马钱子总碱纳米脂质体凝胶的制备及渗透动力学研究  

Preparation and in vitro osmotic kinetics evaluation of total alkaloids of Strychnos nux-vomica L.of nanoliposome gels

作　　者：李海平 王晓慧 谢骥 张运良 李明娟 LI Haiping;WANG Xiaohui;XIE Ji;ZHANG Yunliang;LI Mingjuan(Department of Pharmacy,Hu'nan Shaoyang Hospital of Traditional Chinese Medicine,Shaoyang 422001,China;School of Pharmacy,Hu'nan Shaoyang University,Shaoyang 422000,China)

机构地区：[1]湖南邵阳中医医院药剂科,邵阳422001 [2]湖南邵阳学院药学院,邵阳422000

出　　处：《西北药学杂志》2022年第2期82-87,共6页Northwest Pharmaceutical Journal

基　　金：湖南省中医药科研计划项目重点课题(编号:2021051)。

摘　　要：目的优化马钱子总碱纳米脂质体凝胶(total alkaloids of Strychnos nux-vomica L.of nanoliposome gel,TAS-NL-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(total alkaloids of Strychnos nux-vomica L.,TAS)的载药量并改善其经皮渗透性能。方法用硫酸铵主动载药技术制备马钱子纳米脂质体(total alkaloids of Strychnos nux-vomica L.of nanoliposome,TAS-NL),设置不同促渗剂、混合促渗剂比例、载药量为处方制备的影响因素,单因素确定响应点,正交实验设计L_(9)(3^(4))优化TAS-NL-Gel处方;用Franz扩散装置,通过24 h单位面积累积释药量的测定,比较TAS-NL-Gel和马钱子总碱凝胶(total alkaloids of Strychnos nux-vomica L.gel,TAS-Gel)的体外渗透动力学规律。结果载药量为100μg·g^(-1)、氮酮的质量浓度为30 mg·mL^(-1)、氮酮-丙二醇-桉叶油的比例为2∶2∶1时为最佳处方方案;动力学结果显示,24 h内TAS-NL-Gel中马钱子碱、士的宁单位面积累积释药量和皮肤滞留率均高于TAS-Gel,说明TAS-NL-Gel透皮吸收和缓释作用优于TAS-Gel(P<0.05)。结论TAS-NL-Gel的处方稳定,质量可控,体外渗透动力学性能良好并具有潜在的缓释功能。Objective To prepare the total alkaloids of Strychnos nux-vomica L.nano-liposome gels(TAS-NL-Gel)and to investigate the in vitro osmotic kinetics,therefore to improve the drug loading and transdermal permeability of total alkaloids of Strychnos nux-vomica L.(TAS).Methods TAS-NL was prepared by ammonium sulfate drug loading technology.Different permeability enhancers,the proportion of mixed permeability enhancers and the drug loading were set as the influencing factors.The corresponding points were determined by single factor,and the formulation of TAS-NL-Gel was optimized by orthogonal experimental design L_(9)(3^(4)).Franz diffusion device was used to measure the cumulative drug release rate per unit area for 24 hours,The pharmacokinetics of TAS-NL-Gel and TAS-Gel were compared in vitro.Results When the drug loading was 100μg·g^(-1),azone was 30 mg·mL^(-1),and the ratio of azone-propylene glycol-eucalyptus oil was 2∶2∶1,the optimum prescription scheme can be achieved.Kinetic results showed that the cumulative drug release rate per unit area and skin retention rate of brucine and strychnine in TAS-NL-Gel within 24 hours were higher than those in TAS-Gel,indicating that the transdermal absorption and sustained-release properties of TAS-NL-Gel were better than those of TAS-Gel(P<0.05).Conclusion The formulation of TAS-NL-Gel is stable and its quality is controllable.It has good in vitro osmotic kinetics and potential slow release function.

关 键 词：马钱子 总生物碱 纳米脂质体 Franz扩散池法 渗透动力学 

分 类 号：R94[医药卫生—药剂学]