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Inclusion compound of aureomycin zinc complex and preparation method thereof

A technology of chlortetracycline zinc and complexes, which is applied in the field of drug preparation, can solve the problems of poor solubility and low dissolution rate of chlortetracycline zinc complexes, and achieve the goals of improving drug bioavailability, reducing dosage and increasing stability Effect

Active Publication Date: 2017-06-16
CHONGQING ACAD OF ANIMAL SCI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved in the present invention is that the chlortetracycline zinc complex has poor solubility in water and a small dissolution rate.

Method used

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  • Inclusion compound of aureomycin zinc complex and preparation method thereof
  • Inclusion compound of aureomycin zinc complex and preparation method thereof
  • Inclusion compound of aureomycin zinc complex and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1 Preparation of clathrate of the present invention

[0025] Weigh 10 grams of chlortetracycline zinc complex, add 48 ml of methanol, 48 ml of dimethyl sulfoxide, 2 ml of N,N-dimethylformamide, and 2 ml of tetrahydrofuran into a mixed organic solvent, and dissolve it completely , kept at 55°C, dripped a saturated aqueous solution containing 14 grams of hydroxypropyl-β-cyclodextrin, stirred at 55°C for 2 hours, stopped heating, and continued to stir to room temperature to obtain a yellow solution, which was filtered and spray-dried to obtain gold Inclusion complexes of mycin zinc complexes.

Embodiment 2

[0026] Embodiment 2 Preparation of clathrate of the present invention

[0027] Weigh 10 grams of chlortetracycline zinc complex, add 48 ml of methanol, 48 ml of dimethyl sulfoxide, 2 ml of N,N-dimethylformamide, and 2 ml of tetrahydrofuran into a mixed organic solvent, and dissolve it completely , kept at 60°C, dripped a saturated aqueous solution containing 28 grams of hydroxypropyl-β-cyclodextrin, continued to stir for 30 minutes, stopped heating, and continued to stir to room temperature to obtain a yellow solution, which was filtered and freeze-dried, which was Golden Mold Inclusion complexes of zinc complexes.

Embodiment 3

[0028] Embodiment 3 Preparation of clathrate of the present invention

[0029] Weigh 10 grams of chlortetracycline zinc complex, add 48 ml of methanol, 48 ml of dimethyl sulfoxide, 2 ml of N,N-dimethylformamide, and 2 ml of tetrahydrofuran into a mixed organic solvent, and dissolve it completely , kept at 60°C, dripped a saturated aqueous solution containing 28 grams of hydroxypropyl-β-cyclodextrin, ultrasonicated at 65°C for 30 minutes, filtered through a 0.45 μm membrane, and the resulting solution was spray-dried to obtain aureomycin Inclusion complexes of zinc complexes.

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Abstract

The invention belongs to the technical field of drug preparation, particularly relates to a clathrate compound of an aureomycin zinc complex, and a preparation method thereof, and aims to solve the technical problem that the aureomycin zinc complex is poor in solubility and small in dissolution rate. Through the technical scheme, the clathrate compound of the aureomycin zinc complex comprises a clathrate material and the aureomycin zinc complex according to a weight ratio of (1-3): 1, and the clathrate material is cyclodextrin or a cyclodextrin derivative. The invention further provides an oral preparation prepared from the clathrate compound. The invention further provides a preparation method for the clathrate compound of the aureomycin zinc complex. The aureomycin zinc complex in the clathrate compound is good in solubility in water and high in dissolution rate, and has the advantages of good water solubility, high stability, good curative effect, little side effect and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to an inclusion compound of a chlortetracycline zinc complex and a preparation method thereof. Background technique [0002] Tetracyclines (Tetracyclines) are named after the chemical structure of tetracene mother nucleus, and aureomycin (Chlortetracycline, structure see figure 1 ), also known as chlorotetracycline, is a kind of tetracycline derivative, which mainly inhibits the protein synthesis of sensitive microorganisms. Chlortetracycline has a broad antibacterial spectrum, and can inhibit Gram-positive bacteria, negative bacteria, spirochetes, rickettsia, mycoplasma, chlamydia, and some protozoa. Chlortetracycline mainly binds to the A site of the 30S small subunit of microorganisms, and then interferes with the combination of aminophthalein tRNA and the 30S small subunit, so that aminophthalein tRNA cannot enter the receptor on the mRNA, and inhibits ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/65A61P31/04
Inventor 伍涛杨旭李书至王建华
Owner CHONGQING ACAD OF ANIMAL SCI
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