Saturated phosphatidylcholine as matrix former for oral extended release dosage forms
| Autor: | Marina Kolbina, Martin Körber, Roland Bodmeier |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Drug
Drug Liberation Chemistry Pharmaceutical media_common.quotation_subject Administration Oral Pharmaceutical Science Excipient 02 engineering and technology 030226 pharmacology & pharmacy Dosage form Diffusion Excipients 03 medical and health sciences chemistry.chemical_compound Drug Delivery Systems 0302 clinical medicine Theophylline Caffeine medicine Particle Size Solubility media_common Chromatography Chemistry Osmolar Concentration 021001 nanoscience & nanotechnology Ionic strength Phosphatidylcholines Nanoparticles 0210 nano-technology Hydrophobic and Hydrophilic Interactions Porosity Tablets medicine.drug |
| Zdroj: | European Journal of Pharmaceutical Sciences. 108:86-92 |
| ISSN: | 0928-0987 |
| DOI: | 10.1016/j.ejps.2017.07.017 |
| Popis: | The aim of this study was to evaluate the suitability of saturated phosphatidylcholine (Phospholipon® 90H) as extended release excipient in matrix tablets for three model drugs with different aqueous solubility (theophylline, caffeine and diprophylline). The tablets could be prepared by direct compression because of the favorable phospholipid powder flow properties (Carr's index: 12.64 and angle of repose: 28.85) and good compactibility. Tablets of low porosity were formed already at low pressure of 40MPa and with drug loadings up to 70% due to high plasticity of the phospholipid. Extended drug release was achieved with the drugs of different solubility and at various drug loadings. For example, the caffeine release time (t80%) from 8mm tablets ranged from 1.5h to 18h at 70% and 10% drug loading, respectively. The drug release was governed by diffusion and could therefore be modelled by Fick's law of diffusion. Drug release profiles were thus a function of drug solubility, drug loading and tablet dimension. Matrix tablets of caffeine (20% drug loading) showed robust dissolution with regard to agitation (50-100rpm) and ionic strength of the release media (100-600 mOsmol/kg). Caffeine release was pH-dependent with a faster drug release at acidic pH, which was attributed to a protonization of the phosphatidyl group of the matrix-former and thus a higher hydrophilicity. |
| Databáze: | OpenAIRE |
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