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Solid preparation of levamlodipine or pharmaceutically-acceptable salts thereof, and preparation method thereof

A technology of levamlodipine and solid preparations, which is applied in the field of medicine and can solve problems such as toxicity, easy decomposition, and photosensitivity

Active Publication Date: 2011-02-16
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Therefore, amlodipine besylate and S-(-)-amlodipine besylate have potential toxicity, are sensitive to light, are easy to decompose, and have many adverse reactions caused by vasodilation, such as headache and edema. , fatigue, insomnia, nausea, abdominal pain, flushing, palpitations, dizziness, itching, rash, dyspnea, weakness, muscle cramps, indigestion myocardial infarction and chest pain and other adverse reactions, restricting clinical application, then the development of levamlodipine or its New preparations of pharmaceutically acceptable salts, reducing adverse reactions, are urgent issues in clinical application

Method used

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  • Solid preparation of levamlodipine or pharmaceutically-acceptable salts thereof, and preparation method thereof
  • Solid preparation of levamlodipine or pharmaceutically-acceptable salts thereof, and preparation method thereof
  • Solid preparation of levamlodipine or pharmaceutically-acceptable salts thereof, and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0030] The preparation of embodiment 1 levamlodipine hydrochloride solid preparation

[0031] a. After mixing 15g of xanthan gum and 10g of silk fibroin, stir and melt at 55°C and keep warm, slowly add 10g of micropowder silica gel while stirring, so that the micropowder silica gel is evenly dispersed, and the composition is obtained for use;

[0032] b. Prepare microemulsion with 15g of propoxylated methyl glucoside, 5ml of isobutanol, and 40ml of ethyl acetate, add 245g of levamlodipine hydrochloride (calculated as levamlodipine) into the emulsion, and place at 40°C in a water bath;

[0033] C. Add the composition obtained in step a to 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;

[0034] d. Cool the reaction solution to 0°C, add glutaraldehyde 0.08 times the volume of the react...

Embodiment 2

[0036] The preparation of embodiment 2 levamlodipine fumarate solid preparations

[0037] a. After mixing 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 use;

[0038] B, make microemulsion with propoxylated methyl glucoside 120g, isobutanol 40ml, ethyl acetate 320ml, add levamlodipine fumarate 780g (in levamlodipine) in the emulsion, place In a water bath at 60°C;

[0039] C. Add the composition obtained in step a 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 constant temperature for 2 hours;

[0040] d. Cool the reaction solution to 0°C, add glutaraldehyde 0.125 times the volume of the reaction solution and continue to stir for...

Embodiment 3

[0042] Embodiment 3 The preparation of levamlodipine p-fluorobenzoate solid preparation

[0043] a. 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;

[0044] B, make microemulsion with 60g of propoxylated methyl glucoside, 20ml of isobutanol, 160ml of ethyl acetate, add levamlodipine p-fluorobenzoate 450g (in terms of levamlodipine) to the emulsion, place In a water bath at 50°C;

[0045] C. Add the composition obtained in step a to 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;

[0046] d. Cool the reaction solution to 0°C, add glutaraldehyde 0.1 times the volume of the reaction ...

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Abstract

The invention discloses a solid preparation of levamlodipine or pharmaceutically-acceptable salts thereof, which contains nano-microcapsules of the levamlodipine or the pharmaceutically-acceptable salts thereof, and medicinal auxiliary materials, wherein the nano-microcapsules are prepared from the levamlodipine or the pharmaceutically-acceptable salts thereof and a carrier material according to the weight ratio of 7-12:1; the carrier material is a xanthan gum-silk fibroin-aerosil composition; the ratio of the using amount of xanthan gum to the using amount of silk fibroin to the using amount of aerosil is 1.5-4.5:1:1; and the weight ratio of the levamlodipine or the pharmaceutically-acceptable salts thereof to the medicinal auxiliary materials is 1:1. The solid preparation has a regular and unbroken surface and is stable and not decomposed under the radiation of highlight, has substantially unchanged content, substantially unchanged related substances and a remarkable sustained release function, avoids the burst release of medicaments, solves the problem of potential toxicity of benzene sulfonate, reduces toxic or side effect and improves the compliance of patients.

Description

technical field [0001] The invention relates to a solid preparation and a preparation method thereof, in particular to a solid preparation of levamlodipine or a pharmaceutically acceptable salt thereof, belonging to the technical field of medicine. Background technique [0002] Amlodipine is a long-acting dihydropyridine calcium ion antagonist, which can block the extracellular calcium ion of cardiac muscle and vascular smooth muscle from entering the cell through the calcium ion channel (slow channel) of the cell membrane, and directly relax the vascular smooth muscle. high blood pressure medications. In addition to its antihypertensive effect, amlodipine also has the function of protecting target organs, which meets the requirements of modern antihypertensive treatment. The hardening of the blood vessel wall of the elderly increases with age. The degeneration of elastin fibers and the increase of collagen substances increase the stiffness of the aorta and large arteries, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P9/12A61K47/42A61K31/4422
Inventor 周杰董新明王炫
Owner CSPC OUYI PHARM CO LTD
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