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Drug delivery systems comprising a weakly basic serotonin 5-HT3 selective blocking agent and organic acids
专利权人:
APTALIS PHARMATECH; INC.
发明人:
VENKATESH, GOPI,LAI, JIN-WANG,VYAS, NEHAL
申请号:
ES07717465
公开号:
ES2531215T3
申请日:
2007.01.29
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A multiparticulate pharmaceutical dosage form comprising sustained release beads (LS) and / or one or more populations of pulsed controlled release beads (LPC) of: a weakly basic drug, weakly basic drug comprising a selective blocking agent of the 5-HT3 serotonin containing nitrogen (N), or a pharmaceutically acceptable salt thereof, which has a pKa in the range of about 5 to 14, and a solubility not exceeding about 200 µg / ml at pH 6.8, and at least one pharmaceutically acceptable organic acid as a solubilizer; in which the weakly basic drug and organic acid do not come into contact with each other in the dosage form; wherein said LS beads comprise: a coating (barrier) of LS comprising a water insoluble polymer alone or in combination with a water soluble polymer; said LS coating (barrier) being disposed on immediate release (LI) beads comprising: the weakly basic drug disposed on an inner barrier coating comprising a water insoluble polymer alone or in combination with a water-soluble polymer or an enteric polymer ; said inner barrier coating being disposed on organic acid core particles comprising at least one pharmaceutically acceptable organic acid; and wherein said LPC beads comprise: an outer delay time coating comprising a water insoluble polymer in combination with an enteric polymer, said outer delay time coating providing a delay time of about 2 to about 17 hours before the onset of weakly basic drug release; said outer delay time coating disposed on immediate release beads (LI) comprising: the weakly basic drug disposed on an inner barrier coating comprising a water insoluble polymer alone or in combination with a water soluble polymer or an enteric polymer ; said inner barrier coating being disposed on organic acid core particles comprising at least one pharmaceutically acceptable organic acid; wherein said dosage form is suitable for a once-daily dosing schedule in patients in need of said medication.Una forma de dosificación farmacéutica multiparticu
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