Solubility enhancement of desloratadine by solid dispersion in poloxamers

作者: Nemanja Kolašinac , Kyriakos Kachrimanis , Irena Homšek , Branka Grujić , Zorica Đurić

DOI: 10.1016/J.IJPHARM.2012.06.060

关键词: DissolutionDissolution testingSolubilityFactorial experimentPoloxamerChemistryChromatographyDesloratadinePoloxamer 407Particle size

摘要: The present study investigates the possibility of using poloxamers as solubility and dissolution rate enhancing agents poorly water soluble drug substance desloratadine that can be used for preparation immediate release tablet formulation. Two commercially available poloxamer grades (poloxamer P 188 407) were selected, solid dispersions (SDs) containing different weight ratio prepared by a low temperature melting method. All SDs subjected to basic physicochemical characterization thermal vibrational spectroscopy methods in order evaluate efficiency enhancers. Immediate tablets direct compression powdered according General Factorial Design, statistical significance two formulation (X(1) - type SD X(2) SD) one process variable (X(3) force) on rate. It was found existed amorphous state, largely responsible enhanced intrinsic solubility, which more pronounced 188. Statistical analysis factorial design revealed both investigated variables exert significant effect Increased resulted increased rate, with contributing faster than 407, accordance results tests. Moreover, there is interaction between force. Higher higher force decrease attributed lower porosity bonding particles.

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