发明名称 Use of disulfiram for Neuronal Protection
摘要 This invention discloses a rapid-diffusion injectable formulation, comprising disulfiram or a suitable salt or analog of disulfiram. Unlike slow-release injectable formulations designed to ensure that chronic alcoholics have significant quantities of disulfiram in their blood at all time, the rapid-diffusion injectable formulation disclosed herein is designed to reduce the hypoxic or ischemic damage caused by crisis events such as stroke, heart attack, cardiac arrest, or asphyxiation. A rapid-diffusion injectable formulation can contain disulfiram mixed with water, an organic compound having a plurality of hydroxyl groups (such as pharmaceutically acceptable glycols or polysaccharides; propylene glycol, dextrans, and cyclodextrins are often used for such purposes), and a buffer. When a rapid-release formulation is injected during or immediately after a hypoxic/ischemic crisis or before a patient is subjected to controlled cardiac arrest or bypass during surgery, it can suppress damage by oxygenated free radicals, it can chelate copper and iron which would otherwise promote lipid peroxidation of cell membranes, and it can generate metabolites such as tryptophol that can suppress metabolic activity and demands in neurons and affected tissue.
申请公布号 US5373021(A) 申请公布日期 1994.12.13
申请号 US19930052775 申请日期 1993.04.26
申请人 CYPROS PHARMACEUTICAL CORPORATION 发明人 MARANGOS, PAUL J.
分类号 A61K31/145;A61K45/06;(IPC1-7):A61K31/27;A61K31/16;A61K31/105 主分类号 A61K31/145
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