth cleaning, and the same powder jet device can be used for cleaning and subsequently applying the powder according to the present invention to the cleaned tooth surface. Only the powder needs to be replaced.

[0017] In a preferred embodiment of the present invention, the powder for use in treating tooth surfaces using a powder jet device contains an organic compound having a melting point of 35°C - 170°C and a solubility in water at 25°C of less than 10 g / L, based on the total weight of the powder, of 30% by weight or more, more preferably 50% by weight or more, even more preferably 60% by weight or more, and most preferably 70% by weight or more.

[0018] In a preferred embodiment of the present invention, the powder for use in the treatment of tooth surfaces using a powder jet device contains, based on the total weight of the powder, 40% by weight or less, more preferably 30% by weight or less, even more preferably 20% by weight or less, and most preferably 15% by weight or less of a porous powder-form material.

[0019] According to a preferred embodiment of the present invention, the powder contains 0.01% to 20% by weight, based on the total weight of the powder, of an active compound, i.e., an active ingredient. 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 the active ingredient, based on the total weight of the powder.

[0020] Within the scope of the present invention, it is understood that the amounts of the components of the powder given in weight-% (weight-%) add up to 100%. An example is a powder containing 50% by weight of an organic compound, 40% by weight of a porous material, 7% by weight of an active ingredient, and 3% by weight of additional components such as a flow aid, flavoring agent, etc.

[0021] The organic compound according to the present invention is understood to be a compound containing one or more carbon atoms, particularly a carbon skeleton. In a preferred embodiment of the present invention, the melting point of the organic compound in the powder for use in the treatment of tooth surfaces using a powder jet device is from 35°C to 165°C, more preferably from 37°C to 162°C, even more preferably from 40°C to 158°C, and most preferably from 42°C to 156°C. The low melting point promotes mechanical melting, thus providing an advantageous coating. The solubility of the organic compound in water at 25°C is preferably less than 5 g / L (grams / liter), more preferably less than 2 g / L, and most preferably less than 1 g / L in water at 25°C. The solubility in water relates to distilled water (pH about 7.0). The limited solubility in water enhances the stability of the coating in the oral aqueous environment.

[0022] In the course of the present invention, it was found that the organic compounds of the powder according to the present invention are preferably selected from the group consisting of fatty acids, aliphatic alcohols, sterols, hydroxysubstituted aromatic compounds, and mixtures thereof. Fatty acids, aliphatic alcohols, sterols, and hydroxysubstituted aromatic compounds can, where possible, be optionally substituted, (partially) saturated, or both.

[0023] The fatty acids are preferably carboxylic acids 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.

[0024] The aliphatic 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.

[0025] The sterol is preferably selected from the group consisting of cholesterol, beta-sistosterol, campesterol, stigmasterol, ergosterol, brazicasterol, and mixtures thereof. The sterol is more preferably cholesterol and / or beta-cystosterol.

[0026] The hydroxy-substituted aromatic compound is preferably hydroxybenzene or hydroxytoluene, preferably butylated hydroxytoluene (BHT) or butylated hydroxyanisole (BHA). The most preferred hydroxy-substituted aromatic compound is butylated hydroxytoluene (BHT).

[0027] The advantage of using the above organic compounds as powders to form coatings or depositions is that the organic compounds form a layer on the surface. The porous substrate (tooth) is not clogged, and as a result, the exchange with the tooth surface environment is not significantly altered. Furthermore, biological functions such as tissue adhesion are also not inhibited. In addition, the diffusion of fluids within the medium can also be used to fine-tune the delivery of active ingredients.

[0028] The powder according to the present invention is deposited on the tooth surface by kinetic energy delivered to the powder along with air. Deposition can be made above the gingival margin on enamel or exposed dentin using, for example, a standard EMS Airflow handpiece, or below the gingival margin using, for example, an EMS Perioflow subgingival nozzle. In a preferred embodiment of the present invention, the powder is injected toward the tooth surface using a powder jet device in conjunction with a gaseous carrier medium (particularly air). The powder is injected toward the tooth surface along with air. The air may contain water, preferably less than 10 mL / min, particularly less than 5 mL / min. In a preferred embodiment, the powder jet device is used in the absence of water.

[0029] The use of the powder jet device according to the present invention when treating a tooth surface means spraying powder onto the tooth surface using a conventional powder jet device. The powder then forms a coating on the tooth surface.

