Murali Monohar Pandey1, A Jaipal1, Shrikant Y Charde2, Puneet Goel1, Love Kumar1. 1. a Industrial Research Laboratory, Department of Pharmacy , Birla Institute of Technology & Science , Pilani , Rajasthan , India and. 2. b Department of Pharmacy , Birla Institute of Technology and Science , Pilani, Hyderabad , Andhra Pradesh , India.
Abstract
CONTEXT: Felodipine, a poorly soluble drug, is widely used in the treatment of angina pectoris and hypertension. OBJECTIVE: This study aimed at the preparation of amorphous solid dispersion (SD) of felodipine using an amphiphilic polymer, soluplus, for the potential enhancement in solubility of the drug. MATERIALS AND METHODS: Solid dispersions with varying proportions of drug and soluplus were prepared and the rate and extent of dissolution from SDs was compared with that of the pure drug. FT-IR and (1)H NMR spectroscopic analysis were carried out to examine the formation mechanism of SDs. Various techniques were used for solid state characterization of designed SDs. RESULTS: Formation of amorphous solid dispersions with particle size in nanometer range indicated suitability of polymer and method used in the preparation. FT-IR and (1)H NMR spectroscopy revealed that soluplus was involved in strong hydrogen bonding with felodipine molecules which resulted in the conversion of crystalline felodipine into amorphous form. Solid dispersion with 1:10 drug/polymer ratio showed more than 90% drug dissolution in 30 min whereas pure felodipine showed less than 19% drug dissolution in 1 h. DISCUSSION AND CONCLUSION: Amorphous SDs of felodipine were prepared using soluplus resulting in substantial enhancement in the rate and extent of dissolution of felodipine.
CONTEXT: Felodipine, a poorly soluble drug, is widely used in the treatment of angina pectoris and hypertension. OBJECTIVE: This study aimed at the preparation of amorphous solid dispersion (SD) of felodipine using an amphiphilic polymer, soluplus, for the potential enhancement in solubility of the drug. MATERIALS AND METHODS: Solid dispersions with varying proportions of drug and soluplus were prepared and the rate and extent of dissolution from SDs was compared with that of the pure drug. FT-IR and (1)H NMR spectroscopic analysis were carried out to examine the formation mechanism of SDs. Various techniques were used for solid state characterization of designed SDs. RESULTS: Formation of amorphous solid dispersions with particle size in nanometer range indicated suitability of polymer and method used in the preparation. FT-IR and (1)H NMR spectroscopy revealed that soluplus was involved in strong hydrogen bonding with felodipine molecules which resulted in the conversion of crystalline felodipine into amorphous form. Solid dispersion with 1:10 drug/polymer ratio showed more than 90% drug dissolution in 30 min whereas pure felodipine showed less than 19% drug dissolution in 1 h. DISCUSSION AND CONCLUSION: Amorphous SDs of felodipine were prepared using soluplus resulting in substantial enhancement in the rate and extent of dissolution of felodipine.