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Ivabradine preparation or ivabradine medicinal salt solid preparation and preparation method thereof

A technology of solid preparations and medicinal salts, applied in the field of medicine, can solve problems such as unfavorable left ventricular systolic function, achieve the effects of avoiding sudden release of drugs, overcoming dose dependence, and reducing adverse reactions

Active Publication Date: 2010-12-01
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the most commonly used drug for lowering heart rate clinically is β-blocker, which can effectively reduce the occurrence of angina to a large extent by lowering heart rate, but its side effects (including fatigue, depression and sexual function) Obstacles, etc.) and its contraindications (including airway obstruction, atrioventricular block, decompensated heart failure, etc.) and the inherent negative inotropic effect of β-blockers have adverse effects on left ventricular systolic function , so that the use of β-blockers by clinicians and the compliance of patients are limited to a certain extent

Method used

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  • Ivabradine preparation or ivabradine medicinal salt solid preparation and preparation method thereof

Examples

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Embodiment 1

[0021] The preparation of embodiment 1 ivabradine hydrochloride solid preparation

[0022] (1) After mixing 15g of xanthan gum and 10g of silk fibroin, stir and melt at 55°C and keep warm, slowly add 10g of micropowdered silica gel while stirring, so that the micropowdered silica gel is evenly dispersed, and the composition is obtained for use;

[0023] (2) make microemulsion with propoxylated methyl glucoside 15g, isobutanol 5ml, ethyl acetate 40ml, add ivabradine hydrochloride 175g (in terms of ivabradine) in the emulsion, place in 40 ℃ in water bath;

[0024] (3) Add the composition obtained in (1) into the microemulsion, stir until uniform, use this solution as the reaction solution, adjust the pH value of the reaction solution to 8.0 with 10% NaOH solution, add an appropriate amount of methanol, and react at constant temperature for 1 hour ;

[0025] (4) Cool the reaction solution to 0°C, add glutaraldehyde 0.08 times the volume of the reaction solution and continue to ...

Embodiment 2

[0027] The preparation of the solid preparation of embodiment 2 ivabradine or its pharmaceutically acceptable salt

[0028] (1) Mix 45g of xanthan gum and 10g of silk fibroin, stir and melt at 60°C and keep warm, slowly add 10g of micropowdered silica gel while stirring, so that the micropowdered silica gel is evenly dispersed, and the composition is obtained for later use;

[0029] (2) make microemulsion with propoxylated methyl glucoside 120g, isobutanol 40ml, ethyl acetate 320ml, add ivabradine hydrochloride 975g (in terms of ivabradine) in the emulsion, place in 60 ℃ in water bath;

[0030] (3) Add the composition obtained in (1) to the microemulsion, stir until uniform, use this solution as the reaction solution, adjust the pH value of the reaction solution to 10.0 with 10% NaOH solution, add an appropriate amount of methanol, and react at a constant temperature for 2 Hour;

[0031] (4) Cool the reaction solution to 0°C, add glutaraldehyde 0.125 times the volume of the ...

Embodiment 3

[0033] The preparation of the solid preparation of embodiment 3 ivabradine or its pharmaceutically acceptable salt

[0034] (1) After mixing 25g of xanthan gum and 10g of silk fibroin, stir and melt at 58°C and keep warm, slowly add 10g of micropowdered silica gel while stirring, so that the micropowdered silica gel is evenly dispersed, and the composition is obtained for use;

[0035] (2) Microemulsion was prepared with 60 g of propoxylated methyl glucoside, 20 ml of isobutanol, and 160 ml of ethyl acetate. Add 540 g of ivabradine hydrochloride (calculated as ivabradine) into the emulsion and place at 50° C. in a water bath;

[0036] (3) Add the composition obtained in (1) into the microemulsion, stir until uniform, use this solution as the reaction solution, adjust the pH value of the reaction solution to 9.0 with 10% NaOH solution, add an appropriate amount of methanol, and react at constant temperature for 1.5 hours ;

[0037] (4) Cool the reaction solution to 0°C, add g...

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Abstract

The invention relates to an ivabradine preparation or an ivabradine medicinal salt solid preparation and a preparation method thereof. The preparation comprises ivabradine or ivabradine medicinal salt nanocapsules and a medicinal auxiliary material, wherein the mass ratio of the ivabradine or the ivabradine medicinal salt to a carrier material is 5-15:1; the carrier material is a composition prepared from xanthan, silk fibroin and aerosil; and the mass ratio of the xanthan to the silk fibroin to the aerosil is 1.5-4.5:1:1. The optimization proportions of the xanthan, the silk fibroin and the aerosil, melting temperature, heat preservation measure and the effects of various factors on the preparation are selected so as to determine an optimized preparation condition and achieve an entrapment rate of over 95 percent; and the preparation has the advantages of preventing medicament burst release, reducing adverse reactions, improving the compliance of patients and overcoming side effects such as dosage dependence, visual symptoms and the like.

Description

technical field [0001] The invention relates to a solid preparation and a preparation method thereof, in particular to a solid preparation of ivabradine or a pharmaceutically acceptable salt thereof and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Heart rate is an important risk factor for coronary heart disease and other cardiovascular diseases. Reducing heart rate is not only beneficial to the prevention of angina pectoris, but also more conducive to the prognosis of patients with coronary heart disease, and plays an important role in improving the survival rate of patients with coronary heart disease. At present, the most commonly used drug for lowering heart rate clinically is β-blocker, which can effectively reduce the occurrence of angina to a large extent by lowering heart rate, but its side effects (including fatigue, depression and sexual function) Obstacles, etc.) and its contraindications (including airw...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K9/20A61K9/48A61K9/16A61K31/55A61K47/42A61K47/36A61K47/04A61P9/06
Inventor 高志峰孙鹏刘聪敏
Owner CSPC OUYI PHARM CO LTD
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