Shabbir Maryam, Ali Sajid, Raza Moosa, Sharif Ali, Akhtar Furoan Muhammad, Manan Abdul, Fazli Ali Raza, Younas Neelofar, Manzoor Iqra
Acta Pol Pharm. 2017 Jan;74(1):187-197.
A matrix transdermal patch of bisoprolol fumarate was formulated with different concentrations of Eudragit RS 100 and Methocel E5 with PEG 400 as plasticizer by solvent evaporation technique. Tween 80 was added to the optimized patch to evaluate the effect of permeation enhancer at different concentration through the excised rabbit's skin. The patches were analyzed for weight variation, drug content, swelling index, erosion studies, moisture content, moisture uptake, water vapor transmission rate (WVTR) and water vapor permeability (WVP). In vitro dissolution test was carried out in USP dissolution apparatus V to select the optimized formulation. In vitr skin permeation studies were done in Franz diffusion cell using rabbit skin as a model membrane. The cumulative drug release and flux were determined to compare the result of test patches with a control patch. The greatest enhancement ratio (ER) was obtained in F03-PE with 30% Tween 80. F03-PE seemed to follow zero order kinetics with super case II mechanism of drug release. Statistical ANOVA suggested that there was a significant difference in formulations, steady flux and cumulative permeation rate at different Tween 80 concentrations.
采用溶剂蒸发技术，以不同浓度的丙烯酸树脂RS 100和羟丙甲纤维素E5，并以聚乙二醇400作为增塑剂，制备了富马酸比索洛尔的基质型透皮贴剂。将吐温80添加到优化后的贴剂中，以评估不同浓度的渗透促进剂对离体兔皮渗透的影响。对贴剂进行了重量变化、药物含量、溶胀指数、侵蚀研究、水分含量、吸湿量、水蒸气透过率（WVTR）和水蒸气透过性（WVP）分析。在USP溶出度仪V中进行体外溶出试验，以筛选优化后的制剂。采用兔皮作为模型膜，在Franz扩散池中进行体外皮肤渗透研究。测定累积药物释放量和通量，以将测试贴剂的结果与对照贴剂进行比较。在含30%吐温80的F03-PE中获得了最大增强比（ER）。F03-PE似乎遵循零级动力学，药物释放机制为超Ⅱ型。统计方差分析表明，不同吐温80浓度下的制剂、稳态通量和累积渗透速率存在显著差异。
