LONG ACTING NALMEFENE BIODEGRADABLE INJECTABLE GEL

描述（由申请人提供）：本提案的总体目标是 开发治疗酒精滥用和依赖的新方法 使用独特的专利生物可降解凝胶配方， 纳美芬这些新型生物可降解凝胶制剂将能够 维持纳美芬的治疗浓度持续较长时间， 时间，在单次皮下注射后，从而产生产品 这将大大提高患者的依从性。所以具体 这项研究的目的如下： (1)开发和评价新型注射凝胶的体外药物释放速率 注射了纳美芬。这项研究的第一步将是表征 影响纳美芬体外释放度的关键因素。 (2)确定纳美芬的治疗血药浓度可以持续多久 在单次皮下注射后保持在体内。的持续时间 从两种优化的药物释放的纳美芬的治疗血浆浓度 将在大鼠中检查载药凝胶制剂， 皮下注射凝胶。 我们研究的基本假设是， 载纳美芬的生物可降解凝胶将克服主要缺点 本发明的纳洛酮口服疗法，即，有效第一遍 代谢和患者依从性差。 拟定商业应用： 这种新型生物可降解药物输送系统的美国专利申请已经提交给 并已在其他国家注册。 一种控释药物递送系统， 纳美芬是可生物降解的，可以维持药物的治疗浓度， 酒精依赖患者单次注射后约2-4周， 保证患者依从性，降低治疗成本。

DESCRIPTION (provided by applicant): The overall goal of this proposal is to develop a novel approach for the treatment of alcohol abuse and dependency using unique and patented biodegradable gel formulations for controlled release of nalmefene. These novel biodegradable gel formulations will be able to maintain therapeutic concentrations of nalmefene for a prolonged period of time, following a single subcutaneous injection, thereby creating a product that will significantly improve patient compliance. Therefore, the specific aims of this study are as follows: (1) Develop and Evaluate In Vitro Drug Release Rates from Novel Injectable Gels Loaded with Nalmefene. The first step in this study will be to characterize critical factors affecting in vitro release rates of nalmefene. (2) Ascertain the How Long Therapeutic Plasma Concentrations of Nalmefene can be Maintained In Vivo after a Single Subcutaneous Injection. The duration of therapeutic plasma concentration of nalmefene released from two optimized drug-loaded gel formulations will be examined in rats following a single subcutaneous injection of the gels. The underlying hypothesis of our research is that the novel injectable biodegradable gel loaded with nalmefene will overcome the major disadvantages of the present oral therapy with naltrexone, i.e., significant first pass metabolism and poor patient compliance. PROPOSED COMMERCIAL APPLICATION: A United States patent application for this novel biodegradable drug delivery system has been granted and has also been filed in other countries. A controlled release drug delivery system of nalmefene, which is biodegradable and can maintain therapeutic concentrations of the drug for approximately 2-4 weeks following a single injection in alccoholic dependent patients, will guarantee patient compliance and reduce treatment cost.