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An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability

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2011
1474.pdf (338.0Kb)
Authors
Kocić, Ivana
Homšek, Irena
Dacević, Mirjana
Parojčić, Jelena
Miljković, Branislava
Article (Published version)
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Abstract
The aim of this study was to investigate the influence of experimental conditions on levothyroxine sodium release from two immediate-release tablet formulations which narrowly passed the standard requirements for bioequivalence studies. The in vivo study was conducted as randomised, single-dose, two-way cross-over pharmacokinetic study in 24 healthy subjects. The in vitro study was performed using various dissolution media, and obtained dissolution profiles were compared using the similarity factor value. Drug solubility in different media was also determined. The in vivo results showed narrowly passing bioequivalence. Considering that levothyroxine sodium is classified as Class III drug according to the Biopharmaceutics Classification System, drug bioavailability will be less sensitive to the variation in its dissolution characteristics and it can be assumed that the differences observed in vitro in some of investigated media probably do not have significant influence on the absorptio...n process, as long as rapid and complete dissolution exists. The study results indicate that the current regulatory criteria for the value of similarity factor in comparative dissolution testing, as well as request for very rapid dissolution (more than 85% of drug dissolved in 15 min), are very restricted for immediate-release dosage forms containing highly soluble drug substance and need further investigation. The obtained results also add to the existing debate on the appropriateness of the current bioequivalence standards for levothyroxine sodium products.

Keywords:
bioequivalence / dissolution / immediate release / levothyroxine sodium / solubility
Source:
AAPS PharmSciTech, 2011, 12, 3, 938-948
Publisher:
  • Springer, New York
Funding / projects:
  • Basic and Clinical Pharmacological research of mechanisms of action and drug interactions in nervous and cardiovascular system (RS-175023)

DOI: 10.1208/s12249-011-9660-8

ISSN: 1530-9932

PubMed: 21748540

WoS: 000294492900016

Scopus: 2-s2.0-80052568377
[ Google Scholar ]
9
8
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/1476
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Kocić, Ivana
AU  - Homšek, Irena
AU  - Dacević, Mirjana
AU  - Parojčić, Jelena
AU  - Miljković, Branislava
PY  - 2011
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1476
AB  - The aim of this study was to investigate the influence of experimental conditions on levothyroxine sodium release from two immediate-release tablet formulations which narrowly passed the standard requirements for bioequivalence studies. The in vivo study was conducted as randomised, single-dose, two-way cross-over pharmacokinetic study in 24 healthy subjects. The in vitro study was performed using various dissolution media, and obtained dissolution profiles were compared using the similarity factor value. Drug solubility in different media was also determined. The in vivo results showed narrowly passing bioequivalence. Considering that levothyroxine sodium is classified as Class III drug according to the Biopharmaceutics Classification System, drug bioavailability will be less sensitive to the variation in its dissolution characteristics and it can be assumed that the differences observed in vitro in some of investigated media probably do not have significant influence on the absorption process, as long as rapid and complete dissolution exists. The study results indicate that the current regulatory criteria for the value of similarity factor in comparative dissolution testing, as well as request for very rapid dissolution (more than 85% of drug dissolved in 15 min), are very restricted for immediate-release dosage forms containing highly soluble drug substance and need further investigation. The obtained results also add to the existing debate on the appropriateness of the current bioequivalence standards for levothyroxine sodium products.
PB  - Springer, New York
T2  - AAPS PharmSciTech
T1  - An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability
VL  - 12
IS  - 3
SP  - 938
EP  - 948
DO  - 10.1208/s12249-011-9660-8
UR  - conv_2510
ER  - 
@article{
author = "Kocić, Ivana and Homšek, Irena and Dacević, Mirjana and Parojčić, Jelena and Miljković, Branislava",
year = "2011",
abstract = "The aim of this study was to investigate the influence of experimental conditions on levothyroxine sodium release from two immediate-release tablet formulations which narrowly passed the standard requirements for bioequivalence studies. The in vivo study was conducted as randomised, single-dose, two-way cross-over pharmacokinetic study in 24 healthy subjects. The in vitro study was performed using various dissolution media, and obtained dissolution profiles were compared using the similarity factor value. Drug solubility in different media was also determined. The in vivo results showed narrowly passing bioequivalence. Considering that levothyroxine sodium is classified as Class III drug according to the Biopharmaceutics Classification System, drug bioavailability will be less sensitive to the variation in its dissolution characteristics and it can be assumed that the differences observed in vitro in some of investigated media probably do not have significant influence on the absorption process, as long as rapid and complete dissolution exists. The study results indicate that the current regulatory criteria for the value of similarity factor in comparative dissolution testing, as well as request for very rapid dissolution (more than 85% of drug dissolved in 15 min), are very restricted for immediate-release dosage forms containing highly soluble drug substance and need further investigation. The obtained results also add to the existing debate on the appropriateness of the current bioequivalence standards for levothyroxine sodium products.",
publisher = "Springer, New York",
journal = "AAPS PharmSciTech",
title = "An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability",
volume = "12",
number = "3",
pages = "938-948",
doi = "10.1208/s12249-011-9660-8",
url = "conv_2510"
}
Kocić, I., Homšek, I., Dacević, M., Parojčić, J.,& Miljković, B.. (2011). An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability. in AAPS PharmSciTech
Springer, New York., 12(3), 938-948.
https://doi.org/10.1208/s12249-011-9660-8
conv_2510
Kocić I, Homšek I, Dacević M, Parojčić J, Miljković B. An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability. in AAPS PharmSciTech. 2011;12(3):938-948.
doi:10.1208/s12249-011-9660-8
conv_2510 .
Kocić, Ivana, Homšek, Irena, Dacević, Mirjana, Parojčić, Jelena, Miljković, Branislava, "An Investigation into the Influence of Experimental Conditions on In Vitro Drug Release from Immediate-Release Tablets of Levothyroxine Sodium and Its Relation to Oral Bioavailability" in AAPS PharmSciTech, 12, no. 3 (2011):938-948,
https://doi.org/10.1208/s12249-011-9660-8 .,
conv_2510 .

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