[0030] In the context of the present invention, d 50 The value (average particle size) is such that 50% of the particles are d in terms of volume. 50 Smaller than the value, 50% of the particles are d in terms of volume. 50 The particle size is larger than the value. This is because d 90 This also applies to the values, with 90% of the volume being d 90Less than the value. The d value according to the present invention is determined by the laser diffraction method using a dry dispersion unit (Malvern Mastersizer 2000 manufactured by Malvern, operating at 150 kPa and equipped with a Scirocco dry dispersion unit).

[0031] The average particle diameter d of the material 50 is less than 50 μm, preferably less than 20 μm, more preferably less than 10 μm. d 90 is preferably less than 120 μm, more preferably less than 100 μm, and even more preferably less than 80 μm.

[0032] The porous powder-form material according to the present invention is preferably a porous material. The porous material according to the present invention is understood as a porous material. This means that the porous powder-form material can also be called a porous material in powder form. This porous powder-form material contains pores with a pore diameter of less than 50 nm, preferably less than 50 nm and greater than 2 nm. Such a material can also be called a mesoporous material. According to the present invention, the porous powder-form material preferably contains pores with a pore diameter of less than 20 nm, more preferably less than 10 nm. In any case, the pores are more preferably greater than 2 nm. In a preferred embodiment of the present invention, the porous powder-form material is silica and / or zeolite.

[0033] The pore size or diameter and cumulative pore volume of a material are measured by nitrogen absorption according to the BJH method (Barrett-Joyner-Halenda method) (ISO 9277:2010), which is a BET method. The results of this BJH method are pore volume and cumulative pore volume dependent on pore diameter, i.e., pore size distribution. See EP Barret, LG Joyner, PH Halenda, J. Am. Chem. Soc., Vol.73, 1951, p.373; JC Groen, LAA Peffer, J. Perez-Ramirez, Microporous Mesoporous Mater., Vol.60, 2003, p.1; SJ Gregg, KSW Sing, “Adsorption, Surface Area and Porosity”, 2nd edition, Academic Press, London, 1982.

[0034] In a preferred embodiment of the present invention, 90% of the cumulative pore volume of the material in the form of a porous powder consists of pores with a pore diameter of less than 20 nm, more preferably less than 15 nm, and most preferably less than 8 nm.

[0035] According to the present invention, the active ingredient (active compound) understood to have an effect on teeth or the human or animal body may preferably be a pharmaceutically active compound, a tooth fluoride treatment agent, or a tooth remineralizer. Thereafter, the present invention makes it possible to create an intelligent delivery system for the active ingredient (e.g., a pharmaceutically active compound) that is positioned on the tooth surface and involves the release of the active ingredient.

[0036] The active ingredients according to the present invention are preferably selected from the group consisting of anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, bone growth factors, tooth fluoride treatment agents, and tooth remineralizing agents. Anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, and bone growth factors are understood to be pharmaceutically active compounds, i.e., pharmaceutically active ingredients. The powder may contain one or more active ingredients (e.g., one, two, three, four, or five). The powder may also contain one or more organic compounds and / or one or more porous materials (e.g., one, two, three, four, or five).

[0037] The powder according to the present invention refers to a substance in the form of small particles. The average particle size (d) of the powder according to the present invention (i.e., the entire powder including organic compound particles and material particles) 50 The particle size is preferably 0.5 μm to 500 μm, more preferably 1 μm to 300 μm, even more preferably 2 μm to 200 μm, and most preferably 5 μm to 100 μm. The particle size can be adapted to the application. For example, for treating subgingival tooth surfaces, a smaller average particle size is preferred, particularly about 0.5 μm to 50 μm, and more preferably 1 μm to 30 μm. For treating supragingival tooth surfaces, a larger average particle size, preferably 0.5 μm to 200 μm, and more preferably 2 μm to 100 μm, can be used.

[0038] In a more preferred embodiment of the present invention, the powder further comprises a flow aid, a bleaching agent and / or a flavoring agent. The total amount of these additional substances is preferably 0.2% to 5% by weight, more preferably 0.5% to 2% by weight, based on the total weight of the powder.

[0039] The flow aid is preferably selected from the group consisting of silicon dioxide (silica, especially amorphous silica), aluminum silicate, and / or aluminum hydroxide. Silicon dioxide is more preferred, and in particular, is preferred in an amount of 0.2% to 3% by weight, most preferably 0.5% to 2% by weight, based on the total weight of the powder.

