Zhu Ying-Yin, Liang Jun, Xiao Wu-Qing, Ren Zhi-Yu, Zhong Wan-Ling, Li Hua-Hua, Xi Cheng, Wu Hui-Chao, DU Shou-Ying
School of Chinese Materia Medica, Beijing University of Chinses Medicine Beijing 102488, China.
School of Traditional Chinese Medicine, Beijing University of Chinese Medicine Beijing 102488, China.
Zhongguo Zhong Yao Za Zhi. 2022 Dec;47(24):6607-6614. doi: 10.19540/j.cnki.cjcmm.20220422.301.
This study aimed to improve the transdermal permeation quantity of Baimai Ointment by investigating the enhancing effects of physical and chemical permeation promoting methods on transdermal permeation of Baimai Ointment. The improved Franz diffusion cell method was used for in vitro transdermal experiment. The abdominal skin of mice was used, and the skin was treated with 3% propylene glycol in the chemical enhancement group. Ultrasonic technology was introduced in the physical enhancement group. The conditions of ultrasonic technology were optimized by single factor trial. Taking Q_(EF) and ER as the indexes of penetration promotion performance, the enhancing effects of the two methods were compared. The results showed that the promotion performance of 3% propylene glycol for ammonium glycyrrhizinate, nardosinone and curcumin of the chemical enhancement group were 1.74, 1.60, and 3.73 times higher than those of the blank group, respectively. The overall permeation efficiency of the Baimai Ointment was significantly improved. The comprehensive promoting effect on each component was curcumin>ammonium glycyrrhizinate>nardosinone. In the physical enhancement group, the penetration promoting effect of ultrasonic power 1.0 W was better than that of 2.0 W and 0.5 W, ultrasonic time 5 min was better than 3 min and 8 min, and the ultrasonic frequency 1 MHz was better than 3 MHz. Therefore, the optimal ultrasonic condition was 1.0 W-5 min-1 MHz. Under this condition, in terms of the transdermal permeation for ammonium glycyrrhizinate, the Q_(EF) and ER of the ultrasonic technology were better than those of 3% propylene glycol. In terms of the transdermal permeation for nardosinone and curcumin, the QEF and ER of 3% propylene glycol were better than those of the ultrasonic technology. Therefore, 3% propylene glycol combined with ultrasonic technology can be used to promote permeation of Baimai Ointment that contains both water-soluble and fat-soluble components in the clinical application. This study provides a theoretical basis for the clinical application of Baimai Ointment and other transdermal preparations.
本研究旨在通过考察物理和化学促渗方法对白脉软膏透皮渗透的增强作用,提高白脉软膏的透皮渗透量。采用改良的Franz扩散池法进行体外透皮实验。选用小鼠腹部皮肤,化学增强组皮肤用3%丙二醇处理。物理增强组引入超声技术,并通过单因素试验优化超声技术条件。以Q_(EF)和ER作为促渗性能指标,比较两种方法的增强效果。结果表明,化学增强组3%丙二醇对甘草酸铵、木香烯内酯和姜黄素的促渗性能分别比空白组高1.74倍、1.60倍和3.73倍。白脉软膏的整体渗透效率显著提高。对各成分的综合促渗效果为姜黄素>甘草酸铵>木香烯内酯。在物理增强组中,超声功率1.0W的促渗效果优于2.0W和0.5W,超声时间5min优于3min和8min,超声频率1MHz优于3MHz。因此,最佳超声条件为1.0W-5min-1MHz。在此条件下,对于甘草酸铵的透皮渗透,超声技术的Q_(EF)和ER优于3%丙二醇。对于木香烯内酯和姜黄素的透皮渗透,3%丙二醇的QEF和ER优于超声技术。因此,3%丙二醇联合超声技术可用于促进临床应用中含有水溶性和脂溶性成分的白脉软膏的渗透。本研究为白脉软膏及其他透皮制剂的临床应用提供了理论依据。