洛索洛芬钠大鼠在体肠吸收动力学研究  

Intestinal absorption in situ of loxoprofen sodium in rat

作　　者：汤林熹 钟佳胜 泮卫红 贾菲 强皎 于晓阳 周向荣 王中彦[2] TANG Linxi;ZHONG Jiasheng;PAN Weihong;JIA Fei;QIANG Jiao;YU Xiaoyang;ZHOU Xiangrong;WANG Zhongyan(Sinopharm Zhijun(Shenzhen)Pharmaceutical Co.Ltd.,Guangdong Shenzhen 518110,China;School of Pharmacy,Shenyang Pharmaceutical University,Liaoning Shenyang 110016,China)

机构地区：[1]国药集团致君(深圳)制药有限公司,广东深圳518110 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国医院药学杂志》2023年第15期1701-1704,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:研究洛索洛芬钠大鼠在体肠吸收动力学,为剂型设计提供依据。方法:采用大鼠在体肠灌流方法,采用高效液相色谱法-紫外检测器测定洛索洛芬含量,取麻醉后大鼠的十二指肠、空肠、回肠和结肠段作为受试肠段建立在体肠灌流模型,计算洛索洛芬的吸收速率常数和吸收百分率。结果:洛索洛芬在大鼠各肠段吸收百分率和吸收速率常数均无显著性差异(P>0.05),无特异吸收部位。洛索洛芬在不同质量浓度及pH范围内的肠吸收速率常数基本不变。结论:洛索洛芬大鼠肠吸收为一级动力学过程,各肠段均有吸收,吸收机制为被动扩散,适合制成缓控释制剂。OBJECTIVE To explore the in situ intestinal absorption characters of loxoprofen sodium in rat,and provide theoretical basis for dosage design.METHODS A perfusion model in rat was established,and the concentration of loxoprofen in the perfusion solution was determined by high performance liquid chromatography-ultraviolet detector(HPLC-UV).Duodenum,jejunum,ileum and colon of anesthetized rats were selected as test intestinal segments for establishing the perfusion model,and the absorption rate constant and absorptivity of loxoprofen were calculated.RESULTS The results showed that the absorption rate constant and absorptivity of loxoprofen in different intestinal segments was almost identical(P>0.05),suggesting that loxoprofen was absorbed throughout.The mass concentration and pH value rarely affect the absorption rate constant of loxoprofen.CONCLUSION The intestinal absorption rate of loxoprofen followed first-order kinetics and the mechanism of its intestinal absorption was passive diffusion.These investigations indicated that loxoprofen sodium can be prepared as sustained release preparations.

关 键 词：洛索洛芬钠 肠吸收 在体肠灌流 

分 类 号：R97[医药卫生—药品]