Bolourtchian N, Karimi K, Aboofazeli R
Department of Pharmaceutics, School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services, Tehran, Iran.
J Microencapsul. 2005 Aug;22(5):529-38. doi: 10.1080/02652040500161941.
Ibuprofen was microencapsulated with Eudragit RS using an o/w emulsion solvent evaporation technique. The effects of three formulation variables including the drug:polymer ratio, emulsifier (polyvinyl alcohol) concentration and organic solvent (chloroform) volume on the entrapment efficiency and microspheres size distribution were examined. The drug release rate from prepared microspheres and the release kinetics were also studied. The results demonstrated that microspheres with good range of particle size can be prepared, depending on the formulation components. The drug:polymer ratio had a considerable effect on the entrapment efficiency. However, particle size distribution of microspheres was more dependent on the volume of chloroform and polyvinyl alcohol concentration rather than the drug:polymer ratio. The drug release pattern showed a burst effect for all prepared microspheres due to the presence of uncovered drug crystals on the surface. It was shown that the release profiles of all formulations showed good correlation with the Higuchi model of release.
采用水包油乳液溶剂蒸发技术,用尤特奇RS对布洛芬进行微囊化。考察了药物与聚合物比例、乳化剂(聚乙烯醇)浓度和有机溶剂(氯仿)体积这三个处方变量对包封率和微球粒径分布的影响。还研究了制备的微球的药物释放速率和释放动力学。结果表明,根据处方成分,可以制备出粒径范围合适的微球。药物与聚合物比例对包封率有相当大的影响。然而,微球的粒径分布更多地取决于氯仿的体积和聚乙烯醇的浓度,而不是药物与聚合物比例。由于表面存在未包衣的药物晶体,所有制备的微球的药物释放模式均呈现突释效应。结果表明,所有制剂的释放曲线与Higuchi释放模型具有良好的相关性。