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Levamlodipine besylate crystal and preparation method and application thereof

A technology for levamlodipine besylate and crystals, applied in the field of preparation thereof, and crystals of levamlodipine besylate, can solve the problems such as the lack of clear crystallographic main parameter atomic space positions, the lack of clear crystal water molecules and the like , to achieve the effect of being conducive to stability, improving solubility and stability

Active Publication Date: 2015-12-02
菲洋生物科技(吉林)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the crystal form of levamlodipine besylate has not been reported. For domestic levamlodipine besylate, relevant patents mainly involve dosage forms or production processes, such as Chinese patent applications CN101559043A, CN101721384A, CN102028662A, CN101766582A, etc.
Although Chinese patent applications CN102276516A and CN103193700A relate to a crystal of levamlodipine besylate, the crystal is only ordinary X-ray powder diffraction data, and there are no clear crystallographic parameters and exact atomic spatial positions. The most important What is surprising is that, as hydrated levamlodipine besylate crystals, there is no definite number of crystal water molecules

Method used

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  • Levamlodipine besylate crystal and preparation method and application thereof
  • Levamlodipine besylate crystal and preparation method and application thereof
  • Levamlodipine besylate crystal and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1 Preparation of levamlodipine besylate crystal of the present invention

[0049] 1) Completely dissolve 5 grams of levamlodipine besylate powder sample (provided by Shihuida Pharmaceutical Group (Jilin) ​​Co., Ltd., batch number: 140207-2) into 2.5 mL of a mixed solution of distilled water and acetone with a volume ratio of 1:1 to obtain the reaction solution;

[0050] 2) Raise the temperature of the reaction solution to 30°C, stir for 10 minutes, cool to room temperature, then slowly add 10 mL of distilled water, let it stand, and lower the ambient temperature to 5°C, keep this condition for 1 day, and obtain a large number of needle-shaped or rod-shaped Color transparent crystal, regular crystal form, uniform particle size;

[0051] 3) Filter the obtained crystal product under reduced pressure, wash the original crystal solution, and wash with cold water.

specific Embodiment 2-7

[0052] Following specific examples 2-7, preparation method is the same as embodiment 1, and its concrete process parameter is shown in table 1.

[0053] Table 1

[0054]

[0055]

Embodiment 8

[0056] The measurement of the crystal form of embodiment 8 levamlodipine besylate crystals

[0057] For each of the above examples, select a crystal with a size of 0.6×0.8×2.1 (mm) from the prepared crystal sample, and "rivet" it on the top of the glass filament, and adopt an X-ray single crystal diffractometer of the ApexDuo model of Bruker, Germany The test is carried out, and the test parameters are carried out according to the strategy established by the instrument according to the crystal size. The test temperature is 173K, with MoK α radiation Diffraction data were collected in ω-scan mode and Lp correction was performed. Absorption correction was performed using the SADABS program. Use the direct method to analyze the structure, use the difference Fourier method to find all non-hydrogen atoms, all hydrogen atoms on carbon and nitrogen are obtained by theoretical hydrogenation, and the hydrogen atoms of crystal water molecules are directly found from the difference F...

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Abstract

The invention provides a levamlodipine besylate crystal with the molecular formula being (C20H25ClN2O5) (C6H6O3S) (H2O) 1.5 and the molecular weight being 594.07. Crystallography measurement parameters are a monoclinic system and P21 chirality space groups, and the chirality absolute configuration is determined by crystallography Flack parameter being 0.08(6); the unit cell size is shown in the specification, wherein beta is 95.817(4) degrees, and V is 2880.1(11). The characteristic peak in an X-ray powder diffraction pattern (Cu-Kalpha) is displayed at 2thea being 6.70 degrees, 10.12 degrees, 12.40 degrees, 13.36 degrees, 13.68 degrees, 17.04 degrees, 22.46 degrees and 24.16 degrees. The invention further provides a preparation method and application of the levamlodipine besylate crystal. The levamlodipine besylate crystal has the specific crystal form and the amount of crystal water and specific crystallography main parameters and the exact atom spatial position, the solubleness and stability of existing levamlodipine besylate are improved, the stability and bioavailability of the levamlodipine besylate tablet can be improved, preparation is easy, the cost is low, and the obtained crystal is regular in form, uniform in particle size and suitable for large-scale application and popularization.

Description

technical field [0001] The present invention relates to the technical field of crystal drug molecules, in particular to the technical field of levamlodipine besylate crystal form, and specifically refers to a levoamlodipine besylate crystal, its preparation method and application. Background technique [0002] Most drug molecules are generally designed into solid dosage forms, and among various solid forms of drugs, crystalline drug molecules are preferred due to their advantages in stability, reproducibility, and operability. Crystalline drug molecules include polymorphic forms, hydrates, solvates, and salts of drug molecules. Drug molecules usually have different biological activities due to containing various functional groups. These functional groups can use hydrogen bonds or other non-covalent bonds to form supramolecular compounds with other molecules through intermolecular recognition, that is, drug co-crystals, thereby effectively improving the crystallization prope...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90C07C309/29C07C303/32A61P9/12
CPCC07B2200/13C07D211/90
Inventor 凌云杨彦玲李环陶丽
Owner 菲洋生物科技(吉林)有限公司
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