Delayed release microtablet of b-phenylpropiophenone...

A - Human Necessities – 61 – K

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Details

A61K 31/138 (2006.01) A61J 3/10 (2006.01) A61K 9/22 (2006.01) A61K 9/48 (2006.01) A61P 9/06 (2006.01)

Patent

CA 2437412

The invention concerns cylindrical retarded-action tablets having convex or planar upper and lower surfaces and made of .beta.-phenylpropiophenone derivatives of formula (I) acting as the active ingredient, in which R = n-propyl or 1,1- dimethylpropyl, and pharmacologically acceptable salts of such derivatives, a) tablet height and diameter, independently of each other, being 1 to 3 mm; b) the concentration of the active ingredient lying in the range from 81 to 99.9 % by wt. relative to the weight of the microtablet, neglecting the weight of any coating present; c) the density of the active ingredient being greater than 1; d) at least 80 % of the active ingredient being released between 3 hours and 24 hours when tested using the USP paddle model at 50 rpm; e) the rate of release being virtually independent of the pressure used to compress the tablet; f) the tablet containing no retarding- action auxiliaries but 0.1 to 5 % by wt. of a lubricant and 0 to 18.9 % by wt. of other usual auxiliaries. The invention also concerns a gelatin capsule containing 3 to 200 such tablets with the same or different release rates, plus a method of producing the tablets. (See Formula I)

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