• YAKHAK HOEJI
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• v.37 no.4
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• pp.350-355
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• 1993

The preparation of Streptococcus faecalis RSI is used as a medicinal preparation for human intestinal disorders. But the microbe in this preparation is very sensitive to rifampicin. If this preparation is taken with rifampicin, its therapeutic effect can not be expected. To develope rifampicin resistant mutants, the rifampicin sensitive strain S. faecalis RSI was treated with Nmethyl-N'-nitro-N-nitrosoguanidine(MNNG). Twelve strains of the MNNG-induced mutants showed distinct resistance to rifampicin and five mutants were selected for further studies. They also exhibited identical characteristics with the parent S. faecalis RSI when they were tested for lactic acid formation and growth inhibition of E. coli. From in vitro test, it was identified that rifampicin is not inactivated by certain factors of the rifampicin resistant mutants. Conclusively, the rifampicin resistant mutants are efficient strains that have insensitivity against rifampicin and original biochemical characteristics of the parent strain.

• Korean Journal of Microbiology
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• v.24 no.3
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• pp.276-287
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• 1986

Chlorella ellipsoidea were cultured in the media containing rifampicin for 7 days. Aliquot cells were taken out after the inoculation and at intervals during cultivation and growth rate of Chlorella cells was measured. In order to investigate the effect of rifampicin on the nucleic acid synthesis, nucleic acid and RNA polymerase were extracted from chloroplast isolated from these cells, and the contents of nucleic acid and activity of enzyme were measured to compared with those of the control. The inhibitory concentration of rifampicin on growth was 80 ppm. The DNA contents in chloroplasts isolated were decreased 60% to compared with control, whole cells were markedly decreased 70% by rifampicin. The contents of base in the RNA were decreased 46% by rifampicin in shole cell, and 77% of base contents were decreased in chloroplast. Rifampicin also inhibited the activity of RNA polymerase, therefore whole cell was decreased 10% of activity and chloroplasts were decreased 42% of activity.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.143-143
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• 1993

현재 시판되고 있는 정장용 생균 제제에 함유되어있는 정장 균주의 하나인 Bifidobacterium bifidum은 항결핵제 중 rifampicin에 감수성으로 rifampicin과 병용 투여시 본래의 정장 효과를 기대할 수없다. 따라서, rifampicin에 내성인 돌연변이 균주를 얻기 위해 B. bifidum을 N-methyl-N'-nitro-N-nitrosoguanidine(MNNG)로 처리하여 rifampicin에 내성인 30 종의 균주를 선별하였고, rifampicin에 대한 Minimal Inhibitory Concentration (MIC)를 측정해 본 결과 내성이 1,000 배 이상 상승하였다. 균주 동정을 위하여 fructose-6-phosphate phosphoketolase test를 실시해 본 결과 Bifidobacterium임이 확인되었다. 이들 내성 균주들의 유기산 생산량을 측정하여 그 생산량이 모균주와 가장 유사한 3 종의 균주를 선발하였다. 이들에 대하여 Escherichia coli 생육 억제능을 시험해 본 결과 E. coil 생육 억제능이 모균주와 유사하였다. 또, rifampicin을 함유한 배지에서 돌연변이 균주를 배양시킨 경우 rifampicin이 안정한 상태로 잔존한 것을 알 수 있었다. 이것으로 보아 돌연변이 균주들은 rifampicin을 분해 또는 변형시키는 효소를 생산하지 않는다고 볼 수 있다. 이상의 결과로 본 연구에서 개발한 돌연변이 균주들, 즉 B. bifidum RFRll, RFR21 그리고 RFR61은 rifampicin에 내성이면서 모균주와 동일한 생화학적 특성을 갖는 정장 균주로 여겨진다.

• YAKHAK HOEJI
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• v.31 no.4
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• pp.204-212
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• 1987

Rifampicin is an indispensable drug along with isoniazid for the control of tuberculosis and is usually prescribed as the combination of rifampicin and isoniazid. This paper is attemtped to investigate the interaction of rifampicin and isoniazid. Isoniazid was administered orally at a dose of 30mg/kg of rabbits pretreated with rifampicin 7.5mg/kg, 15mg/kg, and 30mg/kg, respectively twice daily for 9 days. The results are as follows: The blood level and relative bioavailability of isoniazid were decreased significantly (p<0.05) by rifampicin at a dose of 15mg/kg and 30mg/kg. The renal clearance of total isoniazid and ratio of its metabolites to isoniazid were increased significantly (p<0.05) by rifampicin at a dose of 15mg/kg and 30mg/kg. It seemed to be due to enzyme induction by rifampicin. Elimination rate constant ($\beta$) of isoniazid was increased and half life ($t_{1/2$\beta}$) was decreased by rifampicin pretreatment. Dosage regimen of isoniazid after long term administration of rifampicin should be adjusted carefully.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.252-252
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• 1994

