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Development and In-vitro Evaluation of In-situ Nasal Gels of Zafirlukast

机译:扎鲁司特原位鼻凝胶的研制和体外评价

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Zafirlukast is a leukotriene receptor antagonist used for the maintenance treatment of Asthma. It rapidly gets absorbed from gastrointestinal tract because it is subjected to first pass metabolism. The objective of the present research work was to develop and evaluate muco-adhesive in-situ nasal gels of zafirlukast. This drug delivery system can overcome first pass metabolism, enhance nasal residence time due to its mucoadhesive strength and increased viscosity thereby subsequently improving the drugs bioavailability. The in-situ nasal gels of zafirlukast were formulated using different ratios of Guar gum and HPMC-K100M polymers and were subjected to various evaluation tests. From the in-vitro permeation results, it was found that formulation F6 containing guar gum and HPMC-K100M polymers in 0.3% w/v and 1.2% w/v concentrations respectively were found to be better as compared to remaining formulations. These results demonstrate the suitability of guar gum and HPMC-K100M polymers for the fabrication of sustained release mucoadhesive in-situ nasal gels of zafirlukast.
机译:扎鲁司特是用于维持哮喘的白三烯受体拮抗剂。由于它经过首过代谢,因此会迅速从胃肠道吸收。本研究工作的目的是开发和评估Zafirlukast的粘膜黏附性鼻凝胶。该药物递送系统由于其粘膜粘附强度和增加的粘度而可以克服首过代谢,延长鼻腔停留时间,从而随后改善了药物的生物利用度。使用不同比例的瓜尔胶和HPMC-K100M聚合物配制扎鲁司特的原位鼻凝胶,并进行各种评估测试。从体外渗透结果发现,与其余制剂相比,发现分别含有0.3%w / v和1.2%w / v浓度的瓜耳胶和HPMC-K100M聚合物的制剂F6更好。这些结果证明了瓜耳胶和HPMC-K100M聚合物对于制备扎鲁司特缓释粘膜粘附性原位鼻腔凝胶的适用性。

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