Enhancement of ketoconazole dissolution rate by the liquisolid technique

The study was conducted to enhance the dissolution rate of ketoconazole (KCZ) (a poorly water-soluble drug) using the liquisolid technique. Microcrystalline cellulose, colloidal silica, PEG400 and polyvinyl pyrrolidone (PVP) were employed as a carrier, coating substance, nonvolatile solvent and addi...

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Bibliographic Details
Published in:Acta pharmaceutica (Zagreb, Croatia) Croatia), 2018-09, Vol.68 (3), p.325-336
Main Authors: Molaei, Mir-Ali, Osouli-Bostanabad, Karim, Adibkia, Khosro, Shokri, Javad, Asnaashari, Solmaz, Javadzadeh, Yousef
Format: Article
Language:English
Subjects:
Aging
Antifungal agents
Avicel
Calorimetry
Cellulose
Coating effects
Compactibility
Compacts
Crystalline cellulose
Differential scanning calorimetry
Dissolution
dissolution rate
Dosage
Drug delivery systems
Ketoconazole
liquisolid
Load distribution
polymorphic changes
Polyvinyl pyrrolidone
Relative humidity
Silica
Silicon dioxide
Tablets
Water chemistry
X ray powder diffraction
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Summary:The study was conducted to enhance the dissolution rate of ketoconazole (KCZ) (a poorly water-soluble drug) using the liquisolid technique. Microcrystalline cellulose, colloidal silica, PEG400 and polyvinyl pyrrolidone (PVP) were employed as a carrier, coating substance, nonvolatile solvent and additive in the KCZ liquisolid compact formulation, respectively. The drug-to-PEG400 and carrier-to-coating ratio variations, PVP concentration and aging effects on the release behavior were assessed. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD) data revealed no alterations in the crystalline form of the drug and the KCZ-excipient interactions within the process. The load factor and the drug release rate were significantly enhanced compared to directly compressed tablets in the presence of the additive. Increasing the PEG400-to-drug ratio in liquid medications enhanced the dissolution rate remarkably. The dissolution profile and hardness of liquisolid compacts were not significantly altered by keeping the tablets at 40 °C and relative humidity of 75 % for 6 months. With the proposed modification of the liquisolid process, it is possible to obtain flowable, compactible liquisolid powders of high-dose poorly-water soluble drugs with an enhanced dissolution rate.
ISSN:1846-9558
1330-0075
1846-9558
DOI:10.2478/acph-2018-0025