日本化学療法学会雑誌第57巻第S-2号
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- あいり しげまつ
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1 µ µ Key words µ µ µ I
2 Table1. Subjectprofilesin(A)singleand(B)multiple-dosestudies (A)Single-dosestudy Age (yr) Height (cm) Bodyweight (kg) BMI (kg/m ) Ccr(Cockcroft) (ml/min) Ethnicity dose(mg) n 5 5.1±., ±5.1,37 Japanese 75.±5.5,3 1, 5.±3.,3 placebo 1.±5. 1,37 17.±5. 16.± ± ± ± , , , ,1. 15., ± , ± , ± ,7. 1.6± ,.7 6.5± ,75.7.6± ,.7 6.± ,1. 3.±..1 1.,. 61.6± ,75.5.± ,.5 1.6± ± ± ±.5 11.± ,131,1 16,13 16,13 17,15 Caucasian 5 placebo 3 3.3± ± ,3, ± ± , ,1. 77.± ± ,. 6.,..±.3.±1....,.., ± ± ,1,11 (B)Multiple-dosestudy dose(mg) 5 7days nonelderly 5 7days nonelderly placebo 5 7days elderly 5 7days elderly placebo n 3 3 Age (yr) 3.±.5 3,7.7±3. 1,7 7.± ,73 7.3± ,7 Height (cm) 16.5± , ± , ± , ± ,17.3 Bodyweight (kg) 6.6± , ± ,71. 6.± , ± ,.6 BMI (kg/m ) 1.± ,.6.±3.. 1.,.3.± ,7. 5.6±. 6.5.,7. Ccr(Cockcroft) (ml/min) 11.± ,13.±15.,11.1± ,15 1.± ,15
3 (A)Single-dosestudy Hospitalization Dose Subjectbackground Investigator sexamination Height Bodyweight BMI Temperature,bloodpressure,pulserate 1-leadelectrocardiogram Clinicallaboratorytest Immunologicaltest Pharmacokinetic Monitoring Drugtest(urine) Table. Studyscheduleinthe(A)singleand(B)multiple-dosestudies Hematology,blood biochemistry,urinalysis Ccr Plasma 1) Saliva ),3) Urine ) Screening Day- <_ Folow-up 1) Bloodsamplescolected:immediatelybefore(timezero),.5,.5,1,1.5,,3,,,1,,36,,6,and 7h ) Salivarysamplescolected:immediatelybefore(timezero),1,,3,,,1,andh 3) Salivarysampleswerecolectedfrom subjectsadministeredlvfx5mg. ) Urinarysamplescolected:-,,,, 1,1,,and 7h (B)Multiple-dosestudy Hospitalization Dose Subjectbackground Investigator sexamination Height Bodyweight BMI Temperature,bloodpressure,pulserate 1-leadElectrocardiogram Clinicallaboratorytest Immunologicaltest Pharmacokinetic Monitoring Intestinalflora 3) Drugtest(urine) Hematology,blood biochemistry,urinalysis Ccr Plasma 1) Screening Day- <_ Folow-up 1 Urine ) ) ) 1) Bloodsamplescolected:day1;immediatelybefore(timezero),.5,.5,1,1.5,,3,,,and1h day 6;immediatelybefore(timezero)and1.5h day7;immediatelybefore(timezero),.5,.5,1,1.5,,3,,,and1h day;and36h day;and6h day1;7h ) Urinarysamplescolected:day-1;- h days1and7;,,, 1,and1 h 3) OnlynonelderlyJapanese.Fecessamplingwasdoneoncewithineachinterval. ) Asubjecthavingnobowelmovementwashospitalizedinthreedaysatmaximum.
