发明名称 |
FUNCTIONAL COATING OF LINEZOLID MICROCAPSULES FOR ORAL ADMINISTRATION |
摘要 |
The present invention provides taste-masked microcapsules of Linezolid or the like (any member of the orally effective oxazolidinone or macrolide antibiotics), suitable for oral administration as a suspension, a fast-disintegrating, effervescent or chewable tablet, and more specifically relates to such oral dosage forms in which the bitter taste of Linezolid contained therein is masked by a combination of microencapsulation by solvent coacervation and subsequent functional membrane coating on said microcapsules. The taste-masked granules thus obtained release less than 5 %, most preferably less than 3 %, at a pH of 4.0 to 6.0 (pH of the saliva) but rapidly release (as a burst) at pHs of the upper intestinal tract. The taste-masked granules are optionally blended with other pharmaceutically acceptable excipients and filled into unit dose containers or compressed into fast-disintegrating/effervescent/chewable tablets. The contents of the Linezolid unit dose containers are suspended in an aqueous medium prior to oral administration to pediatric and geriatric patients, who are unwilling and/or find it difficult to swallow Linezolid tablets. In contrast, fast-disintegrating tablets on administration without water rapidly disperse into taste masked granules in the mouth.
|
申请公布号 |
WO0152848(A3) |
申请公布日期 |
2001.12.13 |
申请号 |
WO2001US01414 |
申请日期 |
2001.01.16 |
申请人 |
EURAND AMERICA, INC. |
发明人 |
PERCEL, PHILLIP, J.;VENKATESH, GOPI, M.;VISHNUPAD, KRISHNA, S. |
分类号 |
A61K9/00;A61K9/22;A61K9/26;A61K9/36;A61K9/50;A61K31/5377;(IPC1-7):A61K31/422 |
主分类号 |
A61K9/00 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|