Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1993-11-30
1995-04-04
Rose, Shep K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514882, 514925, 514928, A61K 31557, A61K 3134, C07D307935, C07D30777
Patent
active
054038677
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a preparation for treating wounds or hemorrnoids.
TECHNICAL BACKGROUND
Prostaglandin I.sub.2 (PGI.sub.2) and prostaglandin E.sub.1 (PGE.sub.1) are known to have a broad range of pharmacological activities such as high inhibition activity of platelet aggregation and high stimmulatory activity of vasolidating angiotelectasis, and it has been expected to apply these as a drug against peripheral blood circulation impairments. Since, however, PGI.sub.2 and PGE.sub.1 per se are chemically unstable, they are poor in retaining their pharmacological effects and it is difficult to apply them to practical use.
Beraprost which is a derivative of PGI.sub.2 is chemically stable, and it has been therefore developed as an oral preparation for treating peripheral bloodstream impairments and is commercially available as a drug for the therapy of ischemic diseases caused by chronic arterial occlusion.
Meanwhile, it is known that most of wounds such as intractable skin ulcer including bedsore are caused by a failure in peripheral blood circulation. It is therefore desired to develop a drug for topical use since the topical administration thereof, if such is possible, causes lower side effects than systemic administration. However, there is not yet known any topical preparation for the therapy of wounds containing at least one of PGI.sub.2, PGE.sub.1 and derivatives thereof as an active ingredient.
On the other hand, hemorrhoids are generally classified into piles, anal fissure, periproctitis, perirectal abscess and anal fistula, and the preparations for the therapy thereof are largely classified into steroid-containing or no steroid-containing topical preparations against hemorrhoids and topical or systemic preparations against varicosis. The activity mechanism of these preparations for the therapy of hemorrhoids includes the activity for improving peripheral blood circulation, the activity for inhibiting thrombus formation, the anti-inflammatory activity and the activity for tissue restoration, and PGI.sub.2, PGE.sub.1 and derivatives thereof have all of these pharmaceutical activities, which suggests their usefulness as drugs for the therapy of hemorrhoids. However, their applications are not yet known.
It is an object of the present invention to provide a preparation, particularly a topical preparation, for the therapy of wounds or hemorrhoids, which contains at least one of PGI.sub.2, PGE.sub.1 and derivatives thereof as an active ingredient, and a method for the therapy of wounds or hemorrhoids which comprises administering the above active ingredient.
DISCLOSURE OF THE INVENTION
The present inventors have found that a composition which contains at least one of PGI.sub.2, PGE.sub.1 and derivatives thereof as an active ingredient and which is prepared by incorporating it into a pharmaceutically acceptable vehicle has a therapeutical effect on wounds or hemorrhoids.
The present inventors have found that beraprost which is a PGI.sub.2 derivative or a salt thereof can be formed into a topical preparation suitable for symptoms of diseases since beraprost or a salt thereof is a powder which is chemically stable and soluble in water, and further that the preparation exhibits the high activity for promoting the healing of wounds by increasing the exudate amount and expediting the vascularization, granulation and epidermization.
The present inventors have also found that beraprost or a salt thereof has a high therapeutical effect on hemorrhoids when administered.
The present invention therefore relates to a preparation for the therapy of wounds or hemorrhoids (to be abbreviated as "present therapeutical preparation" hereinafter), which contains at least one of PGI.sub.2, PGE.sub.1 or derivatives thereof, particularly beraprost or a salt thereof, as an active ingredient and a pharmaceutically acceptable vehicle.
The present therapeutical preparation contains at least one of PGI.sub.2, PGE.sub.1 and derivatives thereof as an active ingredient. The derivative of PGI.sub.2 inclu
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Nakamura Tsutomu
Okuda Toshiaki
Okumura Makoto
Yajima Motoyuki
Kaken Pharmaceutical Co. Ltd.
Rose Shep K.
Toray Industries Inc.
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