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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Formulation and pharmacodynamic evaluation of captopril sustained release microparticles
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Formulation and pharmacodynamic evaluation of captopril sustained release microparticles

机译：卡托普利缓释微粒的配方和药效学评价

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摘要

Cellulose propionate (CP) microparticles containing captopril (CAP) were prepared by solvent evaporation technique.The effects of polymer molecular weight,polymer composition and drug:polymer ratios on the particle size,flow properties,morphology,surface properties and release characteristics of the prepared captopril microparticles were examined.The anti-hypertensive effect of the selected CAP formulation in comparison with aqueous drug solution was also evaluated in vivo using hypertensive rats.The formulation containing drug:polymer blend ratio 1:1.5 (1:1 low:high molecular weight CP),namely F7,was chosen as the selected formulation with regard to the encapsulation efficiency (75.1%),flow properties (theta = 24 deg,Carr index=5%,Hausner ratio =1.1,packing rate = 0.535) and release characteristics.Initial burst effect was observed in the release profile of all examined formulations.DSC and SEM results indicated that the initial burst effect could be attributed to dissolution of CAP crystals present on the surface or embedded in the superficial layer of the matrix.The release kinetics of CAP from most microparticle formulations followed diffusion mechanism.After oral administration of the selected microparticle formulation (F7) to hypertensive rats,systolic blood pressure decreased gradually over 24 h compared to reference drug solution.These results may suggest the potential application of cellulose propionate microparticles as a suitable sustained release drug delivery system for captopril
机译：采用溶剂蒸发技术制备了含有卡托普利（CAP）的丙酸纤维素（CP）微粒。聚合物分子量，聚合物组成和药物：聚合物比对制备的粒径，流动性能，形貌，表面性质和释放特性的影响检查了卡托普利微粒。使用高血压大鼠在体内还评估了所选CAP制剂与药物水溶液相比的抗高血压作用。药物：聚合物掺混比为1：1.5（1：1低：高分子量）的制剂考虑到包封效率（75.1％），流动性能（θ= 24度，卡尔指数= 5％，豪斯纳比= 1.1，填充率= 0.535）和释放特性，选择CP）（即F7）作为选择配方在所有检查的制剂的释放曲线中观察到初始破裂效应.DSC和SEM结果表明初始破裂效应可能归因于CAP c的溶解多数表面活性剂的释放动力学遵循扩散机制。对高血压大鼠口服选择的颗粒体（F7）后，收缩压在24天内逐渐降低与参比药物溶液相比，这些结果可能表明丙酸纤维素微粒作为卡托普利的合适的缓释药物输送系统的潜在应用

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