Li Hua-Hua, Yang Chang, Yang Yan-Ling, Huang Jia-Yi, Zhu Ying-Yin, DU Shou-Ying, Bai Jie
School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China.
Zhongguo Zhong Yao Za Zhi. 2022 Apr;47(7):1857-1863. doi: 10.19540/j.cnki.cjcmm.20210823.305.
This study aims to establish a method for determination of paeonol(Pae), eugenol(Eug), and piperine(Pip) content in receptor liquid and research on the permeability and pharmacokinetics of Huoxue Zhitong gel patch and microemulsion gel. The Franz diffusion experiment was conducted to assess the percutaneous permeability, and the microdialysis method was employed to assess pharmacokinetics of Huoxue Zhitong gel patch and microemulsion gel. The content of Pae, Eug, and Pip in receptor liquid in vitro and in vivo was determined by HPLC and UPLC-MS. The Q_n and J_(ss) of Pae, Eug, and Pip in the gel patch were significantly higher than those in the microemulsion gel, indicating that the drug release was faster in the gel patch. The C_(max), AUC_(0-760), and MRT of Pae, Eug, and Pip in the gel patch were higher than those in the microemulsion gel, indicating that the gel patch can promote the penetration and prolong the skin residence of the drug. The results of this study provide reference for improving the dosage form of Huoxue Zhitong patch.
本研究旨在建立一种测定受体液中丹皮酚(Pae)、丁香酚(Eug)和胡椒碱(Pip)含量的方法,并研究活血止痛凝胶贴剂和微乳凝胶的透皮性能及药代动力学。采用Franz扩散实验评估其经皮渗透性,采用微透析法评估活血止痛凝胶贴剂和微乳凝胶的药代动力学。通过高效液相色谱(HPLC)和超高效液相色谱-质谱联用(UPLC-MS)测定体外和体内受体液中Pae、Eug和Pip的含量。凝胶贴剂中Pae、Eug和Pip的累积渗透量(Q_n)和稳态渗透速率(J_(ss))显著高于微乳凝胶,表明凝胶贴剂中药物释放更快。凝胶贴剂中Pae、Eug和Pip的血药浓度峰值(C_(max))、药时曲线下面积(AUC_(0-760))和平均滞留时间(MRT)高于微乳凝胶,表明凝胶贴剂可促进药物渗透并延长药物在皮肤中的滞留时间。本研究结果为改进活血止痛贴剂剂型提供参考。