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Development of fixed dose combination tablets containing zidovudine and lamivudine for paediatric applications

Egide Kayitare, Chris Vervaet UGent, JD Ntawukulilyayo, B Seminega, Lucas Van Bortel UGent and Jean Paul Remon UGent (2009) International Journal of Pharmaceutics. 370(1-2). p.41-46
abstract
In view of the lack of suitable paediatric antiretroviral formulations on the market, a novel fixed dose combination (FDC) tablet containing 300 mg zidovudine (AZT) and 160 mg lamivudine (3TC) was developed to improve dosing accuracy and allow flexible drug dosing in function of the body weight of paediatric HIV patients as recommended by WHO. Rectangular tablets with multiple fraction bars were designed and each tablet can be broken into 8 subunits, each subunit containing a drug dose corresponding to a body weight of 5 kg. These fast-disintegrating subunits can easily be administered to children after dispersion in a liquid or mixing with food. in vitro quality control of the FDC tablets was determined and a crossover bioavailability study using 18 adult volunteers was performed after oral administration of the novel FDC tablet and a Duovir tablet. The results of the study showed that the novel tablets as well as its subunits disintegrated fast (<20 s). After 30 min dissolution, AZT and 3TC released from Duovir (R) and the novel tablets was above 95%, the similarity factors Q were above 50 for both AZT and 3TC. A tablet breakability test showed low weight variability (125.1 +/- 5 mg, R.S.D. = 4.4%), with limited weight loss (0.3%). There was no significant difference in pharmacokinetic parameters (C-max, t(max) and AUC(0-12) (h) values) between Duovir and the novel tablets formulated for paediatric applications
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
CHILDREN, HIV, SCORED TABLETS, Antiretroviral fixed dose combination, Paediatric drug formulations, FORMULATION, BIOEQUIVALENCE, MEDICINES, HPLC
journal title
International Journal of Pharmaceutics
Int. J. Pharm.
volume
370
issue
1-2
pages
41 - 46
publisher
Elsevier
Web of Science type
Article
Web of Science id
000264669600006
JCR category
PHARMACOLOGY & PHARMACY
JCR impact factor
2.962 (2009)
JCR rank
78/236 (2009)
JCR quartile
2 (2009)
ISSN
0378-5173
DOI
10.1016/j.ijpharm.2008.11.005
language
English
UGent publication?
yes
classification
A1
copyright statement
I don't know the status of the copyright for this publication
id
603864
handle
http://hdl.handle.net/1854/LU-603864
date created
2009-04-29 14:54:40
date last changed
2009-05-04 09:58:05
@article{603864,
  abstract     = {In view of the lack of suitable paediatric antiretroviral formulations on the market, a novel fixed dose combination (FDC) tablet containing 300 mg zidovudine (AZT) and 160 mg lamivudine (3TC) was developed to improve dosing accuracy and allow flexible drug dosing in function of the body weight of paediatric HIV patients as recommended by WHO.
Rectangular tablets with multiple fraction bars were designed and each tablet can be broken into 8 subunits, each subunit containing a drug dose corresponding to a body weight of 5 kg. These fast-disintegrating subunits can easily be administered to children after dispersion in a liquid or mixing with food. in vitro quality control of the FDC tablets was determined and a crossover bioavailability study using 18 adult volunteers was performed after oral administration of the novel FDC tablet and a Duovir tablet.

The results of the study showed that the novel tablets as well as its subunits disintegrated fast ({\textlangle}20 s). After 30 min dissolution, AZT and 3TC released from Duovir (R) and the novel tablets was above 95\%, the similarity factors Q were above 50 for both AZT and 3TC. A tablet breakability test showed low weight variability (125.1 +/- 5 mg, R.S.D. = 4.4\%), with limited weight loss (0.3\%). There was no significant difference in pharmacokinetic parameters (C-max, t(max) and AUC(0-12) (h) values) between Duovir and the novel tablets formulated for paediatric applications},
  author       = {Kayitare, Egide and Vervaet, Chris and Ntawukulilyayo, JD and Seminega, B and Van Bortel, Lucas and Remon, Jean Paul},
  issn         = {0378-5173},
  journal      = {International Journal of Pharmaceutics},
  keyword      = {CHILDREN,HIV,SCORED TABLETS,Antiretroviral fixed dose combination,Paediatric drug formulations,FORMULATION,BIOEQUIVALENCE,MEDICINES,HPLC},
  language     = {eng},
  number       = {1-2},
  pages        = {41--46},
  publisher    = {Elsevier},
  title        = {Development of fixed dose combination tablets containing zidovudine and lamivudine for paediatric applications},
  url          = {http://dx.doi.org/10.1016/j.ijpharm.2008.11.005},
  volume       = {370},
  year         = {2009},
}

Chicago
Kayitare, Egide, Chris Vervaet, JD Ntawukulilyayo, B Seminega, Lucas Van Bortel, and Jean Paul Remon. 2009. “Development of Fixed Dose Combination Tablets Containing Zidovudine and Lamivudine for Paediatric Applications.” International Journal of Pharmaceutics 370 (1-2): 41–46.
APA
Kayitare, E., Vervaet, C., Ntawukulilyayo, J., Seminega, B., Van Bortel, L., & Remon, J. P. (2009). Development of fixed dose combination tablets containing zidovudine and lamivudine for paediatric applications. International Journal of Pharmaceutics, 370(1-2), 41–46.
Vancouver
1.
Kayitare E, Vervaet C, Ntawukulilyayo J, Seminega B, Van Bortel L, Remon JP. Development of fixed dose combination tablets containing zidovudine and lamivudine for paediatric applications. International Journal of Pharmaceutics. Elsevier; 2009;370(1-2):41–6.
MLA
Kayitare, Egide, Chris Vervaet, JD Ntawukulilyayo, et al. “Development of Fixed Dose Combination Tablets Containing Zidovudine and Lamivudine for Paediatric Applications.” International Journal of Pharmaceutics 370.1-2 (2009): 41–46. Print.