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5-amino salicylic acid pharmaceutical co-crystal and preparation method thereof

A technology of aminosalicylic acid and aminobenzoic acid, which is applied in the field of drug co-crystals, can solve problems such as difficulty in obtaining high-purity crystals, high cost and technical requirements, and products that are easily affected by solvents, so as to extend the market cycle, Effects of improved solubility and simple preparation method

Inactive Publication Date: 2017-10-24
EAST CHINA NORMAL UNIVERSITY
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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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  • 5-amino salicylic acid pharmaceutical co-crystal and preparation method thereof
  • 5-amino salicylic acid pharmaceutical co-crystal and preparation method thereof
  • 5-amino salicylic acid pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Weigh 30mg of 5-aminosalicylic acid and 68.1mg of maleic 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 A mixed solvent of methanol, ultrasonicated until completely dissolved, sealed the test tube mouth and pierced a small hole to stand for volatilization for 6 days, crystals began to precipitate at the bottom of the test tube, and 46 mg of light yellow transparent block crystals were obtained, which were 5-aminosalicylic acid and maleic acid drugs Eutectic with a yield of 89%.

Embodiment 2

[0038] Weigh 30 mg of 5-aminosalicylic acid and 30.2 mg of 2,6-dihydroxybenzoic acid and place them in an agate mortar, grind them evenly, add 20 μL of methanol, grind quickly until the solvent evaporates, and then transfer the mixture to a glass test tube, Add a mixed solvent of 2mL acetone and 2mL methanol, sonicate until it is completely dissolved, seal the test tube mouth and pierce a small hole and let it stand for volatilization for 3 days. Crystals start to precipitate at the bottom of the test tube, and 50 mg of light yellow transparent block crystals are obtained as 5-aminosalicylic acid The drug was co-crystallized with 2,6-dihydroxybenzoic acid with a yield of 83%.

Embodiment 3

[0040] Weigh 30 mg of 5-aminosalicylic acid and 18.4 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 2 mL of acetone and 2mL of methanol mixed solvent, sonicated until completely dissolved, sealed the test tube mouth and pierced a small hole to stand for volatilization for 5 days, crystals began to precipitate at the bottom of the test tube, and 27 mg of light yellow transparent blocky crystals were obtained, which were 5-aminosalicylic acid and 4-aminosalicylic acid Pyridine drug co-crystal with a yield of 56%.

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Abstract

The invention discloses a 5-amino salicylic acid pharmaceutical co-crystal and a preparation method thereof. The preparation method is characterized in that 5-amino salicylic acid is mixed with maleic acid, 2,6-dihydroxybenzoic acid or 4-aminopyridine in a weight ratio of 1:(0.5-8), the mixture is subjected to ultrasonic treatment in a methanol / acetone mixed solvent until the mixture is completely dissolved, and then, the product is placed for 3-10 days, wherein the precipitated flaxen transparent crystal is a pharmaceutical co-crystal of 5-amino salicylic acid and maleic acid, 2,6-dihydroxybenzoic acid or 4-aminopyridine, and the weight-to-volume ratio of 5-amino salicylic acid to maleic acid, 2,6-dihydroxybenzoic acid or 4-aminopyridine to methanol / acetone mixed solvent is 1mg:(0.5-8)mg:(2-5)ml. Compared with the prior art, the 5-amino salicylic acid pharmaceutical co-crystal and the preparation method thereof have the advantages that the preparation method is simple and controllable, the synthesis period is short, the repeatability is good, pharmaceutical properties of nicotinic acid are kept, the solubility is obviously increased, the market period of the original drug is prolonged, and application prospects are extensive.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical co-crystals, in particular to 5-aminosalicylic acid and maleic acid, 5-aminosalicylic acid and 2,6-dihydroxybenzoic acid or 5-aminosalicylic acid and 4 - Aminopyridine drug co-crystal and 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 b...

Claims

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Application Information

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IPC IPC(8): C07C229/64C07C227/00C07C227/42C07D213/73C07C51/41C07C51/43C07C65/03C07C57/145A61P31/06A61P29/00A61P1/00
CPCC07C229/64C07B2200/13C07C57/145C07C65/03C07D213/73
Inventor 赵小莉陈燕洁牛艳霏
Owner EAST CHINA NORMAL UNIVERSITY
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