阿洛司琼联合微生态制剂治疗腹泻型肠易激综合征的临床研究

目的:探究阿洛司琼联合微生态制剂治疗腹泻型肠易激综合征的临床效果。方法:选择2016年1月-2018年1月于我院进行治疗的96例腹泻型肠易激综合征患者为研究对象,按照随机数字表法将其均分为实验组与对照组,每组各48例。对照组患者单纯使用阿洛司琼治疗,实验组患者在对照组患者基础上加用微生态制剂,两组患者治疗时间均为4周,分别于干预前及干预后对两组患者症状进行评分,使用IBS病情严重程度调查表(IBS-SSS)对两组患者干预前后治疗效果进行评估,并比较两组患者干预前后肠道乳酸杆菌、肠球菌及酵母样真菌菌群数及生活质量(SF-36)评分。结果:干预后,实验组患者症状评分及IBS-SSS量表评分均显著低于对照组(P0.05),SF-36生理功能、心理功能及生活功能得分、乳酸菌及肠球菌菌群数均显著高于对照组,而酵母样真菌菌群数低于对照组(P0.05)。结论:阿洛司琼联合微生态制剂治疗腹泻型肠易激综合征能够有效改善患者的肠道菌群、有效缓解临床症状,并可显著提高患者的生活质量。     

Determination of alosetron in human plasma or serum by high-performance liquid chromatography with robotic sample preparation

A method of analysis for the determination of alosetron in human plasma or serum has been developed. The method was fully automated using a laboratory robot in order to improve analytical precision, efficiency and safety. The assay involved solid-phase extraction with reversed-phase HPLC separation and fluorescence detection. A validation exercise over the concentration range of 0.1 to 20 ng/ml demonstrated the selectivity, linearity, sensitivity, accuracy, precision, extraction efficiency, ruggedness and stability of the method. The method has been applied in support of numerous human pharmacokinetic/biopharmaceutic studies over the last five years.     

Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome

Serotonin type 3 (5-HT₃) receptor partial agonists are being targeted as potential new drugs for the treatment of irritable bowel syndrome (IBS). Two new chemical series bearing indazole and indole cores have exhibited nanomolar binding affinity for the h5-HT₃A receptor. A range of partial agonist activities in HEK cells heterologously expressing the h5-HT₃A receptor were measured for the indazole series. Excellent 5-HT₃ receptor selectivity, favorable in vitro metabolic stability and CYP inhibition properties, and good oral in vivo potency in the murine von Bezold-Jarisch reflex model is exemplified thereby indicating the series to have potential utility as improved IBS agents.