Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1994-10-03
1997-03-11
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514573, A61K 31557
Patent
active
056101821
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/00142 filed Feb. 2, 1994.
TECHNICAL FIELD
The present invention relates to a pharmaceutical composition and a method for the therapy of cerebral thrombosis. More specifically, it relates to a pharmaceutical composition for the therapy of cerebral thrombosis, which contains an isocarbacyclin as an active ingredient, and a method for the therapy of cerebral thrombosis.
TECHNICAL BACKGROUND
Prostacyclin is a topical hormone produced mainly on an inner vessel wall of arterial duct of a living body, and due to its high physiological activities such as the platelet aggregation inhibiting activity and the vasodilating activity, it is an essential factor for adjusting the functions of a living body. An attempt has been made to provide it directly as a medicament (P. J. Lewis & J. O. Grady' Clinical Pharmacology of Prostacyclin' Raven Press, N. Y., 1981).
Since, however, natural prostacyclin has, in its molecule, an enol ether bond which is easily hydrolyzable, it is easily deactivated under neutral or acidic conditions, and it cannot be said to be a preferred compound as a medicament due to its chemical instability. Therefore, chemically stable synthetic prostacyclin derivatives having physiological activities equivalent to those of natural prostacyclin have been studied at home and abroad (see R. C. Nickolson, et al, Medicinal Research Reviews, Vol. 5, page 5, 1985). Among these derivatives, isocarbacyclin obtained by replacing oxygen atoms in the 6 and 9 positions of prostacyclin with methylene group (--CH.dbd. group) and converting double bonds in the 5 and 6 positions to single bonds is a derivative which is highly chemically stable and has bioactivities equivalent to those of natural prostacyclin, and studies are under way to apply it to a medicament.
On the other hand, as compounds prepared by stabilizing prostaglandins as fat preparations, fat emulsions containing PGE1 and PGA1 have been proposed in recent years for the purpose of vasodilation activity, platelet aggregation inhibition and depression activity [see Japanese Laid-open Patent Publications Nos. 222014/1983 and 141518/1984, and Ann. Rheum. Diseases, 41 263 (1982); Journal of Pharmacy and Pharmacology, 35, 398 (1983)]. It is also proposed to apply this method to an anticancer agent for increasing the selective targeting of the anticancer agent on a target organ (see Japanese Laid-open Patent Publication No. 122423/1984). However, it has been difficult to prepare prostacyclin into a fat emulsion due to its chemical instability. Attempts have therefore been made to prepare the above isocarbacyclins into fat emulsions, and there have been developed stable preparations having durability in activity, having a targeting effect and having an increased effect (Japanese Laid-open Patent Publication No. 289034/1986).
Meanwhile, it has been studied to apply natural prostacyclin to the therapy of cerebral thrombosis due to its pharmacological effect (see Hsu C. Y. et al, Stroke, Vol. 18, page 352, 1987). However, its activities are not sufficient, and its side effects are problems. Therefore, for overcoming the above defects, Mizushima et al, have attempted to administer preparations of fat emulsions of the above isocarbacyclins to patients having cerebral thrombosis but showing relatively stable symptoms at a chronic stage (see Prostaglandins, Vol. 40, page 155, 1990).
DISCLOSURE OF THE INVENTION
It is an object of the present invention to provide a pharmaceutical composition for the therapy of cerebral thrombosis.
It is another object of the present invention to provide a pharmaceutical composition particularly effective for the therapy of cerebral thrombosis at an acute stage, i.e., at which the symptoms are acute and unstable.
It is further another object of the present invention to provide a pharmaceutical composition for the therapy of cerebral thrombosis, which contains an isocarbacyclin in a specific structure, have excellent safety and is in the form of a far emulsion.
It is still further another object
REFERENCES:
patent: 4493847 (1985-01-01), Mizushima et al.
patent: 5124352 (1992-06-01), Mizushima
patent: 5426115 (1995-06-01), Veno
Peter J. Lewis et al., Clinical Pharmacology of Prostacyclin, Raven Press, New York, pp. 1-8, (1981).
Robert C. Nickolson et al., Medicinal Research Reviews, vol. 5, No. 1, pp. 1-7, 44 and 45, (1985).
Y. Mizushima et al., Annals of Rheumatic Diseases, vol. 41, pp. 263-267 (1982).
Y. Mizushima et al., J. Pharm. Pharmacol., vol. 35, pp. 398-399 (1983).
C. Y. Hsu et al., Stroke, vol. 18, No. 2, pp. 352-358 (1987).
K. Hoshi et al., Prostaglandins, vol. 40, No. 2, pp. 155-164 (1990).
Y. Mizushima et al., Journal of Drug Targeting, vol. 1, pp. 93-100 (1993).
K. Hoshi, et al., Prostaglandins, vol. 40, No. 2, Aug. 1990, Stoneham Ma US, pp. 157-164.
Mizushima, J. Drug Targeting 1993 1 pp. 3-100.
Hoshi, Prostuglandins 40(2);155 1990.
Bannai Kiyoshi
Mizushima Yutaka
Nakayana Shigeru
Gerstl Robert
Mizushima Yutaka
Taisho Pharmaceutical Co. Ltd.
Teijin Limited
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