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Multiple crystal forms of S-Montelukast sodium and preparation method thereof

A technology of manidipine hydrochloride and manidipine, which is applied to the polymorphic form of S-manidipine hydrochloride and the field of preparation thereof, can solve the problems of low solubility of S-manidipine and the like, and achieves a production process. Stable, repeatable and controllable effects with good crystal stability

Active Publication Date: 2016-11-09
YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there are no patents and literature reports on the crystal form of S-manidipine. Because S-manidipine has low solubility in the body, it belongs to low-solubility and hypertonic drugs, and its dissolution behavior has a major impact on the effect of the drug in the body. Therefore, its The stability of the crystal form is critical

Method used

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  • Multiple crystal forms of S-Montelukast sodium and preparation method thereof
  • Multiple crystal forms of S-Montelukast sodium and preparation method thereof
  • Multiple crystal forms of S-Montelukast sodium and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Mix 1 gram of S-manidipine free base (prepared according to Chinese patent application 201510870914.8) and 20 ml of acetone. Then, under stirring, 5 ml of 30% HCl / ethanol solution was added, and the stirring was continued until the solution was completely dissolved. The resulting clear solution was left to stand at room temperature for 8 hours for crystallization, and then filtered to obtain 0.77 g of S-manidipine hydrochloride. As detected by XRD, the crystals were at about 5.86, 8.56, 9.20, 9.88, 11.75, 13.52, 14.25, 15.61, 16.33, 16.96, 17.20, 18.46, 18.80, 19.55, 19.85, 20.08, 21.47, 21.84, 22.42, 22.428, 2 There are characteristic peaks at 24.27, 24.75, 25.95, 26.48, 27.23, 27.40, 27.83, 28.44, 28.77, 29.56, 29.90, and 30.70. Its X-ray diffraction pattern is shown in figure 1 , X-ray diffraction data are shown in Table 1 below. Its DSC spectrum is shown in figure 2 , There is a melting endothermic peak at 235.4°C. This crystal form is defined as II crystal fo...

Embodiment 2

[0076] Mix 1 gram of S-manidipine free base and 20 ml of ethyl acetate. Then, under stirring, 5 ml of 30% HCl / ethanol solution was added, and the stirring was continued until the solution was completely dissolved. The obtained clear solution was left to stand at room temperature for 8 hours for crystallization, and then filtered to obtain 0.81 g of S-manidipine hydrochloride. Its XRD and DSC patterns are researched and compared, and it is determined that the product is in the II crystal form.

Embodiment 3

[0078] Mix 1 gram of S-manidipine free base and 100 ml of methyl isobutyl ketone. Then, under stirring, 5 ml of 30% HCl / ethanol solution was added, and the stirring was continued until the solution was completely dissolved. The resulting clear solution was left to stand at room temperature for 8 hours for crystallization, and then filtered to obtain 0.67 g of S-manidipine hydrochloride. Its XRD and DSC patterns are researched and compared, and it is determined that the product is in the II crystal form.

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Abstract

The invention relates to multiple crystal forms of S-Montelukast sodium and a preparation method thereof, in particular to a crystal form II, a crystal form III and a crystal form IV of S-Montelukast sodium, the preparation method of the crystal forms, pharmaceutical composition containing the crystal forms and a medical application of the crystal forms and the pharmaceutical composition. The crystal form II, the crystal form III and the crystal form IV of S-Montelukast sodium have excellent physicochemical properties and good stability, and are suitable for a preparation technological process and long-term storage. The pharmaceutical composition adopting compounds in the crystal forms as active components can be used for treating diseases such as hypertension and the like.

Description

technical field [0001] The invention relates to a polymorphic form of S-manidipine hydrochloride and a preparation method thereof. In particular, the present invention relates to the II, III and IV crystal forms of S-manidipine hydrochloride and their preparation methods, as well as their pharmaceutical compositions and their medical applications. Background technique [0002] The chemical name of S-manidipine hydrochloride is (4S)-1,4-dihydro-2,6-dimethyl-4-m-nitrophenyl-3,5-pyridinedicarboxylate 2- (4-benzhydryl-1-piperazinyl) ethyl ester hydrochloride, its structure is shown in the following formula (I), [0003] [0004] Manidipine hydrochloride is a lipophilic third-generation calcium channel antagonist, a dihydropyridine antihypertensive drug developed by Japan's Takeda Pharmaceutical Co., Ltd. in 1990. This product has high selectivity to blood vessels, which can relax peripheral blood vessels and reduce blood pressure, but has almost no inhibitory effect on the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90A61K31/496A61P9/12A61P9/10A61P13/12
CPCC07B2200/13C07D211/90
Inventor 刘玉海王建耀刘伟陈东袁峰泉刘文东
Owner YANGTZE RIVER PHARMA GRP BEIJING HAIYAN PHARMA
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