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Capsule formation of pirfenidone and pharmaceutically acceptable excipients
专利权人:
INTERMUNE INC.
发明人:
RADHAKRISHNAN RAMACHADRAN,VLADYKA RONALD,SULTZBAUGH KENNETH
申请号:
NZ60012906
公开号:
NZ600129A
申请日:
2006.09.22
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
600129 Disclosed is a method for preparing a granulation comprising 5-methyl-1-phenyl-2-(1H)-pyridone and pharmaceutically acceptable excipients, the method comprising the step of: preparing the granulation using a type and an amount of an excipient selected to increase the AUC of the 5-methyl-1-phenyl-2-(1H)-pyridone upon oral administration, as compared to 5-methyl-1-phenyl-2-(1H)-pyridone without excipients orally administered in a capsule shell. Also disclosed is a capsule comprising a granulate formulation of 5-methyl-1-phenyl-2-(1H)-pyridone, wherein said granulate formulation comprises pharmaceutically acceptable excipients and 5-methyl-1-phenyl-2-(1H)-pyridone, and the formulation: is stable for at least 9 months at 40 ºC at 75% relative humidity, as measured by a dissolution of at least 85% of the 5-methyl-1-phenyl-2-(1H)-pyridone after the at least 9 months; is stable for at least 18 months at 25ºC at 60% relative humidity, as measured by a dissolution of at least 93% of the 5-methyl-1-phenyl-2-(1H)-pyridone after the at least 18 months; or comprises an effective amount of a binder that interacts with the amide carbonyl group of 5-methyl-1-phenyl-2-(1H)-pyridone to increase the AUC value upon oral administration, as compared to a capsule of 5-methyl-1-phenyl-2-(1H)-pyridone containing no excipients.
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