CN102416002A - Composition for precursor gel type fluoride chewing tablet - Google Patents
Composition for precursor gel type fluoride chewing tablet Download PDFInfo
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- CN102416002A CN102416002A CN2011103756182A CN201110375618A CN102416002A CN 102416002 A CN102416002 A CN 102416002A CN 2011103756182 A CN2011103756182 A CN 2011103756182A CN 201110375618 A CN201110375618 A CN 201110375618A CN 102416002 A CN102416002 A CN 102416002A
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Abstract
According to the invention, fluorides and accessories in pharmacy are prepared to form compact fluoride-containing Carbomer precursor gel particles by using a method in pharmacy; then, the fluoride-containing Carbomer precursor gel particles and pharmaceutically acceptable accessories are pressed to prepare chewing tablets. The chewing tablets can form gel which has a certain degree of viscosity and can cover on the surfaces of teeth, gums and oral cavity, thereby enabling drugs to retain on the surfaces of teeth, gums and oral cavity and to play a good role in inhibiting dental caries.
Description
Background technology
The fluoride preventing decayed tooth is to use the most effectively preventing decayed tooth means at present in the world.Fluorion can combine the apatite crystal of tooth and skeleton, makes it stable, and fluoride also can be attached to enamel surface, increases antiacid preventing decayed tooth ability.Fluoride can make the enamel remineralization of decalcification or hypocalcification, and is all very important to the utilization of the hardness of dentium nitor and skeleton, calcium, phosphorus.
The modes such as toothpaste agent, paste or employing fluoration foam that normally fluoride are prepared at present make tooth fully contact with fluoride with dental bed, absorb fluorion through dental bed, oral mucosa and tooth, reach the purpose of treatment and control dental caries.
At present relevant fluoride dosage form patent has the toothpaste agent; Buccal tablet and collutory etc.; Number of patent application is 95194280.8 to disclose a kind of improvement and stablize the antiseptic toothpaste compositions; Contain quintessence oil and a kind of or contain the antibiotic and dental caries dentifrice composition of improvement stable acidic of kind of fluorine compounds, be between 3.0 to 5.5 at pH value more.96115512.4 patent a kind of dental caries prevention fluoration foam is disclosed by sodium fluoride, stannous fluoride, sodium monofluorophosphate, strontium chloride; Calcium lactate, Ethyl linoleate, sodium laurylsulfate; Essence and distilled water are formulated, and damaged tooth is had mineralising repair once more.Application number is 200910042664.3 to disclose a kind of fluorine-containing anti-caries lozenge, comprises following raw materials by weight percent: sodium fluoride 0.01%, calcium lactate 5%, casein titanium phosphate 8%, stevioside 10%, Sorbitol 12%, microcrystalline Cellulose 14%, magnesium stearate 2%, essence 2%, surplus are the fluorine-containing buccal tablet of starch prescription.
These methods can make tooth and dental bed touch fluoride, have alleviated the symptom of dental caries to a certain extent.But these modes of taking medicine exist consumption to be difficult to fix, and contact site and time are difficult to control, use inconvenient shortcoming, and the effect of fluoride preventing decayed tooth is had a greatly reduced quality.
In the process that dental caries is treated, fluoride can be adsorbed on the surface skin of tooth when dental surface cleans, make tooth firmer, and taking care of one's teeth prevents decayed tooth.Root surface increases fluoride forming " softer " naturally in local fluoride administration, also helps to protect root of the tooth, makes root of the tooth lower sensitivity.The local mode fluoride is from fluorine-containing toothpaste, collutory, gel and directly be coated in the jaqan on the tooth.When the dentistry routine inspection, can coat local fluoride for the child usually, local fluoride contact treatment is to absorb one of fluorine the best way.
The another kind of method that extensively is used is " full mouth is coated with fluorine ".Full mouth is coated with the good opportunity that fluorine provides tooth to contact with fluoride.So-called complete mouthful is coated with fluorine is exactly to be coated on the fluoride of height with concentration uniformly on the surface of all teeth by the dentist, let fluoride absorbed by tooth after, the fluoride that dentist again will be unnecessary is removed totally.
