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

Edmund Kostewicz, Lloyd Sansom, Richard Fishlock, Angelo Morella, Timothy Kuchel

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

In the present study, the ability of the pig to discriminate the in-vivo release characteristics of two 60 mg sustained release nifedipine formulations, an experimental formulation (Faulding) and Procardia XL (Pfizer), under both fasting and fed conditions was assessed. These forms had previously been evaluated in humans, where an alteration in the release profile of the experimental formulation was noted following administration with food. 12 Large White female pigs (mean weight 38 kg) were divided into two groups and each group was orally administered one of the two products under both fasting and fed conditions. The mean area under the plasma concentration-time curve was not significantly different between the formulations under both conditions. The mean maximum observed plasma concentration (C(max)) was significantly higher for the experimental formulation when compared against Procardia XL under both fasting (P < 0.05) and fed (P < 0.05) conditions. Peak concentrations were achieved at approximately 6 h for the experimental formulation and 12 h for Procardia XL. The time for which the plasma concentration exceeded 75% of C(max) was approximately 2.5-fold greater for Procardia XL than for the experimental formulation. There were no significant food effects on the relative bioavailability nor release profiles of the two formulations. The results obtained suggest that the pig may be a useful model in differentiating the release profiles of nifedipine formulations for the fed state in humans as results were similar to the human-fed study, but dissimilar to the human-fasted study.

LanguageEnglish
Pages351-357
Number of pages7
JournalEuropean Journal of Pharmaceutical Sciences
Volume4
Issue number6
DOIs
Publication statusPublished - Nov 1996

Keywords

  • Bioavailability
  • Nifedipine
  • Pig
  • Sustained release

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Kostewicz, Edmund ; Sansom, Lloyd ; Fishlock, Richard ; Morella, Angelo ; Kuchel, Timothy. / Examination of two sustained release nifedipine preparations in humans and in pigs. In: European Journal of Pharmaceutical Sciences. 1996 ; Vol. 4, No. 6. pp. 351-357.
@article{e1900183fc54487db9cc93d85456216c,
title = "Examination of two sustained release nifedipine preparations in humans and in pigs",
abstract = "In the present study, the ability of the pig to discriminate the in-vivo release characteristics of two 60 mg sustained release nifedipine formulations, an experimental formulation (Faulding) and Procardia XL (Pfizer), under both fasting and fed conditions was assessed. These forms had previously been evaluated in humans, where an alteration in the release profile of the experimental formulation was noted following administration with food. 12 Large White female pigs (mean weight 38 kg) were divided into two groups and each group was orally administered one of the two products under both fasting and fed conditions. The mean area under the plasma concentration-time curve was not significantly different between the formulations under both conditions. The mean maximum observed plasma concentration (C(max)) was significantly higher for the experimental formulation when compared against Procardia XL under both fasting (P < 0.05) and fed (P < 0.05) conditions. Peak concentrations were achieved at approximately 6 h for the experimental formulation and 12 h for Procardia XL. The time for which the plasma concentration exceeded 75{\%} of C(max) was approximately 2.5-fold greater for Procardia XL than for the experimental formulation. There were no significant food effects on the relative bioavailability nor release profiles of the two formulations. The results obtained suggest that the pig may be a useful model in differentiating the release profiles of nifedipine formulations for the fed state in humans as results were similar to the human-fed study, but dissimilar to the human-fasted study.",
keywords = "Bioavailability, Nifedipine, Pig, Sustained release",
author = "Edmund Kostewicz and Lloyd Sansom and Richard Fishlock and Angelo Morella and Timothy Kuchel",
year = "1996",
month = "11",
doi = "10.1016/S0928-0987(96)00173-X",
language = "English",
volume = "4",
pages = "351--357",
journal = "European Journal of Pharmaceutical Sciences",
issn = "0928-0987",
publisher = "Elsevier",
number = "6",

}

Examination of two sustained release nifedipine preparations in humans and in pigs. / Kostewicz, Edmund; Sansom, Lloyd; Fishlock, Richard; Morella, Angelo; Kuchel, Timothy.

In: European Journal of Pharmaceutical Sciences, Vol. 4, No. 6, 11.1996, p. 351-357.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Examination of two sustained release nifedipine preparations in humans and in pigs

AU - Kostewicz, Edmund

AU - Sansom, Lloyd

AU - Fishlock, Richard

AU - Morella, Angelo

AU - Kuchel, Timothy

PY - 1996/11

Y1 - 1996/11

N2 - In the present study, the ability of the pig to discriminate the in-vivo release characteristics of two 60 mg sustained release nifedipine formulations, an experimental formulation (Faulding) and Procardia XL (Pfizer), under both fasting and fed conditions was assessed. These forms had previously been evaluated in humans, where an alteration in the release profile of the experimental formulation was noted following administration with food. 12 Large White female pigs (mean weight 38 kg) were divided into two groups and each group was orally administered one of the two products under both fasting and fed conditions. The mean area under the plasma concentration-time curve was not significantly different between the formulations under both conditions. The mean maximum observed plasma concentration (C(max)) was significantly higher for the experimental formulation when compared against Procardia XL under both fasting (P < 0.05) and fed (P < 0.05) conditions. Peak concentrations were achieved at approximately 6 h for the experimental formulation and 12 h for Procardia XL. The time for which the plasma concentration exceeded 75% of C(max) was approximately 2.5-fold greater for Procardia XL than for the experimental formulation. There were no significant food effects on the relative bioavailability nor release profiles of the two formulations. The results obtained suggest that the pig may be a useful model in differentiating the release profiles of nifedipine formulations for the fed state in humans as results were similar to the human-fed study, but dissimilar to the human-fasted study.

AB - In the present study, the ability of the pig to discriminate the in-vivo release characteristics of two 60 mg sustained release nifedipine formulations, an experimental formulation (Faulding) and Procardia XL (Pfizer), under both fasting and fed conditions was assessed. These forms had previously been evaluated in humans, where an alteration in the release profile of the experimental formulation was noted following administration with food. 12 Large White female pigs (mean weight 38 kg) were divided into two groups and each group was orally administered one of the two products under both fasting and fed conditions. The mean area under the plasma concentration-time curve was not significantly different between the formulations under both conditions. The mean maximum observed plasma concentration (C(max)) was significantly higher for the experimental formulation when compared against Procardia XL under both fasting (P < 0.05) and fed (P < 0.05) conditions. Peak concentrations were achieved at approximately 6 h for the experimental formulation and 12 h for Procardia XL. The time for which the plasma concentration exceeded 75% of C(max) was approximately 2.5-fold greater for Procardia XL than for the experimental formulation. There were no significant food effects on the relative bioavailability nor release profiles of the two formulations. The results obtained suggest that the pig may be a useful model in differentiating the release profiles of nifedipine formulations for the fed state in humans as results were similar to the human-fed study, but dissimilar to the human-fasted study.

KW - Bioavailability

KW - Nifedipine

KW - Pig

KW - Sustained release

UR - http://www.scopus.com/inward/record.url?scp=0030297081&partnerID=8YFLogxK

U2 - 10.1016/S0928-0987(96)00173-X

DO - 10.1016/S0928-0987(96)00173-X

M3 - Article

VL - 4

SP - 351

EP - 357

JO - European Journal of Pharmaceutical Sciences

T2 - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

SN - 0928-0987

IS - 6

ER -