title: Preparation and evaluation of nicotinic acid sustained-release pellets combined with immediate release simvastatin.
abstract: This study was performed to prepare high-dose nicotinic acid (NA) loaded sustained-release pellets coated with double polymer and simvastatin (SIM). The uncoated pellets were prepared by extrusion-spheronization and the double ethylcellucose (EC) films were coated in a bottom-spray fluidized bed coater. SIM was milled by wet grinding and then the milled suspension was layered on the coated pellets. Results showed that coated with 1.5% subcoating and 1% outer coating composed of EC and polyvinyl pyrrolidone K30 (PVP(K30)) in ratios of 5:1 and 2:1, NA release behavior was very similar to the reference (NER/S; SIMCOR, Abbott) in different media. And SIM was delivered more rapidly than that of the reference, while the SIM layer had no influence on NA release. During 6-month storage at 40°C/75% RH, the two drugs exhibited stable dissolution behavior. It was observed that the content uniformity of SIM was provided by the present preparation and SIM was stable if adding light magnesium oxide in the grinding procedure. Results indicated it was possible to prepare high-dose sustained-release NA pellets combined with little-dose immediate release SIM by spraying double EC polymer and SIM milled suspension on NA pellets in a bottom-spray fluidized bed coater, respectively.
authors.affiliation: Department of Pharmaceutics, Shenyang Pharmaceutical University, Wen Hua Road No. 103, Shenyang 110016, Liaoning, People's Republic of China.
authors.forename: Xingna
authors.initials: X
authors.lastname: Zhao
authors.forename: Guofei
authors.initials: G
authors.lastname: Li
authors.forename: Lili
authors.initials: L
authors.lastname: Zhang
authors.forename: Xiaoguang
authors.initials: X
authors.lastname: Tao
authors.forename: Tingting
authors.initials: T
authors.lastname: Guan
authors.forename: Mo
authors.initials: M
authors.lastname: Hong
authors.forename: Xing
authors.initials: X
authors.lastname: Tang
mesh_terms: D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004338:Drug Combinations; D004339:Drug Compounding; D004355:Drug Stability; D004356:Drug Storage; D005079:Excipients / Q000737:chemistry; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000737:chemistry*; D008689:Methacrylates / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D009525:Niacin / Q000008:administration & dosage / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D019821:Simvastatin / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility
chemical_list: D003692:Delayed-Action Preparations; D004338:Drug Combinations; C477853:Eudragit NE 30-D; D005079:Excipients; D000960:Hypolipidemic Agents; D008689:Methacrylates; D011108:Polymers; D009525:Niacin; C013517:ethyl cellulose; D002482:Cellulose; D019821:Simvastatin; D011205:Povidone