• 약학회지
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• 제37권5호
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• pp.483-489
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• 1993

Bifidobacterium bifidum, one strain of medical preparations being on the market for human intestinal disorder, is very sensitive to rifampicin. If this preparation is taken with rifampicin, its therapeutic effect can't be expected. To develope rifampicin resistant mutants, B. bifidum was treated with N-methyl-N'-nitro-N-nitrosoguanidine(MNNG). All of thirty strains grown on the plates containing 10 $\mu\textrm{g}$/ml rifampicin were over 1, 000 times more resistant to rifampicin than parental strain and they were identified as B. bifidum by fructose-6-phosphoate phosphoketolase test. Three strains out of thirty, which produced almost same amount of organic acid as parental strain, were selected for further studies. They showed identical growth inhibition activity aganist E. coli compared with that of parental strain. And rifampicin was not inactivated.

• 약학회지
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• 제27권1호
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• pp.11-19
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• 1983

Rifampicin-arginine complex was prepared to increase the solubility and dissolution rate of rifampicin. Solvation method was applied to make the complex and its formation was identified by the solubility method, powder x-ray diffractometry, differential thermal analysis and spectroscopic determination. The complex was formed in the molar ratio of 1 : 1 which was proved by the slope ratio method and continuous variation method. The complex was a non-crystalline form determined by the x-ray powder diffractometric analysis. The solubility of complex in water was significantly higher than that of rifampicin itself. The stability constant and thermodynamical properties of the complex were determined to investigate the solubilization phenomena. The thermodynamic data showed that the complexation between rifampicin and arginine was an exothermic and spontaneous reaction. Simulated absorption studies carried out through the artificial lipid barrier in artificial gastric and intestinal juices. The results showed that the complex had an enhanced absorption rate of rifampicin nearly twice compared with that of rifampicin itself.

• Journal of Chest Surgery
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• 제11권1호
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• pp.12-17
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• 1978

Rifampicin has been widely hailed as the most effective antituberculosis antibiotics since the clinical use of streptomycin, but its immunosuppressive side effect was still annoying problem to be excluded. These studies were carried out to determine the effect of Tuberein-3, tuberculous bacilli extraction with water, on Rifampicin induced T-lymphocytopenia in 5 cases of pulmonary tuberculosis who have never exposed to antimetabolites or steroid compounds. After 2 weeks treatment of Rifampicin, all cases showed T-lymphocytopenia, active $13.0{\pm}2.3$ % and total $43.1{\pm}4.4$%. Followed by another 2 weeks treatment with Rifampicin combined with Tuberein-3, T-lymphocytes in peripheral blood returned to the normal limit, active $21.6{\pm}3.3$% and total $56.3{\pm}1.7$%. Tubercin-3 revealed the restoring activity of suppression of T-lymphocyte rosettes by Rifampicin.

• 약학회지
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• 제43권1호
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• pp.124-127
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• 1999

Bifidobacterium infantis K-525 isolated from healthy Korean was susceptible to rifampicin and fluoroquinolones and resistant to other antituberculosis agents. When the preparation of this strain is taken as a therapeutics for human intestinal disorders with rifampicin or fluoroquinolones, its therapeutic effect can not be expected. So, B, infantis RFR-525 resistant to rifampicin was obtained by treating the parent B. infantis 525 with N-methyl-N'-nitro-N-nitrosoguanidine. B. infantis OFR-525 was produced by serial passage of B. infantis RFR-525 on agar with 2-fold minimal inhibitory concentration of ofloxacin. B. infantis OFR-525 was resistant to antituberculosis agents and fluoroquinolones up to 4∼128 fold higher than that for the original strain. The resistance of B. infantis OFR-525 against rifampicin and ofloxacin was maintained in vivo and in vitro. Conclusively, B. infantis OFR-525 can be regarded as a promising strain which can be developed as the preparation for the treatment of the intestinal disorders of the tuberculosis patients under rifampicin and ofloxacin therapy.

