Composition containing rifampicin and lipiarmycin and application of composition

A technology of rifamycin and leap year mycin, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, antibacterial drugs, etc., can solve the problems of liver toxicity and drug resistance, and achieve low toxicity and no Easy to produce drug resistance, low frequency of natural drug resistance induction

Inactive Publication Date: 2018-04-13
SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] For the treatment of bacterial infections in humans, there are problems of hepatotoxicity and drug resistance when one of the above two antibiotics is used alone

Method used

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  • Composition containing rifampicin and lipiarmycin and application of composition
  • Composition containing rifampicin and lipiarmycin and application of composition
  • Composition containing rifampicin and lipiarmycin and application of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Combination of rifampicin and leap year mycin A4. The weight ratio of rifampicin and leapyearmycin A4 is 10:1 to 1:10, and the preparation is an injection.

experiment example 1

[0032] Rifampicin and Leapyearmycin A4 isobolism analysis.

[0033] With reference to the literature J.infect.Dis.140,629-633(1979) and Pain 98,163-168(2002), the Gram-positive bacteria Staphylococcus aureus (Staphylococcus aureus) CMCC (B) 26 003 (5 × 10 5 ) was cultured at 37°C in M-H broth medium for 14 hours, the synergistic effect of the composition of rifampicin and Leapnianmycin A4 in Example 1 was studied, and the synergistic effect of the two antibiotics was analyzed by the isobologram method .

[0034] Equivalent line analysis diagram as figure 1 . All equivalence points of rifampicin combined with leap year mycin A4 are below the diagonal line, showing that the two antibiotics have complementary synergistic effects. Compared with single use, the combination reduces the concentration of rifampicin to one-twelfth of its minimum inhibitory concentration (MIC), and the concentration of leapyearmycin to half of the MIC (second point on the left), benefiting Concentra...

experiment example 2

[0036] The combination of rifampicin and leap year mycin A4 reduces the rate of natural drug resistance to undetectable levels.

[0037] Determination of Staphylococcus aureus (Staphylococcus aureus) CMCC (B) 26003 (1×10 8 -1×10 12 The frequency of natural drug resistance in cfu / plate) was counted after culturing in M-H broth agar medium at 37°C for 14 hours, and different plates were added with rifampicin, leap year mycin A4 or Example 1 respectively. The test was divided into (1) adding 1×, 2×, 4× MIC concentration of rifampicin alone; (2) adding 1×, 2×, 4× MIC concentration of Leapmycin A4 alone; (3) adding 1× , 2×, 4× the MIC concentration of rifampicin and the addition of 1×, 2×, 4× the MIC concentration of Leapmycin A4. All experiments were repeated 4 times with 4 concentrations of bacteria.

[0038] Table 1 shows that the natural resistance mutation frequency of rifampicin, leap year mycin A4 and the combination of the two were 6×10 -8 , 3×10 -8 and undetectable le...

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PUM

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Abstract

The invention discloses a composition containing rifampicin and lipiarmycin and aims at solving the problems of hepatotoxicity and easiness in producing drug resistance due to independent use of one of two antibiotics in treating bacterial infection in a human body. The weight ratio of the lincomycin to the lipiarmycin is (10 to 1) to (1 to 10). The method disclosed by the invention comprises thefollowing characteristics: firstly, two components generate a synergistic sterilization effect, and the effects at lower dosage and lower toxicity are realized; secondly, lower antibiotic natural drugresistance frequency is obtained. The composition disclosed by the invention can be used for mycobacterium tuberculosis infection which is a disease needing long-term treatment; drug resistance is not easy to produce and toxic or side effects are reduced.

Description

technical field [0001] The present invention relates to a kind of composition containing rifamycin and leap year mycin and application thereof. Specifically, it relates to a composition containing rifamycin and leap year mycin for the treatment of bacterial infections in humans to produce a synergistic effect, which is effective at lower dosages and has lower toxicity; has lower natural Frequency of drug resistance induction. The composition of the invention can be used for diseases requiring long-term treatment such as Mycobacterium tuberculosis infection, is not easy to produce drug resistance, and reduces toxic and side effects. Background technique [0002] Rifamycin antibiotics are a class of antibiotics produced by Streptomyces mediterranei. Acting on RNA polymerase, it can inhibit bacterial DNA transcription and synthesis of RNA. It can be used to treat tuberculosis and enterococcal infection. It has strong antibacterial effect on Gram-positive cocci and Mycobacteri...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K31/395A61P31/04A61P31/06
Inventor 王欣荣褚以文翟龙飞马文博袁阳潘文娟詹良静张新宜林家富刘超兰
Owner SICHUAN INDAL INST OF ANTIBIOTICS CHINA NAT PHARMA GROUP CORP
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