Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-12-10
1998-12-29
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514469, 514557, 514558, 514560, A61K 3134, A61K 3119, A61K 3120
Patent
active
058542817
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/02350, filed Nov. 16, 1995.
TECHNICAL FIELD
The present invention relates to a preparation for percutaneous absorption, which comprises as an effective ingredient a prostaglandin (hereinafter referred to as "PG") I.sub.2 derivative. More particularly, the present invention relates to a preparation to be percutaneously absorbed, which comprises a fatty acid or a derivative thereof as an agent for enhancing percutaneous absorption, thereby percutaneous permeability of the PGI.sub.2 derivative is enhanced.
BACKGROUND ART
PGs are drugs drawing attention in various fields because they widely occur in various organs and body fluids and because they exhibit strong physiological activities in a small amount. Among the PGs, PGI.sub.2 has a strong activity to inhibit platelet aggregation and a strong vasodilation activity, so that use of PGI.sub.2 as therapeutic agents for various diseases is expected.
However, since PGs including PGI.sub.2 are very unstable chemically, the administration route is limited to intravenous administration or the like. Thus, studies are now being made for developing a stable derivative thereof and for looking for a novel administration route and administration form.
Studies of preparations to be percutaneously absorbed are also now intensively being made. Agents for enhancing percutaneous permeability of aqueous drugs are now being studied, and especially, fatty acids and terpenes are mainly studied as candidates of the agents (J. Pharm. Pharmacol., 39, 535 (1987); J. Pharm. Sci., 80, 39 (1991); Drug Des. Delivery, 1, 245 (1987); Drug Des. Delivery, 6, 229 (1990); Drug Delivery System, 6, 5 (1991); Japanese Laid-open Patent Application (Kokai) Nos. 3-261721, 2-3613 and 60-36423; and Japanese Laid-open PCT Application (Kohyo) Nos. 2-503672 and 63-502108).
On the other hand, preparations to be percutaneously absorbed, which comprise PGs such as PGI.sub.2, are also now being intensively studied (Japanese Laid-open Patent Application (Kokai) Nos. 58-124778, 4-22808, 4-138187, 4-243827, 4-164034, 63-211241 and 4-312520; and Japanese Laid-open PCT Application (Kohyo) No. 6-509346).
However, these preparations for subcutaneous absorption containing PGI.sub.2 derivatives do not necessarily have satisfactory percutaneous permeability.
DISCLOSURE OF THE INVENTION
The present invention provides a preparation to be percutaneously absorbed comprising a PGI.sub.2 derivative as an effective ingredient and a fatty acid, a derivative thereof, or a mixture of two or more of these, which has a high percutaneous permeability of the PGI.sub.2 derivative, especially a preparation to be percutaneously absorbed comprising 5,6,7-trinor-4,8-inter-m-phenylene derivative and a C.sub.6 -C.sub.24 fatty acid or a salt or an ester thereof, or a mixture of two or more of these, which has a high percutaneous permeability of the PGI.sub.2 derivative.
BEST MODE FOR CARRYING OUT THE INVENTION
To overcome the above-described problems, the present inventors intensively studied to discover that a preparation for subcutaneous absorption, which gives high percutaneous permeability of the PGI.sub.2 derivative, is obtained by selecting a base component and an agent for enhancing percutaneous permeability, thereby completing the present invention.
That is, the present invention provides a preparation for percutaneous absorption comprising as an effective component a PGI.sub.2 derivative and a fatty acid or a derivative thereof.
As the PGI.sub.2 derivative which may be employed in the present invention, one having excellent stability and having platelet aggregation-inhibition activity and vasodilation activity is selected. For example, the compound of the formula (I): ##STR1## (wherein R.sub.1 represents a pharmaceutically acceptable cation, hydrogen or C.sub.1 -C.sub.12 linear alkyl group; R.sub.2 represents hydrogen, C.sub.2 -C.sub.10 acyl group or C.sub.7 -C.sub.18 aroyl group; R.sub.3 represents hydrogen, C.sub.2 -C.sub.10 acyl group or C.sub.7 -C.sub.18 aroyl group; R.sub.4 repr
REFERENCES:
patent: 5403867 (1995-04-01), Okumura et al.
Mak et al., J. Controlled Release, 12, 67-75 (1990).
Yamashita et al., Drug Delivery System, 8, No. 4, 243-250 (1993).
Hara Michio
Horiuchi Yasuhide
Irie Tetsumi
Uekama Kaneto
Jordan Kimberly
Toray Industries Inc.
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