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[D-最优混合设计结合多种力学指标优化柴枳巴布剂的基质配方及其体外评价]

[Matrix formulation of chaizhi cataplasma optimized by D-optimal mixture design combined with multiple mechanical indicators and its in vitro evaluation].

作者信息

Zhang Ye-Wen, Yu Jing-Xin, Wang Jing-Yan, Ru Qing-Guo, Liu Yan, Wang Yi-Fei, Lin Hong-Mei, Wu Qing

机构信息

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2016 Mar;41(6):1046-1053. doi: 10.4268/cjcmm20160612.

Abstract

To optimize the matrix formulation of Chaizhi cataplasma (CC) and investigate its release and transdermal absorption properties in vitro. The optimized matrix formulation of cataplasma containing liquid herbal extract is determined by using D-optimal mixture design, with initial bonding strength, endurance bonding strength and gel strength as the evaluating indicators. Modified Franz diffusion cells were used to study the in vitro release and transdermal absorption of geniposide in CC. The optimized matrix formulation of CC contained NP700, aluminum glycinate, tartaric acid, glycerin, PVPK90 and water (9∶0.7∶0.8∶30∶5∶30.5). Cumulative release rate of geniposide in CC was (77.02±3.73)% in 24 h. The percutaneous penetration rate of geniposide was 7.25 μg•cm⁻²•h⁻¹ and the 24 h permeated amount was (156.22±4.90) μg•cm⁻². The optimized CC prepared by the D-optimal mixture design showed a good adhesion and formability. The in vitro release of the geniposide in CC was in accordance with the first order equation, while its in vitro transdermal absorption was close to the zero order equation.

摘要

优化柴枳巴布剂(CC)的基质配方,并研究其体外释放和透皮吸收特性。采用D-最优混合设计,以初黏强度、持黏强度和凝胶强度为评价指标,确定含液体中药提取物的巴布剂优化基质配方。采用改良的Franz扩散池研究CC中栀子苷的体外释放和透皮吸收。CC的优化基质配方为NP700、甘氨酸铝、酒石酸、甘油、PVPK90和水(9∶0.7∶0.8∶30∶5∶30.5)。CC中栀子苷24 h的累积释放率为(77.02±3.73)%。栀子苷的经皮渗透速率为7.25 μg•cm⁻²•h⁻¹,24 h渗透量为(156.22±4.90)μg•cm⁻²。采用D-最优混合设计制备的优化CC具有良好的黏附性和成型性。CC中栀子苷的体外释放符合一级方程,而其体外透皮吸收接近零级方程。

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