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Pharmaceutical cocrystal of 5-aminosalicylic acid and 2-aminopyridine and preparation method of pharmaceutical cocrystal

A technology of aminosalicylic acid and aminopyridine, applied in the field of 5-aminosalicylic acid and 2-aminopyridine drug co-crystal and preparation thereof, can solve the problem that high-purity crystals are not easy, the cost and technical requirements are high, The product is easily affected by solvents and other problems, so that the preparation method is simple and controllable, the market cycle is prolonged, and the solubility is improved.

Inactive Publication Date: 2017-12-01
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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  • Pharmaceutical cocrystal of 5-aminosalicylic acid and 2-aminopyridine and preparation method of pharmaceutical cocrystal
  • Pharmaceutical cocrystal of 5-aminosalicylic acid and 2-aminopyridine and preparation method of pharmaceutical cocrystal
  • Pharmaceutical cocrystal of 5-aminosalicylic acid and 2-aminopyridine and preparation method of pharmaceutical cocrystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Weigh 30mg of 5-aminosalicylic acid and 18.4mg of 2-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 2mL of acetone and 2mL methanol mixed solvent, sonicate until completely dissolved, seal the test tube mouth and pierce a small hole and let it stand for volatilization for 7 days. Light yellow transparent block crystals begin to precipitate at the bottom of the test tube, which are 5-aminosalicylic acid and 2-aminopyridine drugs. eutectic.

Embodiment 2

[0025] Weigh 35mg of 5-aminosalicylic acid and 24mg of 2-aminopyridine and place them in an agate mortar, grind them evenly, add 25 μL of methanol, grind quickly until the solvent evaporates, then transfer the mixture to a glass test tube, add 2.5mL of acetone and 2.5mL methanol mixed solvent, sonicate until completely dissolved, seal the test tube mouth and pierce a small hole and let it stand for volatilization for 9 days, the bottom of the test tube begins to precipitate light yellow transparent block crystals, which are 5-aminosalicylic acid and 2-aminopyridine Drug co-crystals.

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Abstract

The invention discloses a pharmaceutical cocrystal of 5-aminosalicylic acid and 2-aminopyridine and a preparation method of the pharmaceutical cocrystal. The preparation method is characterized by comprising the steps: mixing 5-aminosalicylic acid with 2-aminopyridine according to the weight ratio of 1:(1-8), after uniformly grinding the mixture, adding methanol to grind the mixture until a solvent is volatized to be dry; then, carrying out ultrasonic treatment in a methanol / acetone mixed solvent until the mixture is completely dissolved; and next, standing the mixture for 9 days, and separating out a brown yellow transparent bulk crystal, namely the pharmaceutical cocrystal of 5-aminosalicylic acid and 2-aminopyridine. Compared with the prior art, the preparation method is simple and controllable, short in synthesis period and good in repeatability; and the formed pharmaceutical cocrystal of 5-aminosalicylic acid and 2-aminopyridine is remarkably improved in solubility, capable of prolonging the market period of the original drug and wide in application prospect in addition to retaining the characteristic that tuberculosis is treated by 5-aminosalicylic acid.

Description

technical field [0001] The invention relates to the technical field of drug co-crystals, in particular to a drug co-crystal of 5-aminosalicylic acid and 2-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 the molecular components...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/73C07C227/18C07C229/64A61P31/06
Inventor 赵小莉陈燕洁牛艳霏
Owner EAST CHINA NORMAL UNIV
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