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| 1 | Enhanced bioavailability of rebamipide nanocrystal tablets:Formulation and in vitro/in vivo evaluation显示文摘The purpose of this study was to formulate rebamipide nanocrystal tablets(REB-NTs)by wet-milling technique to enhance its dissolution rate and oral bioavailability.The formulation and preparation technology were screened by single factor tests with particle size and distribution as indicators.Rebamipide nanocrystals(REB-NSs)was then achieved by freeze-dry from the prepared nanosuspensions which were characterized by differential scanning calorimetry(DSC)and x-ray powder diffraction(XRD),while the vitro dissolution and the plasma drug concentration of the nanocrystal tablets were investigated.The results indicated that the prepared nanosuspensions got an average particle size of 286 nm,PI of 0.173 and the average Zeta potential of18.2 mv.The average particle size of obtained REB-NSs’redispersibility was 278 nm,and the crystalline of REB-NSs was the same as the rebamipide bulk drug as shown by DSC and XRD.The drug dissolution rate of self-made nanocrystal tablets in different dissolutions was slightly faster than that from the reference tablets,REB-MTs(Mucosta®),while the Cmax and AUC0e24 of REB-NTs were 1 and 1.57 times higher than that of REB-MTs,which means the nanotechnology could significantly improve the oral bioavailability of rebamipide. | Yu Guo Yongjun Wang Lu Xu | 2015 | Asian Journal of Pharmaceutical Sciences2015，10，3： | 2 |
| 2 | 复方九里香颗粒对大鼠空肠黏膜P-糖蛋白的影响显示文摘目的:观察复方九里香颗粒对P-糖蛋白(P-gp)的调控作用,探讨其对临床联合用药的影响。方法:将20只SD雄性大鼠随机分为4组,每组5只,空白组灌胃给予20mL·kg-1的0.9%氯化钠注射液,实验组灌胃给予复方九里香颗粒20g·kg-1,每日2次。1周后采用体外扩散池法评价复方九里香颗粒对罗丹明123(R123)和荧光素钠(CF)经空肠黏膜透过性的影响,用荧光分光光度法测定R123和CF的浓度,并分析各组表观渗透系数(Papp)差异。结果:与空白组相比,实验组对R123吸收和分泌方向的透过性没有显著性影响,P值分别为0.955和0.843;与空白组相比,实验组对CF吸收和分泌方向透过性也没有显著性影响,P值分别为0.892和0.500。结论:复方九里香颗粒对肠黏膜P-gp无显著影响,对细胞间紧密连接也无显著影响,推测在临床联合用药中,不影响其他P-gp底物药物的吸收转运规律,不需要调整给药剂量。 | 孔艺 孙亚彬 李国锋 段炼 陈业豪 | 2010 | 中国药物应用与监测2010，7，5： | 0 |
| 3 | 复方黄甘颗粒对罗丹明123和6-羧基荧光素经肠黏膜转运的影响显示文摘目的:观察复方黄甘颗粒对P-糖蛋白(P-gp)底物罗丹明123(R123)和非P-gp底物6-羧基荧光素(CF)经肠黏膜转运的影响,为复方黄甘颗粒与P-gp底物药物合理联用提供依据。方法:20只SPF级SD雄性大鼠,体重(250±20)g,用随机数字表法分为生理盐水组和复方黄甘颗粒组,每组10只。分别给予生理盐水20mL/kg和1.0g/L复方黄甘颗粒溶液20mL/kg灌胃,2次/d,连续7d。1周后大鼠禁食16~18h,用10%水合氯醛(3mL/kg)腹腔麻醉,取空肠标本3~4cm,用体外扩散池法检测2组大鼠空肠黏膜对R123和CF透过性的影响,比较2组吸收方向转运[黏膜侧(M)-浆膜侧(S)]和分泌方向转运(S-M)的表观渗透系数(Papp)及泵出比(ER)。结果:生理盐水组与复方黄甘组R123吸收方向的Papp分别为(3.54±0.86)×10-6和(2.39±0.44)×10-6cm/s,分泌方向的Papp分别为(8.68±3.76)×10-6和(8.34±2.47)×10-6cm/s;生理盐水组与复方黄甘组CF吸收方向的Papp分别为(5.40±3.20)×10-6cm/s和(3.28±1.41)×10-6cm/s,分泌方向的Papp分别为(5.09±1.71)×10-6cm/s和(3.98±1.02)×10-6cm/s;差异均无统计学意义(均P>0.05)。生理盐水组R123的ER为2.45,CF的ER为0.94;复方黄甘组R123的ER为3.50,CF的ER为1.21。结论:复方黄甘颗粒对肠黏膜P-gp的活性无明显影响,提示复方黄甘颗粒与R123类似的P-gp底物药物联合应用较为安全。 | 孔艺 孙亚彬 李国锋 段炼 陈业豪 | 2010 | 药物不良反应杂志2010，12，5： | 0 |
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