Parenteral Formulations for Synthetic Retinoids

描述（由申请人提供）：SciTech LLC开发新型静脉注射 (IV)物理性质较差的研究药物制剂。 芬维A胺和其他难溶性类维生素A目前正在研究中。 作为化学预防和抗肿瘤药物进行研究，包括孤儿药 比如神经母细胞瘤化疗生理上溶解性差 相容的载体限制了患者获得口服剂型， 生物利用度差。因此，患者必须服用不合理数量的 胶囊（高达90/天）。肠胃外剂型可能更容易被接受， 患者韦恩州立大学的药理学中心发现， 共聚物混合物或脂质乳剂可以是适合的IV载体， 可用于超过表观饱和吸收的芬维A胺 在WSU口服芬维A胺I期试验期间发现。该SBIR旨在 了解物理化学性质和组成如何影响溶解度， 溶出度和稳定性，并确认实现 所需的制剂浓度。在第二阶段，来自 每项战略都将完成IND指导的研究。了解芬维A胺 溶解度也可导致改进的口服剂型。该SBIR涉及 NCI（CTEP）计划感兴趣的剂型，并响应重点 癌症治疗和诊断部（NCI）列出的领域，以及 孤儿产品开发办公室（FDA）。 拟定商业应用： 不可用

DESCRIPTION (provided by applicant): SciTech LLC develops novel intravenous (IV) formulations for investigational drugs with poor physical properties. Fenretinide and other poorly soluble retinoids are currently under investigational as chemopreventive and anti-tumor agents, including orphan indications like neuroblastoma chemotherapy. Poor solubility in physiologically compatible vehicles has limited patient access to oral dosage forms that show poor bioavailability. Consequently patients must take unreasonable numbers of capsules (upto 90/day). Parenteral dosage forms may be more acceptable to patients. The Pharmacology Core at Wayne State University found that novel co-polymer mixtures or lipid emulsions may be suitable IV carriers for fenretinide that may be useful to exceed the apparent saturable absorption identified during the WSU Phase I trial of oral fenretinide. This SBIR aims to understand how physicochemical properties and composition affect solubility, dissolution, and stability and to confirm the feasibility of achieving the required formulation concentration. In Phase II, a clinical formulation from each strategy will complete IND-directed studies. Understanding fenretinide solubility may lead to improved oral dosage forms as well. This SBIR concerns a dosage form of programmatic interest to the NCI (CTEP), and responds to focus areas listed by Division of Cancer Treatment and Diagnosis (NCI), and the Office of Orphan Products Development (FDA). PROPOSED COMMERCIAL APPLICATION: Not available