目的 通过单因素考察优化处方,制备罗替戈汀原位形成植入剂.方法 采用聚乳酸-羟基乙酸共聚物(PLGA)为载体,以体外累积释放度为指标考察PLGA 类型、PLGA 相对分子质量、PLGA 质量浓度和载药量对罗替戈汀原位形成植入剂的影响,优化最佳处方.结果 罗替戈汀原位形成植入剂的最佳处方为:以PLGA 7525 5A 为载体、N-甲基-2-吡咯烷酮为溶剂的PLGA 质量浓度为25%、载药量为50%.制备的罗替戈汀原位形成植入剂体外释药30 d 累积释放度达85%以上,具明显的缓释特征.结论 罗替戈汀原位形成植入剂结合了缓释注射剂和植入剂的优点,体外具有良好的缓释效果.

Objective To optimize the formulation by single factor method, and prepare Rotigotine in situ Forming Implant. Methods Poly (lactide-co-glycolide) acid (PLGA) was used as vehicle to prepare Rotigotine in situ Forming Implant. The optimum formulation was screened by in vitro cumulative release rate as the index, and the type of PLGA, molecular weight of PLGA, concentration of PLGA, and drug loading were studied. Results The optimized formulation of Rotigotine in situ Forming Implant was as following: prepared by PLGA 7525 5A as the vehicle with the concentration of 25% in the N-methyl-2-pyrrolidone solution and 50% drug loading. Rotigotine in situ Forming Implant showed sustained release characteristics with in vitro cumulative release rate above 85% after 30 d. Conclusion Rotigotine in situ Forming Implant has advantages of sustained release injection and implant, and also has good sustained release in vitro.

山东省自然科学基金资助项目(ZR2013HQ009)