JPH0623093B2 - Suppositories for hemorrhoids - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to suppositories for hemorrhoids.

In Japan, many people suffer from hemorrhoids due to their lifestyle and living environment.

Hemorrhoids can be classified into hemorrhoids, hemorrhoids, fistulae, perianal inflammation, and anal fissures, but in any case, initial treatment is essential, and if the timing is missed, the treatment becomes difficult and hospital treatment such as surgery is required. In humans, hemorrhoids occur around the anus, and internal hemorrhoids occur within 5 cm of the anus. However,
Conventional suppositories for hemorrhoids disappeared from the affected area in a short time after insertion into the anus, and the therapeutic effect was not sufficient.

An object of the present invention is to provide a suppository for hemorrhoids which has a high therapeutic effect.

As a result of intensive studies to obtain a suppository that remains in the affected area after insertion of the anus, the present inventors have found that one or more compounds selected from the group consisting of polyvinyl alcohol, pectin and pullulan are used as suppository bases. It was found that the above-mentioned problems can be solved by compounding the agent with the agent, and the present invention was completed.

That is, the present invention is a suppository for hemorrhoids in which one or more compounds selected from the group consisting of polyvinyl alcohol, pectin and pullulan are mixed with the base of a conventional suppository.

In the present invention, the compounding amount of one or more compounds selected from the group consisting of polyvinyl alcohol, pectin and pullulan in the suppository is 20 to 60% by weight, preferably 25 to 50%.
% By weight. If the compounding amount of the above compound is less than the lower limit, the action of the drug on the hemorrhoidal area will be insufficient, and if it exceeds the upper limit, the fluidity of the suppository will deteriorate and the workability will decrease.

In addition, the bases of commonly used suppositories include cocoa butter, lauric fat,
Hydrogenated oil, fatty acid glyceride [eg Witepsol
Oil-based base such as H type, S type, W type, E type (trade name, Dynamite Nobel)
Polyethylene glycol (eg Macrogol 400,
1,500, 1,540, 4,000, 6,000, etc.) and the like.

Drugs used in the suppository of the present invention include cortisone, hydrocortisone, hydrocortisone acetate, dexamethasone,
Dexamethasone acetate, prednisolone acetate, prednisolone acetate, betamethasone, betamethasone valerate, hydrocortisone butyrate propionate hydrocortisone, lysozyme chloride, glycyrrhetinic acid, bufexamac, ibuprofen, bromelain, allantoin, dibucaine hydrochloride, ethyl aminobenzoate, lidocaine hydrochloride, procaine hydrochloride, procaine hydrochloride, procaine hydrochloride. , Diphenhydramine, naphazoline hydrochloride, phenylephrine hydrochloride, chlorhexidine hydrochloride, chlorhexidine gluconate, decalinium chloride, purple root, tocopherol acetate, retinol palmitate, ergocalciferol, camphor, menthol, zinc oxide, etc. Inflammatory agent, granulation promoter,
Local anesthetics, antihistamines, hemostatics, bactericides, vitamins, blood circulation promoters, astringents, etc.

The suppository for hemorrhoids of the present invention can be prepared, for example, by the following method.

That is, the oily or water-soluble base is melted at 80 to 60 ° C., preferably about 70 ° C., and a required amount of the drug,
After adding the compound to be added to the above-mentioned base and other components and stirring well, the mixture was cooled to 60 to 50 ° C with stirring, poured into a suppository mold and cooled to room temperature to produce a suppository. Remove from mold.

The thus-obtained suppository for hemorrhoids of the present invention improves the action of the drug on the hemorrhoidal lesion. That is, the suppository stays in the lower part of the rectum, which can remarkably improve the symptoms of hemorrhoids.

Hereinafter, the present invention will be specifically described with reference to Examples and Test Examples.

Example 1 Witepsol E85 1 g and Witepsol H15 9.71 g
Is melted at about 70 ° C and hydrocortisone acetate 0.05
g, lidocaine 0.6g, chlorhexidine hydrochloride 0.05g, menthol 0.09g, Gohsenol GL05 (trade name, polyvinyl alcohol, Nippon Synthetic Chemical Industry Co., Ltd.) 2g, pectin 4
g was added and well stirred to disperse.

This was cooled to about 50 ° C. with stirring, poured into a suppository mold, and cooled to room temperature to obtain a suppository for hemorrhoids (1.75 g / piece).

Example 2 According to Example 1, a suppository (1.8 g / piece) having the following formulation was prepared.

(Prescription) (per suppository) Bufexamac 20 mg Diphenhydramine 8 mg Tocopherol acetate 20 mg Zinc oxide 100 mg Methylcellulose 300 mg Pullulan 400 mg Cocoa butter 952 mg 1800 mg Example 3 According to Example 1, suppositories (1.7 g / piece) ) Was prepared.

(Prescription) (per suppository) Glycyrrhetinic acid 20 mg Lysozyme chloride 30 mg Gohsenol GL05 510 mg Witepsol E85 100 mg Witepsol S55 100 mg Witepsol H15 940 mg 1700 mg Test Example Using 5 rabbits, the suppository prepared in Example 1 from anus It was inserted and the rectum was taken out 2 hours later. As a control
A suppository containing no Gohsenol GL05 and pectin from the formulation of Example 3 was produced in the same manner as in Example 3, and operated in the same manner as above.

As a result, the control suppository spread from the upper rectum to the large intestine, whereas the suppository of Example 3 existed in the lower rectum.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Fu Murayama 3-24-1 Takada, Toshima-ku, Tokyo Within Taisho Pharmaceutical Co., Ltd. (56) References JP-A-58-140012 (JP, A) JP-A-SHO 57-144214 (JP, A) JP-B-44-11675 (JP, B1)

Claims (1)

[Claims] 1. A hemorrhoidal suppository in which one or more compounds selected from the group consisting of polyvinyl alcohol, pectin and pullulan are mixed with a base of a conventional suppository.