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...
Saved in:
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Sciendo
2018-09-01
|
| Series: | Acta Pharmaceutica |
| Subjects: | |
| Online Access: | https://doi.org/10.2478/acph-2018-0025 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1832569223917862912 |
|---|---|
| author | Molaei Mir-Ali Osouli-Bostanabad Karim Adibkia Khosro Shokri Javad Asnaashari Solmaz Javadzadeh Yousef |
| author_facet | Molaei Mir-Ali Osouli-Bostanabad Karim Adibkia Khosro Shokri Javad Asnaashari Solmaz Javadzadeh Yousef |
| author_sort | Molaei Mir-Ali |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-d38535800af043aeadf008303cbefc54 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2018-09-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-d38535800af043aeadf008303cbefc542025-02-02T23:02:22ZengSciendoActa Pharmaceutica1846-95582018-09-0168332533610.2478/acph-2018-0025acph-2018-0025Enhancement of ketoconazole dissolution rate by the liquisolid techniqueMolaei Mir-Ali0Osouli-Bostanabad Karim1Adibkia Khosro2Shokri Javad3Asnaashari Solmaz4Javadzadeh Yousef5Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz51664, IranCenter for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz51664, IranCenter for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz51664, IranFaculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz51664, IranBiotechnology Research Center, Tabriz University of Medical Sciences, Tabriz51664, IranFaculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz51664, IranThe 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.https://doi.org/10.2478/acph-2018-0025ketoconazoleliquisoliddissolution rateavicelpolymorphic changes |
| spellingShingle | Molaei Mir-Ali Osouli-Bostanabad Karim Adibkia Khosro Shokri Javad Asnaashari Solmaz Javadzadeh Yousef Enhancement of ketoconazole dissolution rate by the liquisolid technique Acta Pharmaceutica ketoconazole liquisolid dissolution rate avicel polymorphic changes |
| title | Enhancement of ketoconazole dissolution rate by the liquisolid technique |
| title_full | Enhancement of ketoconazole dissolution rate by the liquisolid technique |
| title_fullStr | Enhancement of ketoconazole dissolution rate by the liquisolid technique |
| title_full_unstemmed | Enhancement of ketoconazole dissolution rate by the liquisolid technique |
| title_short | Enhancement of ketoconazole dissolution rate by the liquisolid technique |
| title_sort | enhancement of ketoconazole dissolution rate by the liquisolid technique |
| topic | ketoconazole liquisolid dissolution rate avicel polymorphic changes |
| url | https://doi.org/10.2478/acph-2018-0025 |
| work_keys_str_mv | AT molaeimirali enhancementofketoconazoledissolutionratebytheliquisolidtechnique AT osoulibostanabadkarim enhancementofketoconazoledissolutionratebytheliquisolidtechnique AT adibkiakhosro enhancementofketoconazoledissolutionratebytheliquisolidtechnique AT shokrijavad enhancementofketoconazoledissolutionratebytheliquisolidtechnique AT asnaasharisolmaz enhancementofketoconazoledissolutionratebytheliquisolidtechnique AT javadzadehyousef enhancementofketoconazoledissolutionratebytheliquisolidtechnique |