Unusual Pharmacokinetics

Wagner, John G.

doi:10.1007/978-1-4613-2799-8_16

Cited by 7 publications

(3 citation statements)

References 12 publications

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“…A similar double‐peak phenomenon has been observed for some other oral drugs 38–40. Several mechanisms have been proposed to account for the phenomenon: enterohepatic recycling,41 discontinued or variable absorption along the gastrointestinal tract,42 and variable gastric emptying 43. Enterohepatic recycling could be ruled out as the main cause of the secondary peak in the acitretin plasma concentration–time curve, because this phenomenon did not appear after intravenous and oral administration of the acitretin–cyclodextrin complex solution.…”

Section: Discussionmentioning

confidence: 55%

Biopharmaceutics of β-cyclodextrin derivative-based formulations of acitretin in sprague-dawley rats

Liu

Lin

Chan

et al. 2004

Journal of Pharmaceutical Sciences

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Section: Discussionmentioning

confidence: 55%

Biopharmaceutics of β-cyclodextrin derivative-based formulations of acitretin in sprague-dawley rats

Liu

Lin

Chan

et al. 2004

Journal of Pharmaceutical Sciences

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“…Another transporter(s) may be involved in oseltamivir absorption because one‐third of the active transport of oseltamivir was not inhibited by excess dipeptides in Caco‐2 cells 8. The cause of the double‐peak phenomenon is not fully understood, but several possible explanations have been proposed: biphasic gastric emptying,22 enterohepatic ciculation,23 and two different absorption sites 24. The last one may be related to regional differences in expression of the specific transporter(s) as previously speculated in the case of P‐glycoprotein 25.…”

Section: Discussionmentioning

confidence: 99%

Effect of Milk on the Pharmacokinetics of Oseltamivir in Healthy Volunteers

Morimoto

Kishimura

Nagami

et al. 2011

Journal of Pharmaceutical Sciences

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“…The plasma profiles after oral VRC dosing were fitted to a 1-compartment model with first-order absorption and MM elimination [12] :…”

Section: Methodsmentioning

confidence: 99%

An Alternative Approach to Determine Oral Bioavailability of Drugs That Follow Michaelis-Menten Elimination: A Case Study with Vorizonazole

Araújo

Silva²,

Costa³

2010

Pharmacology

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Background/Aims: The determination of oral bioavailability of drugs which follow nonlinear pharmacokinetics is difficult and few methods are available. In this work, an alternative approach to determine oral bioavailability of voriconazole (VRC), used as a model drug, is presented. Methods: VRC pharmacokinetics was investigated in Wistar rats after p.o. (40 mg/kg) and i.v. administration (2.5, 5 and 10 mg/kg). VRC elimination showed saturation in all doses investigated, except the lower i.v. dose in which case a 3-compartment model with linear elimination adequately fitted the data. Data for the 2 higher i.v. doses were best described by a 3-compartment model with Michaelis-Menten elimination. A 1-compartment disposition with a saturable metabolic elimination model described the oral profile. VRC absolute oral bioavailability was determined by simultaneous fitting of the i.v. and oral profiles. Results: The Michaelis constant and the maximum velocity estimated after 5 and 10 mg/kg i.v. dosing were 0.54 ± 0.25 µg/ml and 2.53 ± 0.54 µg/h, and 0.62 ± 0.12 µg/ml and 2.74 ± 0.84 µg/h, respectively. VRC oral bioavailability was determined to be 82.8%. Conclusion: The approach presented is an alternative for determining the bioavailability of drugs with similar nonlinear behavior.

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Unusual Pharmacokinetics

Cited by 7 publications

References 12 publications

Biopharmaceutics of β-cyclodextrin derivative-based formulations of acitretin in sprague-dawley rats

Biopharmaceutics of β-cyclodextrin derivative-based formulations of acitretin in sprague-dawley rats

Effect of Milk on the Pharmacokinetics of Oseltamivir in Healthy Volunteers

An Alternative Approach to Determine Oral Bioavailability of Drugs That Follow Michaelis-Menten Elimination: A Case Study with Vorizonazole

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