WO2009009953A1

WO2009009953A1 - A composition of orally gargle tablet and preparative method

Info

Publication number: WO2009009953A1
Application number: PCT/CN2008/001284
Authority: WO
Inventors: Waiming Wong; Liangyuan Zheng
Original assignee: Waiming Wong; Liangyuan Zheng
Priority date: 2007-07-16
Filing date: 2008-07-07
Publication date: 2009-01-22
Also published as: CN101455620A

Abstract

An orally rapidly disintegrating gargle tablet, which comprising at least one of component for preventing decayed teeth and saprodontia, and/or at least one of component for inhibiting growth and aggregation of oral bacteria, and/or at least one of component for whitening teeth. The tablet is capable of dissolving more than 75% within thirty seconds.

Description

TECHNICAL FIELD The present invention relates to the field of oral hygiene and health care products, and relates to an oral rapid collapse mouthwash composition and a preparation method thereof.

Background technology

Book

Oral health is a mirror of human health. At present, most people's concept of oral care only stays in the understanding of "brushing teeth in the morning and evening." In fact, the method of brushing teeth can only eliminate 50% of dental plaque. "A comprehensive oral care program can't just brush your teeth." To ensure healthy teeth, a complete oral care regimen must be taken. For places where the toothbrush is difficult to reach, the mouthwash with bactericidal function can penetrate deeply and thoroughly clean the mouth. Targeted application of mouthwash not only ensures a healthy oral environment, but also enhances the public image and enhances the confidence of social activities. Mouthwash with a certain function is increasingly important in people's daily oral care. However, since the mouthwash is a liquid form, the package is bulky and inconvenient to carry, and is often restricted to carry when traveling by airplane or the like; it is not convenient for many people to use without a container. Therefore, the invention of a new oral care product with convenient carrying, simple use method and mouthwash effect will be beneficial to open up a new concept of oral health care, satisfying people in modern life, especially office workers, traveling and long time. The need for oral health care for people in outdoor activities. In addition, there are also effervescent tablet types of mouthwashes, but effervescent tablets require severe production conditions, high packaging costs, and use of acid-base pairs, which may cause irritation to the oral cavity and are limited in use. SUMMARY OF THE INVENTION It is an object of the present invention to provide a mouthwash sheet which has anti-caries and/or bacteriostatic and/or whitening functions and which can rapidly disintegrate in the oral cavity. To this end, the technical solution adopted by the present invention is:

The main functional component is a mixture containing one or any two or a mixture of two or more of the following formulas:

(1) at least one functional ingredient for preventing tooth decay and caries;

(2) at least one functional ingredient for inhibiting the growth and aggregation of oral bacteria;

(3) At least one functional ingredient for whitening teeth.

The above components may also contain:

At least one disintegrant to enable rapid disintegration of the tablet in the oral cavity;

The above components may further comprise:

(1) at least one soluble filler to adjust the disintegration speed and mouthfeel of the tablet;

(2) at least one filler having good disintegration properties to promote disintegration of the tablet;

(3) at least one sweetener for regulating the taste of the tablet;

(4) at least one cooling agent to maintain a fresh breath;

(5) at least one lubricant for lubricating when pressed;

(6) At least one binder for increasing the adhesion between the particles during granulation.

The functional component for preventing tooth decay and caries may be one of sodium fluoride (NaF), sodium monofluorophosphate (Na ₂ P0 ₃ F), stannous fluoride (SnF ₂ ), two or three compounds. The functional component for inhibiting the growth and aggregation of oral bacteria may be a cationic surfactant cetylpyridinium chloride, a nonionic surfactant triclosan; the functional component of whitening teeth may be hydrogen peroxide, peroxidation Urea.

The disintegrant is one or a mixture of two or more of the following: 1 crospovidone 2 croscarmellose sodium 3 sodium carboxymethyl starch 4 microcrystalline cellulose 5 hydroxypropyl cellulose.

