A 30-DAY INJECTION FOR TREATMENT OF URINARY INCONTINENCE

描述（逐字从申请人的摘要）：非自愿损失 醒着或睡着时小便是一种恶臭的社会耻辱，通常被隐藏起来， 被尴尬的受害者用堆积如山的吸水垫吸走了估计l 0 100万美国人大小便失禁，每年花费100亿美元。高达25 老年病医院的护理时间的百分比用于处理 失禁 最常见的情况是急迫性尿失禁，压力性尿失禁， 神经性膀胱疾病奥昔布宁通常用于治疗 急迫性尿失禁和神经源性膀胱疾病，但不是压力 失禁传统的奥昔布宁治疗涉及服用3毫克的剂量 每日2次，以片剂的形式。然而，由于其口服生物利用度是 只有6- 9%，注射能够提供1-2毫克/天30天 会覆盖治疗范围该计划的目标是开发一个 可生物降解的可注射微球系统 奥昔布宁微球将有针对性地提供药物一段时间 一个月。 在初步研究中，BIOTEK制备了几种长效注射制剂 奥昔布宁微球使用FDA批准的生物降解 聚乳酸-共-乙交酯聚合物。为期6个月的第一阶段SBIR工作将确认 重现性和优化的方法制备的贮库 公式化。它将表征微球的性质， 测定药物在体外和家兔体内的释放速率。如果 成功，第二阶段将集中在临床评价的配方， 马萨诸塞州西罗克斯伯里退伍军人医院的志愿者。 拟定商业应用： 奥昔布宁的可注射储库形式将在几种条件下使用， 已知该药物的给药是有效的。 美国受试者中 这些疾病的发病率很高，相关的医疗费用每年超过100亿美元。 虽然奥昔布宁不是唯一的治疗方式，但其选择受到低口服给药率的影响。 生物利用度，因此，低剂量的药物。 从商业角度来看，即使 对这一市场的小规模渗透本身就代表着一个令人印象深刻的商业机会 和丰厚的投资回报。

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.