Crystalline compounds
View Patent ↗The present invention relates to a novel crystalline form of zofenopril calcium of formula (I), chemically known as (4S)-1-[(2S)-3-(benzoylthio)-2-methylpropionyl]-4-(phenylthio)-L-proline calcium salt. The present invention further relates to a process for the preparation of the new crystalline form of zofenopril calcium and its use in pharmaceutical preparations.
1. Zofenopril calcium monohydrate.
2. Zofenopril calcium in crystalline form having the following characteristic XRD peaks: 4.9±0.2, 8.1±0.2, 9.1±0.2, 9.9±0.2, 14.5±0.2, 16.0±0.2, 17.5±0.2, 18.5±0.2, 19.0±0.2, 20.0±0.2, 20.5±0.2, 21.5±0.2, 22.3±0.2, 23.9±0.2 and 24.5±0.2 degrees 2θ.
3. Zofenopril calcium in crystalline form having the following characteristic XRD peaks: 5.1±0.2, 8.2±0.2, 9.2±0.2, 10.0±0.2, 14.5±0.2, 16.1±0.2, 17.5±0.2, 18.5±0.2, 19.1±0.2, 20.1±0.2, 20.5±0.2, 21.5±0.2, 22.4±0.2, 24.1±0.2 and 24.6±0.2 degrees 2θ.
4. Zofenopril calcium as claimed in claim 1 , wherein the zofenopril calcium comprises:
(a) less than 10% of zofenopril calcium in other polymorphic forms; and/or
(b) less than 3% of impurities other than zofenopril calcium in other polymorphic forms.
5. A pharmaceutical composition, comprising zofenopril calcium monohydrate, or zofenopril calcium in polymorph form C, or zofenopril calcium in crystalline form having the following characteristic XRD peaks: 4.9±0.2, 8.1±0.2, 9.1±0.2, 9.9±0.2, 14.5±0.2, 16.0±0.2, 17.5±0.2, 18.5±0.2, 19.0±0.2, 20.0±0.2, 20.5±0.2, 21.5±0.2, 22.3±0.2, 23.9±0.2 and 24.5±0.2 degrees 2θ, or zofenopril calcium in crystalline form having the following characteristic XRD peaks: 5.1±0.2, 8.2±0.2, 9.2±0.2, 10.0±0.2, 14.5±0.2, 16.1±0.2, 17.5±0.2, 18.5±0.2, 19.1±0.2, 20.1±0.2, 20.5±0.2, 21.5±0.2, 22.4±0.2, 24.1±0.2 and 24.6±0.2 degrees 2θ, or mixtures thereof, and a pharmaceutically acceptable carrier, excipient or diluent.
6. A pharmaceutical composition as claimed in claim 5 , wherein the composition is in the form of a tablet, capsule, syrup, suspension or elixir for oral administration or in the form of a sterile solution or suspension for parenteral administration.
7. A pharmaceutical composition as claimed in claim 5 , wherein the composition is in unit dosage form comprising zofenopril calcium in an amount of from 1 mg to 500 mg.