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Cobamamide compound and medicinal composition thereof

A technology for adenosylcobalamin and compositions, which is applied in the field of pharmaceutical compositions containing the adenosylcobalamin, can solve the problems of uneven and delicate appearance of samples and poor stability of preparations, and achieve uniform and delicate appearance and stability Improvement, good effect

Inactive Publication Date: 2014-11-05
CHANGSHA BOYA MEDICINE TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Chinese Patent Application No. 201310245278.0 discloses a lyophilized preparation of adenosylcobalamin for injection. Its components include adenosylcobalamin and mannitol, and its dosage is 0.52g:25g. The lyophilized powder injection uses relatively few excipients , but the appearance of the sample prepared according to this patent is not uniform and delicate, and the stability of the preparation is not very good, requiring very strict storage conditions

Method used

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  • Cobamamide compound and medicinal composition thereof
  • Cobamamide compound and medicinal composition thereof
  • Cobamamide compound and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Preparation of adenosylcobalamin compound:

[0054] (1) Add 50 g of adenosylcobalamin solid into 150 mL of a mixed solvent of isopropanol and pyridine, the volume ratio of isopropanol and pyridine in the mixed solvent is 4.0:1.0, and dissolve the adenosylcobalamin solid at room temperature;

[0055] (2) Add 800mL ether to the solution obtained in step (1), while stirring, the stirring rate is controlled at 1600r / min;

[0056] (3) After adding diethyl ether, cool down to -10°C within 5 minutes, and stand at -10°C for 11 hours to precipitate crystals, filter, and wash the filter cake twice with ether (150mL each time). After drying under vacuum for 4 hours, adenosylcobalamin crystalline compound was obtained.

[0057] The adenosylcobalamin compound uses Cu-Kα 1 X-ray powder diffraction for radiographic measurements such as figure 1 shown.

Embodiment 2

[0059] Preparation of adenosylcobalamin compound:

[0060] (1) Add 50 g of adenosylcobalamin solid into 150 mL of a mixed solvent of isopropanol and pyridine, the volume ratio of isopropanol and pyridine in the mixed solvent is 5.0:1.0, and dissolve the adenosylcobalamin solid at room temperature;

[0061] (2) Add 500mL ether to the solution obtained in step (1), while stirring, the stirring rate is controlled at 1800r / min;

[0062] (3) After adding ether, cool down to -15°C within 3 minutes, and let it stand at -15°C for 10 hours to precipitate crystals, filter, and wash the filter cake twice with ether (150mL each time). After drying under vacuum for 3 hours, adenosylcobalamin crystalline compound was obtained.

[0063] The adenosylcobalamin compound uses Cu-Kα 1 Radiographic X-ray powder diffraction showed that, with the attached figure 1 The results shown match.

Embodiment 3

[0065] Preparation of adenosylcobalamin compound:

[0066] (1) Add 50 g of adenosylcobalamin solid into 150 mL of a mixed solvent of isopropanol and pyridine, the volume ratio of isopropanol and pyridine in the mixed solvent is 2.0:1.0, and dissolve the adenosylcobalamin solid at room temperature;

[0067] (2) add 600mL ether in the solution that step (1) obtains, stir simultaneously, stirring rate is controlled at 1500r / min;

[0068] (3) After adding ether, cool down to -10°C within 6 minutes, and stand at -10°C for 10 hours to precipitate crystals, filter, and wash the filter cake twice with ether (150mL each time), at a temperature of 35°C After drying under vacuum for 2 hours, adenosylcobalamin crystalline compound was obtained.

[0069] The adenosylcobalamin compound uses Cu-Kα 1 Radiographic X-ray powder diffraction showed that, with the attached figure 1 The results shown match.

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Abstract

The invention discloses a cobamamide compound. The X-ray powder diffraction of the cobamamide compound is as shown in Fig. 1. The invention further discloses a medicinal composition of the cobamamide compound. The cobamamide compound disclosed by the invention is stable in chemical property and high in stability, and has better treatment effects on neurological diseases. Moreover, the cobamamide compound disclosed by the invention is simple in composition and high in safety. A prepared cobamamide freeze-dried powder for injection is uniform and fine in property, and is high in solubility and high in stability.

Description

technical field [0001] The invention relates to an adenosylcobalamin compound, a preparation method of the adenosylcobalamin compound, and a pharmaceutical composition containing the adenosylcobalamin compound. Background technique [0002] Adenosylcobalamin (Cobamamide) is a cyanocobalamin-type vitamin B 12 Congeners of B 12 The metabolites in the body are substances necessary for cell growth and proliferation and to maintain the integrity of nerve myelin sheaths. Compared with vitamin B 12 It has higher biological activity and bioavailability, and can be directly absorbed and utilized by the human body. Adenosylcobalamin has strong activity, strong affinity with tissue cells, and has a long retention in the body. It is an important coenzyme for cell synthesis of nucleotides and participates in methyl conversion and folic acid metabolism in the body. It promotes the reduction of methyl folic acid to tetrahydrofolate, and also participates in The tricarboxylic acid cycle ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H23/00C07H1/00A61K31/714A61K9/19A61P25/02A61P27/02A61P3/10
Inventor 蒋银妹
Owner CHANGSHA BOYA MEDICINE TECH DEV
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