• 한국임상약학회지
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• 제3권1호
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• pp.1-13
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• 1993

The intraction between cimetidine and rifampicin was studied pharmacokinetically in normal human subjects. The serum level and the area under the serum concentration curve(AUC) of rifampicin administrated orally were elevated significantly by cimetidine. Volume of distribution, total clearance and elimination rate constant of rifampicin were reduced significanyly by cimetidine. Biological half-life of rifampicin was prolonged significantly by cimetidine. The mechanism of this results is probably related to the inhibition of rifampicin metabolism(deacetyl form) or reduction of blood flow in the liver. It is desirable that dosage regimen of rifampicin shoud be adjusted when combined with cimetidine in clinical pharmacy practice.

• 약학회지
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• 제29권4호
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• pp.220-222
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• 1985

Rifampicin reacts with cupric ion to produce rifampicin-Cu(II) chelate (2:1) at pH 6.5, which can be extracted with methylisobutylketone (MIBK). Therefore, rifampicin can be quantitatively, determined by measuring the quantity of Cu(II) in the organic phase by atomic absorption spectrophotometry. Because higher absorbance ratio was obtained in pH 6.0~7.0, buffer solution at pH 6.5 was used in this measurement. Linear relationship was found between absorbance and concentration in the range of 1.0~4.0${\times}10^{-4}M$. This method might be applicable to the determination of rifampicin in the preparations.

• Clinical and Experimental Pediatrics
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• 제45권4호
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• pp.454-458
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• 2002

목 적 : BCG접종 후에 소속 림프절에 발생하는 화농성 림프절염은 비교적 심각한 부작용 중 가장 흔하다. 대부분 치료를 하지 않더라도 결국은 퇴행되지만, 보통 몇 주 또는 몇 개월 동안 배농이 지속되어 매우 불편하고, 상당한 예에서 궤양으로 남게된다. Pan American Health Organization은 isoniazid 또는 rifampicin 국소 주입을 권장하였다. 이에 저자들은 BCG접종 후에 발생한 화농성 림프절염을 rifampicin 국소 주입으로 치료한 경험을 보고하고자 한다. 방 법 : 최근 3년간 대한결핵협회 결핵연구원 및 본원에서 BCG에 의한 림프절염으로 진단된 영아를 대상으로 하였다. BCG 림프절염은 동측의 액와부 또는 쇄골상부에 생긴 림프절염으로, BCG 접종 외에는 림프절염의 다른 원인이 없을 때 진단하였다. 화농하지 않고 림프절이 커져 있는 경우에는 자연 소실될 가능성이 있으므로 경과를 관찰하다가, 화농하면 자연적으로 파열되기 전에 주사기로 림프절을 흡인하고 rifampicin을 국소 주입하였다. 결 과 : BCG에 의한 림프절염 환아 37명을 경험하였다. 1) 림프절염의 양상 : 림프절염은 BCG를 접종한 후 대부분 4개월 이내에 발생하였다. 발생부위는 대부분 좌측 액와부였고, 쇄골상부에 생긴 예도 있었다. 크기는 대부분 2-3 cm였고, 5 cm 이상인 경우도 있었다. 2) 림프절염의 치료 : 37명 중 3명은 림프절염이 화농하지 않고 자연적으로 소실되거나 크기가 감소하였다. 화농하면 rifampicin을 주입하려고 경과를 관찰하다가 9명은 시술 전에 자연적으로 터져서 배농되어 드레싱만으로 치유되었다. 25명은 림프절염이 화농되어 주사기로 흡인한 후에 rifampicin을 국소로 주입하였다. 18명은 한번 시술해서 치유가 되었다. 7명에서는 한번 시술한 후에 다시 유동성이 생겨서 한번 더 시술하였다. 이중 1명은 두번 시술하였으나 크기가 더이상 감소하지 않아서 외과적 절제술을 고려하고 있다. Rifampicin 국소 주입 후 많은 경우에서 몇 일 이내에 배농이 없어지고, 그 이후 크기가 감소하였다. 림프절이 크면 일부에서 배농이 1-2개월 지속되었다. 결 론 : BCG에 의한 림프절염 중 일부는 자연적으로 소실된다. 화농성 림프절염으로 이행되면 침흡인 후에 rifampicin을 국소 주입하는 방법이 효과적이다. 즉 자연적 배농을 방지하고 비교적 빠른 시간 내에 림프절염이 치유된다.

