首页> 美国卫生研究院文献>Journal of Drug Delivery >Characterization and Compatibility Studies of Different Rate Retardant Polymer Loaded Microspheres by Solvent Evaporation Technique: In Vitro-In Vivo Study of Vildagliptin as a Model Drug
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Characterization and Compatibility Studies of Different Rate Retardant Polymer Loaded Microspheres by Solvent Evaporation Technique: In Vitro-In Vivo Study of Vildagliptin as a Model Drug

机译:溶剂蒸发技术对负载不同速率的高分子聚合物微球的表征和相容性研究:维尔格列汀作为模型药物的体外研究

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摘要

The present study has been performed to microencapsulate the antidiabetic drug of Vildagliptin to get sustained release of drug. The attempt of this study was to formulate and evaluate the Vildagliptin loaded microspheres by emulsion solvent evaporation technique using different polymers like Eudragit RL100, Eudragit RS100, Ethyl cellulose, and Methocel K100M. In vitro dissolution studies were carried out in 0.1 N HCl for 8 hours according to USP paddle method. The maximum and minimum drug release were observed as 92.5% and 68.5% from microspheres, respectively, after 8 hours. Release kinetics were studied in different mathematical release models to find out the linear relationship and release rate of drug. The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer. In this experiment, it is difficult to explain the exact mechanism of drug release. But the drug might be released by both diffusion and erosion as the correlation coefficient (R 2) best fitted with Korsmeyer model and release exponent (n) was 0.45–0.89. At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.
机译:已经进行了本研究以微囊化维格列汀的抗糖尿病药以获得药物的持续释放。这项研究的尝试是使用不同的聚合物,例如Eudragit RL100,Eudragit RS100,乙基纤维素和Methocel K100M,通过乳液溶剂蒸发技术来配制和评估载有维格列汀的微球。根据USP桨法,在0.1 N HCl中进行了8小时的体外溶出研究。 8小时后,从微球体中观察到的最大和最小药物释放分别为92.5%和68.5%。在不同的数学释放模型中研究了释放动力学,以找出药物的线性关系和释放速率。已经进行了SEM,DSC和FTIR研究,以确认良好的球形,光滑的表面以及与药物和聚合物的相互作用。在这个实验中,很难解释药物释放的确切机制。但是药物可能通过扩散和腐蚀而释放,因为最适合Korsmeyer模型的相关系数(R 2 )和释放指数(n)为0.45-0.89。最后可以得出结论,所有体外和体内实验均显示了用维格列汀微球治疗II型糖尿病的有希望的结果。

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