In vivo study of pH Dependent and Enzymatically Triggered Colon Targeted Tinidazole Microspheres

Poonam Kushwaha
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Abstract

Introduction: Shellac coated Tinidazole (TNZ) loaded pectin microspheres with the potential for colon targeted delivery has been evaluated to study in-vivo behavior. Materials and Methods: Biodistribution and pharmacokinetic studies were performed for the determination of concentration of TNZ in rats. This method was used to evaluate the colon targeting property of TNZ loaded microspheres. Pure TNZ or TNZ microspheres were given to rats by oral administration. Plasma and the different parts of gastrointestinal (GI) tract were taken after 2, 8, 12 and 24 h of oral administration of pure TNZ or TNZ microspheres to rats and the concentration of TNZ was measured. Results and Conclusion: Results obtained shows that pure TNZ distributes mainly in stomach and in low concentration to small intestine and colon. However, TNZ released from microspheres mainly distributes in colon. Therefore, this approach suggests that shellac coated TNZ loaded pectin microspheres has a good colon targeting property. Key words: Biodistribution study, Colon targeting, Pharmacokinetic study, Pectin microspheres, Tinidazole.
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pH依赖性和酶促结肠靶向替硝唑微球的体内研究
介绍:紫胶包覆的替硝唑(TNZ)负载果胶微球具有结肠靶向递送的潜力,已经被评估以研究其体内行为。材料与方法:采用生物分布和药代动力学方法测定TNZ在大鼠体内的浓度。利用该方法评价了载TNZ微球的结肠靶向性。给大鼠口服纯TNZ或TNZ微球。分别于大鼠口服纯TNZ或TNZ微球2、8、12、24 h后取血浆及胃肠道不同部位,测定TNZ浓度。结果与结论:纯TNZ主要分布于胃内,低浓度分布于小肠和结肠。而微球释放的TNZ主要分布在结肠。因此,该方法表明,紫胶包被负载TNZ的果胶微球具有良好的结肠靶向性。关键词:生物分布研究,结肠靶向,药代动力学研究,果胶微球,替硝唑
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