Composition of L-5-methyltetrahydrofolate or pharmaceutically acceptable salt thereof and pharmaceutical adjuvants and preparing method thereof

A technology of methyltetrahydrofolate and pharmaceutical excipients, which is applied in the fields of drug combination, food science, cardiovascular system diseases, etc., can solve the problems of affecting the bioavailability of drugs, difficult to achieve medicinal and edible, poor chemical stability, etc. Achieve fast dispersion and dissolution rate, improve bioavailability, and good dispersion.

Inactive Publication Date: 2017-08-11
CHANGZHOU AINUOXINRUI PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology describes methods for combining different types of ingredient(L-5-MTHFLIPIDES®or other substances together). By doing this, stable compositions containing these compounds may become available at room temperature without losing their effectiveness due to melting during storage. Additionally, they provide improved properties when added to various medical products like tablets or capsules. Overall, this approach provides technical benefits over existing techniques while avoiding certain drawbacks associated therewith.

Problems solved by technology

This patented describes different ways to make certain drugs like lithium hydroxypropyltriflate or gamma valerolide better suited for medical purposes because they have fewer negative side effects compared to other medicants currently available on market. However, their physical properties can change over time if stored at high temperatures which makes them less effective when taken by patients who require frequent blood tests. To address this problem, researchers explored various techniques involving combining two compounds together called α-,β-unsaturated glucuronosulfoferrumie acid ("α - methoxytetrol," abbreviators). These combinations were found to provide improved results without compromising any beneficial aspects associated with each individual component separately.

Method used

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  • Composition of L-5-methyltetrahydrofolate or pharmaceutically acceptable salt thereof and pharmaceutical adjuvants and preparing method thereof
  • Composition of L-5-methyltetrahydrofolate or pharmaceutically acceptable salt thereof and pharmaceutical adjuvants and preparing method thereof
  • Composition of L-5-methyltetrahydrofolate or pharmaceutically acceptable salt thereof and pharmaceutical adjuvants and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Dissolve L-5-methyltetrahydrofolate calcium salt (50 mg) and povidone K30 (500 mg) in water (10 ml), heat to 60°C and stir to dissolve. The above solution is freeze-dried to obtain the composition of amorphous L-5-methyltetrahydrofolate calcium salt and povidone K30, and the X-ray powder diffraction pattern of the composition is as follows: figure 1 As shown, there is no characteristic peak of the crystal form of L-5-methyltetrahydrofolate calcium salt in the X-ray powder diffraction pattern after deducting the background peak of the pharmaceutical excipient.

Embodiment 2

[0042] Dissolve L-5-methyltetrahydrofolate (50 mg) and povidone K30 (500 mg) in water (2 ml), heat to 60°C and stir to dissolve. The above solution was lyophilized to obtain a composition of amorphous L-5-methyltetrahydrofolate and povidone K30, and no L-5 -Characteristic peaks of the crystalline form of methyltetrahydrofolate.

Embodiment 3

[0044] Add L-5-methyltetrahydrofolate glucosamine salt (0.1 g) and polyethylene glycol 8000 (10 g) into water (300 ml), heat to 60° C. and stir to dissolve. Dry the above solution with JISL micro spray dryer LSD-48, maintain the inlet temperature at 60°C and the outlet temperature at 50°C, collect the outlet material to obtain a white solid, and further vacuum dry to obtain amorphous L-5-methyltetrahydrofolate glucosamine The composition of the salt and polyethylene glycol 8000, in the X-ray powder diffraction diagram of the composition, there is no characteristic peak of the crystal form of L-5-methyltetrahydrofolate glucosamine salt after deducting the background peaks of pharmaceutical excipients.

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Abstract

A composition of L-5-methyltetrahydrofolate or a pharmaceutically acceptable salt thereof and pharmaceutical excipients and a production method thereof, comprising L-5-methyltetrahydrofolate or a pharmaceutically acceptable salt thereof and pharmaceutical excipients, L-5-methyltetrahydrofolate or its pharmaceutically acceptable salts are in an amorphous state, and there is no L after deducting the background peak of the pharmaceutical excipients in the X-ray powder diffraction spectrum of the composition -Characteristic peaks of crystals of 5-methyltetrahydrofolate or its salts. The composition of L-5-methyltetrahydrofolate or its pharmaceutically acceptable salt and pharmaceutical excipients of the present invention has good stability and dispersibility, and increases the dissolution of L-5-methyltetrahydrofolate or its salt It is more conducive to improving the bioavailability of pharmaceutical preparations and the absorption of drugs by the body. Under accelerated test conditions, it can maintain good physical and chemical stability. The preparation method of the amorphous composition of the invention is simple in operation, low in cost, good in reproducibility, easy to implement and suitable for industrialized production.

Description

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Claims

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Application Information

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Owner CHANGZHOU AINUOXINRUI PHARMA LTD
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