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Tosufloxacin tosylate sublingual spray for children and preparation method thereof

A technology of tosufloxacin toluenesulfonate and spray, which is applied in the field of sublingual spray of tosufloxacin toluenesulfonate for children and its preparation, which can solve the problems of induced joint toxicity and achieve strong compliance and remarkable effect , enhance the effect of adaptability

Active Publication Date: 2017-11-24
CP PHARMA QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, the main factor affecting the use of tosufloxacin and other fluoroquinolone antibacterial drugs in children is that these drugs can induce joint toxicity to young animals. my country has not officially approved the use of fluoroquinolones in children, but there are already off-label drugs in China. Use of Fluoroquinolones in the Treatment of Pediatric Infections

Method used

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  • Tosufloxacin tosylate sublingual spray for children and preparation method thereof
  • Tosufloxacin tosylate sublingual spray for children and preparation method thereof
  • Tosufloxacin tosylate sublingual spray for children and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Cyclodextrin inclusion solubilization tosufloxacin tosylate screening test

[0025] Separately prepare α-cyclodextrin, β-cyclodextrin, HP-β-cyclodextrin, DM-β-cyclodextrin and glucosyl-β-cyclodextrin aqueous solutions with the same concentration, and heat and stir at 55°C Add excess tosufloxacin tosylate, heat and stir for 48 hours, filter through a 0.45 μm microporous membrane, take the filtrate, and measure the content of tosufloxacin tosylate. The results are shown in Table 1.

[0026] Table 1 Solubilization of Tosufloxacin Tosylate by Different Cyclodextrins

[0027]

[0028] The results show that the inclusion of tosufloxacin tosylate with glucosyl-β-cyclodextrin can greatly improve its solubility.

Embodiment 2

[0029] Example 2 Preparation of Tosufloxacin Tosylate-Glucosyl-β-cyclodextrin Inclusion Compound 1

[0030] Take an appropriate amount of tosufloxacin tosylate, add an appropriate amount of glacial acetic acid to dissolve it, weigh the glucosyl-β-cyclodextrin inclusion compound according to the ratio of 1:3 tosufloxacin tosylate-β-cyclodextrin For β-cyclodextrin, add an appropriate amount of distilled water to dissolve it completely. Under the condition of heating and stirring in a water bath at 50°C, slowly add the tosufloxacin tosylate solution into the glucosyl-β-cyclodextrin aqueous solution, dropwise After completion, stir under the same conditions for an appropriate time to dissolve completely, evaporate the solvent to dryness by rotary evaporation, and dry the obtained solid under reduced pressure and vacuum to obtain the final product.

Embodiment 3

[0031] Example 3 Preparation of Tosufloxacin Tosylate-Glucosyl-β-cyclodextrin Inclusion Compound 2

[0032] Take an appropriate amount of tosufloxacin tosylate, add an appropriate amount of glacial acetic acid to dissolve it, and weigh the glucosyl-β-cyclodextrin inclusion compound according to the ratio of 1:4 tosufloxacin tosylate-β-cyclodextrin inclusion complex. For β-cyclodextrin, add an appropriate amount of distilled water to dissolve it completely. Under the condition of heating and stirring in a water bath at 55°C, slowly add the tosufloxacin tosylate solution into the glucosyl-β-cyclodextrin aqueous solution, dropwise After completion, stir under the same conditions for an appropriate time to dissolve completely, evaporate the solvent to dryness by rotary evaporation, and dry the obtained solid under reduced pressure and vacuum to obtain the final product.

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PUM

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Abstract

The invention relates to tosufloxacin tosylate sublingual spray for children and a preparation method thereof and belongs to the field of pharmaceutical preparation. The tosufloxacin tosylate sublingual spray preferably comprises 100 parts of glucosyl-beta-cyclodextrin inclusion of tosufloxacin tosylate, 0.3 parts of cherry essence, 0.03 parts of acetone chloroform, an appropriate amount of a pH adjusting agent and 100 parts of distilled water. The glucosyl-beta-cyclodextrin is used as an inclusion material so that an unexpected effect of solubilizing tosufloxacin tosylate is obtained and the tosufloxacin tosylate can be used in a form of sublingual spray. The sublingual spray is seasoned through cherry essence so that the sublingual spray has a slight cherry fragrance. The tosufloxacin tosylate sublingual spray has a small dosage, strong compliance to use of children, stable quality and significant effects.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a sublingual spray of tosufloxacin tosylate for children and a preparation method thereof. Background technique [0002] Tosufloxacin tosilate (tosufloxacin tosilate), common name is tofloxacin, 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, CA registration number is 100490-36-6, molecular formula is C 26 h 23 f 3 N 4 o 6 S·H 2 O, the molecular weight is 594.57, the structure is as follows: [0003] [0004] Tosufloxacin tosylate belongs to the fourth generation of quinolone antibacterial drugs, which has obvious advantages over other drugs. First, it expands the antibacterial spectrum and increases the activity. Tosufloxacin tosylate has a better effect on G-bacteria than ofloxacin, norfloxacin, and is almost equivalent to ciprofloxacin. The effect ...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K47/69A61K47/46A61K31/4375A61P31/04
CPCA61K9/006A61K9/12A61K31/4375A61K47/46
Inventor 王明刚陈阳生刘晓霞孙桂玉臧云龙
Owner CP PHARMA QINGDAO CO LTD
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