Aqil Mohamed, Sultana Yasmin, Ali Asgar
Department of Pharmaceutics, Faculty of Pharmacy, New Delhi--110062, India.
Acta Pharm. 2003 Jun;53(2):119-25.
The monolithic matrix type transdermal drug delivery system of metoprolol tartrate were prepared by the film casting on a mercury substrate and characterised in vitro by drug release studies, skin permeation studies and drug-excipients interaction analysis. Four formulations were developed, which differed in the ratio of matrix-forming polymers. Formulations MT-1, MT-2, MT-3 and MT-4 were composed of Eudragit RL-100 and polyvinyl pyrrolidone K-30 with the following ratios: 2:8, 4:6, 6:4 and 8:2, respectively. All the four formulations carried 10% (m/m) of metoprolol tartrate, 5% (m/m) of PEG-400 and 5% (m/m) of dimethyl sulfoxide in isopropyl alcohol: dichloromethane (40:60). Cumulative amounts of the drug released in 48 hours from the four formulations were 61.5, 75.4, 84.3 and 94.5%, respectively. The corresponding values for cumulative amounts of the permeated drug for the said formulations were 53.5, 62.5, 69.8 and 78.2%. On the basis of in vitro drug release and skin permeation performance, formulation MT-4 was found to be better than the other three formulations and it was selected as the optimized formulation.
通过在汞基质上浇铸薄膜制备了酒石酸美托洛尔的整体基质型透皮给药系统，并通过药物释放研究、皮肤渗透研究和药物-辅料相互作用分析进行体外表征。开发了四种制剂，它们在成膜聚合物的比例上有所不同。制剂MT-1、MT-2、MT-3和MT-4由Eudragit RL-100和聚乙烯吡咯烷酮K-30组成，比例如下：分别为2:8、4:6、6:4和8:2。所有四种制剂在异丙醇:二氯甲烷（40:60）中含有10%（m/m）的酒石酸美托洛尔、5%（m/m）的PEG-400和5%（m/m）的二甲基亚砜。四种制剂在48小时内释放的药物累积量分别为61.5%、75.4%、84.3%和94.5%。上述制剂的药物渗透累积量的相应值分别为53.5%、62.5%、69.8%和78.2%。基于体外药物释放和皮肤渗透性能，发现制剂MT-4优于其他三种制剂，并被选为优化制剂。
