A 30-DAY INJECTION FOR TREATMENT OF URINARY INCONTINENCE

治疗尿失禁的 30 天注射剂

• 批准号: 6298897
• 负责人: ELIE NUWAYSER
• 金额: $ 10万
• 依托单位: BIOTEK, INC.
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-04-01 至 2002-09-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6298897
• 关键词: anticholinergic agent; biodegradable product; dosage; drug delivery systems; drug design /synthesis /production; laboratory rabbit; microcapsule; pharmacokinetics; phenylacetates; polymers; slow release drug; urinary incontinence

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.

描述（逐字摘自申请人摘要）： 非自愿损失 醒着或睡着时尿液是一种恶臭的社会耻辱，通常被掩盖 尴尬的受害者拿着堆积如山的吸水垫。估计l 0 100 亿美国人失禁，每年造成 100 亿美元的损失。多达25个 老年医院护理时间的百分比花在处理 失禁。 最常见的情况是急迫性尿失禁、压力性尿失禁和 神经源性膀胱疾病。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，但不适用于压力 失禁。传统奥昔布宁疗法的剂量为 5 毫克，分 3 次服用 每日一次，以片剂形式服用。然而，由于其口服生物利用度 仅 6-9%，注射一次即可每天 1-2 毫克，持续 30 天 将覆盖治疗范围。该计划的目标是开发一个 可生物降解的可注射微球系统，用于持续释放 奥昔布宁。微球将在一段时间内靶向输送药物 一个月的时间。 在初步研究中，BIOTEK 制备了几种储库注射制剂 使用FDA批准的可生物降解的奥昔布宁微球 聚丙交酯-乙交酯聚合物。为期 6 个月的第一阶段 SBIR 工作将得到确认 重复性和优化储库制备方法 配方。它将表征微球的特性和 确定药物在体外和兔子体内的释放速率。如果 成功后，II 期将重点关注该制剂的临床评估 马萨诸塞州西罗克斯伯里退伍军人医院的志愿者。 拟议的商业应用： 奥昔布宁的注射储库型可用于多种慢性疾病。 已知该药物的施用是有效的。 受苦的美国受试者人数 这些疾病造成的费用很高，相关的健康成本每年超过 100 亿美元。 虽然奥昔布宁不是唯一的治疗方式，但选择受到低口服剂量的影响 生物利用度，因此药物剂量低。 从商业角度来看，即使是 这个市场的小渗透本身就代表着一个令人印象深刻的商机 以及丰厚的投资回报。