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Sarafloxacin hydrochloride clathrate and preparation method thereof

A technology of sarafloxacin hydrochloride and inclusion compound, which is applied in the field of medicine, can solve the problems of no sarafloxacin hydrochloride inclusion compound, etc., and achieve the effect of easy operation and simple preparation method

Inactive Publication Date: 2015-04-29
SHANDONG LONGHAI BIOLOGICAL TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research report on the inclusion compound of sarafloxacin hydrochloride and its preparation method at home and abroad

Method used

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  • Sarafloxacin hydrochloride clathrate and preparation method thereof
  • Sarafloxacin hydrochloride clathrate and preparation method thereof
  • Sarafloxacin hydrochloride clathrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh 6.4g of sarafloxacin hydrochloride, dissolve it in 100ml of 0.02M sodium hydroxide solution, ultrasonicate for 15min in a 60°C water bath at 40KHz, and weigh CH 3 -Add 20.0g of β-CD into sarafloxacin hydrochloride solution, heat and stir at 35°C for 3 hours, add 6.4g of polyvinylpyrrolidone into CH 3 - in β-CD sarafloxacin hydrochloride solution, grind mechanically for 30min, filter with suction, place in a freeze dryer at -30°C, and freeze-dry for 24h to obtain sarafloxacin hydrochloride CH 3 -β-CD clathrate.

[0030] The solubility of sarafloxacin hydrochloride is 0.074mg / mL, and the sarafloxacin hydrochloride CH prepared in Example 1 3 The solubility of -β-CD inclusion complex was 1.71mg / mL, the solubility increased by 23.1 times, the drug loading was 18.1%, and the inclusion rate was 85.9%.

Embodiment 2

[0032] Weigh 5.1g of sarafloxacin hydrochloride, dissolve it in 100ml of 0.03M sodium hydroxide solution, and ultrasonicate for 30min in a 50°C water bath at 38Hz; add 20.0g of HP-β-CD into the sarafloxacin hydrochloride solution, heat Stir, the temperature is 35°C, the time is 2 hours, add polyethylene glycol 6000 25.5g into the HP-β-CD sarafloxacin hydrochloride solution, mechanically grind for 20min, filter with suction, put it in a freeze dryer at -35°C, freeze After drying for 20 hours, the inclusion complex of sarafloxacin hydrochloride HP-β-CD is obtained.

[0033] The solubility of sarafloxacin hydrochloride is 0.074mg / mL, the solubility of the sarafloxacin hydrochloride HP-β-CD inclusion compound prepared in Example 2 is 1.79mg / mL, the solubility is increased by 24.2 times, and the drug loading is 9.7% , The inclusion rate is 92.1%.

Embodiment 3

[0035] Weigh 5.0g of sarafloxacin hydrochloride, dissolve it in 100ml of 0.04M sodium hydroxide solution, and ultrasonicate for 25min in a 42KHz water bath at 40°C; add 10.0g of HP-β-CD into the sarafloxacin hydrochloride solution, heat Stir, the temperature is 30°C, the time is 3 hours, add 15g of hydroxypropylmethylcellulose into the HP-β-CD sarafloxacin hydrochloride solution, mechanically grind for 20min, filter with suction, put in a freeze dryer at -40°C, Freeze-dry for 16 hours to obtain sarafloxacin hydrochloride HP-β-CD inclusion compound.

[0036] The solubility of sarafloxacin hydrochloride is 0.074mg / mL, the solubility of the sarafloxacin hydrochloride HP-β-CD inclusion complex prepared in Example 3 is 1.63mg / mL, the solubility has increased by 22.0 times, and the drug loading is 15.3% , The inclusion rate is 88.6%.

[0037] figure 1 The X-ray diffraction pattern of sarafloxacin hydrochloride shows that sarafloxacin hydrochloride has multiple specific crystal dif...

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Abstract

The invention belongs to a medical field, more specifically a sarafloxacin hydrochloride clathrate and a preparation method thereof. The sarafloxacin hydrochloride clathrate is prepared by the following raw materials by weight: 1 part of sarafloxacin hydrochloride, 2-5 parts of CH-beta-CD or HP-beta-CD and 1-5 parts of polymer drug accessory; wherein the polymer drug accessory is one selected from polyvinylpyrrolidone, polyethylene glycol 6000 or hydroxypropyl methyl cellulose. The sarafloxacin hydrochloride clathrate is prepared by the following steps of: weighting sarafloxacin hydrochloride, adding it into a sodium hydroxide solution, adding CH-beta-CD or HP-beta-CD into a sarafloxacin hydrochloride solution, heating, stirring, adding the polymer drug accessory, mechanically grinding, vacuum-filtrating, and then freezing and drying to obtain the product. The sarafloxacin hydrochloride clathrate increases solubility of sarafloxacin hydrochloride, raises drug loading and yield of sarafloxacin hydrochloride, and enhances chemical stability.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a sarafloxacin hydrochloride inclusion compound and a preparation method thereof. Background technique [0002] Sarafloxacin hydrochloride is a third-generation fluoroquinolone antibacterial drug specially used for animals. It has a broad antibacterial spectrum and strong antibacterial activity. It has good antibacterial activity against Gram-negative bacteria, Gram-positive bacteria and mycoplasma. Antibacterial effect, especially Escherichia coli, Salmonella, Klebsiella, Proteus, Pasteurella multocida, Campylobacter and other enterobacteria. Sarafloxacin hydrochloride absorbs quickly, metabolizes quickly, has almost no residue, and has no cross-resistance with many antibacterial drugs. It is mainly used for the treatment of digestive system, respiratory system, urinary tract infection and mycoplasma caused by sensitive bacteria. However, because sarafloxacin hydrochloride i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K47/40A61K47/34A61K47/32A61P31/04A61K47/10
CPCY02A50/30
Inventor 龙君江李振高振珅
Owner SHANDONG LONGHAI BIOLOGICAL TECH
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