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Calcium channel blocking drug molecule co-crystal and preparation method thereof

A calcium channel blocker and drug molecule technology, which is applied in the field of calcium channel blocker drug molecule co-crystals and its preparation, can solve the problems of drug stability being easily affected by the environment, and is suitable for large-scale application and improved solubility And the effects of stability and crystal form rules

Inactive Publication Date: 2019-10-25
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide a calcium channel blocking drug molecular co-crystal and its preparation method in order to solve the above problems. In terms of structural design, water free volume is small, and it is easy to freely enter and exit in the structure of the co-crystal drug, resulting in hydration. The essential problem that the stability of dihydropyridine drugs is easily affected by the environment, the crystal form of the calcium channel blocker drug molecular co-crystal provided by the present invention uses the large free volume and pharmaceutically acceptable isopropanol molecule as the co-crystal guest Molecules, Preparation of Stable Levo-Amlodipine Co-Crystals

Method used

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  • Calcium channel blocking drug molecule co-crystal and preparation method thereof
  • Calcium channel blocking drug molecule co-crystal and preparation method thereof
  • Calcium channel blocking drug molecule co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] 1) Weigh 0.4 g of crystals in P2 1 2 1 2 1 levamlodipine, it is completely dissolved in 5mL isopropanol, to obtain the reaction solution;

[0045] 2) Under the condition of mechanical stirring at room temperature, add 10 mL of isopropanol solution of benzenesulfonic acid with a concentration of 0.1M drop by drop within one minute;

[0046] 3) Transfer the above solution to a reaction kettle, increase the temperature of the reaction solution to 80° C., keep it warm for 8 hours, and cool to room temperature to obtain a large number of needle-shaped or rod-shaped colorless, transparent, and uniform crystal products;

[0047] 4) Filter the obtained crystalline product under reduced pressure, wash the original crystalline solution, and wash with isopropanol to obtain the product.

Embodiment 2-8

[0049] The preparation method is the same as in Example 1, and its specific process parameters are shown in Table 1.

[0050] Table 1 embodiment 2-8 preparation process parameters

[0051]

Embodiment 9

[0053] 1) Place 0.5 mmol of commercially available levamlodipine salt in a closed space, heat to 50° C. and dry for 2 hours under vacuum degassing condition;

[0054] 2) Cool to room temperature under vacuum, add 5mL of isopropanol solvent by negative pressure siphon, and stir until the levoamlodipine salt is completely dissolved;

[0055] 3) Airtightly heat at 50°C or heat and reflux for 5 hours, let stand and cool to room temperature, and obtain needle-shaped or rod-shaped colorless transparent crystals;

[0056] 4) Filter the obtained crystalline product under reduced pressure, wash the original crystalline solution, and wash with isopropanol to obtain the product.

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Abstract

The invention relates to a calcium channel blocking drug molecule co-crystal and a preparation method thereof. The general molecular formula of the calcium channel blocking drug molecule co-crystal is(C20H25ClN2O5).(X).((CH3)2CHOH)n, wherein X represents one of benzene sulfonic acid, maleic acid and fumaric acid; and n represents the number of isopropanol molecules, and n is greater than 0 and less than and equal to 1. A co-crystal drug provided solves the solubility and stability problems of existing levamlodipine, and is beneficial to the improvement of the stability of levamlodipine tablets, preparation of the co-crystal is simple, the cost is low, the crystal form of the prepared crystal is regular, the particle size is uniform, and industrial production prospects are achieved.

Description

technical field [0001] The invention relates to the technical field of crystalline drugs, in particular to a calcium channel blocking drug molecular co-crystal and a preparation method thereof. Background technique [0002] Amlodipine is a third-generation dihydropyridine calcium channel blocker, which is a potent and long-acting antihypertensive drug. Amlodipine is a racemic mixture of levamlodipine and dexamlodipine in a ratio of 1:1. Pharmacological studies have shown that the antihypertensive effect of levamlodipine is more than 1000 times that of dexamlodipine; Therefore, chiral split levamlodipine, as the fourth-generation calcium ion antagonist antihypertensive drug for the treatment of hypertension, is deeply trusted by doctors and patients due to its high efficacy and small side effects, and is currently a commonly used drug for the treatment of hypertension. [0003] Due to the advantages of stability, reproducibility, bioavailability and operability, crystalline...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90C07C29/78C07C31/10C07C303/32C07C309/29C07C51/41C07C57/15C07C57/145
CPCC07B2200/13C07C29/78C07C31/10C07C51/412C07C57/145C07C57/15C07C303/32C07C309/29C07D211/90
Inventor 凌云周亚明邓名莉杨永泰刘小锋贾瑜
Owner FUDAN UNIV
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