复方血竭微乳体外透皮吸收及抗炎活性研究

Study on transdermal absorption and anti-inflammatory activity of Compound Sanguis Draxonis Microemulsion in vitro

目的考察不同浓度的复方血竭微乳主要活性成分的体外透皮吸收,为该制剂的进一步研究提供实验基础。方法 24只SD大鼠,按照随机数字表法分为3组,即复方血竭微乳高剂量组(5.0%)、复方血竭微乳中剂量组(2.5%)、复方血竭微乳低剂量组(1.0%),每组8只。取其同一部位离体大鼠皮肤为渗透屏障,扩散实验采用改良Franz扩散池,采用HPLC测定复方血竭微乳主要活性成分藁本内酯的含量,通过计算藁本内酯累计渗透量来考察复方血竭微乳的体外透皮吸收情况。40只SD大鼠,按体重随机分为5组,即模型组、醋酸地塞米松乳膏组、复方血竭微乳高剂量组(5.0%)、复方血竭微乳中剂量组(2.5%)、复方血竭微乳低剂量组(1.0%),每组8只。以醋酸地塞米松乳膏组作为阳性对照组,进行角叉菜胶致足肿胀实验,观察复方血竭微乳对急性炎症的抑制效果。结果低、中、高剂量组的复方血竭微乳主要活性成分藁本内酯在24 h内的累积透过量分别为(153.000±6.586)、(311.200±14.520)、(454.100±23.440)μg/cm2;透皮速率常数Jss分别为(6.8130±0.2196)、(13.7100±0.5953)、(20.1900±0.9491)μg/(cm2·h)。与阳性对照组比较,复方血竭微乳高剂量组对角叉菜胶所致大鼠足跖肿胀被显著抑制(P <0.01)。结论复方血竭微乳具有良好的体外透皮性能及抗炎活性。24 h内单位面积累积透过量随药物中主要有效成分藁本内酯含量升高而增加,经皮渗透行为符合零级动力学方程。

Objective To investigate the transdermal absorption of main active components of Compound Sanguis Draxonis Microemulsion with different concentrations in vitro, and provide experimental basis for further study of the preparation. Methods According to the random number table, twenty-four SD rats were randomly divided into 3 groups,which were high-dose group(5.0%), medium-dose group(2.5%) and low-dose group(1.0%) of Compound Sanguis Draxonis Microemulsion, with 8 rats in each group. The isolated rat skin of the same part was taken as the permeation barrier, and the content of ligustilide, the main active ingredient of Compound Sanguis Draxonis Microemulsion, was determined by HPLC using modified Franz diffusion cell. The transdermal absorption of Compound Sanguis Draxonis Microemulsion was investigated by calculating the cumulative permeation amount of ligustilide in vitro. Forty SD rats were randomly divided into 5 groups according to their body weight, which were model group, Dexamethasone Acetate Cream group, high-dose group(5.0%), medium-dose group(2.5%) and low-dose group(1.0%) of Compound Sanguis Draxonis Microemulsion with 8 rats in each group. Experiment of paw swelling in rats induced by carrageenan was operated to observe inflammation inhibited by Compound Sanguis Draxonis Microemulsion, Dexamethasone Acetate Cream group as positive control group. Results The cumulative permeabilities of ligustilide, the main active ingredient of lowdose, medium-dose and high-dose groups of Compound Sanguis Draxonis Microemulsion, within 24 h were(153.000±6.586),(311.200 ±14.520) and(454.100 ±23.440) μg/cm2 respectively. The transdermal rate constants Jsswere(6.8130±0.2196),(13.7100±0.5953),(20.1900±0.9491) μg/(cm2·h),respectively. Compared with the positive control group,the high-dose group of Compound Sanguis Draxonis Microemulsion significantly inhibited carrageenan-induced paw swelling in rats(P < 0.01). Conclusion Compound Sanguis Draxonis Microemulsion has good transdermal performance and anti-inflammatory activity in vitro. The cumulative permeability per unit area within 24 h increased with the content of ligustilide, and the transdermal permeation behavior conformed to the zero-order kinetic equation.