LONG ACTING NALTREXONE BIODEGRADABLE INJECTABLE GEL

描述(由申请人提供)：本项目的总体目标是 开发一种治疗药物滥用的新方法，使用独特的和 获得专利的可生物降解注射凝胶配方，可以控制 纳曲酮的释放。这些新的可生物降解的GET配方得到了维护 纳曲酮治疗浓度至少4周 单次皮下注射，从而创造出一种将克服 当前口腔治疗模式的主要缺点，即显著的第一 通过新陈代谢，患者依从性差。因此，该计划的具体目标 本研究内容如下： (1)新型注射用凝胶剂的研制及体外释药评价 注射了纳曲酮。 这项研究的第一步是制备载药凝胶制剂 纳曲酮的处方因素及体外释放度测定 从凝胶配方中提取。 (2)确定凝胶的生物降解性、生物相容性和多长时间 纳曲酮在体内维持恒定血药浓度 单次皮下注射。 载药凝胶剂的生物降解性、生物相容性及缓释作用 维持纳曲酮的血药浓度不变 优化的载药凝胶形成将在大鼠身上进行检查 单次皮下注射凝胶。 建议的商业应用： 一种可生物降解并可在单次注射后2-4周内以受控速度释放药物的麻醉性拮抗剂的非肠道给药制剂在治疗阿片类药物依赖方面将是重要的。这种药物输送系统的潜在商业影响不仅在鸦片滥用治疗领域，而且在治疗酗酒方面也是如此，酒精中毒是当今社会一个更大的、具有经济破坏性的问题。该系统的美国专利申请正在申请中，预计很快就会获得批准。因此，我们相信，一项已颁发的专利以及第一阶段和第二阶段研究产生的数据将有助于我们将该技术商业化，并制造出可行的产品。

DESCRIPTION (provided by applicant): The overall goal of this project is to develop a novel approach for the treatment of drug abuse using unique and patented biodegradable injectable gel formulations which can control the release of naltrexone. These novel biodegradable get formulations wit maintain therapeutic concentrations of naltrexone for at least 4 weeks, following a single subcutaneous injection, thereby creating a product that will overcome the major disadvantages of current mode of oral therapy, i.e. significant first pass metabolism and poor 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 Naltrexone. The first step in this study is to prepare drug-loaded gel formulations with varying formulation factors and ascertain in vitro release rates of naltrexone from the gel formulations. (2) Ascertain Biodegradability, Biocompatibility of the Gels and How Long Constant Plasma Concentrations of Naltrexone can be Maintained in Vivo after a Single Subcutaneous Injection. Biodegradability and biocompatibility of the drug-loaded gels and the duration of maintaining constant plasma concentration of naltrexone released from two optimized drug-loaded gel formations will be examined in rats following a single subcutaneous injection of the gels. PROPOSED COMMERCIAL APPLICATION: A parenterally administered formulation of a narcotic antagonist that is biodegradable and can release the drug at a controlled rate over a 2-4 week period following a single injection would be important in the treatment of opiate dependence. The potential commercial implications of such drug delivery system will be significant not only in the field of opiate abuse treatment, but also in the treatment of alcoholism, a much larger and economically devastating problem in our society today. A U.S. patent application for this system is pending and is expected to be granted shortly. Therefore, we believe that an issued patent and data generated from both Phase I and phase II studies will help us commercialize the technology and make a viable product.