在某些特殊情況下，口服調(diào)釋制劑中控制釋放的高分子輔料或膜控材料被酒精提前溶解，或部分溶解及變性，導(dǎo)致活性成分的釋放方式、速率或程度發(fā)生變化，使其血液濃度短時(shí)間內(nèi)升高，產(chǎn)生突釋效應(yīng)。綜述了乙醇對(duì)調(diào)釋制劑藥物生物利用度和生物等效性的影響，對(duì)美國(guó)食品藥品監(jiān)督管理局、歐洲藥物管理局等藥品監(jiān)管機(jī)構(gòu)對(duì)劑量突釋試驗(yàn)的要求以及減少酒精引起的調(diào)釋制劑藥物突釋風(fēng)險(xiǎn)的方法進(jìn)行介紹，以指導(dǎo)調(diào)釋制劑的研發(fā)及一致性評(píng)價(jià)，為我國(guó)仿制藥質(zhì)量和療效的一致性評(píng)價(jià)提供借鑒。

In some special cases, high polymer materials or membrane materials of oral controlled release formulation dissolved or partly dissolved and degenerated in advance by alcohol lead to changes of the release mode, rate, and degree of active ingredients, which may result in an uncontrolled and immediate drug release. The effect of alcohol on dose dumping of modified-release preparations and regulatory considerations of US Food and Drug Administration and European Medicines Agency were studied and analyzed. Moreover, the design of modified-release formulations resistant to alcohol-induced dose dumping was discussed. To guide the development and consistency evaluation of release preparations and to provide reference for the agreement evaluation of the quality and efficacy of generic drug products in China.

國(guó)家"重大新藥創(chuàng)制"科技重大專項(xiàng)資助項(xiàng)目（2017ZX09101001）