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https://doi.org/10.2478/acph-2018-0025

Dissolution rate enhancement of ketoconazole by liquisolid technique

MIR-ALI MOLAEI ; Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz 51664, Iran; Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz 51664, Iran
KARIM OSOULI-BOSTANABAD ; Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz 51664, Iran; Students Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran
KHOSRO ADIBKIA ; Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz 51664, Iran; Students Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran
JAVAD SHOKRI ; Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz 51664, Iran
SOLMAZ ASNAASHARI ; Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz 51664, Iran
YOUSEF JAVADZADEH orcid id orcid.org/0000-0001-7283-3560 ; Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz 51664, Iran, Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz 51664, Iran


Puni tekst: engleski pdf 614 Kb

str. 325-336

preuzimanja: 1.048

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Sažetak

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 in vitro 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.

Ključne riječi

ketoconazole, liquisolid, dissolution rate, Avicel, polymorphic changes

Hrčak ID:

195717

URI

https://hrcak.srce.hr/195717

Posjeta: 1.402 *