CONTROLLED-RELEASE IMPLANTS OF DISULFIRAM METABOLITES

双硫仑代谢物的控释植入物

• 批准号: 3487375
• 负责人: KELLY L SMITH
• 金额: $ 5万
• 依托单位: BEND RESEARCH, INC.
• 依托单位国家: 美国
• 财政年份: 1991
• 资助国家: 美国
• 起止时间: 1991-09-01 至 1992-04-10
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3487375
• 关键词: alcoholism /alcohol abuse chemotherapy; aldehyde dehydrogenases; biomaterial development /preparation; biotransformation; diffusion; disulfiram; drug delivery systems; drug metabolism; glycolates; high performance liquid chromatography; implant; laboratory rat; lactates; pharmacokinetics; polymers

The principal objective of this project is to determine the technical feasibility of developing a drug-releasing implant for treatment of alcoholism. Specific aims during Phase I are to develop prototype implants that release disulfiram metabolites and to test the efficacy of these implants in rats. The prototype implants will be made of bioerodible polymers that will be designed to bioerode following complete drug delivery. The metabolites have been determined to be much more potent than disulfiram, which should allow lower release rates, smaller implants, and longer durations. Drug release rates and durations from prototype implants will be determined both in vitro and in vivo, and enzyme inhibition due to the implants will be determined in rats as a preliminary measure of efficacy. If this approach is successful, it could greatly increase both efficacy and patient compliance in treatment programs for alcoholism.

该项目的主要目标是确定技术 开发释放药物植入物以治疗的可行性 酗酒。 第一阶段的具体目标是开发原型植入物 该释放二硫仑代谢物并测试这些代谢性的功效 植入大鼠。 原型植入物将由生物毒素制成 完整药物后将设计为生物座的聚合物 送货。 这些代谢产物被确定为比 二硫胺，应允许较低的释放率，较小的植入物和 更长的持续时间。 药物释放率和原型植入物的持续时间 将在体外和体内确定，以及由于 植入物将在大鼠中确定为 功效。 如果这种方法成功，它可能会大大增加 在酒精中毒治疗方案中的疗效和患者遵守情况。