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Effect of polymorphism on in vitro-in vivo properties of carbamazepine conventional tablets

Elqidra, R.; Ünlü, N.; Çapan, Y.; Sahin, G. LU ; Dalkara, T. and Hincal, A. A. (2004) In Journal of Drug Delivery Science and Technology 14(2). p.147-153
Abstract

The objective of the present study was to investigate the effect of polymorphism on in vitro-in vivo properties of carbamazepine (CBZ). For this purpose, three different polymorphs and a dihydrate of CBZ were obtained and the conventional tablets of these crystalline forms at the dose of 200 mg were prepared. The polymorphs were examined by the IR and DSC analysis. The tablets were investigated by the in vitro dissolution test. Tegretol was selected as a reference. The tablets of β CBZ demonstrated the lowest dissolution rate, while the α from tablets exhibited the highest. Dissolution rates were significantly changed by the polymorphic forms of CBZ. Tegretol, bulk powder and β CBZ tablets were selected for the bioavailability study.... (More)

The objective of the present study was to investigate the effect of polymorphism on in vitro-in vivo properties of carbamazepine (CBZ). For this purpose, three different polymorphs and a dihydrate of CBZ were obtained and the conventional tablets of these crystalline forms at the dose of 200 mg were prepared. The polymorphs were examined by the IR and DSC analysis. The tablets were investigated by the in vitro dissolution test. Tegretol was selected as a reference. The tablets of β CBZ demonstrated the lowest dissolution rate, while the α from tablets exhibited the highest. Dissolution rates were significantly changed by the polymorphic forms of CBZ. Tegretol, bulk powder and β CBZ tablets were selected for the bioavailability study. Six healthy volunteers participated in an open-randomized cross-over designed clinical trial. After a total blood sampling period of 96 h, plasma levels of CBZ were determined by HPLC analysis by using a CN column and an acetonitril-water (30:70) mobile phase. There were no significant differences between the plasma concentration-time curves of Tegretol, bulk powder and β CBZ tablets. The only marked difference was the time required to reach plasma peak concentrations.

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author
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Bioavailability, Carbamazepine, In vitro dissolution, Polymorphism
in
Journal of Drug Delivery Science and Technology
volume
14
issue
2
pages
7 pages
publisher
EDITIONS SANTE
external identifiers
  • scopus:1942441440
ISSN
1157-1489
language
English
LU publication?
no
id
c6e29f62-414d-40ac-a713-74b4a25be91e
date added to LUP
2019-06-14 20:03:12
date last changed
2019-08-16 14:12:00
@article{c6e29f62-414d-40ac-a713-74b4a25be91e,
  abstract     = {<p>The objective of the present study was to investigate the effect of polymorphism on in vitro-in vivo properties of carbamazepine (CBZ). For this purpose, three different polymorphs and a dihydrate of CBZ were obtained and the conventional tablets of these crystalline forms at the dose of 200 mg were prepared. The polymorphs were examined by the IR and DSC analysis. The tablets were investigated by the in vitro dissolution test. Tegretol was selected as a reference. The tablets of β CBZ demonstrated the lowest dissolution rate, while the α from tablets exhibited the highest. Dissolution rates were significantly changed by the polymorphic forms of CBZ. Tegretol, bulk powder and β CBZ tablets were selected for the bioavailability study. Six healthy volunteers participated in an open-randomized cross-over designed clinical trial. After a total blood sampling period of 96 h, plasma levels of CBZ were determined by HPLC analysis by using a CN column and an acetonitril-water (30:70) mobile phase. There were no significant differences between the plasma concentration-time curves of Tegretol, bulk powder and β CBZ tablets. The only marked difference was the time required to reach plasma peak concentrations.</p>},
  author       = {Elqidra, R. and Ünlü, N. and Çapan, Y. and Sahin, G. and Dalkara, T. and Hincal, A. A.},
  issn         = {1157-1489},
  keyword      = {Bioavailability,Carbamazepine,In vitro dissolution,Polymorphism},
  language     = {eng},
  month        = {03},
  number       = {2},
  pages        = {147--153},
  publisher    = {EDITIONS SANTE},
  series       = {Journal of Drug Delivery Science and Technology},
  title        = {Effect of polymorphism on in vitro-in vivo properties of carbamazepine conventional tablets},
  volume       = {14},
  year         = {2004},
}