Abstract
Etodolac (ET) is a nonsteroidal anti-inflammatory drug with proved potential antitumor and uric acid lowering effects. It shows dissolution rate-dependent bioavailability. This work was carried out to improve the dissolution rate of etodolac using three carriers of known potential to improve solubility and hence dissolution rate of poorly soluble drugs through coevaporation technique. The polymeric surfactant inutec, 2-hydroxypropyl-β-cyclodextrin, and tromethamine were used at three different drug/carrier ratios. The dissolution rate of ET at pH 1.2 and 6.8 is improved in all of the solid dispersion systems compared to that of the pure drug and physical mixtures. DSC of coevaporates at 1:5 drug/carrier ratio providing the fastest dissolution rate suggested loss of ET crystallinity which was further confirmed by X-ray diffraction. Inutec-based coevaporate was chosen for the formulation of ET chewable tablets. Chewable tablets (F3) that met the USP monograph specifications for ET tablets, with 86% dissolved amount within 15 min, was chosen for in vivo absorption study in comparison with pure ET-filled hard gelatin capsules. The results showed significantly higher mean C max and shorter mean T max (about 2 h earlier) and about 1.32-fold higher mean AUC0–24 values for the F3 chewable tablets compared to ET-filled capsules.
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Authors are grateful to Beneo Biobased Chemicals, Belgium and JRS CO., Germany for supplying us with the necessary chemicals to participate in the field of research.
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Ibrahim, M.M., EL-Nabarawi, M., El-Setouhy, D.A. et al. Polymeric Surfactant Based Etodolac Chewable Tablets: Formulation and In Vivo Evaluation. AAPS PharmSciTech 11, 1730–1737 (2010). https://doi.org/10.1208/s12249-010-9548-z
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DOI: https://doi.org/10.1208/s12249-010-9548-z