MICROCRYSTAL FORMULATIONS OF ETOPOSIDE

依托泊苷微晶制剂

• 批准号: 2104171
• 负责人: WILLIAM MC CULLOCH
• 金额: $ 8.29万
• 依托单位: SPARTA PHARMACEUTICAL CORPORATION
• 依托单位国家: 美国
• 财政年份: 1994
• 资助国家: 美国
• 起止时间: 1994-04-12 至 1995-01-11
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2104171
• 关键词: crystallization; drug design /synthesis /production; etoposide; injection /infusion; laboratory rat; lyophilization; mannitol; method development; oral administration; pharmacokinetics; phosphatidylcholines; slow release drug; toxicology

This proposal relates to the water-insoluble anticancer agent, etoposide, and the use of Microcrystal Technology to produce an improved intravenous formulation, an improved oral formulation with increased bioavailability and a slow-release formulation for intramuscular or subcutaneous administration. The Microcrystal Technology is a unique delivery system in which a fine aqueous suspension of drug is encapsulated in phospholipids by microfluidization. The suspension is stable, does not precipitate readily and can be lyophilized for longer storage, requiring only saline to reconstitute it later. The advantages of the microcrystal formulation are that it avoids toxic solubilizing agents such as tween 80 or polysorbate (which is found in present formulations of etoposide), all components are tissue compatible, slow-release formulations are possible when i.m. or s.c. administration is used and oral bioavailability of compounds can be substantially increased. The Technology has applicability to other poorly soluble anticancer agents, including taxol, taxotere and camptothecin.

这项提议涉及不溶于水的抗癌剂，依托泊苷，