New Calculation method of mean Total Body Clearance of Drugs and its Application to Dosage Regimens

Chiou, Win L.

doi:10.1002/jps.2600690125

Cited by 140 publications

(87 citation statements)

References 18 publications

(4 reference statements)

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“…The harmonic mean method was employed to calculate the mean values of V ss (Chiou, 1979), terminal half-life (Eatman et al, 1977), and CL (Chiou, 1980). Glomerular filtration rate was calculated by measuring creatinine clearance (CL CR ) assuming that kidney function was stable during the 8-hr experimental period.…”

Section: Methodsmentioning

confidence: 99%

Effects of Acute Renal Failure on the Pharmacokinetics of Chlorzoxazone in Rats

Moon¹,

Lee²,

Chung³

et al. 2003

Drug Metab Dispos

111

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ABSTRACT:The purpose of this study is to report the changes of CYP2E1, CYP1A2, CYP2B1/2, CYP2C11, CYP3A23, and CYP3A2 expression and pharmacokinetics and tissue distribution of chlorzoxazone (CZX) and 6-hydroxychlorzoxazone (OH-CZX) in rats with acute renal failure induced by uranyl nitrate (U-ARF), and the role of CYP3A23 and CYP3A2 in the formation of OH-CZX in rats with U-ARF. In rats with U-ARF, CYP2C11 decreased to 20% of control, whereas CYP2E1 and CYP3A23 increased 2.3 and 4 times, respectively, compared with control. But expression of CYP1A2 and CYP2B1/2 was not changed by U-ARF. After i.v. administration of CZX at a dose of 20 mg/kg to rats with U-ARF, the areas under the plasma concentration-time curve from time 0 to time infinity (AUCs) of CZX and OH-CZX were significantly smaller and greater, respectively, than those in control rats. In rats with U-ARF, CZX was below the detection limit at 120 min in all rat tissues studied, whereas it was detected in all tissues of control rats at both 30 and 120 min. However, in control rats, OH-CZX was below the detection limit at both 30 and 120 min in all rat tissues except kidney, whereas it was detected in all tissues of rats with U-ARF at both 30 and 120 min. Based on results from supporting experiments with DDT and 2,2-bis(4-chlorophenyl)1,1-dichloroethylene treatment of rats, the contribution of CYP3A23 and CYP3A2 to the enhanced formation of OH-CZX in rats with U-ARF is likely to be negligible.

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Section: Methodsmentioning

confidence: 99%

Effects of Acute Renal Failure on the Pharmacokinetics of Chlorzoxazone in Rats

Moon¹,

Lee²,

Chung³

et al. 2003

Drug Metab Dispos

111

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“…Assuming complete absorption, apparent oral clearance (CL) was the quotient of dose divided by total AUC (Wilkinson & Shand, 1975 (Chiou, 1980). Differences among treatments were determined by analysis of variance.…”

Section: Methodsmentioning

confidence: 99%

The paradoxical effect of cimetidine and ranitidine on glibenclamide pharmacokinetics and pharmacodynamics.

Kubacka

Antal

Juhl

1987

Brit J Clinical Pharma

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1 The potential interactions between H2-receptor antagonists, cimetidine and ranitidine, and glibenclamide were studied in 15 non-smoking male volunteers. 2 The study consisted of six treatment phases. Treatment A (3 h oral glucose tolerance test) consisted of 75 g dextrose in 300 ml carbonated water. Treatment B consisted of one 5 mg tablet of glibenclamide in addition to a glucose tolerance test. Treatment C, cimetidine 300 mg orally four times daily for 4 days and Treatment D, ranitidine 150 mg orally twice daily for 4 days were administered in a randomized, crossover fashion. On day 3 of Treatments C and D, subjects received an oral glucose tolerance test. On day 4 of Treatments C and D, subjects received 5 mg of glibenclamide in addition to cimetidine (Treatment E) or ranitidine (Treatment F) and an oral glucose tolerance test. 3 Compared with the control treatment, cimetidine increased the glibenclamide AUC (973 vs 710 ng ml-' h), but during ranitidine dosing glibenclamide AUC (726 ng ml-' h) was not significantly different from the control. 4 Apparent oral glibenclamide clearance decreased from 8.25 1 h-1 under the control treatment to 6.01 h-1 following cimetidine but was unchanged during ranitidine (7.971 h-1). 5 Plasma glucose concentrations were unexpectedly higher when glibenclamide was administered with cimetidine or ranitidine (glucose AUC 237 mg dl-1 h, 228 mg dl-1 h) when compared with glibenclamide administered alone (195 mg dl-1 h, P < 0.0001). Plasma insulin concentrations were significantly elevated when H2-receptor antagonists and glibenclamide were administered concurrently. 6 Plasma glucose concentrations for cimetidine and ranitidine were significantly elevated when compared to the control glucose tolerance test (G1T). Insulin plasma concentrations were not increased. 7 The potential for this interaction should be considered in diabetic patients treated with glibenclamide therapy.

