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Crystalline forms of vilazodone hydrochloride and vilazodone free base

a technology of vilazodone and hydrochloride, which is applied in the field of crystalline forms of vilazodone hydrochloride and vilazodone free base, can solve the problems of no “standard", the inability to predict the number of polymorphic forms of a given compound, and the inability to achieve the effect of increasing the number of polymorphic forms

Inactive Publication Date: 2015-05-07
DR REDDYS LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent text explains what polymorphs are and their importance in drug development. Consequently, regulatory authorities require pharmaceutical companies to identify all polymorphs of new drug substances. The difference in solid forms can significantly influence the properties and quality of a drug, such as bioavailability, handling properties, and stability. This is important for ensuring the safety and effectiveness of the drug, and it also affects the manufacturing process and shelf life of the product.

Problems solved by technology

The existence and possible numbers of polymorphic forms for a given compound cannot be predicted, and there are no “standard” procedures that can be used to prepare polymorphic forms of a substance.

Method used

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  • Crystalline forms of vilazodone hydrochloride and vilazodone free base
  • Crystalline forms of vilazodone hydrochloride and vilazodone free base
  • Crystalline forms of vilazodone hydrochloride and vilazodone free base

Examples

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Effect test

example 1

Preparation of Crystalline Form B of Vilazodone Hydrochloride

example 1a

[0383]Vilazodone free base (118 g) and methanol (2360 mL) were charged into a round bottom flask at ambient temperature. The resulting mixture was cooled to 4° C. and 10% w / w methanolic hydrochloric acid solution (236 mL) was slowly added, stirred the resulting solution at 0-5° C. for 30 minutes. The solid was collected by filtration and dried at 45-50° C. for 3.5 hours to afford the title compound.

[0384]Yield: 107.6 g;

[0385]Water Content: 8.46% w / w as measured by Karl Fischer method.

[0386]The PXRD pattern of crystalline Form B of vilazodone hydrochloride obtained is in accordance with FIG. 1.

example 1b

[0387]Vilazodone free base (1.5 g) and methanol (30 mL) were charged into a round bottom flask at −10° C. 10% w / w Methanolic hydrochloric acid solution (3 mL) was slowly added to the resulting mixture at −10° C. and further stirred for 30 minutes. The solid was collected by filtration and dried at 45-50° C. for 30 minutes to afford the title compound.

[0388]Yield: 1.4 g

[0389]Water Content: 8.46% w / w as measured by Karl Fischer method.

[0390]The PXRD pattern of crystalline Form B of vilazodone hydrochloride obtained is in accordance with FIG. 2.

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Abstract

Provided are crystalline and amorphous vilazodone hydrochloride. Further provided are amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carries. Also provided is a process for the preparation of form I of vilazodone free base.

Description

INTRODUCTION[0001]One aspect of the present application relates to crystalline forms B, C, D, E, F, G and H of Vilazodone hydrochloride. Another aspect of the present application relates to amorphous vilazodone hydrochloride and a process for preparation thereof. Yet another aspect of the present application relates to amorphous solid dispersions of vilazodone hydrochloride. Still another aspect of the present application relates to a process for the preparation of vilazodone free base. Another aspect of the present application relates to crystalline form I of vilazodone free base.[0002]Vilazodone hydrochloride is selective serotonin reuptake inhibitor, which also acts as partial agonist at serotonergic 5-HT1A receptors. It is mainly used for the treatment of major depressive disorder (MDD) and marketed as Viibryd™ in tablet dosage forms. The vilazodone hydrochloride is chemically known as 2-benzofurancarboxamide, 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]-1-piperazinyl]-, hydrochloride ...

Claims

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Application Information

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IPC IPC(8): C07D405/12
CPCC07D405/12A61P25/24C07D405/14C07B2200/13
Inventor IQBAL, JAVEDORUGANTI, SRINIVASRAPOLU, RAJESH KUMARPEDDY, VISHWESHWARBOGE, RAJESHAMPATHIVADA, DEEPIKAVELAGA, DHARMA JAGANNADHA RAOYARRAGUNTLA, SESHA REDDYBADDAM, SUDHAKAR REDDYNAREDLA, ANITHADONIPARTHI, KIRAN KUMARNADGOUD, RAMESH KUMARPAGADALA, NARASIMHA RAOUNNIARAN, SYAM KUMARRAMAKRISHNAN, SRIVIDYA
Owner DR REDDYS LAB LTD
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