摘要
目的考察芍药苷-6-O'-苯磺酸酯(CP-25)体外降解动力学。方法制备大鼠肝匀浆液和肠匀浆液,采用高效液相色谱法(HPLC)法测定匀浆液中CP-25的浓度。结果CP-25在肝匀浆液和肠匀浆液中均显著降解,降解半衰期随匀浆液浓度升高而显著降低;肠道不同区段匀浆液对CP-25代谢作用有差异,十二指肠和结肠代谢作用相对较弱,空肠和回肠相对较强。结论 CP-25口服给药受到小肠和肝脏双重首过消除,通过合适的药物制剂可能会进一步提高CP-25口服吸收。
ObjectiveTo investigate the degradation kinetics of paeoniflorin- 6-O＇- benzenesulfonate （CP-25） in homogenates of liver and intestine were prepared in vitro, and concentrations of CP-25 in ho- mogenates were detected by HPLC. Results CP-25 was obviously degradable in liver and intestine homogenates, and half life of degradation was decreased when levels of homogenates increased; the metabolisms of CP-25 in dif- ferent homogenates of intestine were diverse, the metabolic actions in duodenum and colon were weaker than those of jejunum and ileum. Conclusion Oral administration of CP-25 suffers first pass elimination from intestine and liver, which suggests the absorption of CP-25 could be further improved by appropriate pharmaceutical preparations
出处
《安徽医科大学学报》
CAS
北大核心
2014年第9期1269-1274,共6页
Acta Universitatis Medicinalis Anhui
基金
国家自然科学基金(编号:81330081、81302845、81173075)
安徽省高等学校省级自然科学研究项目(编号:KJ2013A158)
安徽医科大学博士科研资助基金(编号:XJ201211)
关键词
芍药苷-6-O’-苯磺酸酯
芍药苷
肝药酶
酯酶
降解
动力学
paeoniflorin- 6-O＇- benzenesulfonate
paeoniflorin
hepatic microsomal enzyme
esterase
degradation kinetics
