Process for the preparation of a stable polymorphic form of atovaquone
AssigneeTaro Pharmaceutical Industries Ltd.
InventorsWAEL BAIDOSSI, Terese Soudah, Rosa Cyjon
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Abstract
The present invention provides a process for the preparation of a stable polymorph III of Atovaquone exhibiting characteristic peaks (expressed in degrees 20±0.2°θ) at about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5, which comprises: (a) providing a sample of Atovaquone particles; (b) heating the sample of Atovaquone particles at a minimal temperature of between 140° C. to 160° C. depending on the particle size of the sample; and (c) cooling the sample to obtain the stable polymorphic form of Atovaquone.
Claims30
A process for the preparation of a stable polymorph III of Atovaquone which comprises:
- (a) providing a sample of Atovaquone particles;
- (b) heating the sample of Atovaquone particles of step (a) at a temperature of at least about 160° C. for a time sufficient of at least about one hour to obtain a stable polymorphic form of Atovaquone, having characteristic peaks (expressed in degrees 20±0.2° θ) at approximately one or more of the positions:
- about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5;
- and
- (c) cooling the sample of step (b).
A process for the preparation of a stable polymorph III of Atovaquone which comprises:
- (a) providing a sample of Atovaquone particles wherein at least about 90% of the Atovaquone particles have a volume diameter of equal or less than about 40μ;
- (b) heating the sample of Atovaquone particles of step (a) at a temperature of at least about 140° C. for a time sufficient to obtain a stable polymorphic form of Atovaquone, having characteristic peaks (expressed in degrees 20±0.2° θ) at approximately one or more of the positions about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5;
- and
- (c) cooling the sample of step (b).
A process for the preparation of a stable polymorph III of Atovaquone which comprises:
- (a) providing a sample of Atovaquone particles wherein at least about 90% of the Atovaquone particles have a volume diameter of equal or less than about 10μ;
- (b) heating the sample of Atovaquone particles of step (a) at a temperature of at least about 140° C. for a time sufficient to obtain a stable polymorphic form of Atovaquone, having characteristic peaks (expressed in degrees 20±0.2° θ) at approximately one or more of the positions about 6.9, 9.6, 14.1, 14.7, 17.0, 18.5, 19.1, 19.9, 20.3, 22.0, 22.6, 23.2, 24.2, 26.8, and 28.5;
- and
- (c) cooling the sample of step (b).
Dependencies are inferred from the claim text.