Process for producing efonidipine hydrochloride preparations

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United States of America Patent

PATENT NO 6171599
SERIAL NO

09142208

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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An amorphous solid dispersion of efonidipine hydrochloride having a high intestinal absorbability can be formed by subjecting a mixture containing efonidipine hydrochloride of the formula (I), hydroxypropylmethylcellulose acetate succinate and optionally a thermostabilizer to a step A of heat treatment at from 85 to 140.degree. C. or mechanochemical treatment at from 0 to 140.degree. C., and then to a step B of dipping treatment into a water-containing solution, impregnation treatment with a water-containing solution or contacting treatment with a water vapor-containing gas; or treating the above-mentioned mixture with a hot steam at from 100 to 140.degree. C. and a high pressure. Further, in the above-mentioned step A, the mixture is subjected to high frequency heating, making it possible to give a solid dispersion of efonidipine hydrochloride having a high intestinal absorbability without using the step B. This process is quite advantageous in the production in that the use of an organic solvent is not required. Formula (I): ##STR1##

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Patent Owner(s)

Patent OwnerAddress
NISSAN CHEMICAL INDUSTRIES LTDJAPAN
ZERIA PHARMACEUTICAL CO LTDJAPAN

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bunrin, Toyohiko Funabashi, JP 1 4
Miyamoto, Misao Funabashi, JP 11 124
Nishiyama, Tetsuyuki Saitama-ken, JP 2 4
Oda, Toshihisa Funabashi, JP 3 107
Okabe, Toshio Saitama-ken, JP 4 9

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