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Pharmaceutical composition containing nocathiacin antibiotics

A composition and antibiotic technology, applied in the direction of antibacterial drugs, drug delivery, pharmaceutical formulations, etc., can solve the problems of complex preparation safety, limited medicinal value, poor water solubility, etc., and achieve simple and safe equipment and high cost , the effect of fewer process steps

Active Publication Date: 2011-04-20
NANJING BIOTICA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] As a common feature of thiopeptide antibiotics, nocafloxacin, like other similar antibiotics, has a special strong hydrophobic polycyclic structure, which leads to its extremely poor water solubility, thus limiting its medicinal value
In order to improve the water solubility of nocafloxacin, a series of chemical and biological modification studies on its dehydroalanine side chain, indole and pyridine ring hydroxyl groups have been carried out, but all of them are complicated to prepare and lead to safety problems. and other factors without success (see: J Org Chem, 2002, 67 (24): 8699-8702; J Nat Prod, 2005, 68 (4): 550-553; Bioorg Med Chem Lett, 2004, 14 (14): 3743~3746)

Method used

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  • Pharmaceutical composition containing nocathiacin antibiotics

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment one: the solution containing latent solvent.

[0026] prescription:

[0027] Nocafloxacin I 10mg;

[0028] PEG 400 500 μl;

[0029] 0.9% sodium chloride solution (pH 7.4) 500 μl.

[0030]Process: add the prescription amount of nocafloxacin I, 0.9% sodium chloride solution and PEG400 in sequence, vortex and oscillate for 10 minutes, then ultrasonicate for 30 minutes, and centrifuge to remove the insoluble nocafloxacin I to obtain clear and transparent Solution; the solubility of nocafloxacin I is 6.41 mg / ml and the volume fraction of PEG 400 is 50% as detected by high performance liquid chromatography; the solution is diluted 500-1000 times with 0.9% sodium chloride solution and there is no precipitation within 72 hours Precipitate.

Embodiment 2

[0031] Embodiment two: the solution containing latent solvent.

[0032] prescription:

[0033] Nocafloxacin I 10mg;

[0034] PEG 600 400 μl;

[0035] 5% glucose solution (pH 7.4) 600 μl.

[0036] Process: Add the prescribed amount of nocafloxacin I, 5% glucose solution and PEG600 in sequence in the container, vortex for 10 minutes to mix well, then ultrasonicate for 30 minutes, and centrifuge to remove the insoluble nocafloxacin I to obtain a clear and transparent solution agent; the solubility of nocafloxacin I was 7.54mg / ml and the volume fraction of PEG 600 was 40% as detected by high performance liquid chromatography; no precipitation occurred within 72 hours after the solution was diluted 500-1000 times with 5% glucose solution.

Embodiment 3

[0037] Embodiment three: the solution containing solubilizing agent

[0038] prescription:

[0039] Nocafloxacin I 10mg;

[0040] Poloxamer 20mg;

[0041] 5% glucose solution (pH 7.4) 1000 μl.

[0042] Process: add the prescribed amount of nocafloxacin I, poloxamer and 5% glucose solution to the container in turn, vortex and shake for 10 minutes to mix well, then ultrasonicate for 30 minutes, and centrifuge to remove the insoluble nocafloxacin I to obtain a clear Transparent solution; the solubility of nocafloxacin I detected by high performance liquid chromatography is 2.955 mg / ml; the solution is diluted 500-1000 times with 5% glucose solution and no precipitation occurs within 72 hours.

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Abstract

The invention belongs to the field of pharmaceutical compositions and specially relates to a solution agent of a pharmaceutical composition containing nocathiacin antibiotics, in particular to the pharmaceutical composition containing the nocathiacin antibiotics, which comprises nocathiacin, a drug carrier and a hydrophilic substance, wherein the hydrophilic substance is selected from a latent solvent or a solubilizer; the drug carrier is a physiological dissolution medium with the pH of 4-9, the latent solvent is one or the mixture of more than two selected from ethanol, propylene glycol, glycerin or polyethylene glycol, and the solubilizer is one or the mixture of more than two selected from sorbitan fatty acid, polysorbate, polyvidone, poloxamer and lecithin. The pharmaceutical composition can significantly improve the solubility of the nocathiacin, the preparation process is safe, materials used by the pharmaceutical composition are economic, devices used for preparing the pharmaceutical composition are simple, and the process steps are few; and as the nocathiacin has significant anti-drug resistance activity, the pharmaceutical composition has important clinical application value.

Description

technical field [0001] The invention belongs to a pharmaceutical composition, in particular to a solution of a pharmaceutical composition containing nocafloxacin antibiotics and a corresponding gel. Background technique [0002] In the history of human beings fighting against diseases, bacterial infection has always been the number one killer of human death. As people use more and more antibiotics to treat diseases, they also exercise the resistance of bacteria. With the abuse of antibiotics and the rapid evolution of pathogenic bacteria, more and more drug-resistant strains have appeared clinically, especially strains resistant to multiple antibiotics such as methicillin-resistant Staphylococcus aureus (MRSA), Penicillin-resistant Streptococcus pneumoniae (PRSP), as well as the recently discovered "super bacteria", people often seem helpless in the face of the rapid infection rate of these pathogenic bacteria. In addition, with the gradual increase of Gram-positive bacteri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12A61K47/10A61K47/34A61K47/14A61K47/32A61K47/24A61K9/08A61K9/06A61P31/04
Inventor 陈依军冯坤
Owner NANJING BIOTICA PHARMA
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