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Pharmaceutical composition for diseases caused by pathogenic microorganisms such as aspergillus

A composition and protozoan technology, which can be used in drug combinations, respiratory diseases, antibacterial drugs, etc., and can solve the problems of non-protozoan effect and anti-chlamydia effect.

Inactive Publication Date: 2015-09-30
POLA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tetracycline and macrolide antibiotics are effective against chlamydial pneumonia, while the only treatment for trichomonal pneumonia is metronidazole
For example, it is known that bifonazole, miconazole, amorolfine, and butenafine, which are known as antifungal agents against athlete's foot etc., do not have antiprotozoal action and antichlamydial action

Method used

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  • Pharmaceutical composition for diseases caused by pathogenic microorganisms such as aspergillus
  • Pharmaceutical composition for diseases caused by pathogenic microorganisms such as aspergillus
  • Pharmaceutical composition for diseases caused by pathogenic microorganisms such as aspergillus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] The effect of luliconazole among the compounds represented by the general formula (1) on Trichomonas vaginalis was investigated. In other words, the 5 x 10 6 Three clinically isolated Trichomonas vaginalis cells were inoculated in Trichomonas medium F (6.5 mL, contained in a tube) produced by Fujiyakuhin Co., Ltd. containing neutral red as a marker, and then Precultivation was carried out for 72 hours (preculture). Trichomonas growth was confirmed, acid was actively produced, and the neutral red turned yellow. Thereafter, each 100 µL of the preculture was added to Trichomonas medium F, to which 0.5 mL of the test solution was added for main culture. In this case, the number of protozoa in the solution of the preculture was 1.5 x 10 5 cells / mL. Three series of test solutions were prepared in which luliconazole concentrations were 200 μM (final concentration: 35.2 μM), 100 μM (final concentration: 17.6 μM) and 50 μM (final concentration: 8.8 μM) when luliconazole was ...

Embodiment 2

[0072]The same or equivalent study as in Example 1 was performed, with luliconazole replaced by lanoconazole. Therefore, it is clear that lanoconazole also inhibits the growth of Trichomonas as well as luliconazole. It has been revealed that lanoconazole is a clinically applicable substance that inhibits the growth of Trichomonas in addition to metronidazole. In addition, the minimum growth inhibitory concentration (MIC) was revealed to be around 17.6 μM.

[0073] Table 2

[0074] final concentration

Embodiment 3

[0076] In vitro antifungal activity against Candida albicans

[0077] The minimum growth inhibitory concentration (MIC) was measured by means of the broth microdilution method (two serial dilutions of the drug) based on the use of BPMI 1640 medium (pH 7.0) buffered with 0.165M morpholinopropanesulfonic acid. Dispense 100 µL of the test microorganism yeast cell / sterile saline suspension (1 to 5 x 10 3 cells / mL) and 100 μL of culture medium pre-supplemented with each compound and the culture medium without compound added as a control were distributed into each well of a flat-bottomed microculture plate. After culturing at 35°C for 48 hours, the culture turbidity of each well was measured at 630nm to determine the minimum growth inhibitory concentration (MIC 80 : μg / mL), which is the minimum concentration of compound (measured as a suspension) that exhibits 80% growth inhibition relative to the growth of microorganisms in control cultures. The results are shown in Table 3. It ...

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PUM

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Abstract

An object is to provide means for precisely treating pneumonia caused by intracellular parasite, protozoa, and / or fungus. A pharmaceutical composition for pneumonia, comprising a compound represented by the following general formula (1) as an active ingredient:(In the formula, R represents a halogen atom or a hydrogen atom, and X represents a halogen atom.)

Description

technical field [0001] The present invention relates to pharmaceutical compositions. In particular, the present invention relates to pharmaceutical compositions preferably used in pneumonia. Background technique [0002] Pneumonia is in most cases caused by a secondary pneumococcal infection that accompanies eg influenza. However, fungal pneumonia caused by, for example, Candida and / or Aspergillus has rapidly increased in recent years due to decreased immunity due to chemotherapy for cancer or decreased immunity due to the onset or crisis of AIDS. On the other hand, in recent years, the number of patients infected with Chlamydial pneumonia or Trichomonas pneumonia has increased with any particular sexual intercourse activity associated with STDs. Tetracycline and macrolide antibiotics are effective against chlamydial pneumonia, while metronidazole is the only therapeutic agent for trichomonal pneumonia. Furthermore, in the case of metronidazole, resistant strains against ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4178A61K9/20A61K9/28A61P33/00A61P33/02A61P11/00
CPCA61K31/4178A61K9/2866A61P11/00A61P31/04A61P31/10A61P33/00A61P33/02
Inventor 岛村刚宫田善之后藤诚
Owner POLA PHARMA
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