현재 시판되고 있는 정장용 생균 제제에 함유되어있는 정장균주의 하나인 Bifidohacterium bifidum은 항결핵제 중 rifampicin에 감수성으로 rifimpicin과 병용 투여시 본래의 정장 효과를 기대할 수 없다. 따라서, rifampicin에 내성인 돌연변이 균주를 얻기 위해 B. bifidum을 N-methyl-N'-nitro-N-nitroso- -guanidine(MNNG)로 처리하여 rifampicin에 내성인 30종의 균주를 선별 하였고, rifampicin에 대한 Minimal Inhibitory Concentration(MIC)를 측정해 본 결과 내성이 1,000배 이상 상승하였다. 또한 rifampicin에 내성인 균주 RFR61을 자연 돌연변이시켜 ofloxacin에도 내성인 돌연변이 균주 20종을 선별 하였고, MIC를 측정한 결과 내성이 4배 이상 증가하였다. 또, fructose-6-phosphate phosphoketolase test를 실시해 본 결과, 모두 Bifidobacterium임이 확인되었다. 유기산 생성량을 측정하여 모균주의 유기산 생성량과 가장 유사한 3균주, B. bifidum RFRll, RFR21, RFR61 그리고 OFR9을 선별하였다. 이 네 균주의 E. coli 생육 억제능을 측정한 결과 모두 모균주와 유사한 E. coli 생육 억제능을 가지고 있었다. Rifampicin 내성균주들에 대하여 내성 유지 시험을 한 결과 복귀 돌연변이에 의해 내성이 소실될 가능성은 없는 것으로 여겨진다. 마지막으로, 내성 균주에 의한 rifampicin 불활성화 여부를 알아 본 결과 rifampicin이 불활성 화되지 않음을 알 수 있었다. 이상의 결과를 통해 본 연구실에서 개발한 B. bifidum RFR11, RFR21 그리고 RFR61 균주들은 rifampicin에 내성이며, B.bifidum OFR9은 rifampicin과 ofloxacin에 이중 내성을 갖는 균주로서 모균주와 유사한 생화학적 특성을 갖는 우수한 정장 세균으로 여겨진다.

• Journal of Pharmaceutical Investigation
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• v.14 no.3
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• pp.105-121
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• 1984

The bioavailability of rifampicin (brand A, B and C) was studied and the dissolution by foamed plastic rotating method and basket rotating method was also investigated. The results were as follows; 1. In the case of foamed plastic rotating method, it was revealed that dissolution rate of brand C was most rapid, but in the case of basket rotating method the results revealed that brand B was most rapid. Also it was observed that the dissolution rate in artificial gastric juice was more rapid than one in artificial intestinal juice, and that Avicel added in capsule increased additively the dissolution rate, particulary brand B. 2. Relative systemic availability by urine data showed that the results from all capsules filled with brand A, B and C were identical but in the case of the ripamficin capsules filled with Avicel, the results showed that Avicel increased the availability of brand A and B. 3. Area under serum concentration curve $(0{\sim}8hrs)$ was in order of $brand\;A{\fallingdotseq}brand\;C$ > brand B, but Avicel increased significantly the AUC of brand B and showed no effect in others. 4. Relative systemic availability calculated with excreted amount of rifampicin in urine was similar in each rifampicin capsules. In rifampicin (A) and rifampicin (B), Avicel which added in capsules appeared increasing tendency in urine excretion of rifampicin, but in rifampicin (C) it did not appeared. 5. Area under serum concentration curve $(0{\sim}8hrs)$ in rifampicin capsules was in order of $rifampicin(A){\fallingdotseq}rifampicin(C)$>rifampicin(B). In rifampicin (B) with Avicel capsules, area under serum concentration curve (0-8hrs.) increased significantly and in others insignificantly.

