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目的:比较敷胸膏、敷胸巴布剂的体外释放和透皮吸收行为,探讨该复方剂型改良的可行性。方法:应用改良的Franz扩散装置,以离体大鼠皮肤为屏障进行体外透皮试验比较敷胸方不同剂型的体外吸收效果并进行初步评价。采用HPLC测定大黄酚和大黄素含量,流动相甲醇-0.3%磷酸溶液(67∶33),检测波长254 nm。结果:巴布剂中大黄酚的累积渗透量(Q)在给药后的各时间点均高于膏剂,大黄素的Q在给药2 h后的其他时间点亦均高于膏剂,且在给药8 h后的时间点,与膏剂比较,均具有显著性差异。巴布剂与膏剂中大黄酚、大黄素的体外透皮行为均符合零级过程,在2~24 h体外经皮渗透接近恒速;巴布剂中大黄酚、大黄素的渗透曲线方程分别为Q=0.824 1t+1.973 9(r=0.917 7),Q=0.597 7t+1.075 7(r=0.959 7),膏剂中大黄酚、大黄素渗透曲线方程分别为Q=0.524 4t+1.715 3(r=0.954 5),Q=0.297 2t+1.591 7(r=0.925 4)。巴布剂大黄酚、大黄素的24 h累积渗透率分别为77.12%,56.32%,膏剂中则分别为52.24%,31.16%。结论:巴布剂透皮吸收作用良好,且渗透效果优于膏剂,敷胸方的剂型改良可行。
OBJECTIVE: To compare the in vitro release and transdermal absorption behaviors of chest-dressing cream and chest-dressing, and to explore the feasibility of the improvement. Methods: In vitro dermal transdermal test was performed using an improved Franz diffusion device in vitro and compared with the in vitro absorption test of different dosage forms of Fuzhuo Fang for preliminary evaluation. The contents of chrysophanol and emodin were determined by HPLC. The mobile phase consisted of methanol-0.3% phosphoric acid (67:33) and the detection wavelength was 254 nm. Results: The cumulative permeation amount (Q) of chrysophanol in cataplasm was higher than that of ointment at various time points after administration, and the Q of emodin was also higher than that of ointment at other time points after 2 hours of administration, After administration for 8 h, there was a significant difference compared with the ointment. The transdermal behaviors of chrysophanol and emodin in poultice and ointment all accord with the zero-order process, and transdermal penetration in vitro reaches a constant speed in 2 ~ 24 h. The permeation curve equations of chrysophanol and emodin in poultice are Q = 0.824 1t + 1.973 9 (r = 0.917 7) and Q = 0.597 7t + 1.075 7 (r = 0.959 7). The permeation curves of chrysophanol and emodin in the ointment were Q = 0.524 4t + 1.715 3 (r = 0.954 5), Q = 0.297 2t + 1.591 7 (r = 0.925 4). The accumulative permeation rates of chloraphenin and emodin for 24 hours were 77.12% and 56.32% respectively, while those of ointment were 52.24% and 31.16% respectively. Conclusion: The effect of percutaneous absorption of cataplasm is good, and the osmotic effect is better than ointment.