基于薄荷油为油相的红花提取物自微乳凝胶递送系统制备研究  

Preparation of self-microemulsion gel drug delivery system of Carthamus tinctorius extract based on Mentha haplocalyx oil as oil phase

作　　者：贺智勇 邹弢 罗田 李婉蓉 杨佳佳 刘学 肖婷 周雪 吴林菁 刘文 沈祥春 陶玲 HE Zhi-yong;ZOU Tao;LUO Tian;LI Wan-rong;YANG Jia-jia;LIU Xue;XIAO Ting;ZHOU Xue;WU Lin-jing;LIU Wen;SHEN Xiang-chun;TAO Ling(Key Laboratory of Functions and Applications of Medicinal Plants,High Educational Key Laboratory of Natural Medicinal Pharmacology and Druggability of Guizhou Province,Guizhou Medical University-Guiyang Key Laboratory of Natural Medicine Resources,Key Laboratory of Optimal Utilization of Natural Medicinal Resources,School of Pharmacy,Guizhou Medical University,Guiyang 550025,China;Guizhou Orthopedics Hospital,Guiyang 550002,China;Affiliated Hospital of Guizhou Medical University,Guiyang 550004,China;Division of Chemistry,Department of Medical Sciences,Faculty of Medicine,University of Miyazaki,5200 Kihara,Kiyotake,Miyazaki 889-1692,Japan)

机构地区：[1]贵州医科大学药学院贵州省天然药物资源高效利用工程中心,贵州省高等学校天然药物药理与成药性评价特色重点实验室,贵州医科大学-贵阳市联合重点实验室,天然药物资源优效利用重点实验室,贵州贵阳550025 [2]贵州省骨科医院,贵州贵阳550002 [3]贵州医科大学附属医院,贵州贵阳550004 [4]宮崎大学医学部機能制御学講座物質科学分野日本宮崎県宮崎市清武町木原5200番地889-1692,日本

出　　处：《中草药》2020年第11期2922-2928,共7页Chinese Traditional and Herbal Drugs

基　　金：贵州省天然药物成药性人才基地[黔人颁发(2018)3号];贵州省高层次创新型人才“百层次”人才项目[黔科合人才(2015)4029号];贵州省科技厅国际合作项目[黔科合外G字(2012)7041号]。

摘　　要：目的制备以薄荷油(Menthaha plocalyx oil,MPO)为油相的红花提取物(Carthamus tinctorius extract,CTE)自微乳凝胶递送系统(CTE-SMEDDS-BGs)。方法以MPO为油相,CTE为水相,采用伪三元相图法优选载药自微乳处方,采用单因素法筛选凝胶工艺与处方,并对其外观性状、黏度和pH值进行评价。结果所得CTE-SMEDDS-BGs最佳处方工艺:F68为乳化剂,无水乙醇为助乳化剂,乳化剂与助乳化剂比例(Km)为1∶1,乳化剂和助乳化剂总量(TS)与MPO的比例为8∶2,卡波姆2%,甘油6%,CTE5m L。处方量自微乳加入溶胀后的凝胶基质,三乙胺调节pH值至6.0即得CTE-SMEDDS-BGs;其外观为黄色半透明、黏稠度适中、均匀细腻、不油腻,易涂展的胶状凝胶,黏度为4.98×10~4m Pa·s(RSD为1.53%),pH为6.04(RSD为0.44%)。结论制得的薄荷油为油相的CTE-SMEDDS-BGs,制备简便,方法稳定,符合凝胶局部外用制剂要求。Objective To prepare the self-microemulsion gel drug delivery system of Carthamus tinctorius extract based on Mentha haplocalyx oil as oil phase. Methods M. haplocalyx oil was used as the oil phase, and C. tinctorius extract was used as the water phase. The prescription of self-microemulsion were optimized by pseudo-ternary phase diagram, the process and prescription of gel were screened by single-factor method and the appearance, viscosity and pH value were evaluated. Results The optimal formulation of CTE-SMEDDS-BGs was as following: F68 was the emulsifier, anhydrous ethanol was the co-emulsifier, the Km ratio was 1∶1, and the total amount of emulsifier and co-emulsifier to M. plocalyx oil was 8∶2, carbopol-980 was 2%, glycerin was 6%, and C. tinctorius extract was 5 mL. The CTE-SMEDDS-BGs was obtained by adding the CTE-SMEDDS into swelling gel matrix and triethylamine was used to adjust the pH to 6.0. The characteristics of appearance were yellow translucent, moderate viscosity, uniform and delicate, non-greasy, and easy to spread on the skin, the viscosity was 4.98 × 10~4 mPa·s(RSD was 1.53%), pH was 6.04(RSD was 0.44%). Conclusion The CTE-SMEDDS-BGs with M. plocalyx oil as oil phase is simple and stable, and meets the requirements of gel topical preparations.

关 键 词：红花提取物 薄荷油 自微乳 凝胶 递送系统 伪三元相图法 局部外用 

分 类 号：R283.6[医药卫生—中药学]