4 5 mg (n ) 5 mg (n ) Plasma concentration ( g/ml) mg (n ) 1, mg (n ) Time (h) Fig.1. LVFX plasma concentration aftersingle-dose oraladministration to Japanese subjects (). Table3. LVFXpharmacokineticparametersinsingle-dosestudy Dose (mg) n Cmax (μ g/ml) tmax (h) AUC 7h (μ g h/ml) AUC inf (μ g h/ml) t1/ (h) CLt/F (L/h) Vdz/F (L) CLr (L/h) 5 Japanese mean SD Japanese Caucasian mean SD mean SD Japanese mean SD , Japanese mean SD
5 (A) 15 Y.13X 1.1 Cmax ( g/ml) Dose (mg) 75 1, (B) 15 1 Y.3X 1.17 AUC 7 h ( g h/ml) Dose (mg) 75 1, Fig.. TherelationshipbetweenLVFXpharmacokineticparametersversusdoseafter single-doseoraladministrationtojapanesesubjects(x=dose,y=parameter). (A)Cmax,(B)AUC 7h α β α β β
6 (A) 1 Cumulative urinary excretion ( of dose) 6 5 mg (n ) 5 mg (n ) 75 mg (n ) 1, mg (n ) Time (h) (B) Urinary concentrationg/ml 1,6 1, 1, 1, 6 5 mg (n ) 5 mg (n ) 75 mg (n ) 1, mg (n ) Time (h) Fig.3. (A)CumulativeLVFX urinaryexcretionand(b)lvfx urinaryconcentrationafter single-doseoraladministrationtojapanesesubjects(). II µ µ β β β
7 1 1 Saliva (n ) Plasma (n ) Concentration ( g/ml) Time (h) Fig.. LVFXsalivaryandplasmaconcentrationafter5mgsingle-doseoraladministration tojapanesesubjects(). Plasma concentration ( g/ml) 1 6 Nonelderly (n ) Elderly (n ) Time (h) Fig.5. LVFXplasmaconcentrationin5mgmultiple-dosestudy(). β µ µ µ
8 (A)Day1 Group n Table. LVFXpharmacokineticparametersinmultiple-dosestudy Cmax (μ g/ml) Ch (μ g/ml) tmax (h) AUC h (μ g h/ml) LVFX5mg mean nonelderly SD LVFX5mg mean elderly SD (B)Day7 Group n Cmax (μ g/ml) Ch (μ g/ml) tmax (h) AUC h (μ g h/ml) t1/ (h) CLt/F (L/h) Vdz/F (L) CLr (L/h) LVFX5mg mean nonelderly SD LVFX5mg mean elderly SD µ µ µ µ µ µ µ µ µ µ µ µ Clostridium difficile C. difficile III µ µ
9 1 1 Aerobes (log CFU/g) Mean number of aerobic bacteriae (n ): Enterobacteriaceae, NFGNR, Staphylococcus, Streptococcus, Enterococcus, Bacillus, Corynebacterium, Yeast, Total aerobes 1 1 Anaerobes (log CFU/g) Mean number of anaerobic bacteriae (n ): Bacteroidaceae, Fusobacterium, Lecithinase ( ) Clostridium, Lecithinase ( ) Clostridium, Veillonella, Megasphaera, Bifidobacterium, Eubacterium, Peptococcaceae, Lactobacillus, Total anaerobes Fig.6. ImpactsofLVFXadministrationonintestinalflorainnonelderlyJapaneseinmultiple-dose study. Abscissa 1:daysbeforedose-day1 :day1 day3 3:day day6 :day7 day 5:day1 6:day
10 S
11 µ µ
日本化学療法学会雑誌第57巻第5号
in vitro Key words Streptococcus pneumoniae β Haemophilus influenzae Escherichia coli I Table. Antibacteriallevofloxacinactivityagainstclinicalisolates Organism Year Susceptibility(%)(Numberofstrains)
) Meropenem Chemotherapy (Tokyo) ) panipenem/betamipron Chemotherapy (Tokyo) ) Meropenem Chemotherapy (Toky
2.7 2.7.5 1) 199846410-437 2) UTI ( )UTI ( 3 )Chemotherapy (Tokyo) 1986 34408-441 3) () 199745762-778 4) 1992 5) 199543 6) Chemotherapy (Tokyo) 199139687-689 7) Imipenem/Cilastatin sodium (MK-0787/MK-0791)
日本化学療法学会雑誌第54巻第S-1号
β β β Key words β β I HP- -CD CHR RHC R R R R CHR R R R R RHC R R R CHR R R R RHC CHR R H CH CH Fig.. Structuralformulaofhydroxypropyl-β -cyclodextrin(hp-β -CD). CH n H β β β β Table-. Dosageandadministration(Singleadministrationstudy)
日本化学療法学会雑誌第51巻第2号
