CONTROLLED RELEASE SYSTEMS FOR WATER-INSOLUBLE DRUGS

水不溶性药物的控释系统

• 批准号: 6525564
• 负责人: LAGREE M BURKE
• 金额: $ 2.73万
• 依托单位: UNIVERSITY OF AKRON
• 依托单位国家: 美国
• 财政年份: 2002
• 资助国家: 美国
• 起止时间: 2002-09-13 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/6525564
• 关键词: acid base balance; amiodarone; chemical synthesis; drug interactions; drug vehicle; foscarnet; molecular weight; nifedipine; paclitaxel; pharmacokinetics; polymerization; polymers; pyrrolidones; slow release drug; spirane; water solubility

The overall objectives of theis research are: (1) to increase to the apparent water solubilities and dissolution rates of water-insoluble drugs as to enhance their bio-availability, absorption and therapeutic efficacy by incorporating them in water-soluble polymers; (2) to investigate the interactions of drugs with the polymers and to develop an understanding of the dispersion morphologies; (3) to characterize the release of the drugs from the solid dispersions as a function of polymer molecular weight, drug loading and pH of the release medium; (4) to incorporate the solid dispersions in oral controlled-release (CR) systems that provide the delivery of the drugs at controlled rates over a specified time, where delivery is controlled by the device and not by the intrinsic water solubility of the drug; (5) to characterize the overall drug release rates with regard to the device parameters. The specific objectives of the proposed work are: (1) to incorporate griseofulvin (gris)/polyvinyl pyrrolidone (PVP) dispersions in matrix CR systems, (2) to characterize the overall drug release rates with regard to device parameters, and (3) to expand work in this area to include nifedipine, foscarnet, amiodarone and taxol.

本研究的总体目标是：(1)通过将水不溶性药物掺入水溶性聚合物中，提高其表观水溶性和溶出率，从而提高其生物利用度、吸收和治疗效果；(2)研究药物与聚合物的相互作用，并发展对分散形态的理解；(3)表征药物从固体分散体的释放随聚合物分子量、载药量和释放介质pH值的变化；(4)将固体分散体纳入口服控释（CR）系统中，该系统在规定的时间内以控制的速率提供药物的递送，其中递送由设备控制，而不是由药物的固有水溶性控制；(5)表征与器械参数相关的总体药物释放率。该工作的具体目标是：(1)将灰黄霉素(gris)/聚乙烯吡咯烷酮（PVP）分散体纳入基质CR系统，(2)表征与设备参数相关的总体药物释放率，(3)扩大该领域的工作，包括硝苯地平、膦香酯、胺碘酮和紫杉醇。