Preparation and, in vitro, preclinical and clinical studies of aceclofenac spherical agglomerates

Usha, A. N., Mutalik, S., Reddy, M. S., Ranjith, A. K., Kushtagi, P. and Udupa, N. (2008) Preparation and, in vitro, preclinical and clinical studies of aceclofenac spherical agglomerates. European Journal of Pharmaceutics and Biopharmaceutics, 70 2: 674-683. doi:10.1016/j.ejpb.2008.06.010


Author Usha, A. N.
Mutalik, S.
Reddy, M. S.
Ranjith, A. K.
Kushtagi, P.
Udupa, N.
Title Preparation and, in vitro, preclinical and clinical studies of aceclofenac spherical agglomerates
Formatted title
Preparation and, in vitro, preclinical and clinical studies of aceclofenac spherical agglomerates
Journal name European Journal of Pharmaceutics and Biopharmaceutics   Check publisher's open access policy
ISSN 0939-6411
Publication date 2008-01-01
Sub-type Article (original research)
DOI 10.1016/j.ejpb.2008.06.010
Open Access Status
Volume 70
Issue 2
Start page 674
End page 683
Total pages 10
Editor Gurny, R.
Place of publication Netherlands
Publisher Elsevier BV
Language eng
Subject C1
111504 Pharmaceutical Sciences
860899 Human Pharmaceutical Products not elsewhere classified
Abstract Aceclofenac agglomerates were prepared by spherical crystallization technique using a three solvent system comprising acetone: dichloromethane (DCM): water (bridging liquid, good solvent and bad solvent, respectively). Hydroxypropyl methylcellulose-50 cps (HPMC) in different concentrations was used as hydrophilic polymer. The effect of speed of rotation and amount of bridging liquid on spherical agglomeration were studied. The agglomerates were subjected to various physicochemical evaluations such as practical yield, drug content, particle size, loss on drying, porosity, IR spectroscopy, differential scanning calorimetry, X-ray diffraction studies, relative crystallinity, scanning electron microscopy, micromeritic properties, solubility and dissolution studies. The agglomerates showed improved micromeritic properties as well as dissolution behaviour in comparison to conventional drug crystals. The optimized agglomerates (F-9) showed good sphericity as well as high drug release, and hence they were compressed into tablets by direct compression. The tablets were found within the limits with respect to various physicochemical parameters. The dissolution rate of prepared tablets was better than that of marketed tablet and pure drug. The optimized agglomerates and tablet formulations were found to be stable for 6 months under accelerated conditions. The in vivo studies (preclinical pharmacokinetics, pharmacodynamics and toxicity studies, and clinical pharmacokinetics) of optimized agglomerates were carried out. The results of preclinical studies revealed that the agglomerates provided improved pharmacodynamic and pharmacokinetic profiles of drug besides being nontoxic. The results of pharmacokinetic studies of optimized tablet in human subjects indicated improved pharmacokinetic parameters of drug in comparison with that of marketed tablet.
Keyword Aceclofenac
Spherical crystallization
Analgesic
Anti-inflammatory
Pharmacokinetics
Toxicity
Tablets
Direct compression
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
 
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Created: Thu, 16 Apr 2009, 02:00:12 EST by Elizabeth Pyke on behalf of School of Pharmacy