JPS59186913A - Base to be applied to mucosa in oral cavity - Google Patents

Abstract

PURPOSE:The titled base providing a shet pharmaceutical preparation being stuck fast to the gum, capable of being kept in the oral cavity for a long time, releasing a drug gradually, obtained by blending gelatin with gluten, a carboxyvinyl polymer and vinyl acetate resin. CONSTITUTION:1-70wt%, especially 5-40wt% gelatin or agar is blended with 1-70wt%, especially 20-38wt% gluten, 1-50wt%, especially 20-30 carboxyvinyl polymer (e.g., polyacrylic acid), and 1-70wt%, especially 12-38wt% vinyl acetate resin or gum (guar gum, natural chicle) based on total amounts of components in the base, respectively. The components are stirred with purified water under heating to give a pasty composition, which is blended with any of various drugs (preferably water-soluble drug) uniformly, and extended and applied to a proper substrate, dried until water content becomes about 0.5-20wt%, to give a sustained release preparation to be applied to the mucosa in the oral cavity.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a base for application to oral mucosa containing gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate resin or gums.

Troches and buccal dabs have been known as sustained-release preparations for the oral cavity.

However, these preparations are hard and have a certain degree of thickness, so they feel like a foreign body in the oral cavity. Therefore, it is difficult to keep it in the oral cavity for a long time due to the urge to swallow or chew it, and it is not suitable as a preparation for administering drugs over a long period of time.

As a result of various studies on sustained-release preparations that can be retained in the oral cavity for a long period of time, the present inventors added a drug to a base containing gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate or gums. When applied to the gingival mucosa after forming into a sheet, it absorbs the moisture on the mucosa and adheres closely to the gingiva, allowing it to be retained in the oral cavity for a long time without being affected by saliva, and gradually releasing the drug. We have found that it can be made into a sheet preparation suitable for long-term administration of drugs both locally and systemically.

The present invention was completed based on the above findings.

Gluten used in the base of the present invention is widely used in foods and is a mixture of proteins obtained from wheat.

Examples of carboxyvinyl polymers include polyacrylic acid and partially crosslinked polymers, such as acid type polymers such as carbopol.

Vinyl acetate resin refers to a synthetic resin whose main component is vinyl acetate, such as polyvinyl acetate or a copolymer whose main component is vinyl acetate.

Examples of gums include vegetable gums such as guar gum, natural chicle, xanthan gum, gum arabic, gum tragacanth, gum karaya, echo gum, and locust bean gum.

Vinyl acetate resin and gums may be used alone or in combination.

The proportion of each component used in the base of the present invention is gelatin or agar 1 to 70 w/w%, preferably 4 to 50 w/w%, more preferably 5 to 4 Q w %, based on the total amount of those components.
/w%, gluten 1-7Qw/w%, preferably 10-7%
50 w/w%, more preferably 20 to 38 w/w%,
Carboxyvinyl polymer 1 to 50 w/w%, preferably 10 to 40 w/w%, more preferably 20 to 30
w/w%, vinyl acetate resin or gums 1-70w/
w%, preferably about 10 to 50 W/w%, more preferably about 12 to 38 w/wa;b.

The base of the present invention includes base components commonly used in poultices, such as water, glycerin, glopylene glycol, polyethylene glycol, and the like.

Polyhydric alcohols such as 3-butanediol and sorbitol, cellulose derivatives such as methylcellulose, ethylcellulose, propylcellulose, ethylmethylcellulose, hydroxyethylcellulose, hydroxyglobil cellulose, carboxymethylcellulose, cellulose acetate phthalate, sodium polyacrylate,
Polyvinylpyrrolidone or the like may also be added. The mixing ratio of water to the base of the present invention is O~30 w/w
%, preferably about 2 to 25 w/w%, and 0 to 100 w/w%, preferably 30 to 80'w/w% for other components.
It is about w%.

To obtain a preparation for oral mucosa using the base of the present invention, gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate or gums are stirred with purified water under heating to form a paste composition, and then After various drugs are added to this composition and mixed uniformly, it is spread and coated on a suitable support, and the water content is usually 0.5 to 20 w/w.
By drying to about w%, an excellent oral mucosal patch preparation can be obtained.

There are no particular restrictions on the drugs, but for example, betahistine, γ
- Water soluble drugs such as aminobutyric acid, chlorpromazine, schizamethonium chloride, etilefrine, scopolamine, tolbutamide, imipramine are preferred.

The formulation using the base of the present invention gradually releases the drug, has a small amount of drug remaining in the formulation after use, and also absorbs moisture from the application site and adheres well to the application site.
Good shape retention during use, more than 8 hours, 24 hours if necessary
It can be left on for about an hour, so the absorption rate of the drug is good, and the thickness is 10~10cm with moderate flexibility.
Since the thickness can be reduced to about 1000 μm, the usability is also good.

5- Next, the excellent effects of the base material of the present invention will be explained using experimental examples.

Example (1) Preparation of sample Gelatin 141, Gluten 8J1 carboxyvinyl polymer 81, and vinyl acetate resin 61 were mixed, and then 30 ml of purified water was added and heated and stirred to form a paste.
Degas. This paste composition was spread and coated on a vinyl chloride film at a rate of 500 P/m2, and then heated at 30°C.
After drying in a constant temperature room until the moisture content reaches 15%,
Predetermined size (3cb).

(2) Experimental method Samples were applied to the gingival mucosa of two volunteers before going to bed, and their adhesion and feeling of use were examined.

(3) Results The samples affixed to the two volunteers were tested upon waking up (8
Even after several hours), the film remained in close contact with the film without peeling off. Moreover, the feeling of use was good, with none of the 26 volunteers feeling any strangeness that bothered them.

Example 1 40 parts of gelatin, 25 parts of gluten, 20 parts of carboxyvinyl polymer, and 15 parts of guar gum are uniformly kneaded with 50 parts of water to obtain a paste composition.

Next, 9 parts of ethylene hydrochloride and 10 parts of ethylene hydrochloride are added to this paste-like composition, and the mixture is coated on a support and dried until the moisture content becomes 20% to obtain a preparation using the base of the present invention.

Example 2 9 parts of agar, 36 parts of gluten, 24 parts of carboxyvinyl polymer, 18 parts of vinyl acetate resin, and 13 parts of natural chicle were stirred with 100 parts of water under heat to obtain a paste composition.

Next, a preparation using the base of the present invention can be obtained in the same manner as in Example 1.

7- −89=

Claims (1)

[Claims] (1) Base for oral mucosa patch containing gelatin or agar, gluten, carboxyvinyl polymer, and vinyl acetate resin or gums