马钱子总碱脂质液晶纳米粒镇痛凝胶的研制  

Preparation of liquid crystal analgesic gel of total alkaloids of Brucine lipid

作　　者：王晓慧 孙双姣 张运良 李明娟 李成舰 WANG Xiaohui;SUN Shuangjiao;ZHANG Yunliang;LI Mingjuan;LI Chengjian(School of Pharmacy,Shaoyang University,Shaoyang 422000,China;Hunan Engineering Research Center of Development and Utilization of Traditional Chinese Medicine in Southwest Hunan,Shaoyang 422000,China)

机构地区：[1]邵阳学院药学院,湖南邵阳422000 [2]湘西南中药开发利用湖南省工程研究中心,湖南邵阳422000

出　　处：《邵阳学院学报（自然科学版）》2022年第1期97-104,共8页Journal of Shaoyang University：Natural Science Edition

基　　金：湘西南中药开发利用湖南省工程研究中心开放性基金(2021A10);湖南省中医药科研计划重点课题(2021051);湖南省大学生创新创业项目(S202110547046)。

摘　　要：目的优化马钱子总碱脂质液晶纳米粒镇痛凝胶(TAB-LLCN-Gel)的制备工艺,并考察其体外渗透动力学规律,以期提高马钱子总碱(TAB)的载药量和改善其经皮渗透性能。方法采用硫酸铵主动载药技术制备马钱子脂质液晶纳米粒(TAB-LLCN),以马钱子碱含量为考察指标,单因素分析确定响应点,正交设计L_(9)(3^(4))优化制备工艺;利用Franz扩散池,通过测定24 h单位面积累积释药量(Q_(24))和皮肤滞留量(Q_(s24)),比较TAB-LLCN-Gel和马钱子凝胶(TAB-Gel)的体外药动学的差异。结果载药量为100μg/g、氮酮浓度为30 mg/mL、氮酮∶丙二醇∶桉叶油的比例为2∶2∶1时为最佳处方方案。药动学结果显示,24 h内TAB-LLCN-Gel中马钱子碱中Q_(24)和Q_(s24)均高于TAB-Gel。结论最优处方工艺制备的TAB-LLCN-Gel制剂表征稳定,质量可控。透皮吸收和缓释作用均优于TAB-Gel,具有良好的开发前景。Objective In order to improve the drug loading and transdermal permeability of total alkaloids of Brucine(TAB),the liquid crystal analgesic gel of total alkaloids of Brucine lipid(TAB-LLCN-Gel)was optimized,and the in vitro osmotic kinetics was investigated.Methods TAB-LLCN was prepared by ammonium sulfate active drug loading technology.The content of Brucine was used as the index,and the corresponding points were determined by single-factor analysis.Orthogonal design L_( 9)(3^(4))was used to optimize the formulation process.The Franz diffusion pool was applied to measure cumulative drug release per unit area(Q_(24))and skin retention(Q _(s24))for 24 h.The in vitro pharmacokinetic differences of TAB-LLCN-Gel and TAB-Gel were compared.Results The optimal prescription was as follows:the drug-loading capacity was 100μg/g,the concentration of azone was 30 mg/mL,and the ratio among azone,propylene glycol,and eucalyptus oil was 2∶2∶1.Pharmacokinetic results showed that Brucine Q_(24) and Q_(s24 )in TAB-LLCN-Gel were higher than those in TAB-Gel within 24 h.Conclusion The prescription of TAB-LLCN-Gel is stable and its quality is controllable.Transdermal absorption and sustained release are better than those of TAB-Gel,with a good development prospect.

关 键 词：脂质液晶纳米粒 马钱子 马钱子碱 总生物碱 Franz扩散池法 药动学 

分 类 号：TQ46[化学工程—制药化工]