Common treatment means is that fluorine-containing toothpaste is limited for the therapeutic effect of children caries with fluorine-containing toothpaste and sodium fluoride oral formulations at present, because child's tooth-brushing habit is difficult to form, the time of brushing teeth is difficult to control.The application of fluorine-containing oral formulations should be a good route of administration, but the fluorine taken all is to absorb through gastrointestinal tract, and medicine has influence on therapeutic effect in the oral cavity without reserve and absorb.The fluorine-containing glue of chewing is a kind of good selection; Fluoride, gum base and other adjuvants are pressed into the tablet or the tablet of similar chewing gum; In the oral cavity, chew glue, fluoride is discharged in the oral cavity and is absorbed and play a role by mucosa, dental bed, because partially fluorinated thing can remain in the gum base; The mode that the individual chews glue also can cause the magnitude of recruitment of fluorine different with the time, and therapeutic effect has than big-difference.
The treatment means that the specialty oral cavity is coated with fluorine has quite difficulty for child and child; At first will go to the treatment place of specialty, the treatment of dental caries is a quite very long process, and the fluoride magnitude of recruitment is difficult to control in the therapeutic process; If the ill-matched words of child, such therapeutic effect can be very poor.
Fluoride chewable tablet of the present invention can well address these problems, taking convenience, and dosage is fixed; Has the fruit taste; The gel that can produce pastille after chewing covers the surface in dental bed and tooth and oral cavity, has promoted the absorption of fluorine, has guaranteed the therapeutic effect to dental caries.
Summary of the invention
Fluoride of the present invention provides medicine with the form of solid chewable tablet, and the medicine than the fluoride liquid preparation is convenient for carrying, and steady quality is easy to take.
The present invention realizes through following technical scheme; Adopt the macromolecular material carbomer; Earlier the adjuvant in carbomer, fluoride and the pharmaceutics is processed the carbomer precursor gel granule of fine and close fluoride through the method in the pharmaceutics, and then acceptable auxiliary in the carbomer precursor gel granule of fluoride and the pharmaceutics is pressed into chewable tablet.Through the mastication of tooth, tablet was chewed when this chewable tablet was taken, adjuvant dissolvings such as acceptable excipient, correctives in the pharmacy; And the carbomer precursor gel granule of fluoride runs into the moisture in the mouth, and constantly swelling has formed gel; This gel has certain viscosity, can cover the surface in tooth, dental bed and oral cavity, makes medicine be trapped in the surface in tooth, dental bed and oral cavity; Slowly discharge, thereby fluoride is absorbed from oral mucosa, reach best therapeutic effect.
Through the mastication of tooth, tablet is chewed when this chewable tablet is taken, granule and powder are met the continuous swelling of saliva; Form gel, this gel has certain viscosity, can cover the surface in tooth, dental bed and oral cavity; Make medicine be trapped in the surface in tooth, dental bed and oral cavity; Slowly discharge, thereby fluoride is absorbed from oral mucosa, reach best therapeutic effect; Adjuvants such as correctives, excipient discharge in gel simultaneously simultaneously, can improve mouthfeel, have improved the compliance of taking.
Carbomer is to be polymerized by the acrylic acid repetitive, is acrylic acid and allyl sucrose, and pi-allyl tetramethylolmethane ether cross-linked polymeric forms, and can be used as adhesive agent in the pharmacy, emulsifying agent, release regulator, the binding agent of tablet and thickening agent.In the present invention, having adopted carbomer and medicine to granulate becomes the carbomer precursor gel granule of fluoride, the chewing of oral when taking, and Dispersion of Particles, the water in granule and oral cavity combines to form gel, thus the release medicine plays therapeutical effect.
The present invention distinguishes the oral cavity, and to chew the characteristics of glue be the mastication of chewable tablet of the present invention through tooth, and granule runs into the moisture in the mouth, constantly swelling; Formed gel, this gel has certain viscosity, can under the dispute effect, cover tooth more uniformly; The surface in dental bed and oral cavity, thus make medicine be trapped in tooth, the surface in dental bed and oral cavity; Constantly discharge, thereby make fluoride, reach best therapeutic effect from buccal absorption.And to chew glue be in the oral cavity, to chew in the oral cavity, and gum base does not disperse, and its Chinese medicine, sweeting agent and other water soluble ingredient can be through chewing in the oral cavity, and medicine is along with saliva is dispersed in the oral cavity.The effect that can not reach coating, covers and fully absorb.
