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FORMULATIONS OF 3-(6-(1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL) CYCLOPROPANECARBOXAMIDO)-3-METHYLPYRIDIN-2-YL)BENZOIC ACID
专利权人:
VERTEX PHARMACEUTICALS INCORPORATED
发明人:
KESHAVARZ-SHOKRI, ALI,YOUNG, CHRISTOPHER
申请号:
NZ58627208
公开号:
NZ586272A
申请日:
2008.12.04
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed is an aqueous formulation comprising 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid, water, and a viscosity agent, wherein the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid is characterized by one or more peaks at 15.2 to 15.6 degrees, 16.1 to 16.5 degrees, and 14.3 to 14.7 degrees in an X-ray powder diffraction obtained using Cu K alpha radiation. The viscosity agent is selected from the group consisting of methyl cellulose, sodium carboxymethylcellulose, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, sodium alginate, polyacrylate, povidone, acacia, guar gum, xanthan gum, tragacanth, and magnesium aluminium silicate. The composition can further comprise a surfactant. Also disclosed is an oral formulation, the use of the formulation in the manufacture of a medicament for treating cystic fibrosis and a kit comprising the formulation and instructions for use.
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