Use of Entero-Test, a simple approach for non-invasive clinical evaluation of the biliary disposition of drugs
Use of Entero-Test, a simple approach for non-invasive clinical evaluation of the biliary disposition of drugs
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DOI：
10.1111/j.1365-2125.2011.03956.x
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发表时间：
2011-07-01
影响因子：
3.4
通讯作者：
Richards, Duncan
中科院分区：
文献类型：
--
作者：
Guiney, William J.;Beaumont, Claire;Richards, Duncan
AIMTo评估非侵入性收集胆汁从健康人受试者的定性特征的胆汁处置的药物，使用spectrometric techniques.METHODSTwenty受试者进行非侵入性胆汁捕获使用peroral字符串测试（肠测试）设备之前和之后的单次口服剂量的辛伐他汀（80 mg）。该装置由一个装有高吸收性尼龙绳的加重明胶胶囊组成，每个受试者将绳的近端粘在脸上吞下。一旦判断加重的线已经到达十二指肠，刺激胆囊收缩以释放胆汁。然后通过口腔取回该线，并在溶剂提取后使用光谱测定和光谱技术分析胆汁样品中的药物相关物质。并且主要代谢物与使用侵入性技术从接受[C-14]给药的患者中收集胆汁的研究报告一致。辛伐他汀。结论：本研究的结果证明了在人体研究中使用肠试验提供胆汁代谢物的结构信息的实用性。这可以很容易地应用于药物开发研究，包括那些在目标患者群体，并可能消除对更具侵入性的采样技术的需要。
AIMTo evaluate the non-invasive collection of bile from healthy human subjects for the qualitative characterization of the biliary disposition of a drug, using spectrometric techniques.METHODSTwenty subjects underwent non-invasive bile capture using a peroral string test (Entero-Test) device prior to and following a single oral dose of simvastatin (80 mg). The device, consisting of a weighted gelatin capsule containing a highly absorbent nylon string, was swallowed by each subject with the proximal end of the string taped to the face. Once the weighted string was judged to have reached the duodenum, gallbladder contraction was stimulated in order to release bile. The string was then retrieved via the mouth, and bile samples were analysed for drug-related material using spectrometric and spectroscopic techniques following solvent extraction.RESULTSNumerous metabolites of simvastatin were detected, and the major metabolites were consistent with those reported from studies where bile was collected using invasive techniques from patients dosed with [C-14]-simvastatin.CONCLUSIONSThe results from this study demonstrate the utility of deploying the Entero-Test in human studies to provide structural information on biliary metabolites. This can be readily applied in drug development studies, including those in the target patient population and may eliminate the need for more invasive sampling techniques.