孕二烯酮避孕微针的制备和评价  

Preparation and evaluation of gestodene loaded microneedles for contraceptive

作　　者：段雪艳 马佳男 宁美英 DUAN Xueyan;MA Jainan;MING Meiying(National Research Institute for Family Planning,Beijing,100081)

机构地区：[1]国家卫生健康委科学技术研究所生殖健康工程技术研究中心,北京100081

出　　处：《中国计划生育学杂志》2024年第6期1220-1224,共5页Chinese Journal of Family Planning

基　　金：十三五国家重点研发计划课题(2016YFC1000902);中央级公益性科研院所基本科研业务费专项(2023GJM02)。

摘　　要：目的:优化孕二烯酮(GEST)避孕微针的处方及制备工艺,并对其体外特性进行评价。方法:采用模具法制备GEST溶解微针,依据微针成针性和柔韧度,选择微针基质材料,考察制备工艺中加样体积和真空干燥时间对微针形貌的影响,并对GEST微针制剂的溶解性、穿刺性能、机械强度和体外透皮释放行为进行评价。结果:聚乙烯吡咯烷酮(PVPK90)微针成针性好,微针形貌完整,且具有一定的柔韧性,因此优选100 mg/ml PVPK90为最佳基质溶液。加样体积为150μl,真空干燥45min为GEST避孕微针的最佳制备工艺。GEST避孕微针的针体具有一定的机械强度,能够刺穿幼猪皮肤的角质层。GEST避孕微针每天释放药物20μg/cm^(2),可以持续释放7d,符合Higuchi方程。此外,我们还考察了微针在大鼠体内的溶解时间,结果表明针体在2min内几乎溶解完全。结论:由此可见,GEST溶避孕微针制备方法简便,能够缓慢释放药物为人们提供了一种既新颖又便捷的皮下缓释避孕方式。Objective:To optimize the formulation and preparation technology of gestodene loaded microneedles for contraceptive,and to evaluate the in vitro characteristic of the gestodene loaded microneedles.Methods:The mold casting technique was used to prepare the gestodene loaded microneedles.The matrix materials of these microneedles were selected based on their needle-forming ability and the flexibility.The influence of the adding sample volume and the vacuum drying time on the morphology of the microneedles was researched during the preparation process.The solubility,the puncture performance,the mechanical strength and the in vitro transdermal release behavior of the microneedles were evaluated.Results:Because of the good formation and the certain flexibility,100 mg/ml PVPK90 was preferred as the optimal matrix solution.The optimal preparation process of the gestodene loaded microneedles included the adding sample volume of 150μl and the vacuum dry of 45 minutes.The gestodene loaded microneedles had certain mechanical strength,which could penetrate the stratum corneum of the porcine skin.The in vitro gestodene release amount of the microneedles was approximately 20μg/cm^(2) for 7 days consecutively,and which was best fitted by the Higuchi model.The dissolution process of the gestodene loaded microneedles after piercing into the rat skin was evaluated,and the result showed that the microneedles were almost dissolved within 2 min.Conclusion:The preparation method of the gestodene loaded microneedles is simple and the microneedles can slow release gestodene for contraception,and which provides a novel and convenient route for the subcutaneous sustained release contraceptive.

关 键 词：孕二烯酮 聚乙烯吡咯烷酮 避孕微针 体外特性 

分 类 号：R943[医药卫生—药剂学]