右旋布洛芬/酸改性蒙脱土缓释干混悬剂的制备及其体内外研究  

Preparation and in vitro and in vivo study of S(+)-IBU/acid-MMT sustained release dry suspension

作　　者：李婷婷[1] 赵乐乐[1] 孙艺丹[1] 郑子良 张淑秋[1] LI Ting-ting;ZHAO Le-le;SUN Yi-dan;ZHENG Ziqiang;ZHANG Shu-qiu(College of Pharmacy,Shanxi Medical University,Shanxi Taiyuan 030001,China;Translational Medicine Research Center,Shanxi Medical University,Shanxi Taiyuan 030001,China)

机构地区：[1]山西医科大学药学院,山西太原030001 [2]山西医科大学转化医学研究中心,山西太原030001

出　　处：《中国医院药学杂志》2018年第14期1496-1499,共4页Chinese Journal of Hospital Pharmacy

基　　金：山西省青年科技研究基金(编号:201601D202105);山西医科大学校博士启动基金(编号:03201531);山西医科大学青年基金(编号:02201618)资助

摘　　要：目的:研究右旋布洛芬/酸改性蒙脱土缓释干混悬剂体外释放及体内药动学特性。方法:通过沉降体积比和再分散性等检查,初步评价右旋布洛芬/酸改性蒙脱土缓释干混悬剂质量,采用体外溶出装置进行体外释放试验测定右旋布洛芬体外累积释放量;以大鼠为动物模型,测定给药后的血药浓度,采用DAS2.0程序计算药动学参数。结果:右旋布洛芬/酸改性蒙脱土干混悬剂3 h内沉降体积比大于0.9,且混悬剂再分散性好,流动性好;体外释药符合Higuchi方程(r=0.970 1);并具有明显缓释作用;体内试验表明,受试制剂和参比制剂的主要药动学参数Cmax分别为(86.05±5.96),(123.5±41.74)μg·mL^(-1);AUC_(0-24 h)分别为(644.49±73.26),(439.88±84.41)μg·mL^(-1)·h,t_(1/2)分别为(5.58±0.55),(2.36±0.55)h;各参数间比较具有统计学差异(P<0.05),受试制剂的达峰时间tmax延长到2 h,t_(1/2)和MRT比参比制剂分别延长2.36倍和2.47倍,可见右旋布洛芬/酸改性蒙脱土干混悬剂在大鼠体内具有明显缓释作用。结论:右旋布洛芬/酸性蒙脱土干混悬剂体内外均具有良好的缓释作用。OBJECTIVE To study the characteristics of S（＋）-IBU/acid-MMT sustained release in vivo and in vitro.METHODS The quality of the S（＋）-IBU was evaluated by the sedimentation rate and dispersion.The cumulative amount of S（＋）-IBU was tested by in vitro release experiments.In vivo release of the plasma concentration of rats was measured by rat model.DAS2.0 program was used to calculate the pharmacokinetic of S（＋）-IBU.RESULTS The sedimentation ratio of S（＋）-IBU/Acid-MMT dry suspension was greater than 0.9 in 3 h with good redispersibility and liquidity.In vitro release behavior could be described by the Higuchi equation：（r=0.970 1）,in vivo release S（＋）-IBU/acid-MMT and S（＋）-IBU suspension showed that Cmax were（86.05±5.96）and（123.5±41.74）μg/mL,AUC0-24 hwere（439.88±84.41）and（644.49±73.26）μg/mL·h,t1/2 were 0.5 and（5.58±0.55）h.There was remarkable difference in statistics between the parameters of the two formulations（P〈0.05）.The tmaxwas prolonged to 2 h,t1/2 and MRT prolonged by 2.36 times and 2.47 times compared to that of reference formulation.CONCLUSION S（＋）-IBU/acid-MMT composites show sustained-release property in vivo and in vitro.

关 键 词：右旋布洛芬 酸改性蒙脱土 缓释 药动学 

分 类 号：R969.1[医药卫生—药理学]