Fluoride is sodium fluoride and potassium fluoride in the fluoride chewable tablet of the present invention.It is 1mg (in the amount of fluorine)～10mg (in the amount of fluorine) that fluoride is used oral daily dose.A degree and day fluorine-containing amount of drinking water with body weight and scarce fluorine are calculated.
Fluoride chewable tablet of the present invention contains the carbomer precursor gel granule of fluoride, can form the surface that gel covers oral cavity, tooth and mucosa, contains acceptable excipient in the pharmaceutics in addition, filler, sweeting agent, correctives and lubricant etc.
In the present invention, the effect of adjuvant is to prevent that carbomer from assembling and that medicine is disperseed is inhomogeneous in the pharmaceutics, and assistant formation is prepared into fine and close granule, reaches better therapeutic effect.Adjuvant in these medicaments makes carbomer and sodium fluoride can form comparatively fine and close granule, and is easy to tabletting.
After a kind of several kinds of mixing of the adjuvant in medicine, carbomer, maltodextrin and the selected with medicament, sieve, so both prevented carbomer gathering itself; Cause the local bonding in bulk; Also can make the fluoride homodisperse, the granularity of carbomer is outbalance in the preparation process, generally speaking; The granularity of carbomer is controlled at 60 orders～120 orders in the preparation process, and preferred carbomer is that granularity is at 80 orders～100 purpose powder.
Maltodextrin and carbomer combine, and preparation carbomer precursor gel granule is met after the water, inspire particulate viscosity, make it better to stick on oral cavity, periodontal or the tooth.The present invention simultaneously finds to adopt the carbomer precursor gel granule of maltodextrin combined preparation, and density is big, is suitable for tabletting.
The weight ratio of fluoride and carbomer is 1: 20～1: 150, and preferred range was at 1: 80～1: 120.
The carbomer of different molecular weight and viscosity all can use with consumption in the present invention according to a certain percentage, can form the gel of fluoride in the oral cavity.Preferably there is the carbomer type that carbomer 910 is arranged, carbomer 934, Acritamer 940, carbomer 934 p, Carbopol 941 and carbomer 1342.
Prevent that carbomer from assembling and the pharmaceutic adjuvant of molding has microcrystalline Cellulose, sucrose, sorbitol, mannitol, starch, pre-paying starch etc. preferably have microcrystalline Cellulose, sorbitol, starch.Selecting for use of adjuvant in these pharmaceuticss can be one or more mixture wherein, and it is at 1: 0.1～1: 20 with the preferred ratio of carbomer, and preferred range is 1: 0.3～2, and these physicochemical property and technologies according to adjuvant are decided.
The dense granule of described fluoride through extrusion granulator with cross hot melt and extrude etc. and all can realize.Select the different processes preparation for use, the ratio of the adjuvant in fluoride, carbomer and the pharmaceutics is different.
Described extrusion granulator prepares the dense granule of fluoride, and concrete mode is that fluoride and carbomer are mixed, and adds an amount of ethanol moistening, and the preparation soft material joins the fluoride carbomer granule that is prepared in the extrusion granulator machine.。
The method of described hot melt extrusion granulator, concrete mode be that fluoride and carbomer are mixed, and join in the hot melt extruder, and design temperature selects the screen cloth in suitable aperture to process the carbomer granule of the fluoride of different big or small densifications.
Method such as wet granulation, the direct dry granulation of mixing also can be processed fine and close granule with the fluoride carbomer in the pharmaceutics, and the inventor is through contrast, and preferable methods is the method that extrusion granulator and hot melt are extruded.
The fluoride chewable tablet of the present invention's preparation has certain taste masking function, can cover the disagreeable taste of fluoride.
In the carbomer precursor gel preparation of granules process of fluoride, also can add acceptable auxiliary in other pharmacy of part, as: correctives, lubricant, aromatic improve taste and regulate other physicochemical properties.
The preparation of fluoride chewable tablet of the present invention is that sodium fluoride and carbomer are processed fine and close fluoride carbomer precursor gel granule through certain method; Dry; And then, be pressed into tablet with the carbomer granule of fluoride and filler, sweeting agent, correctives and the mix lubricant in the pharmaceutics.
Realization of the present invention adds binding agent to granulate again after also can the carbomer granule of fluoride and filler, sweeting agent, correctives etc. being mixed, and is pressed into the fluoride chewable tablet again with after the mix lubricant.