[0040] Preferred bleaching agents are peroxides such as magnesium peroxide, calcium peroxide, or zinc peroxide, or persulfates such as sodium persulfate, potassium persulfate, or ammonium persulfate, or perborates.

[0041] In preferred embodiments of the present invention, each powder comprises less than 10% by weight of abrasive powder (abrasive powder jet 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, based on the total weight of the powder.

[0042] According to the present invention, polishing powder, or polishing jet cleaning powder, means powder used in a powder jet device for cleaning tooth surfaces. The polishing powder, or polishing jet cleaning powder, is preferably sodium bicarbonate, calcium carbonate, aluminum hydroxide, algitol, amino acids, sugars, cyclodextrin, or a mixture thereof. Therefore, 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, algitol, amino acids, sugars, cyclodextrin, or a mixture thereof, based on the total weight of the powder. Algitol is preferably erythritol, and the amino acid is preferably glycine. The sugar is preferably trehalose or tagatose. Therefore, 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, erythritol, glycine, trehalose, tagatose, cyclodextrin, or a mixture thereof, based on the total weight of the powder.

[0043] In a more preferred embodiment of the present invention, the powder comprises, based on the total weight of the powder, one or more compounds having a melting point higher than 170°C, more preferably higher than 165°C, most preferably higher than 160°C, and / or a solubility in water at 25°C greater than 10 g / L, preferably greater than 5 g / L, more preferably greater than 2 g / L, most preferably greater than 1 g / L, based on the total weight of the powder.

[0044] The powder according to the present invention contains an active ingredient. According to the present invention, the active ingredient is generally understood to be an active ingredient that can have an effect on teeth or the human or animal body. Preferred active ingredients according to the present invention are pharmaceutically active compounds, tooth fluoride treatment agents or tooth remineralizing agents, more preferably anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, bone growth factors, tooth fluoride treatment agents and tooth remineralizing agents (tooth restorative agents).

[0045] The anti-inflammatory agents according to the present invention are preferably aceclofenac, acemetacin, acetaminosarol, acetylsalicylic acid, alclofenac, aluminoprofen, α-bisabolol, amfenac, bromfenac, benoxaprofen, benzpiperilone, belmoprofen, bromosaligenin, bucloxic acid, bufexamac, bumadizone, butibufen, carprofen, cinmethacin, cridanac, clopirac, diclofenac, diclofenac sodium, diflunisal, ditasol, enfenamic acid, bendazac ε-acetamidocaproate, etodolac, etofenamate, felbinac, fenbufen, fenclodic acid, fendosal, fenoprofen, fentiazac, fepraziol, flufenamic acid, flunoxaprofen, flurbipro Fen, gentisic acid, glucamethacin, glycol salicylate, ibufenac, ibuprofen, ibuproxam, indomethacin, indoprofen, isofezolac, isoxepac, isoxicam, ketoprofen, ketorolac, lomoxicam, lonazola, lonazolac, loxoprofen, meclofenamic acid, meloxicam, mesalamine, methiadic acid, mofebutazone, mofezolac, naproxen, niflumic acid, olsalazine, oxaseprole, oxamethacin, oxaprozin, oxicams, oxyfenbutazone, paraniline, parasalmid, perisoxal, phenyl salicylate, pyrazolac, piroxicam, pyrprofen, pranoprofen, propriodic acid The following are selected from the group consisting of Acids, brotidic acid, salacetamide, salicilic acid, salicylamide O-acetic acid, salicylic acid, sulfasalazine, sulindac, suprofen, suxibuzone, tarniflumate, tenoxicam, telofenamate, tiaprofenic acid, tiaramide, tinoridine, tolfenamic acid, tolmetin, tropesin, xymoprofen, zaltoprofen, diloton, and zomepirac.

[0046] The antimicrobial agent is preferably selected from the group consisting of sulfonamides, phenols, quaternary ammonium salts, cetylpyridinium chloride (CPC), chlorhexidine, and salts thereof. The antibacterial agent is preferably penicillins, cephalosporins, tetracyclines, doxycyclines, chloramphenicol, and erythromycin.

