溶剂是以月桂氮上(艹)下(卓)酮对阿昔洛韦透皮速率的影响

 目的：研究溶剂与月桂氮上（艹)下(卓)酮对阿昔洛韦(acyclovir，ACV)透皮性能的影响。方法：采用不同的溶剂系统，测定处方中月桂氮上（艹)下(卓)酮的溶解度，采用离体大鼠皮肤与改良Franz扩散池，测定阿昔洛韦的经皮渗透速率。结果与结论：由于溶剂系统的改变，药物的溶解度与月桂氮上（艹)下(卓)酮的溶解度均发生变化。在不同溶剂中，药物经皮渗透速率与其溶解度无表观相关性，而随月桂氮上（艹)下(卓)酮溶解度的增大而增大。在水-乙醇-丙二醇-月桂氮上（艹)下(卓)酮为8：85：5：2(百分比)的溶剂中，ACV的渗透速率最大，达到(180.83士25.5)μg·cm^-2·h^-1

The effects of solvents and laurocapram on percutaneous penetration of acyclovir across the rat skin

OBJECTIVE:To study the effects of solvents and laurocapram on percutaneous penetration of acyclovir across the rat skin. METHODS:The solubility of laurocapram in various solvents containing water, alcohol and propylene glycol was determined.The percutaneous rates at steady state of ACV in the solvents across rat skin in vitro were determined using improved Franz diffusion cell. RESULTS and CONCLUSION:In the different solvents the solubility of ACV and laurocapram varied with the change of the solvents.The penetration rates of ACV hadn't relationship with its apparent solubility.On the contrary, the more laurocapam dissolved in the solvents,the bigger the penetration rates of ACV would be increased.In the solution which containing water,alcohol,propylene glycol,laurocapam(8∶85∶5∶2,% w/v) the percutaneous penetration rate of ACV was 180.83±25.5（μg·cm^-2·h^-1).