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Comparison of vegetable and volatile oils as skin permeation enhancers for transdermal delivery of losartan potassium

机译:比较植物油和挥发油作为透皮递送氯沙坦钾的皮肤渗透促进剂

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The present work comprises the formulation and evaluation delivery system of transdermal drug with a view of developing and preparing a losartan potassium releasing system utilizing natural oils as permeation enhancers for transdermal applications. Matrix systems were prepared by using polyvinyl pyrrolidine and ethyl cellulose (EC) polymers by incorporating dibutyl phthalate as plasticizer and chloroform as solvent. The physicochemical and in vitro drug release studies indicated that formulation containing PVP and EC in the ratio of 3:2 was better than other combination of polymers.Penetration enhancing potential of vegetable oils (jojoba oil, sunflower oil, sesame oil) and volatile oils (clove oil, peppermint oil, eucalyptus oil) was determined by incorporating oils in different concentration in optimized transdermal patch and in vitro permeation of losartan potassium across goat skin was studied. Maximum transdermal flux of 0.29 mg/cm2/h was obtained with formulation containing 10 % jojoba oil (vegetable oil) as permeation enhancer while in case of volatile oil maximum transdermal flux of 0.27 mg/cm2/h was obtained with 10% peppermint oil as permeation enhancer respectively. The results of permeation fluxes supported the data for prolongation of drug release characteristics of formulated transdermal films. The release kinetics revealed that the release was sustained and it follows zero-order kinetics. Stability studies of optimized formulation were stable at 45° C &75% RH with respect to their physical parameters and in vitro drug release. This suggests the transdermal application of losartan potassium holds promising for improved bioavailability and better alternative to oral dosage form in hypertensive patients.
机译:当前的工作包括透皮药物的配制和评估递送系统,以开发和制备利用天然油作为透皮应用的渗透促进剂的氯沙坦钾释放系统。通过使用聚乙烯基吡咯烷和乙基纤维素(EC)聚合物并结合邻苯二甲酸二丁酯作为增塑剂和氯仿作为溶剂来制备基质体系。理化和体外药物释放研究表明,以3:2的比例包含PVP和EC的制剂优于其他聚合物组合物。渗透增强了植物油(霍霍巴油,葵花籽油,芝麻油)和挥发油(通过在优化的透皮贴剂中掺入不同浓度的油来确定丁香油,薄荷油,桉树油),并研究了氯沙坦钾在山羊皮肤中的体外渗透性。含有10%的荷荷巴油(植物油)作为渗透促进剂的配方获得的最大透皮通量为0.29 mg / cm2 / h,而在挥发油的情况下,以10%的薄荷油作为配方可获得的最大透皮通量为0.27 mg / cm2 / h渗透促进剂。渗透通量的结果支持了延长配制的透皮薄膜的药物释放特性的数据。释放动力学表明释放是持续的,并且遵循零级动力学。就其物理参数和体外药物释放而言,优化制剂的稳定性研究在45°C和75%RH下是稳定的。这表明氯沙坦钾的透皮应用有望改善高血压患者的生物利用度并成为口服剂型的更好替代品。

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