发明名称 |
Methods for coating pharmaceutical core tablets |
摘要 |
A formulation comprising, and process for preparing, improved oral dosage forms of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, a chemical entity with anti-inflammatory properties. Granulation of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea within specified ranges provides improved dissolution of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and oral bioavailability, as well as content uniformity. Incorporation into the formulation of an aqueous soluble inclusion compound capable of forming a complex with 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, such as beta-cyclodextrin provides enhanced stability of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, in particular in highly ionic environments. Chipping and disintegration of tablets containing more than about 10% betacyclodextrin can be prevented by applying a polymeric coat to the surface of the tablet at a temperature below 40° C.
|
申请公布号 |
US2003091636(A1) |
申请公布日期 |
2003.05.15 |
申请号 |
US20020282383 |
申请日期 |
2002.10.29 |
申请人 |
BOEHRINGER INGELHEIM PHARMACEUTICALS, INC. |
发明人 |
CAPPOLA MICHAEL;GEREG GEORGE W.;WAY SUSAN |
分类号 |
A61K9/30;A61K9/36;A61K31/5377;A61K47/48;(IPC1-7):A61K31/724;B05D3/00;B01J13/00;A61K9/28 |
主分类号 |
A61K9/30 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|