Pharmacokinetics of cimetidine in dogs after oral administration of cimetidine tablets

Traon, G. Le; Burgaud, S.; Horspool, L. J. I.

doi:10.1111/j.1365-2885.2008.01026.x

Cited by 7 publications

(3 citation statements)

References 12 publications

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“…Four drugs had conflicting data and therefore were listed twice to include both sets of data. For two drugs (38,48), publications addressing BCS biowaivers for human formulations had data that conflicted with an official web site (27) or other published data (3)(4)(5)(6). These drugs were listed twice to accommodate both data.…”

Section: Resultsmentioning

confidence: 99%

Applying Biopharmaceutical Classification System (BCS) Criteria to Predict Oral Absorption of Drugs in Dogs: Challenges and Pitfalls

Papich

Martinez

2015

AAPS J

112

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Abstract. The Biopharmaceutical Classification System (BCS) has been a prognostic tool for assessing the potential effects of formulation on the human drug oral bioavailability. When used in conjunction with in vitro dissolution tests, the BCS can support the prediction of in vivo product performance and the development of mechanistic models that support formulation assessments through the generation of Bwhat if^scenarios. To date, the applicability of existing human BCS criteria has not been evaluated in dogs, thereby limiting its use in canine drug development. Therefore, we examined 50 drugs for which absolute bioavailability (F) was available both in dogs and humans. The drugs were also evaluated for any potential association between solubility (calculated from the dose number, Do) or lipophilicity (LogP) and F in dogs. In humans, solubility is determined in 250 mL of fluid. However, the appropriate volume for classifying drug solubility in dogs has not been established. In this analysis, the estimated volume of a water flush administered to fasted dogs (6 mL) and a volume of 250 mL scaled to a Beagle dog (35 mL) were examined. In addition, in humans, a Do value greater than 1.0 is used to define a compound as highly soluble and a LogP value greater than 1.72 as high permeability. These same criteria were applied for defining highly soluble and highly permeable in dogs. Whether using 35 or 6 mL to determine Do, the canine solubility classification remained unchanged for all but seven compounds. There were no clear associations between a drug's F in dogs and humans or between the canine value of F and either its human BCS classification, its LogP value, or the canine Do estimate. There was a tendency for those drugs with canine values of F equal to or greater than 80% to have LogP values equal to or greater than 1.0. Exceptions to this observation tended to be those compounds known to be absorbed via mechanisms other than passive diffusion (e.g., via transporters or paracellular transporters). Although there are limitations to the approach used in this study, the results of our assessment strongly suggest that the human BCS classification system requires substantial modification before it can be reliably applied to dogs.

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Section: Resultsmentioning

confidence: 99%

Applying Biopharmaceutical Classification System (BCS) Criteria to Predict Oral Absorption of Drugs in Dogs: Challenges and Pitfalls

Papich

Martinez

2015

AAPS J

112

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“…In contrast, several substances should be applied to fasted animals, as feeding significantly decreases absorption. Examples are ampicillin (Kung et al, 1995, Kluge et al, 1999, oxytetracycline, chlortetracycline (Giguere et al 2006) or cimetidine (Le Traon, 2009). Drug formulations can also influence oral bioavailability.…”

Section: Differences In Oral and Parenteral Absorption In Different Amentioning

confidence: 99%

Comparative Veterinary Pharmacokinetics

Jerzsele¹

2012

Readings in Advanced Pharmacokinetics - Theory, Methods and Applications

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“…1, (15,25,(74)(75)(76)(77)(78)(79)(80)(81) and references included therein). With the CYP450 substrates, excepting tacrolimus (F a ∼15%), most of the drugs assessed are believed to exhibit good oral absorption in man (≥80% (25) data supplemental).…”

Section: Is the Extent Of Intestinal Metabolism Predictable And Can Imentioning

confidence: 99%

Gut Wall Metabolism. Application of Pre-Clinical Models for the Prediction of Human Drug Absorption and First-Pass Elimination

Jones

Hatley

Ungell

et al. 2016

AAPS J

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Abstract. Quantifying the multiple processes which control and modulate the extent of oral bioavailability for drug candidates is critical to accurate projection of human pharmacokinetics (PK). Understanding how gut wall metabolism and hepatic elimination factor into first-pass clearance of drugs has improved enormously. Typically, the cytochrome P450s, uridine 5′-diphosphate-glucuronosyltransferases and sulfotransferases, are the main enzyme classes responsible for drug metabolism. Knowledge of the isoforms functionally expressed within organs of first-pass clearance, their anatomical topology (e.g. zonal distribution), protein homology and relative abundances and how these differ across species is important for building models of human metabolic extraction. The focus of this manuscript is to explore the parameters influencing bioavailability and to consider how well these are predicted in human from animal models or from in vitro to in vivo extrapolation. A unique retrospective analysis of three AstraZeneca molecules progressed to first in human PK studies is used to highlight the impact that species differences in gut wall metabolism can have on predicted human PK. Compared to the liver, pharmaceutical research has further to go in terms of adopting a common approach for characterisation and quantitative prediction of intestinal metabolism. A broad strategy is needed to integrate assessment of intestinal metabolism in the context of typical DMPK activities ongoing within drug discovery programmes up until candidate drug nomination.

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Pharmacokinetics of cimetidine in dogs after oral administration of cimetidine tablets

Cited by 7 publications

References 12 publications

Applying Biopharmaceutical Classification System (BCS) Criteria to Predict Oral Absorption of Drugs in Dogs: Challenges and Pitfalls

Applying Biopharmaceutical Classification System (BCS) Criteria to Predict Oral Absorption of Drugs in Dogs: Challenges and Pitfalls

Comparative Veterinary Pharmacokinetics

Gut Wall Metabolism. Application of Pre-Clinical Models for the Prediction of Human Drug Absorption and First-Pass Elimination

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