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Pharmaceutical compositions comprising N- (4- (2-amino-3-chloropyridin-4-yloxy) -3-fluorophenyl) -4-ethoxy-1- (4-fluorophenyl) -2-oxo-1,2-dihydropyridine- 3-carboxamide
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
BINDRA, DILBIR S.,GOKHALE, MADHUSHREE YESHWANT,NUNES, CLETUS JOHN,ROSSO, VICTOR W.,SCHROEDER, GRETCHEN M.,THAKUR, AJIT B.,YIN, XIAOTIAN
申请号:
ES11717917
公开号:
ES2533075T3
申请日:
2011.04.29
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A pharmaceutical composition comprising (i) particles of Compound (5 I) in Form N-1 (ii) stabilizer; and (iii) at least one pharmaceutically acceptable carrier and / or diluent; wherein said particles have a diameter (D90) in the range of 1 to 50 micrometers and said stabilizer is arranged in said particles; wherein said stabilizer is a cellulose ether polymer; wherein said Form N-1 is characterized by one or more of the following: (a) a simulated powder X-ray diffraction pattern (PXRD) substantially equal to that shown in Figure 1, and / or an observed PXRD pattern substantially equal to that shown in Figure 1; b) a PXRD pattern comprising four or more values of 2q (CuK l>; = 1.5418 Å) chosen from: 6.2 ± 0.2; 7.7 ± 0.2; 11.0>; ± 0.2; 12.2 ± 0.2; 18.5 ± 0.2; 21.6 ± 0.2; 22.2 ± 0.2; and 23.0 ± 0.2, wherein the PXRD pattern of Form N-1 is measured at a temperature of approximately 25 ° C; c) a PXRD pattern comprising five or more values of 2q (CuK l>; = 1.5418 Å) chosen from: 6.2 ± 0.2; 7.7 ± 0.2; 11.0 ± 0.2; 12.2 ± 0.2; 18.5 ± 0.2; 21.6 ± 0.2; 22.2 ± 0.2; and 23.0 ± 0.2, in which the PXRD pattern of Form N-1 is measured at a temperature of approximately 25 ° C; d) unit cell parameters substantially equal to the following: Cell dimensions: a>; = 14.45 Å b>; = 19.21 Å c>; = 8.89 Å α>; = 90.0º β>; = 95, 7th γ>; = 90.0 ° Space group: P21 / c Molecules of Compound (I) / asymmetric unit: 1 where the unit cell parameters of Form N-1 are measured at a temperature of approximately 25 ° C; e) unit cell parameters substantially equal to the following: Cell dimensions: a>; = 14.43 Å b>; = 19.17 Å c>; = 8.83 Å α>; = 90.0º β>; = 95.4º γ>; = 90.0º Space group: P21 / c Molecules of Compound (I) / asymmetric unit: 1 where the unit cell parameters of Form N-1 are measured at a temperature of approximately -30 ° C; and / or f) a melting point in the range of from about 211 ° C to about 217 ° C.Una composición farmacéutica que comprende (i) partículas del C
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