联苯苄唑乳膏体外经皮透过评价试验

Study on percutaneous permeability of bifonazole creams

目的通过离体透过性试验,评估受试联苯苄唑乳膏透过安全性的大小。方法以小型猪全皮皮肤为模型,应用改良的Franz立式扩散池,分别采用生理盐水、PEG400:生理盐水(1:2)混合液为接受液,于1、2、3、4、6、8、10 h定时取样,利用HPLC测定药物浓度。结果对照联苯苄唑乳膏样品和受试样品在生理盐水接受液的条件下,均不能透过离体的小型猪皮肤。在PEG400:生理盐水(1:2)接收液条件下,有微量透过,10 h的累积透过量受试联苯苄唑乳膏为(0.286±0.100)μg/cm2,对照联苯苄唑乳膏为(0.269±0.033)μg/cm2,二者经皮透过曲线基本一致。结论受试联苯苄唑乳膏和对照联苯苄唑乳膏在药物透过安全性大小上具有一致性。

Objective To evaluate the percutaneous permeability of bifonazole creams with miniature pig(the pama fragrant pig)full thickness skin as the model in modified franz diffusion cells. Methods Physiological saline solution and the PEG400:physiological saline solution(1:2)was used as receptor medium.The drug concentration in samples withdrawn at 1,2,3,4,6,8,10 h was determined by HPLC. Results Drug in the commercial product and test preparation could not diffuse across the excised miniature pig skin in physiological saline solution,while both of them has very low permeability under the PEG400:physiological saline solution(1:2)conditions.The cumulative permeation amount(Q,μg/cm2)of the test preparation was(0.286±0.100)μg/cm2,while the commercial product was(0.269±0.033)μg/cm2. Conclusion The commercial product and the test preparation had no difference in permeability safety,with physiological saline solution and PEG400:physiological saline solution(1:2)as receptor medium.