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首页> 外文期刊>International Journal of Pharmaceutics >Enhanced dissolution of megestrol acetate microcrystals prepared by antisolvent precipitation process using hydrophilic additives.
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Enhanced dissolution of megestrol acetate microcrystals prepared by antisolvent precipitation process using hydrophilic additives.

机译:通过使用亲水性添加剂的反溶剂沉淀法制得的乙酸孕甾酮微晶的溶解增强。

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摘要

Microcrystals of megestrol acetate (MA), a poorly water-soluble drug, were successfully prepared using an antisolvent precipitation technique for improving the dissolution rate. The effective hydrophilic polymers and surfactants used were screened for their abilities to produce smaller particle sizes. Raw micronized MA and processed MA microcrystals were ranked by the Student-Newman-Keuls test in order of increasing particle size and SPAN values as follows: processed MA microcrystals in the presence of polymer and surfactant (mean diameter 1048nm)rocessed MA microcrystals in the presence of polymer (1654nm)rocessed MA microcrystals in the absence of polymer and surfactant (3491nm)
机译:使用抗溶剂沉淀技术可提高水溶性,成功制备了水溶性差的醋酸孕甾酮(MA)的微晶。筛选所使用的有效亲水性聚合物和表面活性剂产生较小粒径的能力。通过Student-Newman-Keuls测试对原始的微粉化MA和加工过的MA微晶进行排序,其排列顺序如下:增大粒径和SPAN值:在聚合物和表面活性剂(平均直径1048nm)存在下加工的MA微晶聚合物(1654nm)的存在<加工的MA微晶,而聚合物和表面活性剂(3491nm)的存在<原始的微粉化MA(4352nm)。 BET表面积的顺序相反。在聚合物和表面活性剂存在下加工的MA微晶略微降低了结晶度,改变了晶体习性和较好的取向,而多晶型物没有变化。另外,与原始的微粉化的MA相比,在聚合物和表面活性剂的存在下,加工的MA微晶的溶解性质显着增强。该效果主要是由于粒径减小导致表面积增加。因此,可以得出结论,在温和条件下的抗溶剂沉淀技术可能是一种制备水溶性差的药物颗粒的简单而有用的技术,该药物颗粒的粒径减小,粒径分布窄且溶解性增强。

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