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Two novel dihydralazine sulphate pharmaceutical co-crystals and preparation method thereof

A kind of technology of bishydralazine and sulfuric acid, applied in the field of novel bishydralazine sulfate drug co-crystal and preparation thereof

Inactive Publication Date: 2012-08-08
吉林三善恩科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drug crystal form research and solid-state characterization of drugs are relatively mature and highly valued fields in the European and American pharmaceutical industry, but they are still in their infancy in the domestic pharmaceutical industry

Method used

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  • Two novel dihydralazine sulphate pharmaceutical co-crystals and preparation method thereof
  • Two novel dihydralazine sulphate pharmaceutical co-crystals and preparation method thereof
  • Two novel dihydralazine sulphate pharmaceutical co-crystals and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Synthesis of co-crystal CC-1 using hydralazine sulfate and saccharin:

[0038] Raw material handling:

[0039] Accurately weigh 0.134g of hydralazine sulfate with an analytical balance, add 3ml of 2mol / L NaOH solution, stir for 0.5h, then put the cloudy solution into a 5ml centrifuge tube, centrifuge at 12000r / min for 3min, transfer Take the supernatant, wash it repeatedly with water for 3 times, and put it into a vacuum drying oven for drying.

[0040] Weighing:

[0041] The reactants are fed according to the material ratio of dihydralazine:saccharin=1:1. Accurately weigh 0.134g (0.4 moles) of dried dihydralazine and 0.073g of saccharin with an analytical balance and place them in a transparent glass vial.

[0042] Dissolution of API:

[0043] Use a 10ml pipette to accurately pipette 8ml of ethanol into a transparent glass vial container, and shake slightly to dissolve the solid evenly.

[0044] Solvent volatilization heat method:

[0045] After the solid is comp...

Embodiment 2

[0047] Synthesis of co-crystal CC-2 using hydralazine sulfate and saccharin:

[0048] Raw material handling:

[0049] Accurately weigh 0.134g of hydralazine sulfate with an analytical balance, add 3ml of 2mol / L NaOH solution, stir for 0.5h, then put the cloudy solution into a 5ml centrifuge tube, centrifuge at 12000r / min for 3min, transfer Take the supernatant, wash it repeatedly with water for 3 times, and put it into a vacuum drying oven for drying.

[0050] Weighing:

[0051] The reactants are fed according to the material ratio of dihydralazine:saccharin=1:4. Accurately weigh 0.134g of dried dihydralazine and 0.304g of saccharin with an analytical balance in a transparent glass vial.

[0052] Dissolution of API:

[0053] Use a 10ml pipette to accurately pipette 8ml of ethanol into a transparent glass vial container, and shake slightly to dissolve the solid evenly.

[0054] Solvent volatilization heat method:

[0055] After the solid is completely dissolved, seal the ...

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PUM

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystal, and particularly relates to two novel dihydralazine sulphate pharmaceutical co-crystals and a preparation method thereof. According to the pharmaceutical co-crystal, dihydralazine sulphate is used as an active pharmaceutical ingredient (API), and the selected precursor is saccharin. A dihydralazine sulphate molecule, a saccharin molecule and a water molecule are combined together through hydrogen bonds and an accumulation effect to form a basic structural unit of the dihydralazine pharmaceutical co-crystal. In a preparation process of the pharmaceutical co-crystal, the selected solvent is ethanol and sodium hydroxide solution, the adopted method is a solvent room-temperature volatilization method; and since the boiling point of the selected organic solvent is relatively low, crystals are separated in a solvent volatilization process. The dihydralazine sulphate pharmaceutical co-crystal prepared by the invention has obvious improvement on all dissolution, stability and bioavailability apart from the inheritance of the advantage of the conventional raw material medicine for treating cardiovascular diseases.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to two novel hydralazine sulfate drug co-crystals and a preparation method thereof. Background technique [0002] In 1894, E. Fischer of Germany proposed the "lock-key" model based on the idea of ​​"selective interaction between molecules", which was the prototype of modern supramolecular science theory. In 1937, German K.L.Wolf et al. created the term "supramolecular" to describe highly ordered entities formed by the association of molecules. In a general sense, any collection of molecules has interactions, so people often refer to them as The structural level of matter aggregation state is called "supramolecular". It was not until 1978 that Professor J.M.Lehn of France finally proposed the complete concept of "supramolecular chemistry" based on the traditional research on the host-guest system rooted in organic chemistry. Supramolecular chemistry is a scienc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D237/34
Inventor 赵念张兴晶张婷婷韩冰苏红敏朱广山
Owner 吉林三善恩科技开发有限公司