三七总皂苷多囊脂质体的制备及其质量评价  

Preparation and Quality Evaluation of Panax notoginseng Saponins Multivesicular Liposomes

作　　者：仇坤 周利梅 王朔 陈明 赖树生 尉小慧[1] QIU Kun;ZHOU Limei;WANG Shuo;CHEN Ming;LAI Shusheng;WEI Xiaohui(MOE Key Laboratory of Standardization of Chinese Medicine,Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Guangxi Key Laboratory of Comprehensive Utilization Technology of Pseudo-ginseng,Wuzhou 543002,China)

机构地区：[1]上海中医药大学中药研究所,中药标准化教育部重点实验室,上海201203 [2]广西三七综合利用技术重点实验室,广西梧州543002

出　　处：《中国药学杂志》2023年第24期2259-2266,共8页Chinese Pharmaceutical Journal

基　　金：广西科技基地和人才专项项目资助(桂科AD20297068);三七研究中心项目资助(E4-D2000402)。

摘　　要：目的制备三七总皂苷多囊脂质体,优化制备工艺并进行质量评价,探究该制剂口服给药的可能性。方法采用复乳化溶剂挥发法,分别以天然来源的大豆卵磷脂(SPC)、人工合成来源的二油酰磷脂酰胆碱(DOPC)为主要磷脂成分,以形态、粒径、药物包封率为考察指标,正交实验对处方进行优化,制备2种三七总皂苷多囊脂质体,同时对其稳定性、体外释放和离体肠吸收进行考察。结果制备了三七总皂苷-大豆卵磷脂-多囊脂质体(PNS-SPC-MVLs)、三七总皂苷-二油酰磷脂酰胆碱-多囊脂质体(PNS-DOPC-MVLs),包封率依次为(63.41±3.64)%、(86.42±1.73)%,平均中值粒径依次为(42.50±6.34)、(21.13±4.67)μm,Zeta依次电位为(-23.64±4.34)、(-18.73±3.54)mV,48 h累计释放量依次为(93.54±2.04)%、(82.46±1.05)%。离体肠吸收实验显示2种三七总皂苷多囊脂质体均可提高原料药在十二指肠、空肠和回肠部位的吸收,且PNS-DOPC-MVLs与原料药吸收相比具有统计学差异(P<0.05)。结论采用DOPC为磷脂材料制备的PNS-DOPC-MVLs具有更高的包封率和稳定性,粒径分布较为集中,二者均可有效提高药物在离体肠道的吸收。OBJECTIVE To prepare Panax notoginseng saponins(PNS)multivesicular liposomes and explore the possibility of oral administration of this preparation on the basis of optimizing the preparation process and quality evaluation.METHODS Two kinds of PNS multivesicular liposomes were prepared by double emulsification solvent evaporation method with natural soybean lecithin(SPC)and synthetic dioleyl phosphatidylcholine(DOPC)as the main phospholipid carriers.With morphology,particle size,drug encapsulation efficiency as the evaluation indexes,orthogonal experiment was used to optimize the formulation.Meanwhile,the stability,in vitro release and in vitro intestinal absorption of preparation were investigated.RESULTS Panax notoginseng saponins-soybean lecithin-multivesicular liposomes(PNS-SPC-MVLs)and Panax notoginseng saponins-dioleoylphosphatidylcholine-multivesicular liposomes(PNS-DOPC-MVLs)were prepared.The entrapment efficiency was(63.41±3.64)%,(86.42±1.73)%,and the average medium particle size was(42.50±6.34),(21.13±4.67)μm,respectively.The Zeta potentials was(-23.64±),(-18.73±3.54)mV,and the cumulative release of PNS in 48 h was(63.41±3.64)%,(86.42±1.73)%,respectively.In vitro intestinal absorption showed that these two kinds of PNS-MVLs could improve the drug absorption in the duodenum,jejunum and ileum,and PNS-DOPC-MVLs had a statistical difference compared with the crude drug absorption(P<0.05).CONCLUSION PNS-MVLs prepared with DOPC as phospholipid material have higher encapsulation efficiency and stability,and their particle size distribution is relatively concentrated.Those two kinds of PNS-MVLs can effectively improve the absorption of drugs in the isolated intestine.

关 键 词：三七总皂苷 多囊脂质体 复乳化溶剂挥发法 二油酰磷脂酰胆碱 大豆卵磷脂 

分 类 号：R944[医药卫生—药剂学]