ДЖЕНКИНС Томас Э. (US),ХАСФЕЛД Крэйг О. (US),СЕРУДЖИ Джули Д. (US),РЭЙ Джонатан В. (US)
申请号：
RU2012149438/15
公开号：
RU2012149438A
申请日:
2010.04.21
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
1. A composition comprising: an opioid prodrug comprising an opioid covalently bound to profragment containing GI enzyme cleavable moiety, wherein cleavage of the enzyme-cleavable moiety GI GI enzyme mediates the release of the opioid iingibitor GI enzyme that interacts with GI enzyme that mediates the enzymatically-controlled release of the opioid from the opioid prodrug kompozitsii.2 after ingestion. A unit dose comprising a composition according to claim 1, a prodrug gdeopioidnoe GI enzyme and inhibitor are present in a unit dose in an amount effective to provide a preselected pharmacokinetic (PK) profile after receiving vnutr.3. A unit dose according to claim 2, wherein the preselected RK profile includes at least one value of RK parameter that is less than the value of the parameter PK opioid released after oral administration of equivalent dosages of opioid prodrug absence ingibitora.4. Unit doses according to claim 3, wherein RC is selected from the parameter value Cmax of the opioid, opioid exposure value and the value (1 / Tmax opioid) .5. A unit dose according to claim 2, wherein the unit dose provides a preselected PK profile after oral administration of at least two units dozy.6. The unit dose of claim 5, wherein the preselected profile RK modified relative PK profile after oral administration of equivalent dosages of opioid prodrug absence ingibitora.7. The unit dose of claim 5, wherein a unit dose provides at intake increased number of dose units linear profil.8 RK. The unit dose of claim 5, wherein a unit dose provides at intake An increase
