Prasad Verma Priya Ranjan, Chandak Ashok R
Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi-835215, India.
Acta Pharm. 2009 Jun;59(2):171-86. doi: 10.2478/v10007-009-0014-y.
The present study aimed to develop hydroxypropyl methylcellulose based transdermal delivery of pentazocine. In formulations containing lower proportions of polymer, the drug released followed the Higuchi kinetics while, with an increase in polymer content, it followed the zero-order release kinetics. Release exponent (n) values imply that the release of pentazocine from matrices was non-Fickian. FT-IR, DSC and XRD studies indicated no interaction between drug and polymer.The in vitro dissolution rate constant, dissolution half-life and pharmacokinetic parameters (C(max), t(max), AUC(s), t(1/2), Kel, and MRT) were evaluated statistically by two-way ANOVA. A significant difference was observed between but not within the tested products. Statistically, a good correlation was found between per cent of drug absorbed from patches vs. C(max) and AUC(s). A good correlation was also observed when per cent drug released was correlated with the blood drug concentration obtained at the same time point. The results of this study indicate that the polymeric matrix films of pentazocine hold potential for transdermal drug delivery.
本研究旨在开发基于羟丙基甲基纤维素的喷他佐辛透皮给药系统。在聚合物比例较低的制剂中，药物释放遵循 Higuchi 动力学，而随着聚合物含量的增加，药物释放遵循零级释放动力学。释放指数（n）值表明喷他佐辛从基质中的释放是非 Fick 扩散。傅里叶变换红外光谱（FT-IR）、差示扫描量热法（DSC）和 X 射线衍射（XRD）研究表明药物与聚合物之间没有相互作用。通过双向方差分析对体外溶出速率常数、溶出半衰期和药代动力学参数（C(max)、t(max)、AUC(s)、t(1/2)、Kel 和 MRT）进行统计学评估。在受试产品之间观察到显著差异，但在产品内部未观察到显著差异。统计学上，从贴片中吸收的药物百分比与 C(max) 和 AUC(s) 之间存在良好的相关性。当药物释放百分比与在同一时间点获得的血药浓度相关时，也观察到良好的相关性。本研究结果表明，喷他佐辛的聚合物基质膜具有透皮给药的潜力。
