马鞭草苷在大鼠体肠的吸收动力学  

Studies on the intestinal absorption kinetics of verbenalin in rats

作　　者：任非[1] 段坤峰[2] 吴宗耀[3] 倪旭[3] 陈学军[2] 

机构地区：[1]河北医科大学第二医院药剂科,河北石家庄050000 [2]河北医科大学第三医院药剂科,河北石家庄050051 [3]石家庄市第五医院药剂科,河北石家庄050021

出　　处：《中国医院药学杂志》2012年第5期340-343,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:建立同时测定肠循环液中马鞭草苷及酚红浓度的HPLC/DAD法,探讨马鞭草苷在大鼠各肠段的吸收动力学特征及不同药物浓度对肠吸收的影响。方法:采用大鼠在体肠灌流吸收试验,用HPLC对循环液中的马鞭草苷进行分析,色谱条件为:Diamonsil TMC18色谱柱(250 mm×4.6 mm,5μm),乙腈-0.05%磷酸溶液为流动相,梯度洗脱,流速1.0mL·min-1,检测波长为238 nm(马鞭草苷)和430 nm(酚红),柱温为30℃。结果:在50～200μg·mL-1范围内,马鞭草苷在肠道内的吸收量与浓度成正比例关系,不同药物质量浓度(50,100,200μg·mL-1)条件下的吸收速率常数(Ka)分别为(84.7±5.6)、(86.7±7.3)、(84.4±8.0)h-1,Ka无显著性差异;在十二指肠、空肠、回肠、结肠的Ka分别为(0.054±0.006)、(0.050±0.005)、(0.052±0.004)、(0.049 2±0.002 3)h-1,Ka无显著性差异。结论:马鞭草苷在大鼠肠道的吸收符合一级动力学过程,吸收机制为被动扩散。马鞭草苷在整个肠道均有吸收,可以将马鞭草苷研制成缓、控释制剂。OBJECTIVE To develop a high-performance liquid chromatography coupled with diode array detection （HPLC/ DAD） method for sinmhaneous determination of verbenalin and phenolsulfonphthalein in the circulation and to investigate the absorption kinetics of verbenalin at various intestinal segments of rats and the influence of the drug solution concentration on the intestinal absorption kinetics. METHODS The intestine in rats was cannulated for in situ perfusion. Verbenalin concentration in the flux was measured by the HPLC. The chromatographic procedure was carried out on a CI8 column with the mixture of acetonitrile-0. 05%phosphoric acid solution as a mobile phase and gradient elution. The flow rate was 1. 0 mL·min^-1. The detection wavelength was set at 238 nm for verbenalin and 430 nm for phenolsulfonphthalein. The temperature of column was 30℃. RESULTS When the concentration was raised from 50 to 200/μmL i , the uptake of verbenalin was increased linearly. At the concentration of 50,100 and 200/μg· mL^-1 from the whole intestine, the absorption rate constant （Ka） were （84. 7 ± 5.6）, （86. 7± 7. 3） and （84. 4 ±8. 0）h^-1 , respectively （P〉0. 05）. The Ka, of verbenalin at duodenum, jejunum, ileum and colon were （0. 054± 0. （106）, （0. 050± 0. 005）, （0. 052 ± 0. 004） and （0. 049 2 ± 0. 002 3） h^-1, respectively （P〉0. 05）. CON CLUSION The absorption of verbenalin in rats intestine is a first-order kinetics process with the passive diffusion absorption mechanism. Verbenalin can be absorbed in whole intestine, so it is suggested that verbenalin could be designed as a sustained or controlled-released formulation.

关 键 词：马鞭草苷 肠吸收动力学 高效液相色谱法 

分 类 号：R285[医药卫生—中药学]