Chitosan and enteric polymer based once daily sustained release tablets of aceclofenac: In vitro and in vivo studies

Mutalik, S., Manoj, K., Reddy, M., Kushtagi, P., Usha, A., Anju, P., Ranjith, A. and Udupa, N. (2008) Chitosan and enteric polymer based once daily sustained release tablets of aceclofenac: In vitro and in vivo studies. AAPS PharmSciTech, 9 2: 651-659. doi:10.1208/s12249-008-9075-3


Author Mutalik, S.
Manoj, K.
Reddy, M.
Kushtagi, P.
Usha, A.
Anju, P.
Ranjith, A.
Udupa, N.
Title Chitosan and enteric polymer based once daily sustained release tablets of aceclofenac: In vitro and in vivo studies
Journal name AAPS PharmSciTech   Check publisher's open access policy
ISSN 1530-9932
Publication date 2008-01-01
Sub-type Article (original research)
DOI 10.1208/s12249-008-9075-3
Open Access Status DOI
Volume 9
Issue 2
Start page 651
End page 659
Total pages 9
Editor DeLuca, P. P.
Place of publication United States of America
Publisher Springer
Language eng
Subject C1
111504 Pharmaceutical Sciences
860899 Human Pharmaceutical Products not elsewhere classified
Abstract The purpose of this study was to develop a once daily sustained release tablet of aceclofenac using chitosan and an enteric coating polymer (hydroxypropyl methylcellulose phthalate or cellulose acetate phthalate). Overall sustained release for 24 h was achieved by preparing a double-layer tablet in which the immediate release layer was formulated for a prompt release of the drug and the sustained release layer was designed to achieve a prolonged release of drug. The preformulation studies like IR spectroscopic and differential scanning calorimetry showed the absence of drug–excipient interactions. The tablets were found within the permissible limits for various physicochemical parameters. Scanning electron microscopy was used to visualize the surface morphology of the tablets and to confirm drug release mechanisms. Good equivalence in the drug release profile was observed when drug release pattern of the tablet containing chitosan and hydroxypropyl methylcellulose phthalate (M-7) was compared with that of marketed tablet. The optimized tablets were stable at accelerated storage conditions for 6 months with respect to drug content and physical appearance. The results of pharmacokinetic studies in human volunteers showed that the optimized tablet (M-7) exhibited no difference in the in vivo drug release in comparison with marketed tablet. No significant difference between the values of pharmacokinetic parameters of M-7 and marketed tablets was observed (p > 0.05; 95% confidence intervals). However the clinical studies in large scale and, long term and extensive stability studies at different conditions are required to confirm these results.
Formatted abstract
The purpose of this study was to develop a once daily sustained release tablet of aceclofenac using chitosan and an enteric coating polymer (hydroxypropyl methylcellulose phthalate or cellulose acetate phthalate). Overall sustained release for 24 h was achieved by preparing a double-layer tablet in which the immediate release layer was formulated for a prompt release of the drug and the sustained release layer was designed to achieve a prolonged release of drug. The preformulation studies like IR spectroscopic and differential scanning calorimetry showed the absence of drug–excipient interactions. The tablets were found within the permissible limits for various physicochemical parameters. Scanning electron microscopy was used to visualize the surface morphology of the tablets and to confirm drug release mechanisms. Good equivalence in the drug release profile was observed when drug release pattern of the tablet containing chitosan and hydroxypropyl methylcellulose phthalate (M-7) was compared with that of marketed tablet. The optimized tablets were stable at accelerated storage conditions for 6 months with respect to drug content and physical appearance. The results of pharmacokinetic studies in human volunteers showed that the optimized tablet (M-7) exhibited no difference in the in vivo drug release in comparison with marketed tablet. No significant difference between the values of pharmacokinetic parameters of M-7 and marketed tablets was observed (p > 0.05; 95% confidence intervals). However the clinical studies in large scale and, long term and extensive stability studies at different conditions are required to confirm these results.
Keyword Aceclofenac
Chitosan
Matrix tablet
Pharmacokinetics
Sustained release
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: 2009 Higher Education Research Data Collection
School of Pharmacy Publications
 
Versions
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 10 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 20 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Thu, 16 Apr 2009, 02:22:02 EST by Elizabeth Pyke on behalf of School of Pharmacy