School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China.
Int J Pharm. 2009 Dec 1;382(1-2):165-71. doi: 10.1016/j.ijpharm.2009.08.031. Epub 2009 Aug 28.
The objective of the present investigation was to develop and evaluate a drug-in-adhesive transdermal patch for S-amlodipine (S-AM) free base. Initial in vitro experiments were conducted to optimize the formulation parameters before transdermal delivery in rats. The effects of the type of adhesive and the content of permeation enhancers on S-AM free base transport across excised rat skin were evaluated. For in vivo studies, patches were administered transdermally to rats while orally administered S-AM in suspension and intravenously administered S-AM solution were used as controls. The plasma level of S-AM following transdermal application could be maintained for 72 h. After transdermal administration to rats, the absolute bioavailability was 88.8% for S-AM free base. After dose normalization, the areas under the plasma concentration-time curve (AUC) and mean residence times (MRT) were evidently increased and extended, respectively. This suggests that the transdermal application of S-AM in a drug-in-adhesive transdermal patch may be used for the treatment for hypertension.
本研究旨在开发和评价一种用于 S-氨氯地平（S-AM）游离碱的药物粘附型透皮贴剂。在进行大鼠透皮给药之前，进行了初步的体外实验以优化制剂参数。考察了不同类型的粘合剂和渗透促进剂的含量对游离 S-AM 经皮传递的影响。对于体内研究，将贴片经皮给予大鼠，同时以混悬液形式口服给予 S-AM，以静脉内给予 S-AM 溶液作为对照。经皮应用后，S-AM 的血浆水平可维持 72 小时。在大鼠经皮给药后，游离 S-AM 的绝对生物利用度为 88.8%。剂量归一化后，血浆浓度-时间曲线下面积（AUC）和平均驻留时间（MRT）明显增加和延长。这表明 S-AM 药物粘附型透皮贴剂的经皮给药可能用于治疗高血压。
