陆兆光1,2,3, 闫明1,2,3, 杨晶1,2,3, 张红1,2,3, 吴云1,2,3, 丁岗1,2,3, 王振中1,2,3, 萧伟1,2,3
1. 江苏康缘药业股份有限公司, 江苏 连云港 222001;
2. 中药制药过程新技术国家重点实验室, 江苏 连云港 222001;
3. 中药提取精制新技术重点研究室, 江苏 连云港 222001
【摘要】目的 综合评价剂型改进后的金黄凝胶的体外透皮吸收效果，为金黄凝胶新药开发提供体外渗透动力学方面的实验依据。方法 以离体大鼠背部皮肤为体外模型，采用改良的Franz扩散池进行透皮吸收试验，首先建立金黄凝胶和金黄油膏接收液及皮肤滞留样品的HPLC指纹图谱，并对指纹图谱原始数据进行主成分分析（PCA）；其次确定金黄凝胶与金黄油膏共有的药物组分峰，求出各共有峰的面积，应用PCA法求得PCA载荷图；最后以复方中透皮吸收效果较好的芍药苷为代表，对体外渗透动力学进行考察。结果 金黄凝胶药物组分的整体体外透皮吸收效果优于金黄油膏，芍药苷的体外透皮吸收符合零级动力学过程，且金黄凝胶中芍药苷的累积透过量、透皮速率及皮肤滞留量均高于金黄油膏。结论 改进剂型后的金黄凝胶整体体外透皮吸收效果更好。PCA法是研究中药经皮给药制剂体外透皮吸收实验的有效手段。
【关键词】金黄凝胶; 金黄油膏; 主成分分析; 体外透皮吸收; HPLC; 指纹图谱; 渗透动力学; 芍药苷
In vitro percutaneous penetration studies of Jinhuang Gel based on principal component analysis
LU Zhao-guang1,2,3, YAN Ming1,2,3, YANG Jing1,2,3, ZHANG Hong1,2,3, WU Yun1,2,3, DING Gang1,2,3, WANG Zhen-zhong1,2,3, XIAO Wei1,2,3
1. Jiangsu Kanion Pharmaceutical Co., Ltd., Lianyungang 222001, China;
2. State Key Laboratory of Pharmaceutical Process New-teach for Chinese Medicine, Lianyungang 222001, China;
3. The Key Laboratory for the New Technique Research of TCM Extraction and Purification, Lianyungang 222001, China
【Abstract】Objective To comprehensively evaluate the in vitro percutaneous penetration and provide the experimental basis of in vitro kinetics for new drug development of Jinhuang Gel. Methods The skin penetration of Jinhuang Gel was investigated through in vitro excised rat skin using the improved Franz diffusion cell. HPLC fingerprint of receptive solution and skin retention was established and analyzed using principal component analysis (PCA). The common peaks of HPLC fingerprint between Jinhuang Gel and Jinhuang Ointment were selected and each area was calculated to obtain the PCA biplot. Paeoniflorin as a representative of common peaks was used to investigate the in vitro permeation kinetics. Results The results showed that the PCA biplot based on common peaks areas displayed that the global in vitro transdermal absorption effects of Jinhuang Gel were significantly better than those of Jinhuang Ointment. The in vitro transdermal absorption of paeoniflorin followed zero kinetics, and the cumulative permeation amount, permeation rate, and skin retention of paeoniflorin from Jinhuang Gel were superior to those from Jinhuang Ointment. Conclusion Jinhuang Gel could improve the overall effects of in vitro percutaneous absorption. PCA is an effective means for investigating in vitro percutaneous absorption experiments of Chinese materia medica for transdermal administration.
【Keywords】Jinhuang Gel; Jinhuang Ointment; principal component analysis; in vitro percutaneous penetration; HPLC; fingerprint; penetration kinetics; paeoniflorin
收稿日期：2016-01-26
基金项目：科学技术项目国家重大新药创制项目（2013ZX09402203）
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