公开(公告)号：US20140242193A1

公开(公告)日：2014-08-28

申请号：US14007023

申请日：2012-03-26

申请人： Michael John Zaworotko ,  Roland D. Shytle ,  Tien Teng Ong ,  Padmini Kavuru ,  Ryan N. Cantwell ,  Tranhha Nguyen ,  Adam John Smith

发明人： Michael John Zaworotko ,  Roland D. Shytle ,  Tien Teng Ong ,  Padmini Kavuru ,  Ryan N. Cantwell ,  Tranhha Nguyen ,  Adam John Smith

IPC分类号： A61K33/14 ,  A61K47/22 ,  A61K47/18 ,  A61K33/00

CPC分类号： A61K47/183 ,  A61K9/145 ,  A61K33/00 ,  A61K33/14 ,  A61K45/06 ,  A61K47/186 ,  A61K47/22 ,  A61K2300/00

摘要： 2:1 cocrystals of amino acids and Li+ salts crystallize from hot water to afford water stable cationic networks based upon tetrahedral lithium cations: bilayered square grids, a lithium zeolitic metal-organic material (LiZMOM) and several lithium diamondoid metal-organic materials (LiDMOMs). The compositions may be used as a pharmaceutical for the treatment of suicidality and other disorders that require lithium to penetrate the blood brain barrier and exert therapeutic effects in the CNS. Advantageously, the novel cocrystal forms described herein may be used to lower the oral dose required to achieve therapeutic concentrations of lithium in the brain, thus reducing the peripheral toxicity and potentially broadening the therapeutic index in comparison to conventional lithium forms.

摘要翻译： 2:1的氨基酸和Li +盐的共晶体从热水中结晶，得到基于四面体锂阳离子的水稳定的阳离子网络：双层方形网格，锂沸石金属有机材料（LiZMOM）和几种锂金刚石金属有机材料（LiDMOM ）。 该组合物可用作治疗需要锂透过血脑屏障并在CNS中发挥治疗效果的自杀性和其它障碍的药物。 有利地，本文所述的新型共结晶形式可用于降低在脑中实现治疗浓度的锂所需的口服剂量，从而与常规的锂形式相比降低外周毒性并可能拓宽治疗指数。

公开(公告)号：US10130708B2

公开(公告)日：2018-11-20

申请号：US14007023

申请日：2012-03-26

申请人： Michael John Zaworotko ,  Roland D. Shytle ,  Tien Teng Ong ,  Ryan N. Cantwell ,  Tranhha Nguyen ,  Adam John Smith ,  Padmini Kavuru

发明人： Michael John Zaworotko ,  Roland D. Shytle ,  Tien Teng Ong ,  Ryan N. Cantwell ,  Tranhha Nguyen ,  Adam John Smith ,  Padmini Kavuru

IPC分类号： A61K9/14 ,  A61K33/00 ,  A61K33/14 ,  A61K45/06 ,  A61K47/18 ,  A61K47/22

摘要： 2:1 cocrystals of amino acids and Li+ salts crystallize from hot water to afford water stable cationic networks based upon tetrahedral lithium cations: bilayered square grids, a lithium zeolitic metal-organic material (LiZMOM) and several lithium diamondoid metal-organic materials (LiDMOMs). The compositions may be used as a pharmaceutical for the treatment of suicidality and other disorders that require lithium to penetrate the blood brain barrier and exert therapeutic effects in the CNS. Advantageously, the novel cocrystal forms described herein may be used to lower the oral dose required to achieve therapeutic concentrations of lithium in the brain, thus reducing the peripheral toxicity and potentially broadening the therapeutic index in comparison to conventional lithium forms.