Preparation of stabilized submicron fenofibrate crystals on niacin as a hydrophilic hydrotropic carrier
| Autor: | Ebtessam A. Essa, Gamal M. El Maghraby, Rasha A. Alshaikh |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Scanning electron microscope
Chemical structure Chemistry Pharmaceutical Pharmaceutical Science Administration Oral Biological Availability 02 engineering and technology 030226 pharmacology & pharmacy Niacin 03 medical and health sciences 0302 clinical medicine Fenofibrate X-Ray Diffraction Spectroscopy Fourier Transform Infrared medicine Solubility Particle Size Thermal analysis Dissolution Hypolipidemic Agents Drug Carriers Calorimetry Differential Scanning Chemistry digestive oral and skin physiology nutritional and metabolic diseases food and beverages Hydrogen Bonding General Medicine 021001 nanoscience & nanotechnology Bioavailability Microscopy Electron Scanning 0210 nano-technology Hydrophobic and Hydrophilic Interactions Nuclear chemistry medicine.drug |
| Zdroj: | Pharmaceutical development and technology. 25(2) |
| ISSN: | 1097-9867 |
| Popis: | Fenofibrate is antihyperlipidemic which has low and variable oral bioavailability due to erratic dissolution characteristics. Niacin showed a potential atheroprotective effects suggesting possible co-administration with fenofibrate with a potential for development of fixed dose combination. The chemical structure of both drugs highlights the opportunity for interaction upon co-processing due to the existence of complementary hydrogen bonding sites. Accordingly, fenofibrate and niacin were co-processed by wet co-grinding and the resulting product was assessed using scanning electron microscopy, FTIR, thermal analysis and X-ray diffraction in addition to dissolution studies. The instrumental analysis indicated the development of submicron fenofibrate crystals stabilized over the surface of niacin crystals. The developed submicron crystals showed fast dissolution of fenofibrate depending on the relative proportions of fenofibrate to niacin. Co-processing of both drugs at dose ratio which contained higher proportion of niacin resulted in further enhancement in the dissolution rate. This further enhancement was attributed to the hydrotropic effect of niacin which was proved by solubility study in addition to size reduction. This supposition was confirmed from the inferior dissolution of fenofibrate from the physical mixture. The study introduces fenofibrate/niacin as potential fixed dose combination for augmented dissolution rate and pharmacological effects. |
| Databáze: | OpenAIRE |
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