A sensitive LC-MS/MS method for the determination of potential genotoxic impurities in Cinnarizine

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桂利嗪治疗肠易激综合征临床观察

目的 :观察桂利嗪在临床中治疗肠易激综合征 (IBS)的疗效。方法 :采用随机对照开放实验方法 ,选用复方地芬诺酯作为对照药。结果 :桂利嗪治疗IBS有效率为 86 8% ,复方地芬诺酯治疗IBS有效率为 72 7% ,两组有明显差异 (P <0 0 1)。结论 :桂利嗪治疗IBS是一种可供选择、有效的、可靠的方法。     

Improvement of oral bioavailability of flurbiprofen from flurbiprofen/β-cyclodextrin inclusion complex by action of cinnarizine

Improvement of the oral bioavailability of flurbiprofen (Flu) after oral administration of flurbiprofen/β-cyclodextrin inclusion complex (Flu/β-CD) by the action of cinnarizine (CN) was investigated. Flu and Flu/β-CD were administered orally to fasted rats at a dose of 20 mg/kg as Flu. Thirty minutes after drug administration, CN dissolved in pH 4.0 buffer solution or pH 4.0 buffer solution alone was administered to the rats. The dose of CN was 0.17 mg/kg. Blood samples were taken from rats and Flu concentrations in plasma samples were determined by HPLC. It was found from the comparison of Flu and Flu with CN (Flu + CN) that CN had no effect on plasma concentrations of Flu after oral administration of Flu. The mean plasma levels after oral administration of Flu/β-CD with CN (Flu/β-CD + CN) were larger not only than those of Flu and Flu + CN but also than those of Flu/β-CD. The value of C_max in Flu/β-CD + CN was significantly larger than that of Flu/β-CD. This is considered to be caused by the action of CN as a competing agent. This mechanism was supported by the result of solubility study in which Flu solubility in β-CD solution decreased with the addition of CN. It was found from these results that CN had strong ability as a competing agent in vivo.     

脑益嗪抗运动病时大鼠脑细胞钙离子超微结构定位的变化(论著)

目的：观察脑益嗪抗运动病时脑细胞钙离子（Ｃａ２＋）的变化并探讨其作用机理。方法：采用Ｃａ２＋超微结构定位方法，对ＳＤ大鼠预先给予脑益嗪后，采用正负交变加速度旋转刺激制备运动病模型。观察运动病大鼠和脑益嗪给药组大鼠大脑皮质、小脑皮质和脑干前庭区脑细胞Ｃａ２＋超微结构定位变化。结果：运动病大鼠大脑皮质、小脑皮质和脑干前庭区脑细胞质基质、线粒体和内质网中Ｃａ２＋反应产物增多。预先给予脑益嗪后，大脑皮质、小脑皮质和脑干前庭区脑细胞质Ｃａ２＋反应产物明显下降（Ｐ＜０．０１）。结论：脑益嗪抗运动病的中枢机理之一可能与抑制脑细胞Ｃａ２＋内流有关     

RP-HPLC测定桂利嗪分散片的含量及检查有关物质

目的采用HPLC法测定桂利嗪分散片的含量及有关物质。方法用Kromasil C18色谱柱(250 mm×4.6 mm,5μm);流动相为甲醇-0.2%三乙醇胺-三乙胺(85:15:0.03,盐酸调pH6.5);流速1.0 ml.min-1;检测波长254 nm;柱温为室温。结果桂利嗪的线性范围为20~200μg.ml-1(r=0.9999),最低检测限为0.2 ng.ml-1;样品溶液至少在8 h内稳定,回收率99.4%,RSD=0.92%(n=9)。结论所建方法简便、快速,专属性好,可用于桂利嗪分散片的含量测定和有关物质检查。     

中药配方颗粒天麻、当归、川芎治疗恢复期脑梗死疗效观察及对血脂的影响

目的观察中药配方颗粒天麻、当归、川芎治疗脑梗死的临床疗效及对血脂的影响。方法将120例恢复期脑梗死患者随机分为2组。在控制好原发病的基础上,治疗组60例给予中药配方颗粒天麻2g,当归3g,川芎1.3g,每日2次冲服。对照组60例给予桂利嗪片50mg,每日3次口服。2组均1个月为1个疗程,观察2组疗效及血脂指标变化。结果治疗组总有效率为91.67%,对照组总有效率为80.00%,2组比较差异有统计学意义(P0.01),治疗组疗效优于对照组。治疗组治疗后胆固醇(TC)、甘油三酯(TG)、低密度脂蛋白胆固醇(LDL-C)较治疗前明显下降(P0.01),且与对照组治疗后比较比较下降显著(P0.01)。结论中药配方颗粒天麻、当归、川芎治疗恢复期脑梗死疗效确切,且能明显降低血脂指标。