发明名称 |
Crystalline naloxol-peg conjugate |
摘要 |
Provided are naloxol-polyethlyene glycol conjugates in oxalate or phosphate salt forms including crystalline forms. Further provided are methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms. The methods for preparing the oxalate salt comprise dissolving the naloxol-polyethylene conjugate free base in 2 relative volumes of acetonitrile or ethanol, adding 3 equivalents of water or 8 relative volumes of methyl t-butyl ether to the solution, adding oxalic acid in ethyl acetate or methyl t-butyl ether to the dissolved naloxol-polyethylene conjugate over a period of at least 2 hours to produce a slurry and filtering the slurry to yield the oxalate salt in solid form. |
申请公布号 |
NZ609874(A) |
申请公布日期 |
2014.10.31 |
申请号 |
NZ20110609874 |
申请日期 |
2011.09.29 |
申请人 |
ASTRAZENECA AB;NEKTAR THERAPEUTICS |
发明人 |
ÅSLUND BENGT LEONARD;AURELL CARL-JOHAN;BOHLIN MARTIN HANS;SEBHATU TESFAI;YMÉN BO INGVAR;HEALY ERIC THOMAS;JENSEN DAVID RICHARD;JONAITIS DAVID THOMAS;PARENT STEPHAN |
分类号 |
A61K31/485;A61K31/194;A61K31/765;A61K33/42 |
主分类号 |
A61K31/485 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|