Bhatt Dinesh Chandra, Dhake Avinash Sridhar, Khar Roop Krishen, Mishra Dina Nath
Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, Haryana, India.
Yakugaku Zasshi. 2008 Sep;128(9):1325-31. doi: 10.1248/yakushi.128.1325.
The transdermal matrix films of metoprolol tartrate (MT) were prepared by casting on mercury substrate employing different ratios of polymers, ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP), using dibutyl phthalate (DBT) as a plasticizer. Four formulations were prepared. Formulations MF-1, MF-2, MF-3 and MF-4 were composed of EC and PVP in the following ratios: 4.5:0.5, 4:1, 3:2 and 2:3 respectively. The formulations were subjected to various physical characterization studies namely, thickness, weight variation, drug content, moisture uptake, in vitro drug release and in vitro skin permeation. The in vitro permeation studies were carried out across excised porcine ear skin using Franz diffusion cell. Cumulative amounts of the drug released in 24 hours from the four formulations were 69.58%, 96.13%, 98.85% and 99.60%, respectively. Corresponding values for the cumulated amounts of drug permeated across the porcine skin for the above matrix films were 124.38, 153.22, 156.46 and 163.25 mug/cm(2) respectively. By fitting the data into zero order, first order and Higuchi model, it was concluded that drug release from matrix films followed Higuchi model (r(2)=0.9147-0.9823), and the mechanism of release was diffusion mediated. Based on the physical evaluation, in vitro drug release & permeation characteristics, it was concluded that for potential therapeutic use, monolithic drug matrix films MF-3, composed of EC: PVP (3:2), may be suitable for the development of a transdermal drug delivery system of MT.
采用不同比例的聚合物（乙基纤维素（EC）和聚乙烯吡咯烷酮（PVP）），以邻苯二甲酸二丁酯（DBT）作为增塑剂，通过在汞基质上浇铸的方法制备了酒石酸美托洛尔（MT）的透皮基质膜。制备了四种配方。配方MF - 1、MF - 2、MF - 3和MF - 4中EC和PVP的比例分别为4.5:0.5、4:1、3:2和2:3。对这些配方进行了各种物理特性研究，即厚度、重量差异、药物含量、吸湿率、体外药物释放和体外皮肤渗透。使用Franz扩散池，在切除的猪耳皮肤上进行体外渗透研究。四种配方在24小时内释放的药物累积量分别为69.58%、96.13%、98.85%和99.60%。上述基质膜透过猪皮的药物累积量的相应值分别为124.38、153.22、156.46和163.25μg/cm²。通过将数据拟合到零级、一级和Higuchi模型，得出基质膜中的药物释放遵循Higuchi模型（r² = 0.9147 - 0.9823），且释放机制是扩散介导的。基于物理评价、体外药物释放和渗透特性，得出结论：对于潜在的治疗用途，由EC:PVP（3:2）组成的整体药物基质膜MF - 3可能适用于开发MT的透皮给药系统。
