Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-05-06
1996-05-21
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3140
Patent
active
055190464
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This application is a 371 of PCT/JP92/01446, filed Nov. 6, 1992.
The present invention relates to a fomentation to be used as an external anti-inflammatory analgesic and, in particular, it relates to a fomentation containing ketorolac (generic name), which is a nonsteroidal anti-inflammatory analgesic or 1.0 a salt thereof, as an efficacious ingredient.
BACKGROUND ART
The compound used as the efficacious or active ingredient in the present invention is generally called ketorolac and the formal chemical name thereof is (.+-.)-5-benzoyl-2,3-dihydro-1H-pyrrolidine-1-carboxylic acid (or 5-benzoyl-1,2-dihydro -3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid). Ketorolac was first synthesized by Syntex (U.S.A.) and disclosed as a compound having a remarkable anti-inflammatory analgesic effect in Japanese Patent Gazette No. Sho 62-54109 (54109/1987). Examples of the preparations containing ketorolac or its salt include an internal remedy and an injection disclosed in Japanese Patent Laid-Open Gazette No. Sho 61-191686 (191686/1986), and eye drops for local application described in Japanese Patent Laid-Open Gazette No. Sho 58-172314 ( 172314/1983 ).
Thus, only pharmaceutical preparations such as internal remedies, injections or eye drops each containing ketorolac were disclosed in the prior art, but no plasters containing ketorolac were suggested at all. Therefore, neither description of the fomentation containing ketorolac nor description of its formulation was found at all. Thus it was extremely difficult to anticipate whether ketorolac is usable as the efficacious or active ingredient of a fomentation and an excellent fomentation can be thus developed.
As described above, no attention was directed to the fomentation containing ketorolac as the active ingredient and no investigation was made thereon heretofore. As a matter of course, such a fomentation has not been put into practical use as yet.
Thus the inventors were interested in ketorolac having a remarkable anti-inflammatory analgesic effect in such conventional preparations as above. After their intensive investigations made in an attempt to obtain a fomentation in which ketorolac exhibits a remarkable efficacious effect, the inventors have foundan unexpected fact that ketorolac is difficultly soluble in a fomentation base and is enclosed in the form of crystals therein. The inventors have also found there are raised physical problems of, for example, the compatibility of ketorolac with the base, the stability of the active ingredient, and the reduction in exertion of the medicinal effect due to a decrease in releasability of the active ingredient from the base and percutaneous absorbability of said ingredient. It has been thus found that the development of a desired ketorolac-containing fomentation is difficult unless there are solved problems of the pharmaceutical manufacturing, formulation, design and exertion of the medicinal effect of the desired fomentation.
DISCLOSURE OF THE INVENTION
Therefore, an object of the present invention is to solve the above-described problems and, in particular, it is to provide an optimum anti-inflammatory analgesic ketorolac-containing fomentation by intensively investigating to find a suitable fomentation base comprising a water-soluble high-molecular polymer, a humectant and water, and a suitable formulation of the optimum fomentation; an absorption promoter for promoting the release of the active ingredient from the fomentation and the percutaneous absorption of the released active ingredient; and the base ingredients such as an excipient, an abirritant, a pH regulator, etc.
After their intensive investigations made for the purpose of solving the above-described problems, the inventors have found that an optimum fomentation can be developed by incorporating ketorolac (including a salt thereof; the same shall apply hereinafter) as the active ingredient either into a fomentation base comprising a water-soluble high-molecular polymer, a humectant and water or into the same base further incorporated with
REFERENCES:
patent: 4089969 (1978-05-01), Muchowski et al.
patent: 4454151 (1985-06-01), Waterbury
Yu et al, Chemical Abstracts, vol. 109 (1988) 134901x.
Journal Of Clinical Pharmacology, vol. 31, No. 5, May 1991, pp. 401-418, Vasant V. Ranade, "Drug Delivery Systems. 6. Transdermal. Drug Delivery" *pp. 401 and 410*.
Chemical Abstracts, vol. 115, No. 16, 21 Oct. 1991, Columbus, Ohio, US: Abstract No. 166660h, p. 490; *abstract* & JP-A-03 072 433 (Hisamitsu Pharmaceutical Co. Inc.) 28 Apr. 1989.
Hashiguchi Terushi
Hirano Munehiko
Ikeura Yasuhiro
Kose Yasuhisa
Kyoya Eiji
Hisamitsu Pharmaceutical Co. Inc.
Raymond Richard L.
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