| abstract |
[PROBLEMS] To reduce the number of doses by suppressing the release rate of an active agent contained in a solid release-suppressing oral dosage formulation and extending the period of relief of patient pain after administration while maintaining the drug effect. is there. SOLUTION: The dissolution rate of a dosage formulation in vitro is about 12.5% to about 42.5% (by weight) after 1 hour when measured at 100 rpm with 900 ml of aqueous buffer at 37 ° C. by USP paddle method. Active agent (Obioid analgesic), release about 25% to about 65% (by weight) of active agent after 2 hours, release about 45% to about 85% (by weight) of active agent after 4 hours More than about 60% (by weight) of the opioid analgesic is released after 8 hours, and the release rate in vitro is substantially independent of pH, and the maximum plasma of the active reagent obtained in vivo From a therapeutically effective amount of an opioid analgesic or salt thereof, the level of which is selected to occur between about 2 and about 8 hours after administration of the dosage formulation, prolonging the release period from about 24 hours of pain. A solid release-suppressing oral dosage formulation. [Selection figure] None |