piperacillin piperacillin PIPC. g Cmax CL PIPC CL CLR CLNR CL PIPC g g Cmax PIPC Key words: piperacillin Piperacillin PIPC PIPC g g PIPC Cmax g g ml g g ml g g ml T T T PIPC g g T Ccr ml min AUCCmax PIPC
VOL.36 S-I CHEMOTHERAPY Tabl 1 List of healthy male volunteers
VOL.36 S-I CHEMOTHERAPY Tabl 1 List of healthy male volunteers CHEMOTHERAPY MAY 1988 Table 2 Experimental schedule of CS-807 administration and sampling of feces Table 3 Isolation of aerobic and anaerobic
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日本化学療法学会雑誌第61巻第6号
β Moraxella catarrhalis Escherichia coli Citrobacter Klebsiella pneumoniae Enterobacter cloacae Serratia marcescens Proteus Pseudomonas aeruginosa Acinetobacter Bacteroides fragilis β Haemophilus influenzae
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日本化学療法学会雑誌第55巻第S-1号
µ µ Key words Streptococcus pneu- moniae S. pneumoniae µ µ I γ H H C HN F F O N O CO H H C SO H H O Fig.. ChemicalstructureofGRNX. γ γ II Haemophilus influenzae Pseudomonas aeruginosa Streptococcus intermedius
Vol. 36, Special Issue, S 3 S 18 (2015) PK Phase I Introduction to Pharmacokinetic Analysis Focus on Phase I Study 1 2 Kazuro Ikawa 1 and Jun Tanaka 2
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CHEMOTHERAPY DEC Table 1 Antibacterial spectra of T-1982, CTT, CMZ, CTX, CPZ and CEZ 106 CFU/ml Note: P; Peptococcus, S; Streptococcus, G; Gaffk
VOL. 30 S-3 CHEMOTHERAPY imeumoniae, Serratia marcescens, Proteus sp, CHEMOTHERAPY DEC. 1982 Table 1 Antibacterial spectra of T-1982, CTT, CMZ, CTX, CPZ and CEZ 106 CFU/ml Note: P; Peptococcus, S; Streptococcus,
日本化学療法学会雑誌第57巻第1号
In vitro Streptococcus pneumoniae Escherichia coli in vitro Streptococcus pneumoniae Escherichia coli µs. pneumoniae E. coli µ Key words in vitrostreptococcus pneumoniae Escherichia coli Escherichia coli
CHEMOTHERAPY SEPT. 1991
CHEMOTHERAPY SEPT. 1991 VOL. 39 S-3 Table 1. Background of characteristics and allocation of 9 healthy male volunteers in a single-dose study on betamipron Table 2. Background of characteristics and allocation
Clostridium difficile ciprofloxacin, ofloxacin, norfloxacin Bifidobacterium Lactobacillus Lactobacillus Bacteroides fragilis B. fragilis C. difficile
Clostridium difficile ciprofloxacin, ofloxacin, norfloxacin Bifidobacterium Lactobacillus Lactobacillus Bacteroides fragilis B. fragilis C. difficile Key words: temafloxacin, TA-167, Bacteroides fragilis,
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日本化学療法学会雑誌第57巻第6号
Streptococcus pneumoniae Haemophilus influenzae Moraxella catarrhalis S. pneumoniae S. pneumoniae β β H. influenzae S. pneumoniae H. influenzae M. catarrhalis Key words Otalgia Fever Item Crying,Iritation,
CHEMOTHERAPY NOV S. aureus, S. epidermidis, E. coli, K. pgeumoniae, E. cloacae, S. marcescens, P. mirabilis, Proteus, P. aeruginosa Inoculum siz
VOL.33 S-5 CHEMOTHERAPY 381 Fig. 1 Chemical structure of HAPA-B Chemical name 1-N-[(2S)-3-Amino-2-hydroxypropiony1]-4-0-(6-amino- 6-deoxy-a-D-glucopyranosyl)-6-013-deoxy-4-C-methyl- 3-(methylamino)-ƒÀ-L-arabinopyranosyl]-2-deoxystreptamine
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Streptococcus pneumoniae Haemophilus influenzae Moraxella catarrhalis S. pneumoniae H. influenzae M. catarrhalis S. pneumoniae H. influenzae M. catarrhalis S. pneumoniae H. influenzae M. catarrhalis S.
