title: Preparation, characterization and tableting of cilnidipine solid dispersions.
abstract: Solid dispersion technique has been developed many years for improving solubility of water-insoluble drugs, aiming to achieve a better oral bioavailability. However, this technique exhibits many inconveniences when used for large-scale tableting procedures. The objective of current research work was to develop cilnidipine solid dispersions (SDs) to improve the dissolution behaviors of this water-insoluble drug. Moreover, an innovative granulation method was designed to simplify the traditional tableting technology used in solid dispersion technique. Three different kinds of polymers, polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and poloxamer, were used as carriers to prepare solid dispersions. The interactions in the solid state were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and FT-IR spectroscopy. The designed granulation method was employed to prepare solid dispersion tablets and the formulation was optimized through investigating the dissolution behaviors. The results indicated PEG solid dispersion showed the best effect both on physical characterizations and dissolution studies. Furthermore, all type of solid dispersions significantly improved the dissolution rates when compared to pure drug and its corresponding physical mixture (PM). The solid dispersion tablets prepared in simplified tableting method exhibited better operability, stability and dissolution behavior than the tablets prepared in traditional ways, which brought more opportunities to solid dispersion technique for industrial production.
authors.affiliation: College of Pharmaceutical Sciences, Hebei University, Baoding, China. hbupharm@126.com
authors.forename: Liandong
authors.initials: L
authors.lastname: Hu
authors.forename: Weihua
authors.initials: W
authors.lastname: Song
authors.forename: Feng
authors.initials: F
authors.lastname: Niu
authors.forename: Kuiliang
authors.initials: K
authors.lastname: Jiao
authors.forename: Zheng
authors.initials: Z
authors.lastname: Jia
mesh_terms: D001682:Biological Availability; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004095:Dihydropyridines / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D020442:Poloxamer / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D011208:Powders; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013607:Tablets / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D004095:Dihydropyridines; D004337:Drug Carriers; D011108:Polymers; D011208:Powders; D013607:Tablets; D014867:Water; D020442:Poloxamer; D011092:Polyethylene Glycols; C065927:cilnidipine; D011205:Povidone