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Acyclovir eutectic and preparation method thereof and preparation

A technology of organic solvent and glutaric acid, which is used in the preparation of carboxylates, antiviral agents, active ingredients of heterocyclic compounds, etc., to achieve the effects of low production cost, improved transdermal penetration rate and less solvent amount

Inactive Publication Date: 2013-05-22
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The application also has no experimental data showing that the crystal form of acyclovir has better transdermal absorption

Method used

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  • Acyclovir eutectic and preparation method thereof and preparation
  • Acyclovir eutectic and preparation method thereof and preparation
  • Acyclovir eutectic and preparation method thereof and preparation

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preparation example Construction

[0044] A kind of preparation method of above-mentioned acyclovir-glutaric acid co-crystal, comprises the steps:

[0045] 1) Mix acyclovir and glutaric acid in a molar ratio of 1:1;

[0046] 2) Grinding the mixture of acyclovir and glutaric acid at a frequency not lower than 15Hz, adding an appropriate amount of organic solvent during the grinding process;

[0047] 3) The obtained solid is vacuum-dried, and the obtained white powdery solid is the aciclovir-glutaric acid cocrystal.

[0048] In the above preparation method, the organic solvent is at least one of methanol, ethanol, dichloromethane, and acetonitrile.

[0049] The purpose of adding an organic solvent is to make the acyclovir and glutaric acid have a larger contact reaction area during the grinding process to obtain a better grinding effect. Those skilled in the art can adjust the amount of solvent added according to actual conditions. According to people's experience of the present invention, in above-mentioned pr...

Embodiment 1

[0053] 1) Weigh 150 mg of acyclovir and 88 mg of glutaric acid;

[0054] 2) Add the mixture into the ball mill jar, and add 10 μL of methanol dropwise;

[0055] 3) Grinding for 25 min at a frequency of 15 Hz;

[0056] After drying in vacuo, 233.9 mg of a white powdery solid was obtained, with a yield of 98.3% and a melting point of 168.6 °C.

Embodiment 2

[0058] 1) Weigh 150 mg of acyclovir and 88 mg of glutaric acid;

[0059] 2) Add the mixture into the ball mill jar, and add 20 μL of ethanol dropwise;

[0060] 3) Grinding for 20 min at a frequency of 20 Hz;

[0061] After drying in vacuo, 234.2 mg of a white powdery solid was obtained with a yield of 98.4% and a melting point of 168.6 °C.

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Abstract

The invention discloses an acyclovir eutectic, a preparation method of the acyclovir eutectic, and a preparation. The x-ray powder diffraction of the acyclovir-glutaric acid eutectic has characteristic peaks in the diffraction angles 2 theta at 8.108, 10.890, 13.975, 14.421, 16.125, 16.611, 18.700, 20.468, 21.504, 21.887, 22.495, 23.208, 24.143, 25.015, 26.069, 27.410, 28.506, 29.135, 30.901, 32.524, 32.972, 34.126, 35.609, 36.049 and 37.153. According to the preparation, two ways, namely, a way of adding an organic solvent and grinding and a way of dissolving in the organic solvent, settling, filtering and drying, are respectively adopted, and therefore the higher-purity acyclovir-glutaric acid eutectic is successfully prepared. The preparation method has the advantages that few solvents are needed in the production process, the production cost is low, and less pollution is brought to the environment. Compared with the acyclovir, the acyclovir-glutaric acid eutectic disclosed by the invention has the advantages of being higher in permeability and stable in performance, and shows more advantages in the application of preparing a transdermal absorption preparation.

Description

technical field [0001] The invention relates to acyclovir co-crystal and its preparation method and application. Background technique [0002] Acyclovir (ACV), alias: acyclovir, acyclic guanine, chemical name 9-(2-hydroxyethoxymethyl) guanine, an acyclic analogue of 2'-deoxyguanosine , is a non-glycoside nucleotide antiviral drug, it is the second generation broad-spectrum antiviral drug, successfully developed by Glaxo Wellcome (G·W) company in the UK, it was the first in the world in 1981 The first open-ring nucleoside drug with specific anti-herpes virus on the market is a highly selective and low-toxic antiviral drug widely used at home and abroad. The drug can selectively in virus-infected cells Block herpes virus replication, and less toxic. [0003] US4199574 discloses the use of acyclovir in the treatment of viral infections. So far, acyclovir has been approved for use by more than 50 countries, and it is the antiviral drug with the largest sales volume in the wor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18C07C51/41C07C55/12A61K31/522A61P31/22
Inventor 鲁统部闫岩陈嘉媚
Owner SUN YAT SEN UNIV