Jan THE JAPANESE JOURNAL OF ANTIBIOTICS XL-1 Table 1. Outline of administering doses, routes and sampling times *: 4 ml/hr/kg Bacillus subtilis
THE JAPANESE JOURNAL OF ANTIBIOTICS XL-1 Jan. 1987 Jan. 1987 THE JAPANESE JOURNAL OF ANTIBIOTICS XL-1 Table 1. Outline of administering doses, routes and sampling times *: 4 ml/hr/kg Bacillus subtilis
日本化学療法学会雑誌第54巻第S-1号
β β Key words β Candida krusei Candida glabrata β I β Drugadministration Baselinecharacteristics Clinicalsymptom Mycologicaltests Plasmadrugconcn Adverseevents Laboratorytests ) -leadecg Clinicalphotograph
CHEMOTHERAPY APR. 1982
VOL.30 S-1 CHEMOTHERAPY Table 1 Dose of CTT and subjects i. v.: Intravenous bolus injection d. i. v.: Intravenous drip infusion i. m.: Intramuscular injection Fig. 1 Schedule for examination of CTT, 1.0g
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日本化学療法学会雑誌第57巻第S-2号
Key words β I Table. Observationandtestschedule Testschedule Observation/Tests Beforetreatment Endoftreatment 5 9days aftercompletion oftreatment 4 6weeks aftercompletion oftreatment Informedconsent Patientbackground
6 12 10661 93100 227213202 222208197 85kg cm 20 64.521 106856142 2 1 4 3 9767 100 35 cm 7747 208198 90kg 23 5828 10661 93100 cm 227213202 10639 61 64.521 85kg 78kg 70kg 61 100 197204.5 cm 15 61
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日本化学療法学会雑誌第64巻第4号
β β Moraxella catarrhalisescherichia colicitrobacter Klebsiella pneumoniaeenterobacter cloacaeserratia marcescens Proteus Providencia Pseudomonas aeruginosaacinetobacter Bacteroides fragilis β β E. colik.
日本化学療法学会雑誌第53巻第S-3号
moxifloxacin in vitro moxifloxacin in vitro 17 9 6 17 11 21 moxifloxacinmflx in vitro cefdinir CFDNclavulanic acidamoxicillincvaampcclarithromycincamclindamycincldm levofloxacinlvfx 1MFLX Clostridium clostridiiformeclostridium
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日本化学療法学会雑誌第54巻第1号
Chlamydophila pneumoniae Chlamydophila psittaci Mycoplasma pneumoniae Legionella pneumophila C. pneumoniae C. psittaci C. pneumoniae C. psittaci M. pneumoniae M. pneumoniae C. psittaci L. pneumophila C.
報告書 H22-2A-09
061-0293 1757 TEL 0133-23-1211 2.0% 0.5% in vitro QOL Quality of Life 1 MCE-400 400 mpa s Duck Algin 350M M/G 0.8 70 80 C 20% 50 C 1.0% 5 C SV-10 5 C 10 ml E TV 20H model E 1 34 R24 1 ml 5 C 30 6 12 30
CHEMOTHERAPY Fig. 1 Chemical structure of CXM-AX
Fig. 1 Chemical structure of CXM-AX NOV. 1986 Fig. 2 Sensitivity distribution of clinical isolates organisms (106 cells/ml) a Smurcus 27 strains d) P.m irabilis 15 strains b Ecol i 27 strains 111.morganii
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CHEMO THER APY Table 1. Background of the volunteers in the phase I clinical trial of ME1207 Table 2. Methods for Phase I clinical trial of ME1207 All doses are expressed in terms of potency as ME1206
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日本化学療法学会雑誌第57巻第4号
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β β β β β Streptococcus pneumoniaehaemophilus influenzaemoraxella catarrhalismycoplasma pneumoniaechlamydia pneumoniae β Key wordsβ mys nilc laci ngis Table. Assessmentschedule Parameters Patientcharacteristics
2.7 臨床概要
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Escherichia coli Enterococcus faecalisstreptococcus agalactiae Klebsiella pneumoniae Staphylococcus epidermidis E. colie. faecalispseudomonas aeruginosa K. pneumoniae S. agalactiae E. coli E. coli μ p
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CHEMOTHERAPY VOL.41 S-2 Laboratory and clinical evaluation of teicoplanin CHEMOTHERAPY AUG. 1993 VOL.41 S-2 Laboratory and clinical evaluation of teicoplanin Table 1. Comparative in vitro activity of teicoplanin
Vol. 4, No
1 0.005 71 2 0.005 72 3 0.005 73 4 0.005 74 5 0.005 KRM 75 6 0.005 76 7 0.005 77 8 0.005 78 9 0.005 79 10 0.005 80 11 0.005 TS 81 12 0.005 TOA 82 13 0.005 83 14 0.005 84 15 0.005 NS 85 16 0.005 86 17 0.005
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日本化学療法学会雑誌第56巻第S-1号
Key words Streptococcus pneumoniae µ µ H F Cl H H N N H N F COOH O Fig.1. Sitafloxacinstructure. I γ S. pneumoniae Haemophilus influenzae Table1. Observationandtestschedule Observation/Tests Informedconsent
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CHEMOTHERAPY MAY 1988
VOL. 36 NO. 5 Table 1. Subjects studied B. W. Body weight B. H. Body height Abbreviations Ccr Endogenous creatinine clearance PSP Phenolsulfonphthalein test for 15 min BUN Blood urea nitrogen Scr Serum
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