• The Korean Journal of Physiology and Pharmacology
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• 제13권6호
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• pp.475-482
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• 2009

Rifampicin is a macrocyclic antibiotic which is used extensively for treatment against Mycobacterium tuberculosis and other mycobacterial infections. Recently, a number of studies have focused on the immune-regulatory effects of rifampicin. Therefore, we hypothesized that rifampicin may influence the TLR2 expression in LPS-activated RAW 264.7 cells. In this study, we determined that rifampicin suppresses LPS-induced TLR2 mRNA expression. The down-regulation of TLR2 expression coincided with decreased production of TNF-$\alpha$ Since NF-${\kappa}B$ is a major transcription factor that regulates genes for TLR2 and TNF-$\alpha$, we examined the effect of rifampicin on the LPS-induced NF-${\kappa}B$ activation. Rifampicin inhibited NF-${\kappa}B$ DNA-binding activity in LPS-activated RAW 264.7 cells, while it did not affect IKK$\alpha/\beta$ activity. However, rifampicin slightly inhibited the nuclear translocation of NF-${\kappa}B$ p65. In addition, rifampicin increased physical interaction between pregnane X receptor, a receptor for rifampicin, and NF-${\kappa}B$ p65, suggesting pregnane X receptor interferes with NF-${\kappa}B$ binding to DNA. Taken together, our results demonstrate that rifampicin inhibits LPS-induced TLR2 expression, at least in part, via the suppression of NF-${\kappa}B$ DNA-binding activity in RAW 264.7 cells. Thus, the present results suggest that the rifampicin-mediated inhibition of TLR2 via the suppression of NF-${\kappa}B$ DNA-binding activity may be a novel mechanism of the immune-suppressive effects of rifampicin.

• Archives of Pharmacal Research
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• 제11권3호
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• pp.218-224
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• 1988

The preparation of Clostridium butyricum is used as a normalizing agent for human intestinal flora. When the microbe is simultaneously used with rifampicin, it is inactivated by the antibiotic. To develop rifampicin-resistant mutants, rifampicin-sensitive strain Miyairi II 588 of C. butyricum was treated with nitrosoguanidine (NTG). To ensure stable resistance to rifampicin, we examined whether the resistance was plasmid-mediated or chromosome-mediated. It was found that the resistance of four mutant strains was not mediated by its inherent plasmid, but by the chromosomal mutation. These strains were examined for the susceptibility and resistance to other antituberculosis agents and antibiotics. The results showed that these mutants were resistant to the high concentration of the antituberculosis agents.

• 대한의용생체공학회:학술대회논문집
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• 대한의용생체공학회 1997년도 춘계학술대회
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• pp.31-34
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• 1997

A new method for the prevention of foreign body-associated infections by controlled release of antibiotic was developed. The polyurethane (PU) matrix containing rifampicin was immobilized with hydrophilic photoreactive polyallylamine (PPA) containing azidophenyl groups. The rifampicin release characteristics and the long-lasting antimicrobial activities of the new material was compared with rifampicin-containing PU matrix without PPA membrane. The release rate of antibiotic from rifampicin-containing PU with PPA membrane significantly decreased as the thickness of PPA membrane was increased. The PPA-immobilized rifampicin-containing PU discs immersed in the PBS for 47 days had an efficient antimicrobial activity against both S. aureus and S. epidermidis.