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“…The harmonic mean method was employed to calculate the mean values for V ss (4), terminal half-life (t 1/2 ) (7), and each clearance (5).…”

Section: Methodsmentioning

confidence: 99%

Dose-Dependent Pharmacokinetics of Itraconazole after Intravenous or Oral Administration to Rats: Intestinal First-Pass Effect

Shin

Choi

Kim

et al. 2004

Antimicrob Agents Chemother

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The dose-dependent pharmacokinetics of itraconazole after intravenous (10, 20, or 30 mg/kg) and oral (10, 30, or 50 mg/kg) administration and the first-pass effects of itraconazole after intravenous, intraportal, intragastric, and intraduodenal administration at a dose of 10 mg/kg were evaluated in rats. After intravenous administration at a dose of 30 mg/kg, the area under the plasma concentration-time curve from time zero to infinity (AUC 0-ؕ ) was significantly greater than those at 10 and 20 mg/kg (1,090, 1,270, and 1,760 g ⅐ min/ml for 10, 20, and 30 mg/kg, dose-normalized at 10 mg/kg). After oral administration, the AUC 0-ؕ was significantly different for three oral doses (380, 687, and 934 g ⅐ min/ml for 10, 30, and 50 mg/kg, respectively, dosenormalized at 10 mg/kg). The extent of absolute oral bioavailability (F) was 34.9% after an oral dose at 10 mg/kg. The AUC 0-ؕ (or AUC 0-8 h ) values were comparable between intravenous and intraportal administration and between intragastric and intraduodenal administration, suggesting that the hepatic and gastric first-pass effects were almost negligible in rats. However, the AUC 0-8 h values after intraduodenal and intragastric administration were significantly smaller than that after intraportal administration, approximately 30%, suggesting that the intestinal first-pass effect was approximately 70% of that of an oral dose of 10 mg/kg. The low F after oral administration of itraconazole at a dose of 10 mg/kg could be mainly due to the considerable intestinal first-pass effect.The pharmacokinetics of itraconazole after oral administration to humans (10-12), rats (11,22,31), and rabbits, cats, and dogs (11) have been reported; however, data on the pharmacokinetics after intravenous administration to humans (12), dogs (11), and rats (22, 31) are scarce. It has been reported (12) that after oral administration of itraconazole to humans, the values for the area under the plasma concentration-time curve from time zero to infinity (AUC 0-ϱ ) for the drug were dose dependent (increased in proportion to dose increases); 50, 100, and 200 mg by capsule after a meal and 100 and 200 mg by capsule after breakfast. However, the dose-dependent pharmacokinetics of itraconazole after intravenous administration and the first-pass effects of the drug have not been reported. It has been reported (31) that the hepatic first-pass effect of itraconazole was estimated to be 18.5% in rats.The purpose of this paper is to report the dose-dependent pharmacokinetics of itraconazole after intravenous (at doses of 10, 20, and 30 mg/kg) and oral (at doses of 10, 30, and 50 mg/kg) administration to rats and the intestinal first-pass effect of itraconazole after intravenous, intraportal, intragastric, and intraduodenal administration (at a dose of 10 mg/kg) to rats. MATERIALS AND METHODSChemicals. Sporanox intravenous solution (10 mg/ml as itraconazole as a solution in hydroxylpropyl-␤-cyclodextrin [HP-␤-CD], sorbitol, propylene glycol, HCl, NaOH, and water for injection; lot no. 01-D01A-IW), Spor...

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New Calculation method of mean Total Body Clearance of Drugs and its Application to Dosage Regimens

Cited by 140 publications

References 18 publications

Effects of Acute Renal Failure on the Pharmacokinetics of Chlorzoxazone in Rats

Effects of Acute Renal Failure on the Pharmacokinetics of Chlorzoxazone in Rats

The paradoxical effect of cimetidine and ranitidine on glibenclamide pharmacokinetics and pharmacodynamics.

Dose-Dependent Pharmacokinetics of Itraconazole after Intravenous or Oral Administration to Rats: Intestinal First-Pass Effect

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