摘要
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.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2014年第2期166-170,共5页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
国家重大新药创制资助项目(2009ZX09103-399)
国家自然科学基金资助项目(81001592)
教育部科学技术重点项目(210101)
安徽高校省级自然科学研究重点项目资助(KJ2010A210
KJ2012A186)