Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1991-10-22
1993-10-26
Friedman, S. J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
A61K 3119
Patent
active
052566919
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel oil-in-water type (hereinafter may be referred to "o/w type") emulsified composition comprising a non-steroidal antiphlogistic and analgesic drug. Specifically, the composition in accordance with the present invention contains a monoalkylglyceryl ether and hydrophilic surface-active agent, and thus the composition is to be stabilized and useful for a pharmaceutical preparation for external use.
BACKGROUND ART
In general, it is feared that a non-steroidal antiphlogistic and analgesic drugs (or anti-inflammatories) cause side effects when they are administrated orally or rectally. For the purpose of solving the side effects, a wide variety of pharmaceutical preparations for external use which are administrated directly in topical portions have been developed. In many such pharmaceutical preparations, since most non-steroidal antiphlogistic and analgesic drugs do not easily dissolve in both water and oil, lower alcohols, polyvalent alcohols, fatty acid esters, crotamiton, surfactants, or the like are combined to dissolve the drugs or the medicine is dispersed in a medium in micro-powder form such as crystal, and then water-soluble polymeric compounds are formulated in order to ensure the stabilization of the dispersion. Even the salt compounds of the non-steroidal antiphlogistic and analgesic drugs in the form of sodium salts are only slightly soluble in water, and thus attempts to use various methods have been made for preparation.
With examples of the method, since skin safety is generally lowered when a lower alcohol or a polyhydric alcohol such as propylene glycol is formulated in a large amount for the purpose of dissolving the medicine, an aqueous emulsified preparation not using any lower alcohol has been proposed (see, for example, Japanese Unexamined Patent Publications (Kokai) No. 57-98209, No. 58-185514, No. 59-116212 and No. 61-215320). In almost all of these inventions, the dispersion is thickened with a water-soluble polymeric compound, and thus it is very difficult to enhance their thermodynamic activities in terms of the separation of the medicine with the passage of time and the discharge of the medicine. Further, because of stickiness due to a large amount of the water-soluble polymeric compound being formulated, it is not preferred from the viewpoint of its texture. On the other hand, for the purpose of enhancing the discharge of the medicine from the base, an invention in which the medicine is prepared in the saturated state (see Japanese Unexamined Patent Publication (Kokai) No. 63-150221) has been disclosed. Due to the formulation of a higher alcohol, the invention, however, has the problem that the esterification reaction with the medicine causes a significant impairment in the compound's stability. In particular, in the case where the medicine has a low stable pH region, it is apt to bring about the esterification with the higher alcohol, the reaction being increasingly likely to occur when the water formulation is larger. On the other hand, since there is poor solubility in water even when the non-steroid agent is a salt (or a compound in the form of the salt), the invention in which the preparation is made into an oleaginous ointment has been known (see Japanese Unexamined Patent Publication (Kokai) No. 59-33211). The agent thus prepared is unduly greasy and tends to stain clothes; thus, it is not necessarily preferred. Furthermore, Inventions of a cream preparation (see Japanese Unexamined Patent Publication (Kokai) No. 64-13020) and a solution preparation (see Japanese Unexamined Patent Publication (Kokai) No. 1-242521) have been disclosed.
However, in preparation of the cream, the water-soluble polymeric compound or a higher alcohol is used, and thus preparations using the compounds as described above are associated with common problems.
Also, to provide a cream or ointment, it is known that a pharmaceutical preparation for external use contains a combination of .alpha.-monoglyceryl ether and an oily substance in the for
REFERENCES:
patent: 4465629 (1984-08-01), Maughan
Chem. Abst. 105-102614G (1986).
Friedman S. J.
Shiseido Company Ltd.
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