Preparation method of toltrazuril-cyclodextrin inclusion compound

A technology of cyclodextrin inclusion compound and toltrazuril, which is applied in the direction of active ingredients of heterocyclic compounds, medical preparations of non-active ingredients, drug combinations, etc., can solve high cost, instability, difficulty in use, and transportation, etc. problem, to achieve the effect of low cost, easy control and high inclusion rate

Inactive Publication Date: 2009-09-02
WUHAN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The drinking water agent prepared by this method adopts organic solvents and solubilizers, which are expensive, difficult to use and transport, and unstable when placed for a long time

Method used

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  • Preparation method of toltrazuril-cyclodextrin inclusion compound

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Experimental program
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Effect test

Embodiment 1

[0023] Embodiment 1: Preparation of Toltrazuril-cyclodextrin inclusion compound

[0024] Weigh 0.9g of Toltrazuril, dissolve it in 50ml of NaOH aqueous solution with a concentration of 0.10mol / L, heat to 50°C and continue to stir, add 5.0g of β-cyclodextrin to dissolve, continue to stir for 2h; then slowly add Adjust the solution to pH 7.0 with 1mol / L HCl; place it overnight at 4°C, filter with suction, dry the white solid, crush and sieve to obtain the inclusion complex of Toltrazuril-cyclodextrin.

[0025] The Toltrazuril-cyclodextrin inclusion compound prepared in this embodiment and the physical mixture of Toltrazuril and cyclodextrin with a single Toltrazuril crude drug were carried out in water solubility experiment, and its solubility (inclusion in 100g aqueous solution The amount of solutes) are respectively: 0.6 mg of a single toltrazuril bulk drug, 15.4 mg of a physical mixture of toltrazuril and cyclodextrin, and 76.1 mg of the toltrazuril-cyclodextrin inclusion com...

Embodiment 2

[0026] Embodiment 2: Preparation of Toltrazuril-cyclodextrin inclusion compound

[0027] Weigh 0.9g of Toltrazuril, dissolve it in 50ml of NaOH aqueous solution with a concentration of 0.10mol / L, heat to 50°C and continue to stir, add 5.0g of hydroxypropyl-β-cyclodextrin to dissolve, and continue to stir for 2h; Then slowly add 1mol / L HCl dropwise to adjust the solution to pH 7.0; place it overnight at 4°C, filter with suction, dry the white solid, crush and sieve to obtain the Toltrazuril-cyclodextrin inclusion compound.

[0028] The Toltrazuril-cyclodextrin inclusion compound prepared in this embodiment and the physical mixture of Toltrazuril and cyclodextrin with a single Toltrazuril crude drug were carried out in water solubility experiment, and its solubility (inclusion in 100g aqueous solution The amount of solutes) are respectively: 0.6 mg of a single toltrazuril bulk drug, 15.4 mg of a physical mixture of toltrazuril and cyclodextrin, and 76.1 mg of the toltrazuril-cyc...

Embodiment 3

[0030] It is basically the same as Example 1, except that β-cyclodextrin is replaced by γ-cyclodextrin.

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Abstract

The invention relates to a preparation method of a toltrazuril-cyclodextrin inclusion compound. The method comprises the following steps: the toltrazuril is dissolved in the dilute alkaline solution and performs inclusion with cyclodextrin or the derivative thereof at the temperature of 20 to 80 DEG C, the entire system is neutralized with acid, the resultant is dried and crushed and then the toltrazuril-cyclodextrin inclusion compound is obtained. The invention does not utilize the organic solvent for dissolving and has the advantages of simple process, easy control, low cost and mass production; and the prepared inclusion compound has high security, good stability and good dissolvability and is convenient to use.

Description

technical field [0001] The invention relates to a preparation method of Toltrazuril-cyclodextrin inclusion compound. Background technique [0002] Toltrazuril is a synthetic anticoccidiostat. Chemical name: 1-[3-methyl-4(4-trifluoromethylthiophenazino)phenyl]-3-methyl-1,3,5-triazine-2,4,6[1H, 3H, 5H]-triazone, referred to as xyltriazone, the molecular formula is C 18 h 14 f 3 N 3 o 4 S, relative molecular mass is 425.4, CAS number: 69004-03-1. Its structural formula is: [0003] [0004] Toltrazuril is a white or off-white crystalline powder with a melting point of 194°C. It is insoluble in water but soluble in organic solvents such as polyethylene glycol and propylene glycol. Toltrazuril is a new type of synthetic anticoccidial agent. Its mechanism of action is to induce the expansion of the endoplasmic reticulum and Golgi apparatus in the coccidian cells during the normal development stage of the coccidian, so that the distribution of the space around the nucleu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/53A61P33/02A61K47/69
Inventor 刘永琼祝宏李俊杰李萤祁雯雯刘念
Owner WUHAN INSTITUTE OF TECHNOLOGY
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