Abstract
Objective: This study aims to determine the effect of the inclusion complex formation of ibuprofen (IB) with β-cyclodextrin (β-CD) in improving water solubility and taste masking as well as to study the effect of the combined use of super disintegrants in IB-β-CD ODT (Orally disintegrating tablet).
 Methods: IB-β-CD inclusion complex was prepared by spray drying technique with a 1:1 molar ratio. ODTs were prepared by the direct compression method using various ratios of Ac-Di-Sol® and Kollidon® CL as super disintegrant. The inclusion complex was characterized using spectroscopy FT-IR (Fourier-transform infrared) and DSC (Differential Scanning Calorimetry). The physical properties and dissolution rate of ODTs were evaluated. Dissolved drug concentration at 60 min (Q60) and Dissolution Efficiency (DE60) was calculated using the dissolution test result.
 Results: The unpleasant taste of IB had been successfully masked by IB-β-CD. Formula 1 was observed having 14.5 sec of disintegration, fastest compared to the other formulas. Moreover DE60 value of formula I was higher than the other formulas (113.45).
 Conclusion: IB-β-CD Inclusion complex prepared by spray drying method (1: 1) increased the water solubility and masked the unpleasant taste compared to IB moreover combination of Ac-Di-Sol® and Kollidon® CL increased ODT dissolution rate.
Highlights
Ibuprofen (IB) is an NSAID (Nonsteroidal Anti-Inflammatory Drug) that belongs to the propionic acid derivative
The materials used in this study were ibuprofen, β-cyclodextrin, Ac-Di-Sol®, Kollidon CL, Avicel PH 102, aspartame, magnesium stearate, talc, phosphate buffer pH 7.2, methylene blue, water, methanol p. a., dan ethanol 96%
According to table 2 that the spray drying method had undergone an inclusion complex in which inclusion complex results were ranging from tasteless to sweet which successfully masked its original bitter taste
Summary
Ibuprofen (IB) is an NSAID (Nonsteroidal Anti-Inflammatory Drug) that belongs to the propionic acid derivative. IB mechanism of action is inhibition of cyclooxygenase-1 and cyclooxygenase-2 isoenzymes by interfering synthesis of prostaglandin from arachidonic acid, whereas prostaglandins are messenger molecules in inflammatory processes [1]. According to the Biopharmaceutics Classification System, IB is a BCS class II drug, which has poor solubility but good permeability properties [2]. IB absorption is limited by its poor water solubility. This can hamper its oral bioavailability and onset of action. Several approached have been employed to increase IB water solubility and oral bioavailability, such as solid dispersion [3], size reduction [4], copolymer [5], and surfactant [6]. Especially using cyclodextrin (CD), has been widely used to increase the water solubility of poorly water-soluble drugs as well as enhance bioavailability [7]
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