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Levo-ulifloxacin injection and preparation method thereof

A technology for injections and water for injection, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, and drug delivery to achieve the effects of fast absorption, small poisoning effect, and reliable effect.

Inactive Publication Date: 2011-12-21
GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] So far, there is no bibliographical report levofloxacin injection and preparation method thereof

Method used

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  • Levo-ulifloxacin injection and preparation method thereof
  • Levo-ulifloxacin injection and preparation method thereof
  • Levo-ulifloxacin injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0052] The preparation of embodiment 1 (S)-(-)-ulifloxacin

[0053] Dissolve 105 g of racemic ulifloxacin in 1500 mL of dimethyl sulfoxide, add dropwise a solution of 27 g of D-tartaric acid dissolved in 405 mL of dimethyl sulfoxide under stirring, stir at room temperature for 20 hours, precipitate and filter, and obtain The solid was dried under vacuum to obtain 86 grams, and the solid was recrystallized in dimethyl sulfoxide to obtain 37 grams of levofloxacin-D-tartrate, which was analyzed by element C49.08%, H5.06%, N9. 50%, S7.44% (molecular composition: C 16 h 16 FN 3 o 3 S 1 / 2C 4 h 6 o 6 ·H 2 O, calculated value C48.86%, H4.78, N9.50%, S7.25%); add this salt into water to form a suspension, adjust the pH value to 7-8 with 2% NaOH aqueous solution under stirring, precipitate and filter Dry to obtain (S)-(-)-ulifloxacin 24.5 grams, its chemical name: (S)-(-)-6-fluoro-1-methyl-4-oxo-7-(1-piperazine Base)-1H, 4H-[1,3]thiazetidino[3,2-a]quinoline-3-carboxylic acid

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Embodiment 2

[0059] Example 2 Preparation of 0.1 mg / ml levofloxacin glucose infusion

[0060] Take 1 gram of levo-ulifloxacin, add it to a 20-liter batching bucket, add 7 L of water, add about 5.5 milliliters of 5% (W / W) lactic acid solution under stirring, stir until it dissolves, and measure the pH to 5.56, add 800 grams of glucose, Stir to dissolve, add activated carbon, heat up, keep warm and stir at about 50°C for 30 minutes, cool to 30°C, filter for decarburization, add water for injection to 10L, then filter through a 0.22μm filter membrane, fill and cap , sterilized at 110°C for 30 minutes.

[0061] The infusion solution prepared in this example can be filled into specifications of 25mg:250ml; 50mg:500ml.

Embodiment 3

[0062] Example 3 Preparation of 0.1mg / ml levofloxacin sodium chloride infusion

[0063] Take 1 gram of levofloxacin, add it to a 20-liter batching bucket, add 1000 ml of water, add about 5.5 ml of 5% (W / W) lactic acid solution under stirring, stir until it dissolves, add 90 grams of sodium chloride, and stir to dissolve. Add activated carbon, heat up to 50°C, heat and stir for 30 minutes, cool to 30°C, filter for decarburization, add water for injection to 10L, then filter through a 0.22μm filter membrane, fill, cap, and extinguish at 110°C Bacteria for 30 minutes.

[0064] The infusion solution prepared in this example can be filled into specifications of 25mg:250ml; 50mg:500ml.

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Abstract

Levo-ulifloxacin injection and preparation method thereof, relate to pharmaceutical preparations containing fluoroquinolone antibacterial drugs, in particular to injection of prulifloxacin active body Ulifloxacin (S-(-)-Ulifloxacin) and preparation thereof method. The present invention is based on (S)-(-)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H, 4H-[1,3]thiazetidine Alkane[3,2-a]quinoline-3-carboxylic acid (levofloxacin for short) is the active ingredient of the drug, and the rest are pharmaceutically acceptable additives for injections, which are liquid injections or solid injections Injections, wherein each injection or bottle contains 10-100 mg of active pharmaceutical ingredients. The commonly used dose in clinic may be 10-100 mg of levofloxacin, once or twice a day; 1-10 ml for intramuscular injection and 50-1000 ml for intravenous injection. The invention increases the route of administration, expands the range of application groups, and significantly reduces the cost and risk of medication for patients.

Description

technical field [0001] The invention relates to a pharmaceutical preparation containing fluoroquinolone antibacterial drugs, in particular to an injection of the levorotatory form of prulifloxacin active body Ulifloxacin (S-(-)-Ulifloxacin) and a preparation method thereof. Background technique [0002] Japanese patent JP63107990 discloses the quinolone compound Ulifloxacin, which has strong antibacterial activity against Gram-positive bacteria and negative bacteria in vitro, and its activity against Pseudomonas aeruginosa is significantly higher than that of similar products that have been listed. New high-efficiency, broad-spectrum fluoroquinolone antibacterials. However, Ulifloxacin is a water-insoluble and highly polar drug, with little oral absorption and low bioavailability, and its antibacterial activity in vivo is not ideal. Chinese Patent Application No. 88107689.9 discloses the prodrug prulifloxacin of ulifloxacin, which is used for hydrogen on the terminal nitrog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/496A61P31/04
Inventor 彭锋应军王玉平林丽薇倪庆纯杨威梁金强安穗伟冯颂延陈洁斌
Owner GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTITUTE
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