A 30-DAY INJECTION FOR TREATMENT OF URINARY INCONTINENCE

描述(逐字摘自申请人摘要)：非自愿遗失 醒着或睡着时尿是一种恶臭的社会耻辱，通常被掩盖起来 被尴尬的受害者用堆积如山的吸水垫。预估L 0 数百万美国人大小便失禁，每年的成本为100亿美元。多达25 在老年医院，护理时间的百分比被花费在处理 大小便失禁。 最常见的情况是急迫性尿失禁、压力性尿失禁和 神经性膀胱疾病。奥昔布宁常用于治疗慢性阻塞性肺疾病 强烈要求大小便失禁和神经性膀胱疾病，但不是为了压力 大小便失禁。传统的奥昔布宁治疗需要服用5毫克3 每天以药片的形式出现。然而，由于其口服生物利用度是 只有6-9%，一种能够每天注射1-2毫克，持续30天的注射剂 将覆盖治疗范围。该计划的目标是开发一种 可生物降解注射微球缓释系统的研究 奥昔布宁。微球将在一段时间内被靶向输送药物 一个月的时间。 在初步研究中，Biotek制备了几种仓库注射制剂 使用FDA批准的可生物降解的奥昔布宁微球 聚乳酸-乙交酯共聚物。为期6个月的SBIR第一阶段工作将确认 库房筹建方法的重现性及优化 配方。它将表征微球的性质，并 测定药物的体外释放速率和兔体内释放速率。如果 成功，第二阶段将集中在#年对该配方的临床评估 马萨诸塞州西罗克斯伯里退伍军人医院的志愿者。 建议的商业应用： 一种可注射形式的奥昔布宁可用于以下几种情况 众所周知，这种药物的管理是有效的。美国受苦受难的人数 来自这些条件的费用很高，相关的医疗费用超过100亿美元/年。 虽然奥昔布宁不是唯一的治疗模式，但其选择受到低血压的影响。 生物利用度，因此，药物的低剂量。从商业角度来看，即使是 这个市场的少量渗透本身就代表着一个令人印象深刻的商机 以及充足的投资回报。

DESCRIPTION (Verbatim from the Applicant's Abstract): The involuntary loss of urine while awake or asleep is a malodorous social stigma, commonly concealed by its embarrassed victim with a mountain of absorbent pads. An estimated l 0 million Americans are incontinent, at a cost of $10 billion/year. As much as 25 percent of nursing time in geriatric hospitals is consumed dealing with incontinence. The most common conditions are urge incontinence, stress incontinence, and neurogenic bladder disorders. Oxybutynin is commonly used for the treatment of urge incontinence and neurogenic bladder disorder, but not for stress incontinence. Conventional oxybutynin therapy involves a dose of 5 mg taken 3 times daily in the form of tablets. However, since its oral bioavailability is only 6-9 percent, an injection capable of delivering 1-2 mg/day for 30 days would cover the therapeutic range. The goal of this program is to develop a biodegradable injectable microsphere system for sustained release of oxybutynin. The microspheres will be targeted to deliver the drug for a period of one month. In preliminary studies, BIOTEK prepared several depot injectable formulations of oxybutynin microspheres using FDA approved biodegradable polylactide-co-glycolide polymer. The 6-month Phase I SBIR work will confirm the reproducibility and optimize the method of preparation of a depot formulation. It will characterize the properties of the microspheres and determine the rate of release of the drug m vitro and in rabbits. If successful, Phase II will focus on clinical evaluation of the formulation in volunteers at the West Roxbury VA Hospital in Massachusetts. PROPOSED COMMERCIAL APPLICATION: An injectable depot form of oxybutynin would find use in several conditions where chronic administration of the drug is known to be effective. The number of U.S. subjects who suffer from these conditions is high and the associated health cost is more than $10 billion/year. While oxybutynin is not the only mode of therapy, the choice is influenced by the low oral bioavailability and hence, the low dose of the drug. From a commercial standpoint, even a small penetration of this market would by itself represent an impressive business opportunity and ample return on investment.