• Biomolecules & Therapeutics
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• v.25 no.6
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• pp.634-640
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• 2017

Atopic dermatitis (AD) is a common inflammatory skin disorder mediated by inflammatory cells, such as macrophages and mast cells. Rifampicin is mainly used for the treatment of tuberculosis. Recently, it was reported that rifampicin has anti-inflammatory and immune-suppressive activities. In this study, we investigated the effect of rifampicin on atopic dermatitis in vivo and in vitro. AD was induced by treatment with 2, 4-dinitrochlorobenzene (DNCB) in NC/Nga mice. A subset of mice was then treated with rifampicin by oral administration. The severity score and scratching behavior were alleviated in the rifampicin-treated group. Serum immunoglobulin E (IgE) and interleukin-4 (IL-4) levels were also ameliorated in mice treated with rifampicin. We next examined whether rifampicin has anti-atopic activity via suppression of mast cell activation. Rifampicin suppressed the release of ${\beta}$-hexosaminidase and histamine from human mast cell (HMC)-1 cultures stimulated with compound 48/80. Treatment with rifampicin also inhibited secretion of inflammatory mediators, such tumor necrosis factor-${\alpha}$ ($TNF-{\alpha}$) and prostaglandin $D_2$ ($PGD_2$), in mast cells activated by compound 48/80. The mRNA expression of cyclooxygenase 2 (COX-2) was reduced in the cells treated with rifampicin in a concentration-dependent manner. These results suggest that rifampicin can be used to treat atopic dermatitis.

• Korean Journal of Microbiology
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• v.27 no.2
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• pp.155-161
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• 1989

Lactobacillus sporogenes was treated with N-methyl-N'-nitro-N-nitrosoguanidine (NTG) to obtain resistant mutants to rifampicin. Fifty-eight strains of the NTG-induced mutants showed distinct resistance to rifampicin and nine mutants were selected for further studies. They also exhibited identical characteristics with the parent Lactobacillus sporogenes when they were tested for spore formation, acid formation and growth inhibition of E. coli. From in vitro test it was identified that rifampicin is not inactivated by certain factors of the rifampicin resistant mutants. It is suggested that they can be utilized as efficient normalizing agents for human intestinal flora when they are simultaneously taken with rifampicin

• YAKHAK HOEJI
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• v.42 no.2
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• pp.175-180
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• 1998

Bifidobacterium bifidum OFR9 that exhibits acquired resistance to rifampicin and fluoroquinolones was selected by MNNG and multi-step mutation method. To investigate the resistance mechanism to rifampicin in the strain, RNA polymerase from B. bifidum parent strain and rifampicin-resistance OFR9 was partially purified and its sensitivity to rifampicin was assayed. The profile of RNA polymerase preparation of B. bifidum parent and B. bifidum OFR9 is similar to that of E. coli RNA polymerase that includes the basic subunits of ${\beta}$`, ${\beta},\;{\sigma},\;{\alpha}$ but which are a little different in size when they are compared with E. coli RNA polymerase subunits. RNA polymerase isolated from the parent strain was inhibited by 1${\mu}$g/ml rifampicin but that from B. bifidum OFR9 was not affected by 100${\mu}$g/ml concentration of rifampicin. RNA polymerase activity of B. bifidum OFR9 was maintained over 90% through that rifampicin concentration. This result is consistent with MIC values of in vitro test. It can be concluded that the mechanism of rifampicin resistance in B. bifidum OFR9 is due to an alteration of RNA polymerase.

• Archives of Pharmacal Research
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• v.8 no.3
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• pp.177-186
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• 1985

Effect of food on the absorption characteristics of oral rifampicin was studied in the fasted rats. Rifampicin dissolved in a new cosolvent was also injected to the rats intravenously, and the pharmacokinetic analysis was performed to explain the effect of food on the gastrointestinal absorption of rifampicin. Rifampicin was absorbed rapidly and completely in the fasting state. Food had a profound effect on the gastrointestinal absorption of rifampicin, i. e., bioavailability and the extent of absorption were decreased to less than one-third of the fasting state in the postprandial state. Food seemed to imhibit the absorption and reabsorption of rifampicin in the gastrointestinal tract, but not the absorption rate constant. Hepatobiliary excretion seemed to be the major route of elimination, since the renal clearance accounted for only 8 % of the systemic clearance. Nevertheless, first-pass effect was negligibly small and most of rifampicin absorbed could reach systemic circulation. Serum concentration change of oral rifampicin on multiple dosing differed markedly in the fasting and postprandial state, which suggested the need of careful adjustment of dosage regimen in both states.