Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1992-02-27
1994-09-27
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
5147722, 514781, 514785, 514946, 514947, A61K 3119
Patent
active
053507690
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to an antiinflammatory gel preparation which can contain diclofenac or a salt thereof a high concentration and which exhibits superior stability and excellent percutaneous absorptivity.
DESCRIPTION OF THE BACKGROUND ART
Diclofenac or its salts possess excellent antiinflammatory action, and are widely used in clinics with oral and rectal dosage form. When administered orally or rectally, they are known to cause various side effects, including gastrointestinal tract disturbance. Because of this reason, a preparation for external application has been proposed, by which the drug is percutaneously absorbed without going through gastrointestinal tract and exhibits its action locally or systemically. However, since diclofenac and its salts are scarcely absorbed percutaneously, such a preparation has not been commercially sold.
Gel preparations, on the other hand, possess an advantage over other preparations for external application in terms of the good feeling upon use. When a gel preparation contains diclofenac or its salts as an active ingredient there are problems that a high concentration of diclofenac or its salts may destruct the gel structure, liquefying the gel or crystallizing over time.
In view of this situation the present inventors have undertaken extensive studies and found that if base components comprising a dibasic ester and a lower alcohol are gelatinized by using a nonionic polymer as a gelling agent, diclofenac or its salts can be contained at a high concentration and in a stable manner, providing gel preparations with excellent percutaneous absorptivity. The finding has led to the completion of the present invention.
DISCLOSURE OF THE INVENTION
The present invention provides an antiinflammatory gel preparation characterized by comprising diclofenac or its salts, a nonionic polymer, a dibasic ester, and a lower alcohol.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 shows a comparison of plasma concentration of dicrofenac after abdominal administration of gel ointments A-2 and B-2 in rats. FIG. 2 shows a comparison of plasma concentration of decrofenac after administration of gel ointments A-2, A-19, and B-2 in the back of guinea pigs. FIG. 3 shows plasma concentration of declofenac after administration of gel ointment A-2 in the back of man. FIG. 4 shows an antiphlogistic effect of gel ointment A-2 against edema induced by carrageenan in the sole of rats.
BEST MODE FOR IMPLEMENTING THE INVENTION
There are no specific restrictions as to the salts of diclofenac, so long as they are pharmaceutically acceptable compounds. Given as examples of such salts are salts of alkali metal, alkaline earth metal, ammonia, and primary, secondary, or tertiary alkanolamine; e.g., sodium, potassium, calcium, ammonium, dimethylamine, diethylamine, trimethylamine, triethylamine, monoethanolamine, diethanolamine, diisopropanolamine, triethanolamine, triisopropanolamine, and the like. Especially preferable salts are sodium salts and ammonium salts. There are no limitations to the amount of diclofenac or its salts in the preparation; it may be the amount by which the medicinal effect is exhibited. Generally, an amount of 0.1-20%, especially 0.5-10%, is preferable.
A nonionic polymer is an important component of the present invention. The gel preparation comprising diclofenac or its salts can be obtained without destructing the gel structure by using a nonionic polymer as a gelling agent. In addition, the nonionic polymer enables the preparation to include a large amount of lower alcohol which helps to promote the percutaneous absorption of diclofenac or its salts and to enhance their dissolution into the base components. Examples of nonionic polymers which can be given are those capable of forming a gel in a mixed solution of an ester of dibasic acid, a lower alcohol and water; e.g., ethylcellulose, hydroxyethylmethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, polyvinyl pyrrolidone, poly
REFERENCES:
patent: 4746675 (1988-05-01), Makino et al.
patent: 4873081 (1989-10-01), Ogiso
patent: 5030629 (1991-07-01), Rajadhyaksha
patent: 5039513 (1991-08-01), Chatterjee et al.
Enomoto Satoru
Ikeda Yasuo
Imamori Katsumi
Iwasa Akira
Kasai Shuichi
Cintins Marianne M.
Jarvis William R. A.
SS Pharmaceutical Co., Ltd.
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