title: Preparation and evaluation of solid dispersion of atorvastatin calcium with Soluplus® by spray drying technique.
abstract: The aim of the present study was to investigate the effect of Soluplus® on the solubility of atorvastatin calcium and to develop a solid dispersion formulation that can improve the oral bioavailability of atorvastatin calcium. We demonstrated that Soluplus® increases the aqueous solubility of atorvastatin calcium. Several solid dispersion formulations of atorvastatin calcium with Soluplus® were prepared at various drug : carrier ratios by spray drying. Physicochemical analysis demonstrated that atorvastatin calcium is amorphous in each solid dispersion, and the 2 : 8 drug : carrier ratio provided the highest degree of sustained atorvastatin supersaturation. Pharmacokinetic analysis in rats revealed that the 2 : 8 dispersion significantly improved the oral bioavailability of atorvastatin. This study demonstrates that spray-dried Soluplus® solid dispersions can be an effective method for achieving higher atorvastatin plasma levels.
authors.affiliation: College of Pharmacy, Pusan National University.
authors.forename: Eun-Sol
authors.initials: ES
authors.lastname: Ha
authors.forename: In-hwan
authors.initials: IH
authors.lastname: Baek
authors.forename: Wonkyung
authors.initials: W
authors.lastname: Cho
authors.forename: Sung-Joo
authors.initials: SJ
authors.lastname: Hwang
authors.forename: Min-Soo
authors.initials: MS
authors.lastname: Kim
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000069059:Atorvastatin; D001682:Biological Availability; D003890:Desiccation; D006538:Heptanoic Acids / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D008297:Male; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000494:pharmacology*; D011145:Polyvinyls / Q000737:chemistry* / Q000494:pharmacology*; D011758:Pyrroles / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility / Q000187:drug effects; D014867:Water / Q000737:chemistry
chemical_list: D006538:Heptanoic Acids; D011145:Polyvinyls; D011758:Pyrroles; C572167:polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer; D014867:Water; D011092:Polyethylene Glycols; D000069059:Atorvastatin