Pakistan journal of pharmaceutical sciences · 2016
Formulation, evaluation and optimization of the felodipine nanosuspension to be used for direct compression to tablet for in vitro dissolution enhancement.
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Mori Dhaval, Makwana Jalpa, Parmar Ramesh, Patel Kalpesh, Chavda Jayant
Аннотация
The oral bioavailability of felodipine very low, nearly just 15% due to its limited solubility and high first pass metabolism. The present study was aimed to improve the rate of the dissolution of Felodipine by formulating a nano suspension of it by combination of high-speed homogenization and media milling technique. Stabilizers screened in this study were Poloxamer 401, HPMC K15M and Tween 80. Concentration of stabilizers were optimized by simplex lattice design for Mean Particle Size (MPS), Poly dispersity Index (PDI), saturation solubility (SS) and in vitro drug release in 30 min. The particle size of 201 nm and increase in saturation solubility of nearly 9 folds were obtained for optimize batch. The prepared nano suspension of drug was used as a granulating agent to form tablets having Microcrystalline Cellulose (MCC) as diluents. In vitro Drug release study indicates that more than 90% of the drug releases in 30 minutes. Preparing the nano suspension of the low solubility drug is an effective method to increase its saturation solubility. This nano suspension can be prepared effectively by combination of high-speed homogenization and media milling which is also very economical as well.