MICRODIALYSIS AND PHARMACOKINETIC STUDY OF TR-701

TR-701 的微量透析和药代动力学研究

• 批准号: 7950762
• 负责人: HARTMUT DERENDORF
• 金额: $ 2.16万
• 依托单位: UNIVERSITY OF FLORIDA
• 依托单位国家: 美国
• 财政年份: 2008
• 资助国家: 美国
• 起止时间: 2008-12-01 至 2009-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7950762
• 关键词: Adipose tissue; Antibiotics; Clinical Research; Computer Retrieval of Information on Scientific Projects Database; Dose; Drug Kinetics; Drug resistance; Funding; Gram-Negative Bacteria; Gram-Positive Bacteria; Grant; Infection; Institution; Legionella pneumophila; Measures; Methods; Microdialysis; Muscle; Mycobacterium tuberculosis; Oral; Oxazolidinones; Pharmaceutical Preparations; Pharmacodynamics; Plasma; Prodrugs; Research; Research Personnel; Resources; Sampling; Site; Skin; Source; Structure; Techniques; Tissues; Treatment Protocols; United States National Institutes of Health; acid fast bacteria; response; skeletal; soft tissue; subcutaneous

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. TR-701, an oxazolidinone antibiotic, is a prodrug of the microbiologically-active molecule, TR-700. TR-700 has activity against drug-susceptible and drug-resistant Gram-positive bacteria, and some Gram-negative bacteria such as Legionella pneumophila and the acid-fast bacterium Mycobacterium tuberculosis. Since one of the indications for this compound is complicated skin and skin structure infections, it is important to know the concentration of the drug at the site of infection. This includes subcutaneous adipose tissue and skeletal muscle. Traditionally, however, for lack of an appropriate method to measure the concentration at these sites, plasma samples have been taken to examine the pharmacodynamic response. The FDA and other regulatory agencies have been recommending that companies examine pharmacokinetic/pharmacodynamic relationships more intensely to develop optimal dosing regimens. To do so, the drug concentrations at the target site must be known. Recently, a new sampling technique has become useful in measuring drug concentrations in virtually every tissue, microdialysis. The aim of this study is to use the microdialysis technique to examine the soft tissue concentrations after a single oral dose of TR-701 compared to plasma samples.

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 一种恶唑烷酮类抗生素TR-701是具有微生物活性的分子TR-700的前药。TR-700对药物敏感和耐药的革兰氏阳性菌，以及一些革兰氏阴性菌，如嗜肺军团菌和抗酸细菌结核分枝杆菌具有活性。 由于这种化合物的适应症之一是复杂的皮肤和皮肤结构感染，因此了解感染部位的药物浓度是很重要的。这包括皮下脂肪组织和骨骼肌。然而，传统上，由于缺乏适当的方法来测量这些部位的浓度，因此通常采取血浆样本来检查药效反应。FDA和其他监管机构一直建议公司更严格地检查药代动力学/药效关系，以开发最佳剂量方案。要做到这一点，必须知道目标部位的药物浓度。最近，一种新的采样技术在测量几乎每一个组织中的药物浓度时变得有用，这就是微透析。这项研究的目的是使用微透析技术来检测单剂量口服TR-701后软组织的浓度，并与血浆样本进行比较。