Poster Presentations
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NEBICAPONE THIRD GENERATION SOLID DISPERSION
Teofilo Vasconcelos, Researcher/Formulation Scientist, Laboratorios BIAL
Nebicapone (BIA 3-202) is a novel catechol-O-methyltransferase (COMT) inhibitor being developed for use as a levodopa-sparing agent in Parkinson’s disease. [1]. This new chemical entity presents poor water solubility which may result in poor bioavailability. Presenting the compound as a molecular dispersion combines the benefits of a local (i.e. within the solid solution) increase in solubility and of maximizing the surface area of the compound that comes in contact with the dissolution medium as the carrier dissolves [2-4]. In our present work we developed a third generation solid dispersion [5].
A solid dispersions was prepared by the melting method. The third generation solid dispersion was composed of nebicapone, PEG6000 and polysorbate 80. The resulting product was characterized by Differential Scanning Calorimetry (DSC) and compressed into tablets. Tablets underwent dissolution studies.
DSC data show that the nebicapone in the solid dispersion was in its amorphous state. The dissolution studies showed a 50 fold increase in the dissolution of the solid dispersion compared to the pure API, after one hour.
In conclusion, the third generation solid dispersion composed of the API, a carrier a one surfactant was effective to improve the solubility of nebicapone.
RESVERATROL SOLUBILITY ENHANCEMENT BY USING THIRD GENERATION SOLID DISPERSION
Teofilo Vasconcelos, Researcher/Formulation Scientist, Laboratorios BIAL
Resveratrol is an antioxidant widely studied in for its anti-aging effect, as well as its cardiovascular, neuroprotective and antidiabetic effects [1].
This drug presents poor water solubility [2], which has been one of the reasons for its controversial clinical output [3]. Delivering this drug as an amorphous solid dispersion would improve its solubility and consequently reduce its bioavailability variability which may improve its clinical output [4]. In our present work we developed a third generation solid dispersion [4].
Solid dispersions were prepared by the melting method and physical mixtures by simple blend. The third generation solid dispersion was composed of resveratrol, PEG6000 and polysorbate 80. The resulting products were characterized by Differential Scanning Calorimetry (DSC) and compressed into tablets. Tablets underwent dissolution studies.
DSC data show that the resveratrol in the solid dispersion was in its amorphous state, while in the physical mixture its crystalline state was maintained. The dissolution studies showed a 3 fold increase in the dissolution of the solid dispersion compared to the pure API, and a 2 fold increase over the physical mixture, after one hour.
In conclusion, the third generation solid dispersion composed of the drug, a carrier and a surfactant was effective to improve the solubility of resveratrol.
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