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Tosufloxacin tosylate sublingual spray for children and preparation method thereof

A technology of tosufloxacin tosufloxacin tosufloxacin and spray, applied in the field of tosufloxacin tosufloxacin tosylate sublingual spray for children and its preparation, can solve problems such as inducing joint toxicity, and achieve strong compliance and stable quality , the effect of low dose

Active Publication Date: 2021-02-26
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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Abstract

The invention relates to a sublingual spray of tosufloxacin tosylate for children and a preparation method thereof, belonging to the field of pharmaceutical preparations. The sublingual spray of the present invention preferably comprises 100 parts of tosufloxacin tosufloxacin glucosyl-β-cyclodextrin inclusion compound, 0.3 part of cherry essence, 0.03 part of chlorobutanol, an appropriate amount of pH regulator, distilled water 100 parts, the present invention adopts glucosyl-β-cyclodextrin as clathrate material, has obtained the unexpected effect of solubilizing tosufloxacin tosylate, so that it can be used in the form of sublingual spray, The dosage form is flavored with cherry essence, so that the spray has a faint cherry fragrance, and the dosage is small, and the children have strong compliance, stable quality and remarkable effect.

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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Patent Type & Authority Patents(China)
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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