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Drug delivery systems comprising weakly basic selective serotonin 5-HT3 blocking agent and organic acids
专利权人:
发明人:
申请号:
EP11001973.4
公开号:
EP2363117B1
申请日:
2007.01.29
申请国别(地区):
EP
年份:
2015
代理人:
摘要:
A pharmaceutical dosage form such as a capsule, a conventional or orally disintegrating tablet capable of delivering a weakly basic, nitrogen (N)-containing selective serotonin 5- HT3 blocking agent having a pKa in the range of from about 5 to 14 and a solubility of not more than about 200 µg/mL at pH 6.8 into the body in a sustained-released fashion, suitable for a once-daily dosing regimen, comprises at least one organic acid, which solubilizes said weakly basic selective serotonin 5-HT3 blocking agent prior to releasing it into the hostile intestinal environment wherein the blocking agent is practically insoluble. The unit dosage form may be composed of a multitude of multicoated particulates and is designed in such a way that the weakly basic blocking agent and the organic acid do not come into close contact during processing and/or storage thereby avoiding in-situ formation of acid addition compounds while ensuring that the acid is not depleted prior to completion of the drug release.
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