Amino acid (-) ofloxacin water soluble salt

A technology of ofloxacin and water-soluble salts, applied in the field of medicine, can solve the problems of low solubility of levofloxacin and difficult to meet clinical needs, etc., increase dissolution rate and bioavailability, and the preparation process is simple and easy, The effect of improving solubility

Inactive Publication Date: 2006-06-14
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The solubility of levofloxacin in water is very small, which is difficult to meet the clinical needs. At present, its inorganic acids such as hydrochloride and organic acid salts such as lactate and methanesulfonate are mainly used.

Method used

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  • Amino acid (-) ofloxacin water soluble salt
  • Amino acid (-) ofloxacin water soluble salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Preparation of levofloxacin aspartate:

[0016] Raw material: (-)ofloxacin hemihydrate 370g

[0017] (-) aspartic acid 133g

[0018] Pure water 2L

[0019] 95% ethanol 10L

[0020] Preparation:

[0021] (-) ofloxacin hemihydrate (370 g) and (-) aspartic acid (133 g) were added into water together to obtain a clear solution with a measured pH of 5.0-7.0. This solution is injected in the container that 95% ethanol (10 liters) is housed, separates out off-white crystalline substance, dries to obtain light yellow crystalline powder and is (-) ofloxacin (-) aspartate, product yield About 70%.

[0022] Confirmation and analysis of (-) ofloxacin (-) aspartate:

[0023] 1. Solubility comparison:

[0024] (-) ofloxacin (-) aspartate is very soluble in water (1 g (-) ofloxacin aspartate can be dissolved in more than 0.5 ml and less than 1 ml of pure water); And its raw materials (-) ofloxacin and (-) aspartic acid are respectively slightly soluble in wat...

Embodiment 2

[0028] (-) Preparation of Ofloxacin (-) Glutamate:

[0029] Raw material: (-)ofloxacin hemihydrate 370g

[0030] (-) glutamic acid 147g

[0031] Pure water 2L

[0032] 95% ethanol 10L

[0033] Preparation:

[0034] (-) ofloxacin hemihydrate (370 g) and (-) glutamic acid (133 g) were added to water together to obtain a clear solution with a measured pH of 5.0-7.0. This solution is injected in the container that 95% ethanol (10 liters) is housed, separates out off-white crystalline substance, dries to obtain light yellow crystalline powder and is (-) ofloxacin (-) glutamic acid salt, and product yield is about 70%.

Embodiment 3

[0036] prescription for tablets

[0037] (-) Ofloxacin (-) Aspartate 140g

[0038] Microcrystalline Cellulose 30g

[0039] Starch 60g

[0040] HPMC 10g

[0041] Magnesium Stearate 5g

[0042] Makes 1000 pieces

[0043] Preparation method: mix the (-) ofloxacin (-) aspartate of the prescription amount with microcrystalline cellulose and 1 / 2 of the recipe amount of starch, add 1% HPMC solution to make a soft material, and use a 16-mesh sieve Granulate, dry at 70°C for 6 hours, add the remaining starch and magnesium stearate, mix well, and press into tablets to obtain the product.

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Abstract

A water-soluble salt of amino acid (-) ofloxacin with high solubility and antibacterial effect has a molecular formula C18H20FN3O4 A*nH2O is prepared from the semi-hydrated (-) of loxacin (C18H20FN3O4 / 2H2O) and aspartic acid or glutamic acid through dissolving in water, adding it to alcohol, educing out white crystals, and drying.

Description

Technical field: [0001] The present invention relates to the technical field of medicine, specifically it is a kind of amino acid salt of quinolone antibacterial drug (-) ofloxacin and a pharmaceutical preparation composed of this salt-a water-soluble salt of amino acid (-) ofloxacin . Background technique: [0002] Levofloxacin (L-ofloxacin) is the third generation of quinolone antibacterial drugs, in vitro against Staphylococcus, Streptococcus (including Enterococcus), Streptococcus pneumoniae, Neisseria gonorrhoeae, Escherichia coli, Citrobacter, Shigella Bacillus, Klebsiella pneumoniae, Enterobacter, Serratia, Proteus, Haemophilus influenzae, Mycobacterium mycobacterium, Helicobacter, etc. all have good antibacterial effects, and have certain inhibitory effects on Pseudomonas aeruginosa and Chlamydia trachomatis effect. It can be used for acute and chronic infections of the respiratory tract, throat, tonsils, urinary tract, skin and soft tissues, gallbladder and bile d...

Claims

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Application Information

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IPC IPC(8): A61K31/5383A61K9/02A61K9/06A61K9/08A61K31/195A61P11/02A61P11/04A61P13/02A61P31/04
Inventor 王东凯宋涛徐飒
Owner SHENYANG PHARMA UNIVERSITY
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