[0047] The bone growth factor is preferably Emdogain® (enamel matrix derivative), BMP (bone morphogenetic protein), or calcium phosphate. The tooth fluoride treatment agent may be any fluoride-containing compound or delivery compound such as fluoride salts (e.g., sodium fluoride or amino fluoride). The remineralizing agent is preferably selected from the group consisting of bioglass, nano-hydroxyapatite, amorphous hydroxyapatite, and calcium phosphate.

[0048] Furthermore, the powder used in tooth surface treatment using the powder jet device according to the present invention preferably consists of the described components. Preferably, when the deposition efficiency of the powder according to the present invention (defined as the amount of powder attached to the surface divided by the amount of powder injected toward the surface), measured in percent, is 1% or more, more preferably 3% or more, and even more preferably 5% or more, a coating of the tooth surface can be obtained by using the powder jet device in a typical process also used for cleaning teeth with a powder jet device.

[0049] Surprisingly, fatty acids, hydroxy-substituted aromatic compounds, and sterols were found to be particularly efficient in terms of deposition efficiency, defined as the amount of powder adhering to the surface versus the amount of powder delivered from the device. Fatty acids, sterols, and hydroxy-substituted aromatic compounds have a deposition efficiency 10 times higher than that of PLGA (poly(lactic acid-co-glycolic acid)) used in the prior art.

[0050] Since PLGA typically has a melting point of about 170°C–200°C depending on the ratio of lactic acid to glycolic acid in the PLGA (95:5 has a melting point of about 173°C, and 10:90 has a melting point of about 200°C), one of the reasons for this enhanced efficiency is considered to be the melting points of fatty acids, sterols, and hydroxy-substituted aromatic compounds, as exemplified. However, the melting point of the powder below 165°C according to the present invention provides a much more efficient coating when the powder is used in a powder jet device for treating tooth surfaces, and therefore a much more efficient deposition efficiency of the powder.

[0051] For drug release, the powder may contain active ingredients such as anti-inflammatory agents (e.g., aspirin), bone growth factors (e.g., BMP, Emdogain®, calcium phosphate), antimicrobial agents (e.g., CPC, chlorhexidine, antibiotics), fluoride treatment agents (e.g., sodium fluoride, amino fluoride), dental restorative agents (nanohydroxyapatite (nano-hap), amorphous hap, calcium phosphate), or desensitizers (arginine, potassium chloride). The concentration of the additive is usually between 0.1% and 30% by weight, based on the total weight of the powder.

[0052] The powder for use in tooth surface treatment using a powder jet device is preferably a powder for therapeutic use in tooth surface treatment using a powder jet device. The present invention also relates to a coating obtained by applying the powder according to the present invention to a surface (preferably a tooth surface) using a powder jet device. The coating preferably has an average thickness of less than 100 μm, more preferably less than 50 μm, and most preferably less than 20 μm.

[0053] The above coating thickness is the average thickness determined by calculating the arithmetic mean of 3 to 5 thickness measurements. The thickness is determined by optical measurement, e.g., 3D microscopy, or step height measurement between the uncoated and coated surfaces (Keyence, VH-6000).

[0054] The present invention also relates to the use of the powder according to the present invention in tooth surface treatment, i.e., the application of powder to the tooth surface. The present invention further relates to the use of the powder according to the present invention in a powder jet device. This use includes powder jetting, in which the powder according to the present invention is jetted onto the tooth surface using a powder jet device in conjunction with a gaseous carrier medium (particularly air).

[0055] The present invention further relates to a process for forming a coating on a tooth surface by applying the powder according to the present invention to the tooth surface using a powder jet device. The present invention also relates to a coating on a tooth surface obtained by applying the powder according to the present invention to the tooth surface using a powder jet device.

[0056] The following examples provide preferred embodiments of the present invention and further illustrate the present invention. Examples The carrier used is mesoporous silica named MESOPOROSIL®. This powder has an average pore size (d) measured by the BJH method. 50 The pore size is 4 nm, and the pore volume is 0.3 cm³. 3 g -1 That is the case.

[0057] Mix 50 mg of chlorhexidine diacetate (CAS 206986-79-0, model number C6143, SIGMA-Aldrich) with 2.5 mL of a water-ethanol mixture of 70% ethanol and 50 mg of MESOPOROSIL®. Stir this mixture for 24 hours to ensure that the active ingredient penetrates deeply into the pores.

