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Adefovir pharmaceutical co-crystal and preparation method thereof

A drug and a combined technology, applied in the field of new adefovir drug co-crystal and the preparation of the drug co-crystal, to achieve the effect of improving stability and bioavailability

Active Publication Date: 2011-08-17
JILIN UNIV
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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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  • Adefovir pharmaceutical co-crystal and preparation method thereof
  • Adefovir pharmaceutical co-crystal and preparation method thereof
  • Adefovir pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Synthesis of co-crystals using adefovir and 2,6-pyridinedicarboxylic acid:

[0026] Weighing:

[0027] The reactant is fed according to the mass ratio of adefovir:2,6-pyridinedicarboxylic acid=3:2. Accurately weigh 30.0 mg of adefovir and 20.0 mg of 2,6-pyridinedicarboxylic acid in a round bottom flask with an analytical balance;

[0028] Dissolution of API:

[0029] Accurately measure 2ml of CH with a 5ml pipette 3 CH 2 OH and 2ml H 2 O in a round-bottomed flask, then put a 1cm magnetic stirrer, set up a reflux device, raise the temperature of the reaction system to 90°C, stir and reflux for 3h.

[0030] Reflux-solvent room temperature volatilization heat method:

[0031] After refluxing for 3 hours, take out the stirring bar, filter, and place the filtrate in a transparent glass vial at room temperature. Afterwards, the solvent is slowly volatilized at room temperature, and transparent flaky crystals are formed after 30 hours, which is the adefovir drug eutecti...

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystals, and particularly relates to a novel Adefovir pharmaceutical co-crystal and a preparation method thereof. An Adefovir molecule and a 2,6-dipicolinic acid molecule are bonded by a hydrogen bond to form a basic structural unit of the Adefovir pharmaceutical co-crystal. The space group of the Adefovir pharmaceutical co-crystal is a triclinic system, and the Adefovir pharmaceutical co-crystal has the following cell parameters: axial lengths: a=7.03-7.53, b=11.85-12.38, and c=11.99-12.49; and axial angles: alpha=76.35-76.85, beta=76.50-77.00, and gamma=77.16-77.66. The XRD (X-ray diffraction) spectrum characteristic peak appears at 12.00-12.50 degrees, 13.17-13.67 degrees, 13.98-14.48 degrees, 15.96-16.46 degrees, 17.72-18.22 degrees, 23.58-24.08 degrees and 25.46-25.96 degrees. The pharmaceutical co-crystal provided by the invention not only has the characteristics of the traditional active pharmaceutical ingredient in treating hepatitis b, but also obviously improves the solubility, stability and bioavailability.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a novel adefovir drug co-crystal and a preparation method of the drug co-crystal. 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 scien...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561C07D213/79C07D213/803
Inventor 张婷朱广山
Owner JILIN UNIV
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