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Nicotinic acid pharmaceutical co-crystal and preparation method thereof

A nicotinic acid and drug technology, applied in the field of drug co-crystals, can solve the problems that high-purity crystals are not easy, high cost and technical requirements, products are easily affected by solvents, etc., achieving a simple and controllable preparation method and extending the market. The effect of improving cycle and solubility

Inactive Publication Date: 2017-08-04
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The pharmaceutical eutectic in the prior art has many factors affecting the operation, and has high requirements for cost and technology, and the product is easily affected by the solvent, so it is not easy to obtain high-purity crystals

Method used

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  • Nicotinic acid pharmaceutical co-crystal and preparation method thereof
  • Nicotinic acid pharmaceutical co-crystal and preparation method thereof
  • Nicotinic acid pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Weigh 30mg of nicotinic acid and 37.6mg of 2,6-dihydroxybenzoic acid in an agate mortar, grind them evenly, add 20μL of methanol, grind quickly until the solvent evaporates, then transfer the mixture to a glass test tube, add 2mL of acetone and 2mL of methanol mixed solvent, sonicate until completely dissolved, seal the test tube mouth and pierce a small hole and let it evaporate for 7 days, white transparent long crystals begin to precipitate at the bottom of the test tube, which is the drug of niacin and 2,6-dihydroxybenzoic acid eutectic.

Embodiment 2

[0029] Weigh 30 mg of nicotinic acid and 26.4 mg of 4-aminopyridine and place them in an agate mortar, grind them evenly, add 20 μL of methanol, grind quickly until the solvent evaporates, then transfer the mixture to a glass test tube, add a mixture of 2 mL of acetone and 2 mL of methanol Solvent, sonicate until completely dissolved, seal the test tube mouth and pierce a small hole and let it evaporate for 9 days. White columnar transparent crystals begin to precipitate at the bottom of the test tube, which is the drug co-crystal of niacin and 4-aminopyridine.

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Abstract

The invention discloses a nicotinic acid pharmaceutical co-crystal and a preparation method of the nicotinic acid pharmaceutical co-crystal. The nicotinic acid pharmaceutical co-crystal is characterized by mixing nicotinic acid with 2,6-dihydroxy benzoic acid or 4-aminopyridine in a weight ratio of 1:(1-8), adding methanol to be ground until a solvent is volatilized after grinding uniformly, then carrying out ultrasonic treatment in a methanol / acetone mixed solvent until being dissolved completely, and then standing for 5 to 10 days for separating out a white transparent crystal, namely the pharmaceutical co-crystal of nicotinic acid and 2,6-dihydroxy benzoic acid or nicotinic acid and 4-aminopyridine. Compared with the prior art, the nicotinic acid pharmaceutical co-crystal disclosed by the invention is simple and controllable in preparation method, short in synthesis cycle and good in repeatability, not only keeps drug characteristics of nicotinic acid, but also has obviously improved solubility, prolongs the market cycle of the original drug and has broad application prospects.

Description

technical field [0001] The invention relates to the technical field of drug co-crystals, in particular to a drug co-crystal of niacin and 2,6-dihydroxybenzoic acid or niacin and 4-aminopyridine and a preparation method thereof. Background technique [0002] Crystal engineering is based on the principles and methods of supramolecular chemistry and the control of intermolecular interactions on crystals to design and manufacture strange, novel, varied crystals with specific physical and chemical properties. These crystals are usually multidimensional supramolecular aggregates that extend infinitely in space, and the arrangement of molecular building units in the solid state determines the physical and chemical properties of the crystal material. Therefore, by selecting the appropriate molecular building blocks, the information of the interactions (such as coordination bonds and hydrogen bonds) that can be adopted between these molecules can be mastered, so that the functions of...

Claims

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Application Information

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IPC IPC(8): C07D213/80C07D213/803C07D213/73C07C65/03
CPCC07D213/80C07B2200/13C07C65/03C07D213/73C07D213/803
Inventor 赵小莉陈燕洁牛艳霏
Owner EAST CHINA NORMAL UNIV
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