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设计并体外评价酒石酸唑吡坦多颗粒漂浮型给药系统。

Design and in vitro evaluation of multiparticulate floating drug delivery system of zolpidem tartarate.

机构信息

Shri Neminath Jain Brahmacharyashram's, Shriman Sureshdada Jain College of Pharmacy (PG Course), Neminagar, Chandwad, Maharashtra, India.

出版信息

Colloids Surf B Biointerfaces. 2012 Jan 1;89:182-7. doi: 10.1016/j.colsurfb.2011.09.011. Epub 2011 Sep 14.

Abstract

Zolpidem tartarate is a non-benzodiazepine, sedative-hypnotic, which finds its major use in various types of insomnia. The present work relates to development of multiparticulate floating drug delivery system based on gas generation technique to prolong the gastric residence time and to increase the overall bioavailability. Modified release dosage form of zolpidem tartarate adapted to release over a predetermined time period, according to biphasic profile of dissolution, where the first phase is immediate release phase for inducing the sleep and the second phase is modified release phase for maintaining the sleep up to 10 h. The system consists of zolpidem tartarate layered pellets coated with effervescent layer and polymeric membrane. The floating ability and in vitro drug release of the system were dependent on amount of the effervescent agent (sodium bicarbonate) layered onto the drug layered pellets, and coating level of the polymeric membrane (Eudragit(®) NE 30D). The system could float completely within 5 min and maintain the floating over a period of 10 h. The multiparticulate floating delivery system of zolpidem tartarate with rapid floating and modified drug release was obtained.

摘要

酒石酸唑吡坦是一种非苯二氮䓬类镇静催眠药,主要用于各种类型的失眠症。本工作涉及到基于气体生成技术开发多颗粒漂浮药物递送系统,以延长胃滞留时间并提高整体生物利用度。酒石酸唑吡坦的改良释放剂型适应于在预定时间段内释放,根据溶解的双相曲线,第一相是立即释放相,用于诱导睡眠,第二相是改良释放相,用于维持睡眠长达 10 小时。该系统由酒石酸唑吡坦包衣颗粒与泡腾层和聚合物膜组成。系统的漂浮能力和体外药物释放取决于分层在药物包衣颗粒上的泡腾剂(碳酸氢钠)的量,以及聚合物膜(Eudragit(®) NE 30D)的涂层水平。该系统可以在 5 分钟内完全漂浮,并在 10 小时内保持漂浮。获得了具有快速漂浮和改良药物释放的酒石酸唑吡坦多颗粒漂浮给药系统。

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