Chitosan and Enteric Polymer Based Once Daily Sustained Release Tablets of Aceclofenac: In Vitro and In Vivo Studies

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...

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Bibliographic Details
Published in:AAPS PharmSciTech 2008-06, Vol.9 (2), p.651, Article 651
Main Authors: Mutalik, Srinivas, Manoj, Krishnan, Reddy, Meka Sreenivasa, Kushtagi, Pralhad, Usha, Achutha Nayak, Anju, Parambil, Ranjith, Averineni Kumar, Udupa, Nayanabhirama
Format: Article
Language:English
Subjects:
Administration, Oral
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Calorimetry, Differential Scanning
Cellulose - analogs & derivatives
Cellulose - chemistry
Chemistry, Pharmaceutical
Chitosan - chemistry
Cross-Over Studies
Delayed-Action Preparations
Diclofenac - administration & dosage
Diclofenac - analogs & derivatives
Diclofenac - chemistry
Diclofenac - pharmacokinetics
Double-Blind Method
Drug Administration Schedule
Drug Carriers
Drug Compounding
Drug Stability
Humans
Hydrogen-Ion Concentration
Methylcellulose - analogs & derivatives
Methylcellulose - chemistry
Microscopy, Electron, Scanning
Pharmacology/Toxicology
Pharmacy
Research Article/Themed Issue: Oral/Guest Editors: Stephen A. Howard and Jian-Xin Li
Solubility
Spectrophotometry, Infrared
Surface Properties
Tablets, Enteric-Coated
Technology, Pharmaceutical - methods
Themed Issue: Oral/Guest Editors: Stephen A. Howard and Jian-Xin Li
Therapeutic Equivalency
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Summary: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.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-008-9075-3