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

Nayak , Achutha Usha and Mutalik, Srinivas and Reddy, Meka Sreenivasa and Ranjith, Averineni Kumar and Kushtagi, Pralhad and Udupa, Nayanabhirama (2008) Preparation and, in vitro, preclinical and clinical studies of aceclofenac spherical agglomerates. European Journal of Pharmaceutics and Biopharmaceutics, 70. pp. 674-683.

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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.

Item Type: Article
Uncontrolled Keywords: Aceclofenac, Spherical crystallization, Analgesic Anti-inflammatory, Pharmacokinetics, Toxicity, Tablets Direct compression
Subjects: Medicine > KMC Manipal > Obstetrics & Gynaecology
Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Manipal
Date Deposited: 17 Jun 2011 07:06
Last Modified: 17 Jun 2011 07:06
URI: http://eprints.manipal.edu/id/eprint/298

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