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Levoamlodipine maleate eutectic medicine crystallized to triclinic system and preparation method and application of levoamlodipine maleate eutectic medicine

A technology of levoamlodipine and triclinic crystal system, applied in the field of crystal drugs, can solve the problems of affecting dissolution and absorption efficiency, differences in physical and chemical properties, low bioavailability, etc. The effect of regular shape and uniform particle size

Pending Publication Date: 2020-09-18
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This new type of medicine called Levamidopiron Maleate (LVM) was discovered during research on neurotransmitter receptors found at different levels within central nervous systems such as brain neurons that help control pain signals. It's made from certain chemical compounds mixed together. Lvm also works differently than other drugs like amitriptyline but it doesn’t require any modifications before being able to function properly inside our body.

Problems solved by technology

This patented technical problem addressed in this patents relates to improving the performance or usableness of certain types of medications called lisdexamidopropion Bromide hydrochlorides ("LIS"), such as levosimendazole sodium phosphate," while also addressing issues like lack of sufficient data needed for understanding these new substances' characteristics during manufacturing processes.

Method used

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  • Levoamlodipine maleate eutectic medicine crystallized to triclinic system and preparation method and application of levoamlodipine maleate eutectic medicine
  • Levoamlodipine maleate eutectic medicine crystallized to triclinic system and preparation method and application of levoamlodipine maleate eutectic medicine
  • Levoamlodipine maleate eutectic medicine crystallized to triclinic system and preparation method and application of levoamlodipine maleate eutectic medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of levoamlodipine fumarate co-crystal drug crystal form of the present invention

[0037] 1) Weigh 2.06 g of L-Amlodipine free alkali and 0.58 g of maleic acid in the reaction kettle;

[0038] 2) Configure a mixed solvent of 23mL ethanol and 10mL ethyl acetate and add it to the reaction kettle;

[0039] 3) Seal the reaction kettle, raise the temperature to 60°C, keep it for 5 hours, and then let it stand and slowly cool to room temperature to obtain a colorless, transparent, uniform crystal product;

[0040] 4) Filter the obtained crystal product under reduced pressure, and wash the original crystal solution to obtain it.

specific Embodiment 2-8

[0041] The following specific Examples 2-8, the preparation method is the same as that of Example 1, and the specific process parameters are shown in Table 1.

[0042] Table 1 Specific process parameters of Examples 2-8

[0043]

Embodiment 9

[0045] X-ray single crystal diffraction test

[0046] Take the eutectic crystal of levoamlodipine maleate prepared in Example 1 as an example, select the crystal whose quality and size meet the requirements of the test instrument, and use the D8 VENTURE X-ray single crystal diffractometer of German Bruker Company to test. The parameters are carried out according to the strategy established by the instrument. Use MetalJet liquid gallium alloy target light source, use Ga-Kα radiation Diffraction data is collected in ω scan mode and Lp correction is performed. The absorption correction uses the SADABS program. The structure is analyzed by direct method, and all non-hydrogen atoms are found by difference Fourier method. All hydrogen atoms on carbon and nitrogen are obtained by theoretical hydrogenation, and the least square method is used to modify the structure. All the parsing process is completed using SHELXTL package.

[0047] In the above measurement, the crystal test can be t...

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Abstract

The invention provides a levoamlodipine maleate eutectic medicine crystallized to triclinic system and a preparation method and application of the levoamlodipine maleate eutectic medicine. The chemical general formula of the eutectic medicine is (C20H26ClN2O5).(C4H3O4).(H2O)n, wherein C20H26ClN2O5 is a molecular formula that primaquine in levoamlodipine (free alkali ) is protonated,C4H3O4 is 2-butenedioic acid (Z) of which one proton is removed, n is greater than or equal to 0 and smaller than 1, the eutectic medicine molecule is crystallized to the triclinic system, P1 chirality space group and crystal cell size are as below: alpha==97.7-97.9 degrees, beta= 92.6-93.0 degrees, and gamma =109.2-109.6 degrees. The eutectic medicine provided by the invention has explicit crystal form, crystalparameters and precise atom space positions, and is different from commercially available levoamlodipine maleate. The preparation method is simple, the granule crystal form is clear, and quality control and large-scale production are easy to perform.

Description

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Claims

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Application Information

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Owner FUDAN UNIV
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