Delta d-crystalline form of ivabradine hydrochloride, a process for its preparation and pharmaceutical compositions containing it

A technology of crystallization of ivabradine hydrochloride, applied in the direction of drug combination, organic chemical method, active ingredient of heterocyclic compound, etc., can solve the problem of obtaining without explanation

Inactive Publication Date: 2007-04-18
SERVIER LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this document does not describe the conditions for obtaining ivabradine i

Method used

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  • Delta d-crystalline form of ivabradine hydrochloride, a process for its preparation and pharmaceutical compositions containing it
  • Delta d-crystalline form of ivabradine hydrochloride, a process for its preparation and pharmaceutical compositions containing it

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Ivabradine hydrochloride in δd-crystalline form

[0034] 160ml of acetonitrile was preheated to 70°C, then 2g of ivabradine hydrochloride obtained by the method described in the patent specification EP0534859 was added part by part, while stirring until completely dissolved. The solution was then kept at ambient temperature for 2 days. Crystals were vacuum filtered and spread on crystallization trays. The crystals were then heated to 85°C at a rate of 10°C / min and held at 85°C for 4 hours.

[0035] Powder X-ray Diffraction Pattern:

[0036] The powder X-ray diffraction pattern (diffraction angles) of the δd-form of ivabradine hydrochloride is given in the following table with highlighted lines:

[0037]

[0038] 4

Embodiment 2

[0039] Embodiment 2: pharmaceutical composition

[0040] Formulation for the preparation of 1000 tablets each containing 5 mg ivabradine base:

[0041] Compound of Example 1 ................................. 5.39g

[0042] corn starch................................................ .20g

[0043] Anhydrous colloidal silica...................................0.2g

[0044] Mannitol................................................ 63.91g

[0045] PvP................................................................ .....10g

[0046] Magnesium stearate.............................................. ..0.5g

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Abstract

The invention relates to the dd crystalline form of ivabradine hydrochloride having general formula (I), which is characterised by its X-ray diffraction pattern on powder. The invention is suitable for medicaments.

Description

technical field [0001] The present invention relates to ivabradine hydrochloride (ivabradine) of formula (I) in δd-crystalline form, a process for its preparation and pharmaceutical compositions comprising it. [0002] Background technique [0003] Ivabradine and its addition salts with pharmaceutically acceptable acids, especially its hydrochloride, have very valuable pharmacological and therapeutic properties, especially bradycardic properties, which make These compounds are useful in the treatment or prophylaxis of various clinical conditions of myocardial ischemia, such as angina pectoris, myocardial infarction and related cardiac rhythm disturbances, and also in various pathologies involving cardiac rhythm disturbances, especially supraventricular cardiac rhythm disturbances, and heart failure. [0004] European patent specification EP 0 534 859 already describes the preparation and therapeutic use of ivabradine and its addition salts with pharmaceutically acceptabl...

Claims

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Application Information

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IPC IPC(8): C07D223/16A61K31/55A61P9/10A61P9/06A61P9/04
CPCC07D223/16A61P9/00A61P9/04A61P9/06A61P9/10A61K31/55C07B2200/13
Inventor S·霍瓦特M-N·奥古斯特G·达米安
Owner SERVIER LAB
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