Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-10-14
1999-08-24
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540575, C07D40112
Patent
active
059425059
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to a novel hydrate of 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride. More particularly, the present invention is concerned with a 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate having a water content of from 2.5 to 15.5% by weight as measured by the Karl Fischer method, represented by the following formula (I): ##STR2## wherein n means a number in the range of from 1/2 to 3.
Since the 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate of the present invention has excellent shapeability as compared to a 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride anhydride, a tablet having satisfactory hardness can be obtained even with a relatively low compression pressure in a tableting process. Further, due to a reduction in the compression pressure needed for tableting, various advantages are brought about, such as improved disintegratability of the resultant tablet when the tablet is orally taken, so that good dissolution of 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride from the tablet can be achieved, as well as suppression of abrasion of the die and punch used in producing tablets by compression, and the like.
PRIOR ART
1-(5-Isoquinolinesulfonyl)homopiperazine is an isoquinolinesulfonamide compound developed by Asahi Kasei Kogyo Kabushiki Kaisha (Asahi Chemical Industries, Ltd.), Japan, and various production methods thereof are known Application Laid-Open Specification No. 61-227581 (corresponding to U.S. Pat. No. 4,678,783 and Examined European Patent Publication No. 0,187,371)!. 1-(5-Isoquinolinesulfonyl)homopiperazine hydrochloride 1-(5-isoquinolinesulfonyl)homopiperazine! (hereinafter, frequently referred to simply as "fasudil hydrochloride") is a highly water-soluble anhydrous crystal having a melting point of 217-223.degree. C.
1-(5-Isoquinolinesulfonyl)homopiperazine hydrochloride has excellent vasodilative activity and is clinically used for treating cerebral vasospasm (which is likely to occur after the operation of a patient suffering from subarachnoid hemorrhage), cerebral ischemic symptoms accompanying the cerebral vasospasm, and the like, wherein the above-mentioned 1-(5-Isoquinolinesulfonyl)homopiperazine hydrochloride is used in the form of an oral preparation or a parenteral preparation which is available under tradename "Eril Inj." (registered trademark for the product produced and sold by Asahi Kasei Kogyo Kabushiki Kaisha, Japan). Usually, Eril Inj. is diluted with an appropriate amount of an aqueous solution of an electrolyte or sugar and then, administered by intravenous drip in an amount of 30 mg in terms of the amount of 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride for one administration (for adult) over 30 minutes, wherein the administration is conducted twice or thrice a day. It is preferred that the administration of Eril Inj. is started in the early stage of the postoperative treatment of subarachnoid hemorrhage and conducted thrice a day for two weeks.
Conventionally, as a crystal of 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride (fasudil hydrochloride), only an anhydrous crystal has heretofore been reported, which has a water content of 1% by weight (the "% by weight" is hereinafter, frequently referred to simply as "%") or less as measured by the Karl Fischer method (all of the water contents of the crystals mentioned in the present specification are measured by the same method).
The infrared absorption (IR) spectrum of the anhydrous crystal of fasudil hydrochloride as measured by the Nujol mull method using an infrared spectrometer (all of the infrared absorption spectra mentioned in the present specification are measured in the same method) is shown in FIG. 1 of the accompanying drawings. The anhydrous crystal exhibits, in the IR spectrum thereof, characteristic peaks, i.e., a peak at approximately 1618 cm.sup.-1 due to the skeletal stretching vibration of an isoquinoline skeleton, (.nu. aromatic); a peak at approximately 1588 cm.sup.-1 due to the skeleta
REFERENCES:
patent: 4678783 (1987-07-01), Hidaka et al.
Kawakubo Hiromu
Ohno Masaru
Asahi Kasei Kogyo Kabushiki Kaisha
Rao Deepak R.
Raymond Richard L.
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