马钱子总碱-白芍总苷配伍凝胶剂的制备及其经皮吸收性能的考察

Preparation of Total Alkaloids of Strychni Semen-Total Qlucosides of Paeony Gel and Its Transdermal Absorption

目的旨在制备马钱子总碱-白芍总苷配伍凝胶剂,研究配伍前后2种马钱子生物碱(马钱子碱和士的宁)体外经皮吸收的影响。方法采用改良Franz扩散池,以离体小鼠皮肤为透皮屏障,选择合适的接收液,HPLC测定配伍前后接收液和皮肤中2种马钱子生物碱的含量,计算其累积渗透量和透皮速率等渗透动力学参数。结果以20%乙醇-生理盐水做接收液,与单独马钱子总碱凝胶比较,1∶1、1∶3、1∶6马钱子总碱-白芍总苷配伍凝胶剂中马钱子碱和士的宁24h累积透过量分别下降了22.7%、48.4%、69.1%和5.93%、23.8%、80.7%。且随着配伍比例的增加,渗透速率及皮肤滞留率也逐渐降低。结论马钱子总碱配伍白芍总苷经皮给药可以减少毒性成分的透过量,有一定的"减毒"作用,效果最佳比例为1∶6。

OBJECTIVE To prepare the total alkaloids of Strychni Semen（TASS） -total glucosides of Paeony （TGP） gel and stud- y its in vitro transdermal absorption of two alkaloids（ strychnine and brucine） after the combination of TASS and TGP. METHODS The excised abdominal skin of mice was used as the permeation model. Utilizing the modified Franz diffusion cell, the suitable receiv- ing solution was elected to test the content of two alkaloids by HPLC, and thus the percutaneous rates and permeability coefficients were obtained. RESULTS 20% Ethanol-normal saline was taken as receiving solution. With combination use of TASS and TGP, the pen- etration quantities of strychnine and brucine in different （ 1 ： 1,1 ： 3,1 ： 6 ） gels were felled by 22. 7 %, 48. 4%, 69. 1% and 5. 93 %, 23.8% ,80. 7% after 24 h. And with the increase of compatibility proportion, infiltration rate and skin retention rate also gradually reduced. CONCLUSION The compatibility of TASS and TGP drug delivery can reduce the toxic ingredients through capacity, there is a ＂attenuated＂ effect, the best ratio is 1：6.