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Formulation, in-vitro & in-vivo evaluation of Ethyl cellulose microspheres of Glipizide

机译:格列吡嗪乙基纤维素微球的配制,体外和体内评估

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Objective: The objective of the present study was to formulate sustained release glipizide loaded microspheres and evaluate the effect of various variables on their properties. Materials and Methods: The microspheres were prepared by non solvent addition coacervation method. Ethyl cellulose used as a polymer, petroleum ether (60-40o) for induced coacervation and n-hexane as non solvent for microspheres preperation. Results: Microspheres were characterized in term of percent yield, percent entrapment and release pattern of drug. The shape, color and particle size of microspheres were also evaluated. According the result of formulation, n-hexane used as non solvent resulted in enhances rigidization of coating and petroleum ether (60-40o) for induced coacervation. The maximum percent yield of GEN6 formulation was 75.7; particle size in the range of 50-450 μ, maximum entrapment was 89.8 ± 0.11% for GEN3 formulation. GEN1 formulation with low polymer ratio showed better in-vitro release between 95-100%. Formulation GEN4 showed 40-50% reduction in plasma glucose level than conventional dosage forms when tested in-vivo . Conclussion: Result of the present study supported that the formulation showed sustenance release with the potential application of n-hexane for improving the physical properties as well as the release profile of this water insoluble drug.
机译:目的:本研究的目的是配制缓释格列吡嗪负载的微球,并评估各种变量对其性质的影响。材料与方法:采用非溶剂加成凝聚法制备微球。乙基纤维素用作聚合物,石油醚(60-40o)用于诱导凝聚,正己烷作为非溶剂用于微球制备。结果:微球通过收率,药物截留率和释放模式进行了表征。还评估了微球的形状,颜色和粒径。根据配方结果,正己烷用作非溶剂可增强涂层和石油醚(60-40o)的刚性,以诱导凝聚。 GEN6制剂的最大产率为75.7;粒径在50-450μm的范围内,GEN3制剂的最大截留率为89.8±0.11%。具有低聚合物比率的GEN1制剂在95-100%之间显示出更好的体外释放。当体内测试时,制剂GEN4显示出血浆葡萄糖水平比常规剂型降低40-50%。结论:本研究结果支持该制剂显示出维持性释放以及正己烷的潜在应用,以改善该水不溶性药物的物理性质以及释放曲线。

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