In vitro permeation of tetramethylpyrazine across porcine buccal mucosa  

川芎嗪的猪口腔粘膜透过特性(英文)

作　　者：柳晨 徐惠南[1] 李霄凌[2] 

机构地区：[1]复旦大学药学院药剂学教研室,上海200032 [2]美国太平洋大学药学院

出　　处：《Acta Pharmacologica Sinica》2002年第9期792-796,共5页中国药理学报（英文版）

摘　　要：AIM: To examine the in-vitro transport route of tetramethylpyrazine (TMP) across porcine buccal mucosa and to investigate the effects of drug concentration, pH in donor chamber, and 1-octanol/buffer partition coefficient on transbuccal permeation. METHODS: In-vitro permeation of TMP through porcine buccal mucosa was studied by using in-line flow through diffusion cells at 37 ℃. The permeability of TMP was evaluated at different donor pH and drug concentration. Permeability of unionized (Pu) and ionized TMP (Pi) was calculated by using the Scientist?software. RESULTS: The steady state flux of TMP increased linearly with the donor concentration (r2=0.96) at pH 7.4. The permeability and the partition coefficient increased with pH. Pu and Pi were 9.05× 10-1 cm·s-1 and 2.99 × 10-7cm·s-1, respectively. The total permeability coefficient increased with the fraction of unionized form. CONCLUSION: TMP permeated through buccal mucosa by a passive diffusion process. The partition coefficient and pH dependency of drug permeability indicated that the drug was transported mainly via the transcellular route by a partition mechanism.目的:确定川芎嗪(TMP)在猪口腔粘膜的主要渗透途径并用体外方法研究药物浓度、供给池pH和TMP油水分配系数对药物透过性的影响.方法:采用在线流通扩散池法进行透过实验,并用Scientist^((R))软件对数据进行处理.结果:稳态流量随药物浓度呈线性增大;透过系数和油水分配系数均随pH的增大而增大,且经细胞内的透过系数 9.05 ×10^(-6)cm·s^(-1)远远大于经细胞间的透过系数 2.99 ×10^(-7)cm·s^(-1).结论:药物经猪口腔粘膜吸收是一个被动扩散过程;药物转运的主要通道为细胞内途径.

关 键 词：TETRAMETHYLPYRAZINE PERMEABILITY mucous membrane 

分 类 号：R285[医药卫生—中药学]