Polymorphs of dolutegravir and salts thereof
AssigneeLaurus Labs Limited
InventorsRam Thaimattam, Rajesh Edupuganti, Venkata Sunil Kumar Indukuri, Srihari Raju Kalidindi, Satyanarayana Chava
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Abstract
The present invention relates to novel crystalline forms of dolutegravir, process for its preparation and pharmaceutical composition comprising them.
Claims10
Dolutegravir morpholine solvate.
Crystalline Form-I of dolutegravir morpholine solvate, characterized by a powder X-Ray diffraction pattern having one or more peaks at about 6.30, 7.28, 8.86, 9.90, 10.52, 11.44, 12.14, 13.76, 14.62, 15.04, 15.76, 16.50, 17.24, 18.00, 19.88, 20.76, 21.08, 22.48, 23.24, 23.84, 24.62, 25.04, 26.46, 26.94, 28.60, 29.58 and 32.14±0.2° 2θ.
A process for preparation of crystalline Form-I of dolutegravir morpholine solvate, which comprise of:
- a) dissolving dolutegravir in a suitable chloro solvent,
- b) adding morpholine to step a) solution,
- c) adding a suitable anti-solvent to step b) solution;
- and
- d) isolating the dolutegravir crystalline Form-I.
Crystalline Form-II of dolutegravir morpholine solvate, characterized by a powder X-Ray diffraction pattern having one or more peaks at about 6.78, 8.80, 11.56, 13.76, 14.80, 16.64, 17.56, 18.48, 19.34, 19.66, 20.40, 20.80, 21.48, 21.90, 22.74, 23.38, 25.24, 25.72, 27.56, 28.44, 29.54, 30.48 and 31.88±0.2° 2θ.
A process for the preparation of crystalline Form-II of dolutegravir morpholine solvate, which comprise of
- a) dissolving dolutegravir in morpholine;
- and
- b) isolating the dolutegravir crystalline Form-II.
A pharmaceutical composition comprising:
- dolutegravir morpholine solvate;
- and
- at least one pharmaceutically acceptable excipient,
- wherein the dolutegravir morpholine solvate is one of
- crystalline Form-I of dolutegravir morpholine solvate characterized by a powder X-Ray diffraction pattern having one or more peaks at about 6.30, 7.28, 8.86, 9.90, 10.52, 11.44, 12.14, 13.76, 14.62, 15.04, 15.76, 16.50, 17.24, 18.00, 19.88, 20.76, 21.08, 22.48, 23.24, 23.84, 24.62, 25.04, 26.46, 26.94, 28.60, 29.58 and 32.14±0.2° 2θ, and
- crystalline Form-II of dolutegravir morpholine solvate characterized by a powder X-Ray diffraction pattern having one or more peaks at about 6.78, 8.80, 11.56, 13.76, 14.80, 16.64, 17.56, 18.48, 19.34, 19.66, 20.40, 20.80, 21.48, 21.90, 22.74, 23.38, 25.24, 25.72, 27.56, 28.44, 29.54, 30.48 and 31.88±0.2° 2θ.
Dependencies are inferred from the claim text.