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Amlodipine mesylate monohydrate and its preparation method and use

A technology of amlodipine mesylate and monohydrate, which is applied in the field of amlodipine mesylate monohydrate and its preparation, can solve the problems of unsatisfactory particle size and uniformity, fluidity and compressibility, etc. Achieve uniform and controllable particle size distribution, good content uniformity, and stable quality

Active Publication Date: 2021-08-13
KUNMING SINOWAY NATURAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the raw material drug that the existing amlodipine mesylate preparation process makes can not meet the requirement of using high-speed rotary tablet press powder direct compression in terms of particle size and uniformity, fluidity, compressibility, etc.

Method used

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  • Amlodipine mesylate monohydrate and its preparation method and use
  • Amlodipine mesylate monohydrate and its preparation method and use
  • Amlodipine mesylate monohydrate and its preparation method and use

Examples

Experimental program
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Effect test

experiment example 1

[0080] Experimental example 1 amlodipine free base is that raw material is that starting material prepares amlodipine mesylate monohydrate

[0081] Add 100 g of amlodipine free base (245.1 mmol), ethyl acetate (500 mL) and purified water (5.29 mL, 1.2 equivalents) to a 2000 mL three-necked flask in sequence, and stir for 15 minutes to dissolve. Under room temperature conditions, first weigh 5.88g methanesulfonic acid (61.3mmol), quickly add in the reaction solution through a constant pressure dropping funnel under stirring, control the dropping rate to be 5mL / min, and control the stirring speed at 160 rpm to obtain A clear solution. At room temperature, 1.25 g of amlodipine mesylate monohydrate seed crystals were added to the solution to obtain a suspension, and the stirring speed was controlled at 70 rpm. Separately take by weighing 17.6g methanesulfonic acid (183.9mmol), carry out slowly dropwise under stirring by constant pressure dropping funnel, rate of addition is 0.5...

experiment example 2

[0083] Experimental Example 2 Amlodipine free base is the raw material for the preparation of amlodipine mesylate monohydrate as the starting material

[0084] Add 100 g of amlodipine free base (245.1 mmol), ethyl acetate (500 mL) and purified water (5.29 mL, 1.2 equivalents) to a 2000 mL three-necked flask in sequence, and stir for 15 minutes to dissolve. At room temperature (25°C), first weigh 5.88g methanesulfonic acid (61.3mmol), quickly add it into the reaction solution through a constant pressure dropping funnel under stirring, control the dropping rate to 5mL / min, and control the stirring speed at 160 rpm / min to obtain a clear solution. At room temperature, 1.25 g of amlodipine mesylate monohydrate seed crystals were added to the solution to obtain a suspension, and the stirring speed was controlled at 70 rpm. Take by weighing 17.6g methanesulfonic acid (183.9mmol) separately, carry out slowly dropwise under stirring by constant pressure dropping funnel, rate of add...

experiment example 3

[0085] Experimental Example 3 Amlodipine free base is the raw material for the preparation of amlodipine mesylate monohydrate as the starting material

[0086] Add 210g of amlodipine free base (514.7mmol), ethyl acetate (1000mL) and purified water (11.1mL, 1.2 equivalents) to a 3000mL three-necked flask in sequence, and stir for 15 minutes to dissolve. Under low temperature conditions (5°C), first weigh 12.3g methanesulfonic acid (128.7mmol), quickly add it into the reaction solution through a constant pressure dropping funnel under stirring, control the dropping rate to 5mL / min, and control the stirring speed at 160 rpm / min to obtain a clear solution. At room temperature, 2.6 g of amlodipine mesylate monohydrate seed crystals were added to the solution to obtain a suspension, and the stirring speed was controlled at 270 rpm. Another 37.1g methanesulfonic acid (386.0mmol) was weighed, slowly added dropwise with stirring through a constant pressure dropping funnel, and the ...

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Abstract

The present invention relates to amlodipine mesylate monohydrate and its preparation method and use. The amlodipine mesylate monohydrate is a crystal, and the particle size range of the crystal is D 10 : 20‑40 μm, D 50 : 55‑85 μm, D 90 : 95‑140μm, Carr index 10‑25%, angle of repose 15‑35°, bulk density 0.25‑0.45g / mL, purity greater than 99.5%. The amlodipine mesylate monohydrate has high purity, good fluidity and compressibility, and is suitable for the direct tablet compression process of a high-speed tablet machine.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to amlodipine mesylate monohydrate and its preparation method and application. Background technique [0002] Most drugs are weakly acidic or weakly basic organic small molecules. Among the drugs approved by the FDA in the United States, the drugs listed as salt compounds account for more than half of the total number of drugs on the market. Drugs with different acid groups or bases After salt formation, it can not only improve some of its undesirable physical and chemical properties (crystallinity, thermodynamic properties, hygroscopicity and stability, etc.), but also improve the biopharmaceutical properties of the drug (solubility, dissolution rate and bioavailability, etc.) . Physicochemical properties such as crystal form, particle size, and compressibility of raw materials also have a major impact on the formability and stability of drugs, especially solid ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/90C07C309/04C07C303/32C07C303/44A61K31/4422A61P9/12A61K9/20
CPCA61K9/2059A61K31/4422A61P9/12C07C303/32C07C303/44C07C309/04C07D211/90
Inventor 郝振平徐溧
Owner KUNMING SINOWAY NATURAL PHARMA CO LTD
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