Evaluation of Pharmacokinetic Parameters of Cibenzoline after Administration of a Single Oral Dose in Healthy Volunteers.

The pharmacokinetics (PK) of ordinary tablets and sustained release capsules of diltiazem hydrochloride in human clinical trials had been studied. The PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules, a new dosage form, has not been reported, although it is very important to clinical use. In this paper, we investigated the PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules and the food influence in Chinese healthy volunteers. The PK parameters indicated that the diltiazem hydrochloride delay-onset sustained-release pellet capsules appeared marked characteristics of delayed and controlled release. An opened-label, randomized and parallel clinical trial was conducted in 36 Chinese healthy volunteers with single oral dose (90 mg, 180 mg or 270 mg) and a multiple oral dose (90 mg d-1×6 d) administration. The effect of food on the PK of one single oral dose (360 mg) was investigated in 24 healthy Chinese volunteers. Plasma diltiazem concentration was determined by reversed-phase high-performance liquid chromatography (RP-HPLC) and the main pharmacokinetic parameters were analyzed by PKSolver (Ver 2.0). All clinical studies were conducted in the Clinical Pharmacological Center (No. JDX1999064) of Xiangya Hospital Affiliated Central South University, China. The PK parameters suggested that the new formulation had marked characteristics of delayed and controlled release of diltiazem, and food intake did not alter significantly diltiazem pharmacokinetic parameters.

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Faculty Opinions recommendation of Decreased [18F]MPPF binding potential in the dorsal raphe nucleus after a single oral dose of fluoxetine: a positron-emission tomography study in healthy volunteers.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1115675.571742 ◽

2008 ◽

Author(s):

Ahmad Hariri ◽

Patrick Fisher

Keyword(s):

Positron Emission Tomography ◽

Oral Dose ◽

Healthy Volunteers ◽

Single Oral Dose ◽

Dorsal Raphe Nucleus ◽

Raphe Nucleus ◽

Emission Tomography ◽

Positron Emission Tomography Study ◽

Binding Potential ◽

Positron Emission

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Urinary Excretion and Bactericidal Activities of a Single Oral Dose of 400 Milligrams of Fleroxacin versus a Single Oral Dose of 800 Milligrams of Pefloxacin in Healthy Volunteers

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.42.7.1659 ◽

1998 ◽

Vol 42 (7) ◽

pp. 1659-1665 ◽

Cited By ~ 15

Author(s):

Kurt G. Naber ◽

Ursula Theuretzbacher ◽

Martina Kinzig ◽

Orlin Savov ◽

Fritz Sörgel

Keyword(s):

Oral Dose ◽

Healthy Volunteers ◽

Single Oral Dose ◽

E Coli ◽

Wide Range ◽

The Mean ◽

Bactericidal Activities ◽

Tract Infections ◽

Time Kill ◽

Randomized Crossover Study

ABSTRACT Twelve healthy volunteers participated in this randomized crossover study to compare the concentrations and recovery levels of fleroxacin and pefloxacin in urine and to assess their bactericidal activities against 12 strains of urinary pathogens with different susceptibilities over a wide range of MICs. The volunteers received a single oral dose of 400 mg of fleroxacin or 800 mg of pefloxacin. The mean cumulative renal excretion of unchanged fleroxacin,N-demethyl-fleroxacin, and N-oxide-fleroxacin accounted for 67, 7, and 6% of the total dose, respectively. The total urinary recovery of pefloxacin and the active metabolite norfloxacin was 34%. In the time-kill and the urinary bactericidal titer (UBT) studies, only the subjects’ urine not supplemented with broth was used. With most tested organisms and both quinolones it took more than 8 h to achieve a reduction in CFU of 99.9% (3 log units). Overall, there was a good correlation between UBTs and MICs for the strains. Against Escherichia coli ATCC 25922 the median UBTs were similar for both antibiotics and at least 1:8 for 96 h; against the E. coli strain for which the MIC was 0.5 μg/ml the UBT was at least 1:4 for 48 h. The UBTs of both drugs against Klebsiella pneumoniae were at least 1:16 for 72 h. The UBTs for Staphylococcus aureus (the MIC for which was 16 μg/ml) of both antibiotics were low, and in some of the samples, no bactericidal titers were observed. UBTs for Proteus mirabilis of pefloxacin are significantly higher than those of fleroxacin. For Pseudomonas aeruginosa the median UBTs were present for the 24-to-48-h interval. The same is true forEnterococcus faecalis. Against Staphylococcus saprophyticus, UBTs were present for at least 48 h with both quinolones. Overall, a single oral dose of 400 mg of fleroxacin exhibits UBTs comparable to those of 800 mg of pefloxacin. Therefore, it may be expected that half of the dose of fleroxacin gives comparable results in the treatment of urinary tract infections; this should be substantiated in comparative clinical trials.

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C14.4 Concentrations in plasma, urinary excretion, and bactericidal activity of levofloxacin (500) versus those of ciprofloxacin (500 milligrams) in healthy volunteers receiving a single oral dose

International Journal of Antimicrobial Agents ◽

10.1016/s0924-8579(05)80279-1 ◽

2005 ◽

Vol 26 ◽

pp. S98

Keyword(s):

Oral Dose ◽

Urinary Excretion ◽

Healthy Volunteers ◽

Single Oral Dose ◽

Bactericidal Activity

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Pharmacokinetic (PK) study of a single oral dose of NEPA in Chinese healthy volunteers (HVs)

Annals of Oncology ◽

10.1093/annonc/mdx388.015 ◽

2017 ◽

Vol 28 ◽

pp. v548 ◽

Cited By ~ 1

Author(s):

R. Chen ◽

S. Chessari ◽

C. Lanzarotti ◽

A. Bernareggi ◽

P. Hu

Keyword(s):

Oral Dose ◽

Healthy Volunteers ◽

Single Oral Dose

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Urinary Bactericidal Activity of Extended-Release Ciprofloxacin (1,000 Milligrams) versus Levofloxacin (500 Milligrams) in Healthy Volunteers Receiving a Single Oral Dose

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00477-06 ◽

2006 ◽

Vol 50 (11) ◽

pp. 3947-3949 ◽

Cited By ~ 14

Author(s):

Florian M. E. Wagenlehner ◽

Martina Kinzig-Schippers ◽

Uwe Tischmeyer ◽

Christine Wagenlehner ◽

Fritz Sörgel ◽

...

Keyword(s):

Oral Dose ◽

Healthy Volunteers ◽

Single Oral Dose ◽

Bactericidal Activity ◽

Proteus Mirabilis ◽

Extended Release

ABSTRACT Twelve volunteers received a single oral dose of 1,000 mg extended-release (XR) ciprofloxacin versus 500 mg levofloxacin to assess urinary bactericidal titers (UBTs) against common uropathogens. Areas under UBT-time curves were significantly larger for Proteus mirabilis with XR ciprofloxacin and for staphylococci with levofloxacin.

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