Crystalline forms of atorvastatin
AssigneeTeva Pharmaceutical Industries Ltd.
InventorsPaul Adriaan Van Der Schaaf, Fritz Blatter, Martin Szelagiewicz, Kai-Uwe Schoning
Life of this patent
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Abstract
The present invention is directed to new crystalline forms of Atorvastatin calcium (2:1), referred to hereinafter as polymorphic Forms X, A, B1, B2, C, D and E. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and pharmaceutical compositions comprising the crystalline forms.
Claims16
A crystalline polymorph of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (Å) at
- 27.9 (s), 20.9 (w), 18.9 (w), 16.1 (w), 11.1 (m), 10.5 (m), 9.1 (m), 5.53 (m), 5.07 (w), 4.77 (vw), 4.55 (m), 4.13 (w), 3.69 (w);
- wherein (s)=strong intensity;
- (m)=medium intensity;
- (w)=weak intensity;
- (vw)=very weak intensity.
A crystalline polymorph of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (Å) at
- 31.0 (vw), 18.6 (m), 17.0 (w), 15.3 (vw), 12.8 (w), 11.2 (m), 9.6 (s), 9.3 (w), 8.6 (w), 7.4 (m), 6.5 (vw), 6.2 (vw), 5.47 (w), 5.21 (m), 4.64 (vs), 4.46 (s), 4.14 (m), 3.97 (m), 3.74 (m), 3.62 (vw), 3.38 (w), 3.10 (m);
- wherein (vs)=very strong intensity;
- (s)=strong intensity;
- (m)=medium intensity;
- (w)=weak intensity;
- (vw)=very weak intensity.
A crystalline polymorph of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (Å) at
- 27.9 (m), 17.0 (m), 14.2 (w), 12.1 (vs), 10.1 (s), 8.6 (m), 7.1 (m), 6.1 (vw), 5.27 (m), 4.89 (m), 4.68 (m), 4.46 (m), 4.22 (m), 3.90 (w), 3.70 (w), 2.36 (vw);
- wherein (vs)=very strong intensity;
- (s)=strong intensity;
- (m)=medium intensity;
- (w)=weak intensity;
- (vw)=very weak intensity.
A crystalline polymorph of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (Å) at
- 28.1 (m), 17.2 (m), 14.0 (VW), 12.3 (s), 10.4 (s), 8.6 (m), 7.5 (w), 7.0 (m), 5.28 (m), 4.88 (m), 4.55 (m),4.27 (m), 3.88 (vw), 3.73 (m);
- wherein (s)=strong intensity;
- (m)=medium intensity;
- (w)=weak intensity;
- (vw)=very weak intensity.
A crystalline polymorph of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (Å) at
- 28.8 (m), 24.0 (m), 17.1 (m), 11.3 (s), 9.8 (vw), 8.3 (w), 7.7 (vw), 6.9 (vw), 5.64 (vw), 5.21 (w), 4.59 (m), 4.39 (w), 4.16 (w), 3.70 (w);
- wherein (s)=strong intensity;
- (m)=medium intensity;
- (w)=weak intensity;
- (vw)=very weak intensity.
A crystalline polymorph of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (Å) at
- 33.7 (w), 31.0 (m), 16.9 (m), 10.3 (s), 7.7 (w), 6.4 (vw), 4.84 (s);
- wherein (s)=strong intensity;
- (m)=medium intensity;
- (w)=weak intensity;
- (vw)=very weak intensity.
A crystalline polymorph of [R-(R*,R*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid calcium salt which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (Å) at
- 26.8 (s), 9.4 (w), 4.6 (m);
- wherein (s)=strong intensity;
- (m)=medium intensity;
- (w)=weak intensity.
Dependencies are inferred from the claim text.