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Ceftiofur hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof

A technology of cyclodextrin inclusion complex and thifuryl hydroxypropyl is applied in the directions of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Solubility, improving bioavailability, increasing water solubility

Active Publication Date: 2014-04-30
河南华牧生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, it is used to improve the stability and bioavailability of hydrophobic drugs. There are some reports on the inclusion action in the solution, but the preparation and properties of the cyclodextrin ceftiofur solid inclusion compound have not been reported.
Ceftiofur is very slightly soluble in water, limiting its scope of application

Method used

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  • Ceftiofur hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof
  • Ceftiofur hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof
  • Ceftiofur hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof

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Embodiment Construction

[0021] The preferred embodiments of the present invention will be described below in conjunction with the accompanying drawings. It should be understood that the preferred embodiments described here are only used to illustrate and explain the present invention, and are not intended to limit the present invention.

[0022] 1. Study on Phase Solubility Method

[0023] In the low concentration system, the dilution effect makes the effect of hydroxypropyl-β-cyclodextrin (HP-β-CD) on the UV absorption of ceftiofur negligible. The obtained standard curve is Y=0.0279X+0.0118 (R 2 =0.9997) ( figure 1 ).

[0024] According to the results of the standard curve, when the concentration of HP-β-CD is 0, the intrinsic solubility of ceftiofur is equal to 4.70×10 -7 mol / L.

[0025] 2. Optimization of inclusion conditions

[0026] 1. The influence of different proportions of raw materials on inclusion

[0027] When ceftiofur and hydroxypropyl-β-cyclodextrin (HP-β-CD) were mixed at a temp...

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Abstract

The invention discloses a preparation method of a solid inclusion compound of ceftiofur and hydroxypropyl-beta-cyclodextrin (CD). The preparation method comprises the following steps of taking ceftiofur and hydroxypropyl-beta-cyclodextrin in a molar ratio of 1: (1 to 3) as reaction raw materials; adding water which is 5 times the total weight of the reaction raw materials under a temperature of 20 to 50 DEG C; grinding for 2 to 5 hours; drying for 12 hours under vacuum; and filtering to obtain white powder which is the inclusion compound. The prepared inclusion compound has the effects of effectively preventing a chemical compound from oxidation reaction or hydrolysis reaction and other reactions, improving the water solubility of a medicine, enhancing the stability, reducing the toxic and side effects, controlling the medicine release, and improving the bioavailability. The prepared hydroxypropyl-beta-CD inclusion compound improves the solubility and bioavailability of ceftiofur serving as a raw medicine. The prepared inclusion compound shows remarkable capacity of improving oxidation resistance of the raw medicines under light, high temperature, humidity and other conditions, and brings effective means for developing a novel form of ceftiofur.

Description

technical field [0001] The invention relates to an inclusion compound of ceftiofur. Background technique [0002] Ceftiofur is a third-generation cephalosporin developed in the 1980s mainly for veterinary use. Its mechanism of action is to act on bacterial transpeptidase to block the synthesis of cell wall, presenting a bactericidal effect, and is used to treat and control bacterial intestinal and respiratory infections in livestock. Due to the poor water solubility of ceftiofur and the existing ceftiofur preparations have many problems, the development of new ceftiofur preparations has always been a focus of researchers. With the development of related science and technology fields, the research on antimicrobial dosage forms is developing in the direction of high efficiency, targeting, and intelligence. The ideal dosage form should have the advantages of small dose, low toxicity, and small side effects. Drug delivery systems represented by controlled release and targeting...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K47/48A61P31/04A61K47/69
Inventor 梁剑平陶蕾赵凤舞王学红尚若锋贾忠郝宝成
Owner 河南华牧生物科技有限公司
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