克班宁透皮贴剂的制备及其体外经皮渗透实验研究

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

目的:制备克班宁透皮贴剂,筛选促渗剂并考察其体外经皮渗透作用。方法:以初黏力和持黏力为指标进行贴剂基质处方的正交试验。采用改良的FRANZ扩散池,以累积渗透量和增渗系数为指标,考察1%,3%,5%,7%和10%的氮酮和丁香挥发油对克班宁透皮贴剂经小鼠皮肤的促渗作用,并用裸鼠进行验证。结果:优选的贴剂处方为丁二酸0.15 g,Eudragit EPO 2 g,邻苯二甲酸二乙酯0.8 g,甘油0.3 g。1%氮酮组和3%丁香挥发油的Q48分别为(0.691 5±0.541 8)和(0.805 1±0.435 4)mg·cm-2,增渗系数分别为1.89和2.15。结论:在优选处方下制备的贴剂黏附力适宜;3%丁香挥发油能显著提高克班宁在贴剂中的渗透量。

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 of flos 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 of flos caryophyllii as test group,the average cumulative permeation amount of crebanine in 48 h（ Q48,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 of flos caryophyllii could enhance permeation amount of crebanine through mouse skin obviously.