Development and evaluation of dexibuprofen formulation with fast onset and prolonged effect

In the present study, in order to improve the solubility and bioavailability of poorly water-soluble dexibuprofen, a novel dexibuprofen-loaded solid dispersion was developed using the spray-drying technique. The controlled-release dexibuprofen formulation was developed by combining the immediate-rel...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2019-06, Vol.45 (6), p.895-904
Main Authors: Choi, Yoonho, Min, Kyoung Ah, Kim, Chong-Kook
Format: Article
Language:English
Subjects:
controlled release
dexibuprofen
HPMC
Pain reliever
solid dispersion
spray drying
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Summary:In the present study, in order to improve the solubility and bioavailability of poorly water-soluble dexibuprofen, a novel dexibuprofen-loaded solid dispersion was developed using the spray-drying technique. The controlled-release dexibuprofen formulation was developed by combining the immediate-release dispersion powder and the sustained-release formula. The solid dispersion composed of dexibuprofen/poloxamer 407/hydroxypropyl methylcellulose (HPMC) 2910 (50 cps)/sodium lauryl sulfate (SLS) (10/1/4/0.1 mg) was selected as the immediate-release formulation due to its increased solubility and dissolution rate. This immediate-release formulation showed a significantly higher initial plasma concentration, AUC, and C max of dexibuprofen than those of dexibuprofen powder. Based on the prolonged effect of high plasma concentration, the formulation consisting of dexibuprofen/ethylcellulose/HPMC 2910 (4000 cps)/magnesium stearate (66/16.5/16.5/1 mg) was selected as the sustained-release formulation. Finally, the controlled-release (CR) formulation was prepared by encapsulating the immediate-release and sustained-release formulations in hard gelatin capsules. The proposed CR formulation showed enhanced AUC (5.5-fold) and C max (3.5-fold) compared to dexibuprofen powder. The results of the present study suggest that the CR formulation containing dexibuprofen may be a potential oral dosage form for a fast onset and a prolonged effect of poorly water-soluble dexibuprofen.
ISSN:0363-9045
1520-5762
DOI:10.1080/03639045.2019.1576720