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Intravenous application form of thalidomide for the therapy of immunological diseases

机译:沙利度胺静脉应用治疗免疫性疾病

摘要

Stable, aqueous form of (+)-(R)-thalidomide or (-)-(S)-thalidomide contains the enantiomer of thalidomide dissolved in pure form in isotonic glucose solution and has a pH 5.5. An Independent claim is also included for the production of the aqueous thalidomide solution, comprising: (a) adding (+)-(R) or (-)-S-thalidomide to isotonic glucose at pH 4-5; (b) shaking until dissolution is complete; and (c) treating with ultrasound and filtering under aseptic conditions. Use of pure enantiomers of thalidomide allows water-stable solutions that do not give rise to toxicological effects. The enantiomers have higher solubility in water than the racemate. At pH 5.5, hydrolysis of thalidomide does not occur. Solutions are suitable for parenteral administration.
机译:(+)-(R)-沙利度胺或(-)-(S)-沙利度胺的稳定的水性形式包含以纯形式溶于等渗葡萄糖溶液中的沙利度胺的对映异构体,且pH 5.5。还包括用于制备沙利度胺水溶液的独立权利要求,其包括:(a)在pH 4-5的等渗葡萄糖中加入(+)-(R)或(-)-S-沙利度胺。 (b)摇动直至完全溶解; (c)在无菌条件下进行超声波处理和过滤。沙利度胺的纯对映体的使用可使水稳定,而不会产生毒理学作用。对映异构体在水中的溶解度高于外消旋体。在pH 5.5时,沙利度胺不会发生水解。溶液适合肠胃外给药。

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