含柠檬酸他莫昔芬的聚乳酸-羟基乙酸共聚物缓释微球的制备与评价

Formulation and evaluation of sustained release microspheres of poly-lactide-co-glycolide containing tamoxifen citrate.

作者信息

Sehra S, Dhake A S

机构信息

Department of Pharmaceutical Sciences, Guru Jambheshwar Univeristy, Hisar, Haryana, India.

出版信息

J Microencapsul. 2005 Aug;22(5):521-8. doi: 10.1080/02652040500162170.

DOI:10.1080/02652040500162170

PMID:16361195

Abstract

Tamoxifen citrate, a non-steroidal anti-oestrogen has potential applications in treatment of breast cancer. Biodegradable microspheres of' PLGA 65:35 were prepared by o/w emulsification solvent evaporation method. In this study, different batches of varying concentration of drug, polymer, polyvinyl alcohol and solvent were prepared. All the batches prepared were characterized by particle size distribution, encapsulation efficiency and in vitro release behaviour. Drug, polymer and PVA concentrations were varied to obtain optimum release profile for sustaining the action of drug.

摘要

柠檬酸他莫昔芬是一种非甾体类抗雌激素药物，在乳腺癌治疗中具有潜在应用价值。采用水包油乳化溶剂蒸发法制备了聚乳酸-羟基乙酸共聚物（PLGA 65:35）的可生物降解微球。在本研究中，制备了不同批次、含有不同浓度药物、聚合物、聚乙烯醇和溶剂的样品。对所有制备的批次进行了粒径分布、包封率和体外释放行为表征。改变药物、聚合物和聚乙烯醇的浓度以获得最佳释放曲线，从而维持药物的作用。