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    • 7. 发明授权
    • Process for preparing phenolic acid salts of gabapentin
    • 加巴喷丁酚酸盐的制备方法
    • US07550628B2
    • 2009-06-23
    • US10806022
    • 2004-03-22
    • Jeffrey S. KielH. Greg ThomasNarasimhan Mani
    • Jeffrey S. KielH. Greg ThomasNarasimhan Mani
    • C07C61/08A61K31/195
    • A61K31/7024A61K31/195C07C229/28C07H13/08
    • The present invention provides a novel process for preparation of the tannate salt of gabapentin for human and veterinary pharmaceutical use. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. However, the prior art neither discloses nor suggests the preparation of gabapentin tannate. The process for preparing gabapentin tannate includes the mixing of gabapentin and tannic acid together in the presence of one or more solvents. The method may further include the step of selecting the one or more solvents from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol and mixtures thereof. The process may also include the steps of isolating and purifying the tannate salt. This may be accomplished by filtration, drying, centrifugation and lyophilization. The process may utilize either natural or synthetic tannic acid.
    • 本发明提供了用于人和兽药用途的加巴喷丁的鞣酸盐的制备新方法。 活性药物成分的鞣酸盐用于持续释放应用,并改善某些感官特性如味道。 然而,现有技术既没有公开也没有提出加巴喷丁丹宁酸盐的制备。 加巴喷丁鞣酸盐的制备方法包括在一种或多种溶剂的存在下将加巴喷丁和单宁酸混合在一起。 该方法还可以包括从由纯水,乙醇,甘油,丙二醇,二乙醚,二氯甲烷,丙酮,异丙醇及其混合物组成的组中选择一种或多种溶剂的步骤。 该方法还可以包括分离和纯化鞣酸盐的步骤。 这可以通过过滤,干燥,离心和冻干来完成。 该方法可以使用天然或合成的单宁酸。