The soluble filler is one or a mixture of two or three of the following: 1 mannitol 2 xylitol 3 sorbitol; a filler having good disintegration performance may be one of microcrystalline cellulose and hydroxypropyl cellulose. The sweetener is one or a mixture of any two or three of the following: 1 sucralose 2 stevioside 3 aspartame; the cooling agent is one or both of the following or Mixture of three kinds: 1 menthol 2 cool alcohol 3 spearmint; lubricant is one of the following or a mixture of any two or more: 1 stearic acid sodium fumarate sodium thiocyanate

3 decyl sulphate 4 polyethylene glycol 40005 polyethylene glycol 6000; the binder is one of the following or a mixture of any two or three: 1 povidone K30 2 hypromellose 3 carboxylate Methylcellulose.

The mouthwash sheet of the present invention has a time to disintegrate in the oral cavity within 30 seconds.

The mouthwash tablet of the present invention is a solid tablet which can rapidly disintegrate in the oral cavity and rapidly dissolve the active ingredient. When using, it is only necessary to use a small amount of water to directly contain strontium in the oral cavity, or to dissolve it with a small amount of water and then to contain strontium in the oral cavity.

The functional ingredients of the compositions of the present invention are, inter alia: sodium fluoride (NaF), cetylpyridinium chloride and urea peroxide; the main components thereof include:

Sodium fluoride 0.025%~20.0%

Cetylpyridinium chloride 铛 0.005%~30.0%

Urea peroxide 1.0%~60.0%

Soluble filler 30%~95%

Filler with good disintegration performance 2%~30%

Disintegrant 0.1%~15%

Lubricant 0.2%~5%

Sweetener 0.2%~4%

Cooling agent 0.1%~8% All percentages are mass percentage.

Sodium fluoride 0.15%~1.0% hexadecanoylpyridinium chloride 0.3%~2.0% carbamide peroxide 3.5%~20% soluble filler 51%~88% Filler with good disintegration performance 5%~20%

Disintegrant 0.3%~10%

Lubricant 0.5%~2%

Sweetener 0.5%~2%

Cooling agent 1%~5%

All percentages are by mass.

The mouthwash tablet of the present invention is specifically used by: using a small amount of water to directly contain strontium in the oral cavity, and the tablet disintegrates and disperses in 1 minute to form a suspension having a particle size within a certain range, and the active ingredient is rapidly formed. Dissolve, thoroughly clean the mouth, and play a role in preventing tooth decay and/or inhibiting bacteria and/or whitening teeth. Or first dissolve it with a small amount of water and then contain it in the mouth.

The oral rapid collapse mouth piece according to the present invention is a solid tablet containing a mouthwash component, which has the same efficacy as mouthwash, but is superior in some respects:

(1) The oral rapid collapse mouth piece according to the present invention is a solid tablet, which is used without a specific container for quantification;

(2) The oral rapid collapse mouth piece according to the present invention can be directly contained in the oral cavity only by ordinary drinking water;

(3) The active ingredient in the oral rapid collapse mouth piece of the invention is solid form, has good stability, long shelf life, and does not need to add other preservatives;

(4) The oral rapid collapse mouth piece according to the present invention is small in size, light in weight, convenient to carry, and can be used by many people, and is particularly suitable for use in working, traveling, and long-term outdoor activities.

In addition, the oral rapid collapse mouth piece according to the present invention is a non-effervescent system orally disintegrating tablet, which adopts excipients with good disintegration performance and special preparation technology to achieve the purpose of rapid collapse. It also has significant advantages over effervescent tablets:

(1) The oral rapid collapse mouth piece according to the present invention has loose production conditions and can be produced under the production conditions of ordinary tablets, compared with the severe production conditions in which the relative humidity of the effervescent tablet is 30% or less and the temperature does not exceed 25 °C. , can greatly reduce production costs; (2) The oral rapid collapse mouth piece according to the present invention is a non-effervescent disintegration system, and the requirements for packaging materials are comparable to those of ordinary tablets, and the packaging cost is relatively low;

