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Daptomycin freeze-dried preparation for injection and preparing method

A technology of daptomycin and freeze-dried preparations is applied in the field of freeze-dried preparations and preparations of daptomycin for injection, which can solve the problems of low drug solubility of daptomycin, drug precipitation and crystallization, increase cost and the like, and achieve clinical use. Safe and effective, stable pharmaceutical preparations, easy to store

Inactive Publication Date: 2005-05-18
魏雪纹 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because daptomycin is slightly soluble in water, the current pharmaceutical technology is to make daptomycin into a large infusion solution with a concentration below 4mg / ml, otherwise the drug will easily crystallize in the injection, and if drug precipitation occurs, it cannot for intravenous infusion
Solution-type injections are also very inconvenient in transportation and are prone to damage, which is not conducive to the carrying and transportation of drugs, which increases freight and costs
In order to overcome the above-mentioned unfavorable factors, we have developed a freeze-dried powder preparation of daptomycin for injection, which successfully solved the problem of low solubility of daptomycin in water

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Formula 1: Each bottle (cartridge) of lyophilized preparation contains 125 mg of daptomycin

[0020] Daptomycin 1250mg

[0021] Mannitol 1250mg

[0022] Dextran 40 125mg

[0023] 1mol / L HCl solution 12.5ml

[0024] 1mol / L NaOH solution appropriate amount

[0025] Add water for injection to 135ml

[0026] 10 bottles, 12.5ml each

[0027] Preparation method: Take daptomycin plus x.1mol / L HCI solution in the prescription, heat in a water bath at 60-80°C, stir to dissolve all daptomycin, add about 80% of the total amount of water for injection, and use 1mol / L Adjust the pH value of the NaOH solution to 3-5, add the prescribed amount of mannitol and dextran 40, stir to dissolve them all, add 30 mg of activated carbon, and add water for injection to the full amount of the prescription, and stir for 15 minutes. Use No. 3 vertical melting funnel to remove activated carbon, and the filtrate is finely filtered with a 0.22 μm microporous membrane. After testing, the filtrat...

Embodiment 2

[0029] Formula 2: Each bottle (cartridge) of lyophilized preparation contains 250 mg of daptomycin

[0030] Daptomycin 2500mg

[0031] Lactose 1000mg

[0032] 50% lactic acid 20ml

[0033] 5% NaI-IC03 solution appropriate amount

[0034] Add water for injection to 25ml

[0035] 10 bottles, 2.5ml each

[0036] Preparation method: add 50% lactic acid to the daptomycin in the prescription, heat and stir to dissolve the daptomycin completely, adjust the solution to pH 3-5 with 5% NaHCO3, add 40 mg of activated carbon, add water for injection to the full amount of the prescription, and stir for 15 minute. Other methods are the same as in Example 1.

Embodiment 3

[0038] Formula 3: Each bottle (cartridge) of lyophilized preparation contains 500 mg of daptomycin

[0039] Daptomycin 5000mg

[0040] Dextran 40 750mg

[0041] Citrate (anhydrous) 75mg

[0042] 5% NaHCO3 solution appropriate amount

[0043] Add water for injection to 5ml

[0044] 10 bottles, 5ml each

[0045] Preparation method: Take daptomycin, dextran 40, and citric acid in the prescription, add about 40ml of water for injection, heat and stir in a water bath at 80°C to dissolve them all, adjust the pH of the solution to 3-5 with 5% NaHCO3, and add 40mg of activated carbon , and add water for injection to the full amount of the prescription, and stir for 15 minutes. Other methods are the same as in Example 1.

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PUM

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Abstract

Active medicine daptomycin is mixed with certain amount of sodium hydroxide and pH regulator, the mixture is compounded with injection water to form solution in certain concentration, and the solution is filled into antibiotic bottle and freeze dried for 30-60 hr to prepare loose and water soluble freeze dried preparation. The freeze dried daptomycin preparation for injection has excellent medicine stability and convenience in carrying and clinical application. The preparation is used specially for intravenous injection to treat skin infection with resistance to other antibiotics.

Description

technical field [0001] The invention relates to a freeze-dried preparation of daptomycin for injection and a preparation method thereof. Background technique [0002] Daptomycin (C 72 h 101 N 17 o 26 ), molecular weight: 1620.67, chemical name: N-decanoyl-L-tryptophanyl-L-asparagyl-L-threonylglycyl-L-urinyl-L-aspartyl- D-lactamyl-L-aspartylglycyl-D-seryl-threo-3-methyl-L-glutamyl-3-anthranilicyl-L-alanyl E1- Lactone. Daptomycin is white or off-white crystal or crystalline powder. [0003] Daptomycin mainly prevents and treats infections caused by bacteria, and its mechanism of action is different from that of various antibacterial drugs currently on the market, which means that daptomycin will not be affected by cross-resistance caused by other antibiotics. influences. Second, daptomycin rapidly kills most clinically important Gram-positive cocci in vitro, including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecalis, and vancomyci...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K38/12A61P31/04
Inventor 魏雪纹王小树申洁
Owner 魏雪纹
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