LONG ACTING NALMEFENE BIODEGRADABLE INJECTABLE GEL

描述(由申请人提供)：本提案的总体目标是 开发一种治疗酗酒和依赖的新方法 使用独特和专利的生物可降解凝胶配方进行控制释放 纳美芬。这些新型的可生物降解凝胶配方将能够 在较长时间内维持纳美芬的治疗浓度 时间，在一次皮下注射后，从而创造出一种产品 这将显著提高患者的依从性。因此，具体的 这项研究的目的如下： (1)新型注射用凝胶剂的研制及体外释药评价 注射了纳美芬。这项研究的第一步将是确定 影响纳美芬体外释放度的关键因素。 (2)确定纳美芬的血药浓度可维持多久 在单次皮下注射后在体内维持。持续的时间 两种优化方法释放纳美芬的治疗血药浓度 载药凝胶制剂将在大鼠身上进行检查，遵循单一的 皮下注射凝胶。 我们研究的基本假设是，新的可注射 携带纳美芬的可生物降解凝胶将克服主要缺点 目前使用纳曲酮的口腔治疗，即有意义的首次通过 新陈代谢和患者依从性差。 建议的商业应用： 这种新型可生物降解给药系统的美国专利申请已经完成 已获批准，并已在其他国家提交。一种控释给药系统 纳美芬，它是可生物降解的，可以维持药物的治疗浓度 在酒精依赖患者单次注射后约2-4周内，将 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.