(3) The excipients used in the rapid disintegration mouthparts of the present invention are mild in nature, do not contain acid and alkali, and are non-irritating to the oral cavity;

(4) After the oral rapid disintegration mouthpiece of the present invention is contained in the oral cavity, the dissolution rate of the main active ingredient in 30 seconds is more than 75 %. BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the content of the present invention will be further clarified with reference to the embodiments, but the present invention is not limited to the scope of the following embodiments. Example 1 Preparation of sodium fluoride containing tablets

According to the prescription, sodium fluoride and mannitol were weighed separately, mixed, and the povidone K30 solution was added, stirred, sieved through a 40 mesh sieve, and dried. The above granules were mixed with other raw materials and punched with a 13 mm shallow arc, and the tablet hardness was controlled at 4 kgf. The disintegration time in the mouth is 20 seconds. Composition 2:

The preparation method is the same as above. The disintegration time in the mouth was 21 seconds.

Example 2 Preparation of sodium fluoride containing sodium and cetylpyridinium chloride valproate tablets Composition 1:

Povidone K30 5.6mg

PROSOLV SMCC 50 44mg

Cross-linked povidone XL-10 22mg

Stevioside 2.2mg

Menthol 17.5mg

Total 438.3mg According to the prescription, sodium fluoride, hexadecanoylpyridinium chloride and mannitol were weighed separately, mixed, and the povidone K30 solution was added, stirred, sieved through a 40 mesh sieve, and dried. Other materials were dispersed in PROSOLV SMCC 50 and mixed with the above particles. Using a 13mm shallow arc punching piece, the hardness of the tablet is controlled at 4kgf. The disintegration time in the mouth is 20 seconds.

Composition 2:

The preparation method is the same as above. The disintegration time in the mouth was 18 seconds.

Composition 3:

Sodium fluoride 5.0mg

Cetylpyridinium chloride 5.0mg

Mannitol 197.6mg

Hypromellose 2.4mg

Optimized microcrystalline cellulose 50mg

Cross-linked povidone XL-10 15mg Sucralose 1.8mg

Peppermint Oil 3.2mg

Menthol 4.8mg

Tween -80 2.75mg

Micronized silica gel 8.0mg

Total 295.55mg Preparation method:

1. Preparing mannitol blank particles by using a hypromellose aqueous solution as a binder;

2. Mix sodium fluoride and cetylpyridinium through a 100 mesh sieve and mix well with the blank particles;

3. Dissolve menthol in peppermint oil, add Tween-80 to mix evenly, add micro-powder silicon to grind evenly, pass 80 mesh sieve;

4. Mixing the 3 mixture with the optimized microcrystalline cellulose;

5. Mix the mixture of 2 and 4 and press it evenly. The hardness is controlled at 40~50N. Example 3 Preparation of sodium fluoride containing sodium, cetylpyridinium chloride and carbamide peroxide

According to the prescription, sodium fluoride, hexadecanoylpyridinium chloride and mannitol were weighed separately, mixed, and the povidone K30 solution was added, stirred, sieved through a 40 mesh sieve, and dried. Other materials were dispersed in PROSOLV SMCC 50 and mixed with the above particles. The sheet was punched with a 13 mm shallow arc, and the hardness of the tablet was controlled at 4 kgf. The disintegration time in the mouth is 20 seconds.

Composition 2:

600.7 mg was prepared as above. The disintegration time in the mouth was 28 seconds.

Composition 4:

According to the prescription, sodium fluoride, hexadecanoylpyridinium chloride and mannitol were weighed separately, mixed, and the povidone K30 solution was added, stirred, sieved through a 40 mesh sieve, and dried. The other materials were dispersed in hydroxypropylcellulose and mixed with the above granules. With a 13mm shallow arc punching piece, the tablet hardness is controlled to 25 seconds in a 4kgfo mouth.

