In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers

Samar Al-Behaisi, I. Antal, György Morovján, József Szúnyog, Sándor Drabant, Sylvia Marton, I. Klebovich

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

The in vitro dissolution profiles of deramciclane 30 mg film-coated tablets, an acid-labile new 5-HT receptor antagonist, were studied under simulated fasting and fed conditions. Artificial gastric juice with pH adjusted to that of fasting conditions was applied either alone or after adding different dietary components. The use of the USP dissolution apparatus II (paddle method) showed that the presence of dietary components has markedly affected the amount of unchanged drug dissolved. As a similar tendency had been observed in food-effect studies in healthy volunteers, cumulative area under the curve (AUCcum) for both fed and fasting conditions were compared and an in vitro-in vivo correlation (IVIVC) was evaluated. A linear relationship was established between logarithmic in vivo blood sampling time and in vitro dissolution time assigned to equal AUCcum ratios (AUCcum, fed/AUCcum, fasting). Despite its limitations, in vitro modelling of in vivo conditions might help provide a base for predicting in vivo drug behaviour.

Original languageEnglish
Pages (from-to)157-162
Number of pages6
JournalEuropean Journal of Pharmaceutical Sciences
Volume15
Issue number2
DOIs
Publication statusPublished - 2002

Fingerprint

Tablets
Fasting
Healthy Volunteers
Food
Serotonin Antagonists
Gastric Juice
Serotonin Receptors
Pharmaceutical Preparations
Area Under Curve
Acids
deramciclane
In Vitro Techniques

Keywords

  • AUC
  • Deramciclane
  • Dissolution
  • Food effect
  • In vitro-in vivo correlation

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers. / Al-Behaisi, Samar; Antal, I.; Morovján, György; Szúnyog, József; Drabant, Sándor; Marton, Sylvia; Klebovich, I.

In: European Journal of Pharmaceutical Sciences, Vol. 15, No. 2, 2002, p. 157-162.

Research output: Contribution to journalArticle

@article{49bf98566fcf4faba6eda26fd9402e62,
title = "In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers",
abstract = "The in vitro dissolution profiles of deramciclane 30 mg film-coated tablets, an acid-labile new 5-HT receptor antagonist, were studied under simulated fasting and fed conditions. Artificial gastric juice with pH adjusted to that of fasting conditions was applied either alone or after adding different dietary components. The use of the USP dissolution apparatus II (paddle method) showed that the presence of dietary components has markedly affected the amount of unchanged drug dissolved. As a similar tendency had been observed in food-effect studies in healthy volunteers, cumulative area under the curve (AUCcum) for both fed and fasting conditions were compared and an in vitro-in vivo correlation (IVIVC) was evaluated. A linear relationship was established between logarithmic in vivo blood sampling time and in vitro dissolution time assigned to equal AUCcum ratios (AUCcum, fed/AUCcum, fasting). Despite its limitations, in vitro modelling of in vivo conditions might help provide a base for predicting in vivo drug behaviour.",
keywords = "AUC, Deramciclane, Dissolution, Food effect, In vitro-in vivo correlation",
author = "Samar Al-Behaisi and I. Antal and Gy{\"o}rgy Morovj{\'a}n and J{\'o}zsef Sz{\'u}nyog and S{\'a}ndor Drabant and Sylvia Marton and I. Klebovich",
year = "2002",
doi = "10.1016/S0928-0987(01)00195-6",
language = "English",
volume = "15",
pages = "157--162",
journal = "European Journal of Pharmaceutical Sciences",
issn = "0928-0987",
publisher = "Elsevier",
number = "2",

}

TY - JOUR

T1 - In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers

AU - Al-Behaisi, Samar

AU - Antal, I.

AU - Morovján, György

AU - Szúnyog, József

AU - Drabant, Sándor

AU - Marton, Sylvia

AU - Klebovich, I.

PY - 2002

Y1 - 2002

N2 - The in vitro dissolution profiles of deramciclane 30 mg film-coated tablets, an acid-labile new 5-HT receptor antagonist, were studied under simulated fasting and fed conditions. Artificial gastric juice with pH adjusted to that of fasting conditions was applied either alone or after adding different dietary components. The use of the USP dissolution apparatus II (paddle method) showed that the presence of dietary components has markedly affected the amount of unchanged drug dissolved. As a similar tendency had been observed in food-effect studies in healthy volunteers, cumulative area under the curve (AUCcum) for both fed and fasting conditions were compared and an in vitro-in vivo correlation (IVIVC) was evaluated. A linear relationship was established between logarithmic in vivo blood sampling time and in vitro dissolution time assigned to equal AUCcum ratios (AUCcum, fed/AUCcum, fasting). Despite its limitations, in vitro modelling of in vivo conditions might help provide a base for predicting in vivo drug behaviour.

AB - The in vitro dissolution profiles of deramciclane 30 mg film-coated tablets, an acid-labile new 5-HT receptor antagonist, were studied under simulated fasting and fed conditions. Artificial gastric juice with pH adjusted to that of fasting conditions was applied either alone or after adding different dietary components. The use of the USP dissolution apparatus II (paddle method) showed that the presence of dietary components has markedly affected the amount of unchanged drug dissolved. As a similar tendency had been observed in food-effect studies in healthy volunteers, cumulative area under the curve (AUCcum) for both fed and fasting conditions were compared and an in vitro-in vivo correlation (IVIVC) was evaluated. A linear relationship was established between logarithmic in vivo blood sampling time and in vitro dissolution time assigned to equal AUCcum ratios (AUCcum, fed/AUCcum, fasting). Despite its limitations, in vitro modelling of in vivo conditions might help provide a base for predicting in vivo drug behaviour.

KW - AUC

KW - Deramciclane

KW - Dissolution

KW - Food effect

KW - In vitro-in vivo correlation

UR - http://www.scopus.com/inward/record.url?scp=0036181818&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0036181818&partnerID=8YFLogxK

U2 - 10.1016/S0928-0987(01)00195-6

DO - 10.1016/S0928-0987(01)00195-6

M3 - Article

C2 - 11849912

AN - SCOPUS:0036181818

VL - 15

SP - 157

EP - 162

JO - European Journal of Pharmaceutical Sciences

JF - European Journal of Pharmaceutical Sciences

SN - 0928-0987

IS - 2

ER -