新藤黄酸大鼠在体肠吸收动力学研究

Studies on absorption kinetics of gambogenic acid in rat's intestines

目的：探讨新藤黄酸在大鼠各肠段的吸收动力学特征，为设计新藤黄酸新型给药系统提供可靠的生物药剂学依据。方法：采用大鼠在体肠灌流吸收实验模型，并考察新藤黄酸在浓度为3．0、10、30ug／mL、以及不同肠段（结肠、回肠、空肠、十二指肠）对新藤黄酸吸收的影响，用HPLC－UV测定新藤黄酸的浓度。结果：在3．0～30ug／mL范围内新藤黄酸的浓度与吸收速率成线性关系，新藤黄酸在结肠、回肠、空肠、十二指肠的吸收速率常数（K。）分别为（0．03944±0．00158）、（0．04012±0．00103）、（0．04104±0．00124）、（0．08620±0．00272）h_。。结论：新藤黄酸在大鼠肠道符合一级动力学的吸收过程，在大鼠肠道为被动扩散的吸收机制。新藤黄酸在大鼠的各个肠道都有吸收，因此将新藤黄酸设计为控释制剂是可行的。

To investigate the absorp- tion kinetic characteristics of Gambogenic acid at different intestine segments in rats and provide reliable biopharmaceutics basis of novel drug de livery systems of Garnbogenic acid. METHODS： The rat intestinal absorption model was estab lished to investigate the influence of different concentrations （3.0,10.0,30 /lg/mL） and intes tine segments on the intestinal absorption of GNA. Gambogenic acid ured by the RP-HPLC. concentration was meas RESULTS. Within the range from 3.0-30.0 lag/mL, the absorption rate and the quality concentration of Gambogenic acid had a linear relation. The permeability coefficient of Gambogenic acid num, duodenum were （ （0. 04012 ± 0. 00103）, （ （0. 08620 4± 0. 00272） h at colon, 0. 03944 ileum, jeju 0. 00158 ） 04104±0.00124） , respectively. CON CLUSION： The absorption of Gambogenic acid conforms to passive diffusion mechanism and first-order kinetics. Gambogenic acid could be absorbed in whole intestinal segments, so it is feasible for Gambogenic acid to be designed as a controlled-release formulation.