Transmucosal oral diphenhydramine-rapid relief of nausea

经粘膜口服苯海拉明-快速缓解恶心

• 批准号: 6401308
• 负责人: EDWARD J CONE
• 金额: $ 18.57万
• 依托单位: PINNEY ASSOCIATES
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-09-18 至 2002-10-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6401308
• 关键词: antiemetics; diphenylhydramine; drug delivery systems; drug design /synthesis /production; mastication; nausea; oral administration; oral mucosa; pharmacokinetics

DESCRIPTION (Provided by the applicant): Development of a transmucosal oral gum (TOG) delivery system is proposed for diphenhydramine, a first-line antiemetic for treatment of nausea, including patients with HIV disease. Although many antiemetics are available for use, nearly all are administered by oral ingestion with slow onset of effects. A buffered TOG delivery system will provide advantages over existing medications including: a) rapid delivery of diphenhydramine into the bloodstream followed by sustained release, providing early and lasting nausea relief; b) avoidance of first-pass effects; c) improved bioavailability; d) user control over dosing; and e) convenience of use. Transmucosal systems invented by this research team with demonstrated efficacy will be adapted for diphenhydramine. Standardized, in vitro, mechanical gum chewing methodology and a validated HPLC assay will be used in dissolution studies to optimize performance. Gum prototypes targeted for medication release necessary for rapid and sustained nausea relief will be developed. Optimization of a diphenhydramine TOG delivery system will allow for future assessment in humans and subsequent commercialization. A safe and effective TOG medication, available over-the-counter, with a rapid onset and sustained action will improve nausea treatment significantly. PROPOSED COMMERCIAL APPLICATION: The need for medication delivery systems capable of rapid relief of nausea is considerable. For people with HIV disease, nausea and vomiting are often side effects of medications or symptoms of an underlying illness. Although many antiemetics are available for use, nearly all ere administered by oral ingestion with slow onset of effects. The proposed oral transmucosal delivery of diphenhydramine by a buffered gum would provide an innovative means of rapid and sustained, safe, and effective over-the-counter treatment of nausea. A large commercial market exists for treatment of nausea in adults, especially for those suffering with HIV disease.

描述（由申请人提供）：跨粘膜口香糖的开发 (TOG) 输送系统被提议用于一线止吐药苯海拉明 用于治疗恶心，包括艾滋病毒患者。虽然很多 可以使用止吐药，几乎所有药物都是通过口服给药 摄入后起效缓慢。缓冲 TOG 传输系统将 与现有药物相比具有以下优点：a) 快速输送 苯海拉明进入血液，然后持续释放，提供 尽早且持久地缓解恶心； b) 避免首过效应； c) 提高生物利用度； d) 用户对剂量的控制； e) 方便 使用。该研究小组发明的跨粘膜系统已被证明 功效将适应苯海拉明。标准化，体外， 机械口香糖咀嚼方法和经过验证的 HPLC 测定将用于 溶出度研究以优化性能。口香糖原型针对 快速和持续缓解恶心所需的药物释放将 发达。苯海拉明 TOG 输送系统的优化将允许 未来对人类的评估和随后的商业化。一个安全且 有效的 TOG 药物，非处方药，起效快， 持续的行动将显着改善恶心治疗。 拟议的商业应用： 对能够快速缓解恶心的药物输送系统的需求是巨大的。对于艾滋病毒感染者来说，恶心和呕吐通常是药物的副作用或潜在疾病的症状。尽管有许多止吐药可供使用，但几乎所有止吐药都是通过口服给药，起效缓慢。所提出的通过缓冲口香糖口服经粘膜递送苯海拉明将提供一种快速、持续、安全和有效的非处方治疗恶心的创新方法。治疗成人恶心有一个巨大的商业市场，特别是对于那些患有艾滋病毒的人。