冲和凝胶有效成分的体外透皮行为研究

In vitro transdermal behavior of effective constituents in Chonghe gel

冲和凝胶源自古方,可用于糖尿病足的治疗。该实验以芍药苷、蛇床子素为指标,考察冲和凝胶体外透皮特性,探索冲和凝胶透皮机制。实验采用Franz扩散池法,以大鼠腹皮为模型,用HPLC测定。实验筛选了接收液的种类,并比较冲和凝胶、冲和油膏内指标成分的透皮特性,考察药物累积透皮率、皮肤内滞留率以及皮肤外残率。结果显示,乙醇-生理盐水(2∶8)更适于作为接收液;冲和凝胶给药0.5 g,芍药苷、蛇床子素透皮速率分别为78.07,7.08μg·cm-2·h-1,其24 h累积透过率分别为(31.51±1.33)%,(12.38±1.28)%,皮肤滞留率分别为(0.92±0.45)%,(4.81±1.03)%。蛇床子素能在皮肤中形成贮库。冲和凝胶释药性优于油膏。芍药苷、蛇床子素透皮行为分别符合Weibull方程与Higuchi方程。

Chonghe gel originated from the Chinese ancient prescription, can be used for the treatment of diabetic foot. This experiment was to study the transdermal absorbability of paeoniflorin and osthole in Chonghe gel . Franz diffusing cells method was adopted for the in vitro model of rat belly skins. Paeoniflorin and osthole in the receiving liquid, skins and gel were determined by HPLC. The receiving liquid were screened, and Chonghe gel and Chonghe ointment were compared by transdermal absorbability. Re- sult showed that ethanol-normal saline （2： 8） solution was the appropriate receiving liquid. The penetration rates of paeoniflorin and os- thole were 78.07, 7.08μg·cm^-2·h^-1 respectively. In 24 h, the accumulated penetration rates were （31.51±1.33） %, （ 12. 38±1.28）%, respectively. The retention rates of paeoniflorin and osthole in skin were （0. 92±0.45）%, （4. 81±1.03）%, respective- ly. The retention of osthole in skins was a drug reservoir. Transdermal behavior of effective constituents in Chonghe gel was more effi- cient than that in ointment. In vitro, the transdermal behavior of paeoniflorin in Cbonghe gel was close to a Weibull process, while the behavior of osthole was close to Higuchi process.