[0058] After this contact time, the solids are centrifuged twice at 6000 rpm for 10 minutes each. The supernatant is then replaced first with a fresh water-ethanol 70% mixture, and then with demineralized water. The residue is then filtered, washed with demineralized water, and dried in an oven at 40°C for 24 hours.

[0059] Next, 20 mg of supported MESOPOROSIL is added to 180 mg (10% by weight) of crushed cholesterol powder (d 50 Add to (20 μm). To ensure a uniform distribution, magnetically stir this mixture in a beaker for 30 minutes.

[0060] Next, pour this 200 mg of powder into a Handy 3.0 Perio (model number: FT-221, EMS, Switzerland). Operate the Handy dry using only air at an inlet static pressure of 0.3 MPa. Spray the powder onto a glass plate (75 x 25 mm, VWR, 631-1553) for 20 seconds in a high-speed sweeping motion to cover the largest possible surface area. The distance from the nozzle to the plate was 3 mm. Remove any powder that did not adhere to the glass using compressed air at 0.3 MPa.

[0061] Next, a glass plate is placed in 15 mL of artificial saliva (Ringer's solution, Merk, 1.15525.0001), and aliquots are periodically taken and measured by standard HPLC to determine the concentration of the active ingredient in the solution.

[0062] A typical release profile is shown below, indicating the percentage of released active material relative to the total active material added to the initial mixture.

[0063] [Table 1]

Claims

1. A powder for use in tooth surface treatment using a powder jet device, wherein the powder is (a) an organic compound in powder form having a melting point of 35°C–170°C and a solubility of less than 10 g / L in water at 25°C, (b) A material in the form of a porous powder, comprising pores with a diameter of less than 50 nm and an average particle size d ５０ Materials with a thickness of less than 50 μm, (c) A powder comprising the active ingredient absorbed into the pores of the material.

2. The powder according to claim 1, wherein the material contains pores with a pore diameter of less than 20 nm.

3. The average particle size d of the material ５０ The powder according to claim 1 or 2, wherein the particle size is less than 20 μm, preferably less than 10 μm.

4. The powder according to any one of claims 1 to 3, wherein 90% of the cumulative pore volume of the material consists of pores with a pore diameter of less than 20 nm, preferably less than 15 nm.

5. The powder according to any one of claims 1 to 4, wherein the melting point of the organic compound is 35°C to 160°C, or the solubility of the organic compound in water at 25°C is less than 5 g / L, or both.

6. The powder according to any one of claims 1 to 5, wherein the organic compound is selected from the group consisting of fatty acids, aliphatic alcohols, sterols, hydroxysubstituted aromatic compounds, and mixtures thereof.

7. The powder according to claim 6, wherein 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; the aliphatic alcohol is selected from the group consisting of stearyl alcohol and lauryl alcohol; the sterol is selected from the group consisting of cholesterol, β-cystosterol, and mixtures thereof; and the hydroxy-substituted aromatic compound is selected from the group consisting of butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), and mixtures thereof.

8. (a) Based on the total weight of the powder, 60% by weight or more of the organic compound, (b) Based on the total weight of the powder, the material in the form of a porous powder at a concentration of 30% by weight or less, and (c) The powder according to any one of claims 1 to 7, comprising 0.1% to 10% by weight of one or more of the active ingredients based on the total weight of the powder.

9. The powder according to any one of claims 1 to 8, wherein the material is silica, zeolite, or both.

10. The powder according to any one of claims 1 to 9, wherein the active ingredient is selected from the group consisting of pharmaceutically active compounds, tooth fluoridating agents, tooth remineralizing agents, and mixtures thereof, and preferably selected from the group consisting of anti-inflammatory agents, antimicrobial agents, antibacterial agents, antiviral agents, bone growth factors, tooth fluoridating agents, tooth remineralizing agents, and mixtures thereof.

11. The powder according to any one of claims 1 to 10, wherein the powder contains less than 5% by weight of a compound selected from the group consisting of sodium bicarbonate, calcium carbonate, aluminum hydroxide, algitol, amino acids, sugars, cyclodextrin, and mixtures thereof.

12. The powder according to any one of claims 1 to 11, wherein the use in treatment of a tooth surface using a powder jet device is the use in coating a tooth surface using a powder jet device.

13. A coating on a tooth surface obtained by applying the powder described in any one of claims 1 to 12 to the tooth surface using a powder jet device.

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