The particulate granularity of carbomer precursor gel of fluoride has considerable influence to the preparation of chewable tablet; In the present invention; No matter be to adopt the carbomer composition granule of fluoride and the direct mixed pressuring plate of adjuvant in the pharmacy, still carbomer granule and the adjuvant in the pharmacy with fluoride mixes, and granulates; The bake drying tabletting, it is the most suitable that the particulate granularity of the carbomer of fluoride is controlled between 18 orders～60 orders.Preferred granularity is 24 orders～40 orders size.
Because the existence of carbomer, the carbomer granule of fluoride has certain taste masking effect, has reduced the disagreeable taste of fluoride in the tablet.Use the consumption of correctives to reduce, mouthfeel is better simultaneously.
After the granule of preparation and the correctives in the pharmacy, pigment and other excipient fully mix, be pressed into the chewable tablet of 8～10kg hardness.
Acceptable correctives in any pharmacy naturally or synthetic all is applicable to chewable tablet of the present invention
Used lubricant can be silica sol, magnesium stearate, stearic acid, Pulvis Talci, magnesium stearate among the present invention, sodium stearyl fumarate, Macrogol 4000, the mixture of one or more of polyethylene glycol 6000.
Embodiment
Embodiment 1
The particulate preparation of the carbomer of fluorinated sodium
Sodium fluoride 1
Carbomer 50
Microcrystalline Cellulose 100
Microcrystalline Cellulose and 150 parts of weight ripple nurses of the sodium fluoride of 1 part of weight, 100 parts of weight are mixed, with 3 parts of dehydrated alcohol moistenings, the preparation soft material, 24 eye mesh screens are granulated, 60 ℃ of dryings, the carbomer granule of preparation fluoride is subsequent use.
The preparation of sodium fluoride chewable tablet:
Total amount:
With fluorinated sodium carbomer granule, mix with above-mentioned adjuvant, tabletting, the pressure 5～8kg of chewable tablet, diameter are 8mm.
Embodiment 2
The particulate preparation Unit Weight of fluorinated sodium carbomer (mg)
Sodium fluoride 1
Carbomer 50
Microcrystalline Cellulose 100
Microcrystalline Cellulose and 50 parts of weight ripple nurses of the sodium fluoride of 1 part of weight, 100 parts of weight are mixed, with 3 parts of dehydrated alcohol moistenings, mix, the preparation soft material is put in the extrusion granulator machine, and it is subsequent use to prepare fluoride carbomer granule through 24 eye mesh screens.
The preparation of sodium fluoride chewable tablet:
The carbomer granule and the above-mentioned adjuvant of fluorinated sodium are mixed, tabletting, pressure 5～8kg, diameter are 8mm.
Instance 3
Microcrystalline Cellulose and 40 parts of weight ripple nurses of the sodium fluoride of 3 parts of weight, 50 parts of weight are mixed, and with an amount of part of dehydrated alcohol moistening, the preparation soft material is put in the hot melt extruder, preparation fluorinated sodium carbomer granule, 60 ℃ of dry for standby.
Carbomer granule, microcrystalline Cellulose, sorbitol, maltodextrin, strawberry essence and the carmine lake of fluorinated sodium are mixed, and are that binding agent prepares soft material to contain the 5%HPC aqueous solution, and 24 eye mesh screens are granulated, 60 ℃ of oven dry, 24 eye mesh screen granulate; With the magnesium stearate of recipe quantity, micropowder silica gel mixes again, tabletting, and the pressure 5～8kg of chewable tablet, diameter are 9mm.
Embodiment 4
But the microcrystalline Cellulose of the sodium fluoride of 3 parts of weight, 50 parts of weight and the ripple nurse of 40 portions of weight sucrose and 80 parts of weight are mixed, join in the dry granulation machine, 60 mesh sieve granulate, the carbomer granule of preparation fluoride is subsequent use.
Fluorinated sodium carbomer granule, sorbitol, grape essence and purple lakes are mixed, and are that binding agent prepares soft material to contain 5% 30 POVIDONE K 30 BP/USP, 30 aqueous solutions, and 24 eye mesh screens are granulated, 60 ℃ of oven dry, 24 eye mesh screen granulate; Mix with the magnesium stearate of recipe quantity, tabletting, the pressure 5～8kg of chewable tablet, diameter are 9mm.
