Tosufloxacin tosylate dispersible tablets and preparation method thereof

A technology of tosufloxacin tosylate and dispersible tablets, which is applied in the field of medicine, can solve the problems of low bioavailability, poor capsule stability, and poor antibacterial effect, and achieve good antibacterial effect, stable properties, and good disintegration effect Effect

Active Publication Date: 2016-12-07
ZHUHAI TONGYUAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Kohno investigated and organized the clinical application of tosufloxacin tosylate. The investigation mainly focused on the antibacterial ability of respiratory tract infection. Some bacteria showed resistance to cephalosporins, carbapenems and other antibacterial drugs , tosufloxacin tosylate will receive more attention in the future application. Tosufloxacin tosylate is a poorly soluble drug, which has poor water solubility when prepared into ordinary tablets, slow drug effect and low bioavailability and other shortcomings, which limit its application
[0005] Chinese patent CN104546735A discloses a kind of tosufloxacin toluenesulfonate granules for children. Among them, sucrose is diluent and sweetener, aspartame is sweetener, hydroxypropyl cellulose SSL is binder, fresh orange powder essence is flavoring agent, silicon dioxide is glidant, carmine Tosufloxacin Tosulacin Tosylate Granules for Children prepared by the present invention uses carmine instead of iron oxide as a coloring agent to solve the problems of color dullness, hue and corrosiveness. The powder essence is used as a flavoring agent, and the mouthfeel and taste of the prepared granules are all good, but the capsules of the present invention have poor stability, poor dissolution rate, long disintegration time, and poor antibacterial effect

Method used

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  • Tosufloxacin tosylate dispersible tablets and preparation method thereof
  • Tosufloxacin tosylate dispersible tablets and preparation method thereof
  • Tosufloxacin tosylate dispersible tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) At a temperature of 40°C, dissolve the crude product of tosufloxacin tosylate in a mixed solution of ethanol and water with a volume fraction of 95%, mix and stir to dissolve evenly, wherein the volume ratio of ethanol to water is 1 : 1, the mass volume ratio of tosufloxacin tosylate and ethanol and water mixed solution is 1g: 10ml.

[0040] (2) adding an appropriate amount of mass fraction to the above solution is 0.2% activated carbon, and then filters;

[0041] (3) The filtered solution is cooled to 30°C, left to stand for 15 hours, and crystallized;

[0042] (4) After the crystals are completely precipitated, they are washed and dried at 50° C. to obtain the tosufloxacin tosylate crystals.

[0043] The X-ray powder diffraction spectrum that the tosufloxacin tosylate crystal that obtains uses Cu-Kα ray measurement to obtain is as follows figure 1 Shown, the X-ray powder diffraction of tosufloxacin tosylate crystal is 10.13°, 10.61°, 13.21°, 15.42°, 15.81°, 18.4...

Embodiment 2

[0045] (1) At a temperature of 45°C, dissolve the crude product of tosufloxacin tosylate in a mixed solution of ethanol and water with a volume fraction of 95%, mix and stir to dissolve evenly, wherein the volume ratio of ethanol to water is 10 : 1, the mass volume ratio of tosufloxacin tosylate and ethanol and water mixed solution is 1g: 5ml.

[0046] (2) adding an appropriate amount of mass fraction to the above solution is 0.1% activated carbon, and then filters;

[0047] (3) The filtered solution is cooled to 28°C, left to stand for 10 hours, and crystallized;

[0048] (4) After the crystals are completely precipitated, they are washed and dried at 40° C. to obtain the tosufloxacin tosylate crystals.

[0049]The X-ray powder diffraction spectrum obtained by measuring the obtained tosufloxacin tosylate crystals using Cu-Kα rays is basically consistent with that of Example 1.

Embodiment 3

[0051] (1) At a temperature of 80°C, dissolve the crude product of tosufloxacin toluenesulfonate in a mixed solution of ethanol and water with a volume fraction of 95%, mix and stir to dissolve evenly, wherein the volume ratio of ethanol to water is 5 : 1, the mass volume ratio of tosufloxacin tosylate and ethanol and water mixed solution is 1g: 3ml.

[0052] (2) adding an appropriate amount of mass fraction to the above solution is 0.3% activated carbon, and then filters;

[0053] (3) The filtered solution is cooled to 32°C, left to stand for 20 hours, and crystallized;

[0054] (4) After the crystals are completely precipitated, they are washed and dried at 60° C. to obtain the tosufloxacin tosylate crystals.

[0055] The X-ray powder diffraction spectrum obtained by measuring the obtained tosufloxacin tosylate crystals using Cu-Kα rays is basically consistent with that of Example 1.

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Abstract

The invention discloses tosufloxacin tosylate dispersible tablets. The tosufloxacin tosylate dispersible tablets are prepared from, by weight, 20-45 parts of tosufloxacin tosylate, 35-44 parts of microcrystalline cellulose, 7-20 parts of gelatinized starch, 2-10 parts of mannitol, 1-5 parts of silica, 0.8-1.2 parts of povidone K30, 1-4 parts of sodium carboxymethyl starch, 1-4 parts of aspartame, 0.8-1.2 parts of magnesium stearate and 0.8-1.2 parts of strawberry essence. The tosufloxacin tosylate dispersible tablets are shorter in disintegration time, high in dissolution, good in stability and good in antibacterial effect. The invention further discloses tosufloxacin tosylate dispersible tablets prepared by utilizing prepared tosufloxacin tosylate crystals. The tosufloxacin tosylate dispersible tablets has better stability and contains less impurities after long-term storage.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a tosufloxacin tosylate dispersible tablet and a preparation method thereof. Background technique [0002] Tosufloxacin tosylate, its chemical name is: 7-[3-amino-1-(pyrrolidinyl)]-1-(2,4-difluorophenyl)-6-fluoro-1,4- Dihydro-4-oxo-1,8-naidine-3-carboxylic acid p-toluenesulfonate monohydrate, molecular formula C 26 h 23 f 3 N 4 o 6 S·H 2 O, with a molecular weight of 594.57, is a broad-spectrum quinolone antibacterial drug. It is a white to light yellow powder, odorless, slightly bitter, hygroscopic, and becomes darker when exposed to light. It is slightly soluble in sodium hydroxide test solution. Almost insoluble in water or chloroform, easily soluble in dimethylformamide or glacial acetic acid. [0003] Tosufloxacin tosylate, as a quinolone antibacterial drug, was developed by Japan Toyama Chemical Industry Co., Ltd., and was first listed in Japan in 1990....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4375C07D471/04A61K47/36A61K47/38A61K47/26A61P31/04
CPCA61K9/2018A61K9/2054A61K9/2059A61K31/4375C07B2200/13C07D471/04
Inventor 陈敏李旭丰刘伟袁剑魏光琍
Owner ZHUHAI TONGYUAN PHARMA CO LTD
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