Claims

Claim

A mouthwash tablet which can be rapidly disintegrated in the oral cavity, characterized in that the main component contains one or a mixture of two or three of the following formulas:

(1) at least one functional ingredient for preventing tooth decay and caries;

(3) At least one functional ingredient for whitening teeth.

2. A mouthwash according to claim 1 wherein said component further comprises: at least one disintegrant to enable rapid disintegration of the tablet in the oral cavity.

3. A mouthwash according to claim 2, wherein said components further comprise:

(3) at least one sweetener for regulating the taste of the tablet;

(4) at least one cooling agent to maintain a fresh breath;

(5) at least one lubricant for lubricating when pressed;

The mouthwash sheet according to claim 1 or 2 or 3, wherein the functional component for preventing tooth decay and caries is a compound of sodium fluoride, sodium monofluorophosphate, stannous fluoride or both , a mixture of three compounds.

The mouthwash tablet according to claim 1 or 2 or 3, wherein the functional component for inhibiting the growth and aggregation of oral bacteria comprises a cationic surfactant, cetylpyridinium chloride, and a nonionic surfactant. Chlorine.

6. A mouthwash according to claim 1 or 2 or 3, wherein the functional components of the whitening tooth comprise hydrogen peroxide, urea peroxide.

The mouthwash sheet according to claim 2 or 3, wherein the disintegrant in the component is one of the following formulas or a mixture of any two or more of: 1 crospovidone 2 croscarmellose sodium 3 sodium carboxymethyl starch 4 microcrystalline cellulose 5 hydroxypropyl cellulose.

8. A mouthwash according to claim 3, wherein the soluble filler in the composition is one of the following formulas or a mixture of any two or three:

1 mannitol 2 xylitol 3 sorbitol.

The mouthwash sheet according to claim 3, wherein the filler having good disintegration properties in the component is one or a mixture of microcrystalline cellulose and hydroxypropyl cellulose.

10. A mouthwash according to claim 3, wherein the sweetener in the composition is one of the following formulas or a mixture of any two or three:

1 sucralose 2 stevioside 3 aspartame.

11. A mouthwash according to claim 3, wherein the cooling agent in the component is one of the following formulas or a mixture of any two or three:

1 menthol 2 cool alcohol 3 spearmint.

12. A mouthwash according to claim 3, wherein the lubricant in the component is one of the following formulas or a mixture of any two or more of:

1 sodium stearate fumarate 2 sodium decyl sulfate 3 decyl sulphate 4 polyglycol 40005 polyethylene glycol 6000.

13. A mouthwash according to claim 3, wherein the binder in the composition is one of the following formulas or a mixture of any two or three:

1 povidone K302 hypromellose 3 carboxymethyl cellulose.

14. A mouthwash according to any of claims 1-3, wherein the mouthpiece disintegrates in the mouth for less than one minute.

The mouthwash sheet according to any one of claims 1 to 3, characterized in that the mouth piece is directly contained in the mouth with a small amount of water, or is dissolved in the mouth with a small amount of water. rinse.

16. A mouthwash according to claim 3, wherein the ratio of major components is as follows: Sodium fluoride 0.025%~20.0%

Cetylpyridinium chloride 铛 0.005%~30.0%

Urea peroxide 1.0%~60.0%

Soluble filler 30%~95%

Filler with good disintegration performance 2%~30%

Disintegrant 0.1%~15%

Lubricant 0.2%~5%

Sweetener 0.2%~4%

Cooling agent 0.1%~8%

All percentages are by mass.

17. A mouthwash according to claim 16, wherein the ratio of major components is as follows: sodium fluoride 0.15% to 1.0%

Cetylpyridinium chloride 0.3%~2.0%

Urea peroxide 3.5%~20%

Soluble filler 51%~88%

Filler with good disintegration performance 5%~20%

Disintegrant 0.3%~10%

Lubricant 0.5%~2%

Sweetener 0.5%~2%

Cooling agent 1%~5%

All percentages are by mass.