Embodiment 5
The microcrystalline Cellulose of the potassium fluoride of 3 parts of weight, 50 parts of weight, 20 portions of mannitol and 80 parts of weight ripple nurses are mixed,, mix with 5% an amount of polyvidone aqueous solution moistening, the preparation soft material, 40 eye mesh screens prepare fluoride carbomer granule, 60 ℃ of dry for standby.
Gross weight:
Carbomer granule, microcrystalline Cellulose, sorbitol, maltodextrin, flavoring banana essence, the yellow lake of fluorinated potassium are mixed, and are that soft material prepares soft material to contain 5% 30 POVIDONE K 30 BP/USP, 30 aqueous solutions, and 24 eye mesh screens are granulated, 60 ℃ of oven dry, 24 eye mesh screen granulate; With the magnesium stearate of recipe quantity, micropowder silica gel mixes again, tabletting, and the pressure 5～8kg of chewable tablet, diameter are 7mm.
Claims (7)
1. a precursor gel type fluoride chewable tablet compositions of treating children caries is made up of the carbomer precursor gel granule of fluoride and the adjuvant in the pharmaceutics.
2. the described fluoride of claim 1 is sodium fluoride and potassium fluoride.
3. the carbomer precursor gel granule of the described fluoride of claim 1 is to be extruded with the extrusion granulator method through hot melt by the adjuvants such as filler in fluoride, carbomer and the pharmaceutics to process fine and close granule.
4. the precursor gel granule of the carbomer of the described fluoride of claim 3, the granularity of carbomer is controlled at 60 orders～120 orders before the preparation, and preferably the granularity of carbomer is at 80 orders～100 orders.
5. the described carbomer of claim 4, preferred carbomer model is a carbomer 910, carbomer 934, Acritamer 940, carbomer 934 P, Carbopol 941 and carbomer 1342.
6. the carbomer precursor gel granule of the described fluoride of claim 5, the granularity behind its granulate is controlled between 18 orders～60 orders and is advisable.Most preferred granule is 24 orders～40 orders.
7. the described precursor gel type of claim 1 fluoride chewable tablet is to cover tooth, dental bed and oral mucosa place release fluoride performance therapeutical effect through chewing the gel that forms fluoride in the oral cavity.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011103756182A CN102416002A (en) | 2011-11-23 | 2011-11-23 | Composition for precursor gel type fluoride chewing tablet |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2011103756182A CN102416002A (en) | 2011-11-23 | 2011-11-23 | Composition for precursor gel type fluoride chewing tablet |
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| CN102416002A true CN102416002A (en) | 2012-04-18 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110812331A (en) * | 2018-08-10 | 2020-02-21 | 北京普德康利医药科技发展有限公司 | Flurbiprofen pharyngeal retention particle |
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| CN1758897A (en) * | 2003-01-15 | 2006-04-12 | 高露洁-棕榄公司 | Liquid tooth whitening gel |
| CN101378722A (en) * | 2006-02-10 | 2009-03-04 | 株式会社Lg生活健康 | In-situ melting and gelling tablet composition for oral care |
| CN101829329A (en) * | 2010-05-11 | 2010-09-15 | 李少君 | Tooth antiallergic composition |
| CN101829026A (en) * | 2010-05-11 | 2010-09-15 | 李少君 | Composition for clearing tooth stains |
-
2011
- 2011-11-23 CN CN2011103756182A patent/CN102416002A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1758897A (en) * | 2003-01-15 | 2006-04-12 | 高露洁-棕榄公司 | Liquid tooth whitening gel |
| CN101378722A (en) * | 2006-02-10 | 2009-03-04 | 株式会社Lg生活健康 | In-situ melting and gelling tablet composition for oral care |
| CN101829329A (en) * | 2010-05-11 | 2010-09-15 | 李少君 | Tooth antiallergic composition |
| CN101829026A (en) * | 2010-05-11 | 2010-09-15 | 李少君 | Composition for clearing tooth stains |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110812331A (en) * | 2018-08-10 | 2020-02-21 | 北京普德康利医药科技发展有限公司 | Flurbiprofen pharyngeal retention particle |
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Application publication date: 20120418 |