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为提高抗精神分裂症药物帕利哌酮的脂溶性,设计了其酯前药isoperidone。采用o/w型乳化溶剂蒸发法制备了载isoperidone的长效聚乳酸-羟基乙酸共聚物(PLGA)微球,其外观呈平整光滑的球形,且包封率达92%。在pH 7.4介质中的体外释药呈双相释放特征,最初8d内几乎不释药(即无突释),d8~d20的释放呈近零级释放特征,此阶段释出总药量的
To increase the lipid solubility of the anti-schizophrenic drug paliperidone, its ester prodrug isoperidone was designed. The long-acting poly (lactic-co-glycolic acid) (PLGA) microspheres containing isoperidone were prepared by o / w emulsification solvent evaporation. The appearance of the microspheres was smooth and spherical, and the encapsulation efficiency was 92%. The in vitro release in pH7.4 medium showed biphasic release with almost no release in the first 8 days (ie, no burst release), and the release of d8-d20 was nearly zero-order release characteristic.