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氧化苦参碱磷脂复合物自乳化释药系统的研制
引用本文:王益,李婉蓉,杨佳佳,周雪,吴林菁,甘诗泉,沈祥春,陶玲. 氧化苦参碱磷脂复合物自乳化释药系统的研制[J]. 中草药, 2018, 49(18): 4277-4283
作者姓名:王益  李婉蓉  杨佳佳  周雪  吴林菁  甘诗泉  沈祥春  陶玲
作者单位:贵州医科大学药学院;贵州医科大学天然药物资源优效利用重点实验室;药用植物功效与利用省部共建国家重点实验室;贵州省普通高等学校天然药物药理与成药性评价重点实验室;贵阳市天然药物药理与成药性评价重点实验室
基金项目:贵州省高等教育科技创新团队(黔教合人才团队字[2014]31);贵州省科技创新创新团队(黔科合人才团队[2015]4025号);贵州省高层次创新型人才百层次人才(贵州科技厅黔科合人才[2015]4029号);贵州医科大学药学国际科技合作基地(黔科合平台人才[2017]5802);贵州省科学技术基金重点项目(黔科合JZ字[2015]2002号);遵义医学院基础药理省部共建教育部重点实验室项目(黔教合KY字[2017]379);贵阳医学院博士启动基金项目(院博合J字[2017-24]号)
摘    要:目的制备氧化苦参碱(OMT)磷脂复合物(PC)自乳化释药系统(OMT-PC-SEDDS),并对其进行质量评价及体外释放度考察。方法通过伪三元相图的绘制,以乳化区域面积为指标,筛选处方中乳化剂、助乳化剂种类及混合乳化剂比值(K_m),以溶解度大小考察油相种类,确定最佳处方;并对OMT-PC-SEDDS的外观、平均粒径、自乳化时间、体外释放特性及稳定性进行评价。结果 OMT-PC-SEDDS最佳处方为乳化剂Kolliphor HS 15与助乳化剂乙醇质量比为2∶1,中链甘油三酯(MCT)与Kolliphor HS 15和乙醇的总质量的质量比为2∶8。制备得到的OMT-PC-SEDDS外观呈澄明液体,稳定性良好,加水稀释后形成浅乳白色并带淡蓝色乳光的乳液,透射电子显微镜(TEM)观察呈类球形,分布均匀;平均粒径为(355.00±19.50)nm,Zeta电位为(-12.80±0.66)mV。在pH 6.8磷酸缓冲液中,OMT、OMT-PC和OMT-PC-SEDDS的体外释放在4 h分别达到93.84%、88.39%、88.61%。结论考察所得最佳处方制备的OMT-PC-SEDDS粒径适宜,稳定性良好。

关 键 词:氧化苦参碱  磷脂复合物  伪三元相图  自乳化释药系统  体外释放  稳定性
收稿时间:2018-04-21

Development of self-emulsifying drug delivery system for oxymatrine phospholipid complex
WANG Yi,LI Wan-rong,YANG Jia-ji,ZHOU Xue,WU Lin-jing,GAN Shi-quan,SHEN Xiang-chun and TAO Ling. Development of self-emulsifying drug delivery system for oxymatrine phospholipid complex[J]. Chinese Traditional and Herbal Drugs, 2018, 49(18): 4277-4283
Authors:WANG Yi  LI Wan-rong  YANG Jia-ji  ZHOU Xue  WU Lin-jing  GAN Shi-quan  SHEN Xiang-chun  TAO Ling
Affiliation:School of Pharmacy of Guizhou Medical University, Guiyang 550025, China,School of Pharmacy of Guizhou Medical University, Guiyang 550025, China,School of Pharmacy of Guizhou Medical University, Guiyang 550025, China,School of Pharmacy of Guizhou Medical University, Guiyang 550025, China,School of Pharmacy of Guizhou Medical University, Guiyang 550025, China,Key Lab of Optimal Utilization of Natural Medicine Resources, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Key Laboratory of Pharmacology and Druggability for Natural Medicines, GMC-Guiyang City United Laboratory for Natural Medicinal Pharmacology and Drugability, Guizhou Medical University, Guiyang 550014, China,School of Pharmacy of Guizhou Medical University, Guiyang 550025, China;Key Lab of Optimal Utilization of Natural Medicine Resources, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Key Laboratory of Pharmacology and Druggability for Natural Medicines, GMC-Guiyang City United Laboratory for Natural Medicinal Pharmacology and Drugability, Guizhou Medical University, Guiyang 550014, China and School of Pharmacy of Guizhou Medical University, Guiyang 550025, China;Key Lab of Optimal Utilization of Natural Medicine Resources, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Key Laboratory of Pharmacology and Druggability for Natural Medicines, GMC-Guiyang City United Laboratory for Natural Medicinal Pharmacology and Drugability, Guizhou Medical University, Guiyang 550014, China
Abstract:
Keywords:oxymatrine  phospholipid complex  pseudo-ternary phase diagram  self-emulsifying drug delivery system  in vitro release  stability
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