Examination of two sustained release nifedipine preparations in humans and in pigs

Kostewicz, Edmund; Sansom, Lloyd; Fishlock, Richard; Morella, Angelo; Kuchel, Timothy R.

doi:10.1016/s0928-0987(96)00173-x

Cited by 5 publications

(2 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…investigated nifedipine sustained formulations in pigs, as described in Table , the obtained data were similar to data from a previously performed human study. Kostewicz et al . came to the conclusion that the obtained results suggested that the pig can be a useful model in differentiating the release profiles of nifedipine for the fed state in humans.…”

Section: The Use Of the Pig Model For Assessing In Vivo Performance Omentioning

confidence: 99%

“…The distinguishing feature of PBPK models, relative to empirical computational models, is the application of prior physiological knowledge in the mechanistic mapping of model compartments and in the processes that determine absorption . This physiological knowledge, incorporating parameters such as gastrointestinal transit, pH and luminal volume, is combined with physiochemical measurements, for example, dissociation constants and partition coefficients, and in vitro measurements, such as solubility and dissolution rates and enzymatic degradation kinetics, into the PBPK model to provide a simulated PK profile .…”

Section: Role Of In Vitro and In Silico Models For Predicting The Suimentioning

confidence: 99%

See 1 more Smart Citation

The pig as a preclinical model for predicting oral bioavailability and in vivo performance of pharmaceutical oral dosage forms: a PEARRL review

Henze

Koehl

O’Shea

et al. 2019

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

Objectives In pharmaceutical drug development, preclinical tests in animal models are essential to demonstrate whether the new drug is orally bioavailable and to gain a first insight into in vivo pharmacokinetic parameters that can subsequently be used to predict human values. Despite significant advances in the development of bio-predictive in vitro models and increasing ethical expectations for reducing the number of animals used for research purposes, there is still a need for appropriately selected pre-clinical in vivo testing to provide guidance on the decision to progress to testing in humans. The selection of the appropriate animal models is essential both to maximise the learning that can be obtained from such experiments and to avoid unnecessary testing in a range of species. Key findings The present review, provides an insight into the suitability of the pig model for predicting oral bioavailability in humans, by comparing the conditions in the GIT. It also contains a comparison between the bioavailability of compounds dosed to both humans and pigs, to provide an insight into the relative correlation and examples on why a lack of correlation may be observed. Summary While there is a general trend towards predicting human bioavailability from pig data, there is considerable variability in the data set, most likely reflecting species specific differences in individual drug metabolism. Nonetheless, the correlation between pigs vs. humans was comparable to that reported for dogs vs. humans. The presented data demonstrate the suitability of the pig as a preclinical model to predict bioavailability in human.

show abstract

Section: The Use Of the Pig Model For Assessing In Vivo Performance Omentioning

confidence: 99%

Section: Role Of In Vitro and In Silico Models For Predicting The Suimentioning

confidence: 99%