镓maltolate的化学和药物动力学与高口服生物利用度镓化合物。

文章的细节

引用

复制到剪贴板

伯恩斯坦LR,坦纳T,戈弗雷C,诺尔B

镓maltolate的化学和药物动力学与高口服生物利用度镓化合物。

满足基础药物。2000;7 (1):33-47。doi: 10.1155 / MBD.2000.33。

PubMed ID

18475921 (在PubMed

]

文摘

镓maltolate,三羟甲基氨基甲烷(3-hydroxy-2-methyl-4H-pyran-4-onato)镓液(GaM)是一种口服镓化合物治疗使用。是适度溶于水(10.7 + / - 0.9毫克/毫升25复合functionC)与辛醇分区系数是0.41 + / - -0.08。分子在水溶液电中性中性pH值;稀溶液(2.5 x10 - (5) M)显示小离解pH值在5.5 - -8.0。单晶x射线衍射分析发现GaM分子由三个maltolate配体双齿绑定到一个中央镓原子在一个螺旋推进器的安排下,与一个配体无序的两种可能的方向。斜方晶系的复合,空间群Pbca、单元计算单元a = 16.675 (3), b = 12.034 (2), c = 18.435(2)在158 k。访问被管理的健康志愿者单剂量的100,200,300,500毫克每剂(三个科目)。GaM非常良好的耐受性。口服吸收的Ga等离子体相当快速(吸收一半的生活= 0.8 - -2.0 h),与核心舱17-21h排泄半衰期。吸收剂量比例出现在剂量范围研究。 Estimated oral gallium bioavailability was approximately 25-57%, based on comparison with published data on intravenous gallium nitrate. Urinary Ga excretion following oral GaM administration was approximately 2% of the administered dose over 72h, in contrast to 49-94% urinary Ga excretion over 24h following i.v. gallium nitrate administration. We suggest that oral administration of GaM results in nearly all plasma gallium being bound to transferrin, whereas i.v. administration of gallium nitrate results in formation of considerable plasma gallate [Ga(OH)(4) (-)], which is rapidly excreted in the urine. These data support the continued investigation of GaM as an orally active therapeutic gallium compound.

DrugBank数据引用了这篇文章

药物载体

药物	航空公司	类	生物	药理作用	行动
硝酸镓	Serotransferrin	蛋白质	人类	未知的	粘结剂	细节