地西泮经皮吸收凝胶的制备与生物利用度

Preparation of diazepam transdermal gel and its bioavailability

目的:制备地西泮凝胶剂,研究它的生物利用度。方法:采用卡波姆934作为凝胶基质,以甘油为保湿剂,加入月桂氮卓艹酮作为经皮吸收促进剂,用三乙醇胺调节pH值制备地西泮凝胶剂。选用家兔皮进行体外渗透试验,用HPLC法测定地西泮浓度,求算经皮渗透速率。以地西泮片剂作对照,在家兔中进行地西泮凝胶剂生物利用度试验。结果:地西泮凝胶的经皮渗透速率为39.26μg/cm2/h,其相对生物利用度为36.25%。结论:地西泮凝胶有望成为新的经皮给药制剂。

Objective： To prepare diazepam transdermal gel and to assess its bioavailability. Methods： Using Carbopol 934 as a gel matrix,the diazepam transdermal gel was prepared with glycerol as the humectant and azone as penetration enhancer.The penetration rate of diazepam through excised rabbit skin was measured by Franz diffusion cell and HPLC method.Using diazepam tablets as control,the relative bioavailability of diazepam gel was determined in rabbits. Results： The transdermal flux of diazepam gel was 39.26 g/cm2/h and the bioavailability of diazepam gel was 36.25%. Conclusion： Diazepam gel prepared in the study would be developed as a novel transdermal preparation.