Polymorphic Form of Lercanidipine Hydrochloride and Process for the Preparation Thereof
AssigneeGlenmark Generics Ltd
InventorsMangesh Shivram Sawant, Maloyesh Mathuresh Biswas, Mubeen Ahmed Khan, Sukumar Sinha, Nitin Sharad Chandra Pradhan
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Abstract
Processes for the purification of lercanidipine hydrochloride are provided which uses a binary system of an alcohol-containing solvent such as methanol and an aliphatic ester-containing solvent such as isopropyl acetate. Processes for the preparation of substantially amorphous lercanidipine hydrochloride are also provided. Also provided is lercanidipine hydrochloride substantially in polymorph form V.
Claims35
A process for preparing substantially pure lercanidipine hydrochloride, the process comprising:
- (a) dissolving lercanidipine hydrochloride in an alcohol-containing solvent to form a solution;
- (b) adding an aliphatic ester-containing solvent to the solution;
- and
- (c) recovering substantially pure lercanidipine hydrochloride from the solution.
2-7. (canceled)
Lercanidipine hydrochloride having a purity equal to or greater than about 98.5%.
10-17. (canceled)
Lercanidipine hydrochloride substantially in polymorph form V.
24-25. (canceled)
27-29. (canceled)
31-33. (canceled)
A process for the preparation of lercanidipine hydrochloride substantially in polymorph form V, the process comprising:
- (a) dissolving lercanidipine hydrochloride in an alcohol-containing solvent to obtain a solution;
- (b) adding an aliphatic ester-containing solvent to the solution;
- and
- (c) recovering lercanidipine hydrochloride substantially in polymorph form V.
36-38. (canceled)
(canceled)
42-46. (canceled)
48-50. (canceled)
A process for the preparation of substantially pure lercanidipine hydrochloride, the process comprising:
- (a) reacting a solution comprising butanoic acid, 2-[(3-nitrophenyl)methylene]-3-oxo-2-[(3,3-diphenyl propyl)methylamino]-1,1-dimethyl ethyl ester hydrochloride and methylene dichloride, with methyl 3-amino crotonate and n-propanol and adjusting the pH of the solution to about 8 to about 9 with a base;
- (b) distilling out n-propanol to obtain a residue;
- (c) dissolving the residue in isopropyl acetate;
- (d) treating the solution containing isopropyl acetate with a clarifying agent to form a clarified solution;
- (e) concentrating the clarified solution to form a concentrated clarified solution;
- (f) dissolving the concentrated clarified solution in methanol and isopropyl acetate;
- (g) seeding the solution with a lercanidipine hydrochloride substantially in polymorph form V, and
- (h) recovering the lercanidipine hydrochloride substantially in polymorph form V.
A process for the preparation of amorphous lercanidipine hydrochloride, the process comprising (a) dissolving lercanidipine hydrochloride substantially in polymorph form V in an organic solvent;
- and (b) recovering the amorphous form of lercanidipine hydrochloride.
54-61. (canceled)
A process for the preparation of amorphous lercanidipine hydrochloride, the process comprising (a) dissolving substantially pure lercanidipine hydrochloride in an organic solvent;
- (b) treating the solution with a clarifying agent to form a clarified solution, and (c) recovering the amorphous form of lercanidipine hydrochloride.
63-67. (canceled)
69-70. (canceled)
Lercanidipine hydrochloride substantially free of 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 2-[N-(3,3-diphenyl propyl)-N-methylamino]-1,1-dimethyl ethyl propyl diester.
72-74. (canceled)
Dependencies are inferred from the claim text.