目的 通過單因素考察優(yōu)化處方,制備羅替戈汀原位形成植入劑.方法 采用聚乳酸-羥基乙酸共聚物(PLGA)為載體,以體外累積釋放度為指標考察PLGA 類型、PLGA 相對分子質(zhì)量、PLGA 質(zhì)量濃度和載藥量對羅替戈汀原位形成植入劑的影響,優(yōu)化最佳處方.結(jié)果 羅替戈汀原位形成植入劑的最佳處方為:以PLGA 7525 5A 為載體、N-甲基-2-吡咯烷酮為溶劑的PLGA 質(zhì)量濃度為25%、載藥量為50%.制備的羅替戈汀原位形成植入劑體外釋藥30 d 累積釋放度達85%以上,具明顯的緩釋特征.結(jié)論 羅替戈汀原位形成植入劑結(jié)合了緩釋注射劑和植入劑的優(yōu)點,體外具有良好的緩釋效果.

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.

山東省自然科學基金資助項目(ZR2013HQ009)