Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1994-07-27
1996-02-13
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514560, 514573, 514966, 514967, A61K 3120, A61K 3119, A61K 31557
Patent
active
054911710
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of Pat./JP92/01431 filed Nov. 5, 1992.
TECHNICAL FIELD
The present invention relates to a pharmaceutical preparation for rectal or vaginal administration, which contains a pharmaceutically useful prostaglandin compound (hereinafter referred to as PG). The pharmaceutical preparation allows superior absorption of PG.
BACKGROUND ART
PG is a group of physiologically active substances synthesized in animal tissues from eicosapolyenoic acid such as arachidonic acid. Said compound is known to show a wide range of pharmacological actions such as hypotensive action, platelet aggregation-inhibitory action, vasodilating action, blood flow increasing action, gastric juice secretion-suppressing action, intestine hyperkinetic action, oxytocic action, diuretic action, bronchodilating action, contracting action and so on.
PG is hardly absorbed by oral administration and therefore generally administered by injection. Injections, however, give pain to patients.
Injections, moreover, require patients to go to the doctor by themselves, giving burdens on the patients in terms of time and physical labor, and development and practical application of a dosage form other than injection have been desired. In doing so, it is essential to solve technical problems with regard to achieving high bioavailability of a slightly-absorbable drug and the stabilization of unstable PG.
The present invention aims at solving the above-mentioned problems. That is, the present invention aims at solving the above problems by providing PG, which has been conventionally administered as injections, in other dosage forms and employing other administration method.
DISCLOSURE OF THE INVENTION
In order to solve the aforementioned problems, the present inventors have studied the relations between the dosage form of PG, administration route etc. and bioavailability and found that rectal or vaginal administration of PG surprisingly results in effective absorption of PG from these mucosal layers and exertion of the desired pharmacological effects; that presence of an alkali metal salt of a fatty acid having 8 to 12 carbon atoms therealong results in easy absorption of PG from rectum or vagina and migration thereof into blood; and that the use of an oily base as a base for a pharmaceutical preparation and the presence of an alkali metal salt of a fatty acid having 8 to 12 carbon atoms result in stabilization of PG and easy absorption of PG from rectum or vagina, based on which findings the present invention has been completed.
There has been no report on a pharmaceutical preparation of PG for rectal or vaginal administration, or its bioavailability. In addition, it is not possible to easily predict what pharmaceutical agent shows high bioavailability by rectal or vaginal administration.
The present invention is as follows: administration, containing PG and an alkali metal salt of a fatty acid having 8 to 12 carbon atoms. in the presence of an alkali metal salt of a fatty acid having 8 to 12 carbon atoms.
The present invention is explained in detail in the following.
The PG per se which is an active ingredient in the present invention is a compound substantially known and having a prostanic acid as a basic structure, and classified into respective groups of A through I according to the presence of oxygen atom bonded to a 5-membered ring and a double bond therein. In the present invention, various types of prostaglandin and derivatives thereof which are generally called prostaglandin are all encompassed. For example, the derivatives thereof include a 7-thia compound, a 9-acyloxy compound, an alkyl ester compound, an alkoxycarbonylalkyl ester compound, an acyloxycarbonylalkyl ester compound and so on with diverse pharmacological activities as mentioned above.
The dose of PG in the pharmaceutical preparation of the invention is 1-10,000 .mu.g per administration to an adult. According to the present invention, a significant effect and sufficient duration of the effect are evidently achieved by administering PG via rectum or vagina.
REFERENCES:
patent: 4289785 (1981-09-01), Wilks
patent: 4352790 (1982-10-01), Johansson et al.
patent: 4485033 (1984-11-01), Kitao et al.
Chemical Abstracts, vol. 112, No. 4, 22 Jan. 1990, Abstract No. 25693.
Kakeya Nobuharu
Kikuchi Masahiro
Kondoh Nobuo
Mori Takayoshi
Nishimura Ken-ichi
Jordan Kimberly
Kyoto Pharmaceutical Industries, Ltd.
The Green Cross Corporation
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