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    • 3. 发明申请
    • ORAL FORMULATIONS FOR CONTROLLED RELEASE OF ALCOHOL DETERRENTS
    • 用于控制释放酒精残留的口服制剂
    • WO98058642A1
    • 1998-12-30
    • PCT/US1998/013191
    • 1998-06-25
    • A61K9/16A61K9/52A61K31/275A61K31/485A61K33/06
    • A61K9/1635A61K31/275A61K31/485Y10S514/811Y10S977/773Y10S977/904Y10S977/906
    • An oral controlled release dosage form for cyanamide whereby a portion of a cyanamide dose administered to a patient remains transiently partitioned within encapsulating material, thereby retarding metabolism of the total administered cyanamide dose, is described. No investigator has reported the use of dosage forms enabling controlled release of cyanamide. The preparation, when administered to ethanol metabolizing individuals, can elevate blood acetaldehyde to such levels, and for such periods of time, that the individuals will be deterred from future alcohol consumption. The controlled release of cyanamide provides an optimal time-profile of alcohol deterrence specific for individual patients. The formulation avoids the side-effects associated with the relatively high concentrations of cyanamide and cyanamide-metabolites, and the attendant untoward toxic effects, caused by a typical bolus cyanamide dose, thereby attenuating the intensity of the sickness caused by acetaldehyde, and increasing patient compliance with cyanamide therapy.
    • 描述了一种用于氰胺的口服控制释放剂型,其中给患者施用的一部分氨腈剂量保持短暂地分隔在封装材料内,从而延缓总投与氨酰胺剂量的代谢。 没有研究者报告使用可以控制释放氰胺的剂型。 当给乙醇代谢个体时,该制剂可以将血液乙醛提高到这样的水平,并且在这样的时间段内,这些个体将被阻止以后的饮酒。 氰胺的控制释放提供了针对个体患者的酒精威慑的最佳时间特征。 该配方避免了与较高浓度的氨腈和氰胺代谢物相关的副作用,以及由典型的推注青酰胺剂量引起的伴随的不利毒性作用,从而减轻了由乙醛引起的疾病强度,并增加了患者依从性 用氨腈治疗。