Research on the preparation of Kebannin transdermal patch and its transdermal permeation in vitro

LI Jing-yu; MA Yun-shu; YANG Zi-xian; XU He; HUANG Qiu-yan; TAN Ya; XIONG Lei

Abstract：Objective:To prepare crebanine transdermal patch,the penetrating enhancer was screened and the percutaneous permeation of crebanine in vitro was investigated.Methods:Taking the initial adhesion force and adhesion force as indexes,the matrix formula of patches were screened by orthogonal test;modified Franz diffusion cell method was used,with cumulative permeation amount and permeability coefficient as indicators,the penetration enhancing effects of 1％,3％,5％,7％,10％ azone and volatile oil offlos caryophyllii on crebanine in 48 h through mouse skin were investigated.The optimized penetrating enhancer was verified with nude mouse skin.Results:The optimizing matrix formula of patches was 0.15 g succinic acid,2 g Eudragit EPO,0.8 g diethyl phthalate,and 0.3 g of glycerin.Taking crebanine patches with 1％ azone as positive control group,and crebanine patches without penetraing enhancers as negative controlgroup,3 ％ volatile oil offlos caryophyllii as test group,the average cumulative permeation amount of crebanine in 48 h (Q4s,mg· cm-2) of the positive control and the test groups were (0.691 5 ±0.541 8) and (0.805 1 ±0.435 4) mg·cm-2,respectively;and the enhancing rates(ER) were 1.89 and 2.15 respectively.Conclusion:Under the optimized process of the preparation,the patch has suitable adhesion force;3％ volatile oil offlos caryophyllii could enhance permeation amount of crebanine through mouse skin obviously.