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Actarit cyclodextrin, clathrate compound of cyclodextrin derivant and preparation thereof

A technology of actarid and cyclodextrin, which is applied in the field of inclusion complexes of actarid cyclodextrin and cyclodextrin derivatives and their preparation, and achieves increased solubility, improved bioavailability, and improved stability Effect

Inactive Publication Date: 2008-08-20
TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, by preparing the clathrate of actarit with cyclodextrin and its derivatives to improve the solubility of actarit in water, increase drug stability, reduce toxic and side effects, improve patient compliance, and then improve the biological The method of utilization has not been reported

Method used

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  • Actarit cyclodextrin, clathrate compound of cyclodextrin derivant and preparation thereof
  • Actarit cyclodextrin, clathrate compound of cyclodextrin derivant and preparation thereof
  • Actarit cyclodextrin, clathrate compound of cyclodextrin derivant and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Weigh 8g of β-cyclodextrin, add a certain amount of water to make it saturated, heat to dissolve, cool to 40°C, weigh 1.36g of actarit, dissolve it with 80% ethanol, and slowly add it dropwise to the β-cyclodextrin In the fine solution, stir at a constant temperature of 40°C for 3 hours, refrigerate overnight in the refrigerator, filter with suction, and wash with appropriate amount of water and ethanol respectively to remove unincluded β-dextrin and actarit, collect the precipitate, and dry it in vacuum Grind it finely and pass through an 80-mesh sieve to obtain the inclusion complex of actarit β-cyclodextrin.

Embodiment 2

[0035]Weigh 4g of β-cyclodextrin and dissolve in 250ml of water, heat to dissolve, cool to 50°C, weigh 0.68g of actarit and dissolve in 80% ethanol, slowly add dropwise to the β-dextrin solution, and stir at 50°C After 4 hours, freeze-dry in a vacuum, grind into fine powder, and sieve to obtain the inclusion complex of actarit β-cyclodextrin.

Embodiment 3

[0037] Others are the same as in Example 2, except adding actarit solution dropwise to the β-dextrin solution instead of adding actarit powder, stirring, drying and finely grinding to obtain the inclusion complex of actarit β-cyclodextrin.

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Abstract

The invention relates to actarit cyclodextrin and the inclusion compound of cyclodextrin derivative and the preparation method, which comprises the following compositions: actarit, cyclodextrin and the derivative with mass ratio of 1:40 to 2:1. The preparation method can adopt solvent method, ultrasonic method or grinding method. The cyclodextrin and the cyclodextrin derivative can be used as inclusion compound produced from inclusion material, which can improve actarit solubility and increase stability and furthermore improve bioavailability. The inclusion compound can be used for producing various preparations such as tablets, capsules, slow-release formulation and injection. The actarit cyclodextrin and the inclusion compound of cyclodextrin derivative have the advantages of simple process, convenient operation, short cycle and low energy consumption. The actarit cyclodextrin and inclusion compound of cyclodextrin derivative can be used for industrial production.

Description

technical field [0001] The invention relates to an inclusion technology of actarit, in particular to an inclusion compound of actarit cyclodextrin and cyclodextrin derivatives and a preparation method thereof. Background technique [0002] Rheumatoid arthritis (rheumatoid arthritis, RA) is a chronic inflammatory disease, mainly involving the movement of the joints, and often invades many other organs, is a common rheumatic disease, the greater the harm to the human body. Clinically, non-steroidal anti-inflammatory drugs, adrenocortical hormones and other drugs are mainly used for treatment, but there is no drug with definite curative effect at present. Therefore, the development of anti-rheumatoid arthritis drugs with good curative effect and small side effects has always been a hot spot of people's attention. [0003] The chemical name of Actarit (Acta) is p-acetamidophenylacetic acid, which is a new type of anti-rheumatic drug developed by Mitsubishi Chemical Corporation o...

Claims

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Application Information

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IPC IPC(8): A61K31/196A61K47/40A61P29/00A61P19/02A61P19/04
Inventor 戴玉杰张雯雯
Owner TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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