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Pharmaceutical composition of azelnidipine

A technology of azendipine and its composition, which is applied in the field of pharmaceutical compositions of dihydropyridine calcium ion antagonists, and can solve the problems of azendipine’s stability, influence on drug quality and curative effect, slow degradation, etc.

Active Publication Date: 2015-04-01
NANJING CHIA TAI TIANQING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although the above technologies have taken into account the influence of the pH environment on the stability of azelnidipine, the alkaline stable "microenvironment" constructed by the water-soluble alkaline auxiliary materials used in patents CN1762354A, CN101103979A, and CN102921008A will gradually weaken over time, thereby Affect the stability of Azedipine, and ultimately affect the quality and efficacy of the drug
Although the patent CN1436077A uses non-water-soluble alkaline auxiliary materials, it is the same as the patents CN1762354A, CN101103979A, and CN102921008A. The construction of its alkaline "microenvironment" only focuses on the slowest and most stable "microenvironment" of azedipine degradation at room temperature 25°C. Environmental" pH value (10.0), did not pay attention to changes in the pH value of the most stable alkaline "microenvironment" of azedipine caused by environmental temperature changes during transportation and storage

Method used

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  • Pharmaceutical composition of azelnidipine
  • Pharmaceutical composition of azelnidipine
  • Pharmaceutical composition of azelnidipine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Tablet 1:

[0045]

[0046]

[0047] Preparation process: Mix the prescribed amount of Azhedipine with a part of direct-pressed mannitol and pass through a 60-mesh sieve, then add the remaining prescription mannitol, low-substituted hydroxypropyl cellulose, meglumine, magnesium oxide, and calcium carbonate and mix through a 60-mesh sieve , and finally add the prescribed amount of magnesium stearate and mix well. Then punch the tablet with a shallow circular arc with a diameter of 7.5 mm to obtain the Azhedi flat tablet.

[0048] The dissolution rate of this preparation was measured in 75prm, 0.1M hydrochloric acid for 45min, and the dissolution rate was 99.4%.

Embodiment 2

[0050] Capsule 1:

[0051] According to the prescription of the above-mentioned embodiment 1, the mixed powder obtained in the above example is packed into 3# capsules with the powder direct filling process. The dissolution rate of this preparation was measured in 75prm, 0.1M hydrochloric acid for 45min, and the dissolution rate was 99.6%.

Embodiment 3

[0053] tablet 2

[0054]

[0055] Preparation process: Mix the prescribed amount of Azedipine with mannitol, microcrystalline cellulose, croscarmellose sodium, magnesium oxide, calcium carbonate, and micropowder silica gel in a high-efficiency wet mixer, and then add the dissolved prescription Stir the 5% HPMC aqueous solution of meglumine to make soft material, sieve with 20-mesh stainless steel screen to make wet granules; put the wet granules in a ventilated and constant temperature drying oven at 50°C for drying, and sieve the granules with 20-mesh sieve after drying , while adding magnesium stearate and mixing evenly to obtain dry granules of azedipine. Then punch the tablet with a shallow circular arc with a diameter of 7.5 mm to obtain the Azhedi flat tablet.

[0056] The dissolution of the preparation was measured in 75prm, 0.1M hydrochloric acid for 45min, and the dissolution rate was 99.5%.

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Abstract

The invention relates to a pharmaceutical composition of azelnidipine and particularly relates to a composition of jointly applying three alkaline auxiliary materials. The medicine has good storage stability and solves the problem of poor stability of azelnidipine and short storage time.

Description

technical field [0001] The invention relates to a pharmaceutical composition of a dihydropyridine calcium ion antagonist, in particular to a stable oral preparation of azendipine. Background technique [0002] Azhedipine is a dihydropyridine calcium antagonist developed by Japan’s Sankyo and Ube Industries Co., Ltd. It was approved in Japan on January 31, 2003, and it went on sale in May of the same year. The dosage form is tablets, and the trade name is Calblock. , the chemical structural formula is as follows: [0003] [0004] It belongs to the long-acting calcium antagonist, and its antihypertensive effect is gentle and lasting. In addition, the accumulation of azedipine around blood vessels may have a protective effect on vascular atherosclerosis. Therefore, the drug has been increasingly valued by clinicians and patients, and its market share has also been continuously increased and consolidated. However, the pharmaceutical composition of azedipine has poor stabi...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K9/00A61K31/4427A61K47/18A61K47/04A61P9/12A61P9/10
Inventor 石勇平郭璇章晓骅徐丹杨治旻田舟山
Owner NANJING CHIA TAI TIANQING PHARMA
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