Solubility and Dissolution Rate Enhancement of Ezetimibe by Solid Dispersion and Pelletization Techniques Using Soluplus as Carrier

Abstract

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets.
 Methods: Ezetimibe solid dispersions were prepared by kneading method using soluplus. Crospovidone was added as a disintegrant in pellets. Ezetimibe pellets were prepared by dissolving soluplus and crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. Various physicochemical parameters like particle size, friability, angle of repose and drug content were evaluated for the prepared solid dispersions and pellet formulations. In vitro dissolution studies were carried out in 1% SLS using USP apparatus II. FTIR and SEM analysis were performed for solid dispersions, pellet formulations and its polymers to determine the interactions and surface characteristics.
 Results: The physicochemical parameters were within the specified I. P limits. It was observed that the solid dispersion formulation ED5 showed better dissolution rate to the extent of 1.07 folds and 1.95 folds when compared to a marketed formulation and the pure drug, respectively. Similarly, pellet formulation EP5 containing 1:5 ratio of ezetimibe to soluplus showed an improved dissolution rate to the extent of 1.173 folds and 2.136 folds when compared to the marketed formulation and the pure drug, respectively. FTIR analysis revealed that there was no major interaction between the drug and the excipients. 
 Conclusion: From the present study, it was observed that the solubility of ezetimibe was enhanced by soluplus in pellet formulations when compared to solid dispersions.

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“…FT-IR spectroscopy Fig. 2B represents the FT-IR spectrum of PCL-PEG-PCL copolymer, DOX+EZ@PCEC, EZ@PCEC, DOX@ PCEC NPs, free EZ, 35 and free DOX, 36 respectively . In the spectrum of PCL-PEG-PCL copolymer, the absorption peaks at 1727 cm -1 belonged to C=O stretching vibrations of the ester carbonyl group.…”

Implementation of Factorial Design to Optimize the Formulation Method of Ezetimibe Polymeric Nanoparticle by Homogenization Cum Ultra-Sonication Method

“…In the FTIR instrument (Bruker, Germany) equipped with the OPUS Spectrum software, prepared KBr pellets are scanned throughout a wave number range of 4000 to 500 cm-1 with a resolution of 4 cm-1. Samples were placed on the sample stage using a force gauge of 100 N, ensuring regular contact between both the specimen and the crystal holder for scanning [13,14].…”

“…The greatest percent yield and percent entrapment efficiency for the Ezetimibe PNs (R7) formulation were 96.45±2.42 and 94.28±2.56 percent, respectively. It is also possible to conclude from the above-mentioned findings that the medication concentration was distributed uniformly in the PNs [12][13][14][15][16][17][18][19][20][21][22][23][24][25].…”