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Razvoj matriksnih sustava za transdermalnu isporuku pentazocina: In vitro/in vivo ispitivanje

机译:喷他佐辛透皮给药基质系统的开发:体外/体内研究

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摘要

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 (Cmax, tmax, AUC(s), t1/2, 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. Cmax, 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.
机译: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。在聚合物含量较低的配方中,药物的释放遵循Higuchi动力学,而随着聚合物含量的增加,药物遵循零级释放动力学。释放指数(n)值表明戊唑嗪从基质的释放是非菲克式的。 FT-IR,DSC和XRD研究表明药物与聚合物之间没有相互作用。体外溶出速率常数,溶出半衰期和药代动力学参数(Cmax,tmax,AUC(s),t1 / 2,Kel和MRT)为通过双向方差分析进行统计学评估。在被测产品之间观察到显着差异,但未见差异。从统计学上看,从贴剂吸收的药物百分比与Cmax和AUC之间存在良好的相关性。当释放的药物百分比与同一时间点获得的血液药物浓度相关时,也观察到良好的相关性。这项研究的结果表明,喷他佐辛的聚合物基质薄膜具有透皮给药的潜力。

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