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(6S)-5-methyl tetrahydrofolate crystal form and preparation method thereof

A technology of methyltetrahydrofolate and methyltetrahydrofolate, which is applied in the field of pharmaceutical crystal forms, can solve problems such as easy degradation and instability of 5-methyltetrahydrofolate, and achieve high bioavailability and suitable for Industrial scale preparation, good stability

Active Publication Date: 2012-07-18
LIANYUNGANG JINKANG HEXIN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] For medicinal compounds, their physical and chemical stability under different storage conditions is very important, but (6S)-5-methyltetrahydrofolate is very unstable and easily degraded, especially highly sensitive to oxygen and moisture, so Difficult to obtain products of sufficient purity for pharmaceutical active ingredients and food additives

Method used

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  • (6S)-5-methyl tetrahydrofolate crystal form and preparation method thereof
  • (6S)-5-methyl tetrahydrofolate crystal form and preparation method thereof
  • (6S)-5-methyl tetrahydrofolate crystal form and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0047] Put 40 ml of deionized water in a container, add 3.0 g of (6S)-5-MTHF, neutralize with 2mol / L liquid caustic soda under stirring until the pH value is 7.5 to completely dissolve (6S)-5-MTHF, transfer to frequency In an ultrasonic reactor with a frequency of 40KHz and a power of 500w, heat to 30° C., add 10% calcium chloride solution (containing 1.0 g of calcium chloride), perform ultrasonic reaction for 0.5 hours, filter and wash with water. Vacuum-dried at 30° C. to obtain 2.11 g of white type B (6S)-5-MTHF calcium salt. The chemical purity is 99.7% (HPLC detection), the content is 101.5%, and the water content is 15.0%.

Embodiment 2

[0049] Put 30 ml of deionized water in a container, add 2.0 g of (6S)-5-MTHF, neutralize with 2mol / L liquid caustic soda under stirring until the pH value is 7.0 until (6S)-5-MTHF is completely dissolved, and transfer to frequency In an ultrasonic reactor with a frequency of 60KHz and a power of 100w, heat to 43° C., add 10% calcium chloride solution (containing 0.5 grams of calcium chloride), filter and wash after ultrasonic reaction for 0.5 hours. Vacuum-dried at 25° C. to obtain 1.59 g of white type B (6S)-5-MTHF calcium salt. The chemical purity is 99.5% (HPLC detection), the content is 100.1.1%, and the water content is 14.9%.

Embodiment 3

[0051] Put 30 ml of deionized water in a container, add 2.0 g of (6S)-5-MTHF, neutralize with 2mol / L liquid caustic soda under stirring until the pH value is 7.3 until (6S)-5-MTHF is fully dissolved, and transfer to frequency In an ultrasonic reactor with a frequency of 80KHz and a power of 1000w, heat to 40° C., add 10% calcium chloride solution (containing 1.2 grams of calcium chloride), perform ultrasonic reaction for 0.5 hours, filter and wash with water. Vacuum-dried at 30° C. to obtain 1.70 g of white type B (6S)-5-MTHF calcium salt. The chemical purity is 99.2% (HPLC detection), the content is 99.4%, and the water content is 14.4%.

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Abstract

The invention discloses a (6S)-5-methyl tetrahydrofolate crystal form and a preparation method thereof. The crystal form is a B-type (6S)-5-methyl calcium tetrahydrofolate crystal form, and diffraction peaks exist at the positions where 2theta angle is 3.2+ / -0.2 and 18.9+ / -0.2 in an X-ray diffraction map of the B-type crystal form; or the crystal form is a C-type (6S)-5-methyl calcium tetrahydrofolate crystal form, and diffraction peaks exist at the positions where 2theta angle is 6.3+ / -0.2 and 19.2+ / -0.2 in the X-ray diffraction map of the C-type crystal form. The B-type (6S)-5-methyl calcium tetrahydrofolate crystal form and the C-type (6S)-5-methyl calcium tetrahydrofolate crystal form disclosed by the invention has the advantages of excellent physicochemical property, good stability, high purity, good repeatability and the like and are suitable for industrial large-scale preparation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical crystal forms, and in particular relates to two (6S)-5-methyltetrahydrofolate crystal forms and a preparation method and use thereof. Background technique [0002] (6S)-5-Methyltetrahydrofolate is the main form of folic acid in tissues and blood, and participates in many important biochemical reactions in the body, such as the biosynthesis of purine and thymine. It does not need to go through cumbersome enzymatic steps in the human body and can be directly utilized. In addition, (6S)-5-methyltetrahydrofolate is the only drug among folic acid drugs that can penetrate the blood-brain barrier, and has the effect of preventing and treating Alzheimer's disease (senile dementia), so it has the advantages of other folic acid drugs. Incomparable superiority. It is mainly used in active ingredients of medicines and food additives. It can prevent fetal neural tube defects, arteriosclerosis, and treat megalob...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D475/04A61K31/519A61P7/06A61P9/00A61P25/00A61P39/02A61P17/06A61P19/02A61P29/00A61P37/00A61K47/22A23L1/30
Inventor 王哲清成永之黄恒
Owner LIANYUNGANG JINKANG HEXIN PHARMA CO LTD
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