title: Preparation and optimization of glyceryl behenate-based highly porous pellets containing cilostazol.
abstract: The aim of this study was to prepare a highly porous multiparticulate dosage form containing cilostazol for gastroretentive drug delivery. The floating pellets were prepared with glyceryl behenate as a matrix former and camphor as a sublimating agent by extrusion/spheronization and sublimation under vacuum. Granules prepared with sublimation at 60 °C displayed a slower dissolution rate and smoother surface morphology than those prepared at lower temperatures. This was unexpected as the reported melting point of glyceryl behenate is higher than 69 °C. The DSC study revealed that melting began at a lower temperature owing to the multicomponent property of glyceryl behenate, which led to a sintering effect. The prepared pellets were spherical with unimodal size distribution. They also had porous structures with increased porosity, which led to immediate buoyancy. As cilostazol is a hydrophobic drug that has an erosion-based release mechanism, drug release profile was highly correlated with the percentage of disintegrated pellets. Various excipients were added to the glyceryl behenate-based formulation to increase the floating duration. When hydroxyethyl cellulose was added to the glyceryl behenate-based pellets, acceptable dissolution rate and buoyancy were acquired. This system could potentially be used for gastroretentive delivery of various hydrophobic drugs, which was generally considered difficult.
authors.affiliation: a School of Pharmacy , Sungkyunkwan University , Suwon , Republic of Korea.
authors.forename: Kyu-Mok
authors.initials: KM
authors.lastname: Hwang
authors.affiliation: a School of Pharmacy , Sungkyunkwan University , Suwon , Republic of Korea.
authors.forename: Woojin
authors.initials: W
authors.lastname: Byun
authors.affiliation: a School of Pharmacy , Sungkyunkwan University , Suwon , Republic of Korea.
authors.forename: Cheol-Hee
authors.initials: CH
authors.lastname: Cho
authors.affiliation: a School of Pharmacy , Sungkyunkwan University , Suwon , Republic of Korea.
authors.forename: Eun-Seok
authors.initials: ES
authors.lastname: Park
mesh_terms: D001993:Bronchodilator Agents / Q000008:administration & dosage* / Q000737:chemistry; D000077407:Cilostazol; D003890:Desiccation; D004339:Drug Compounding; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry*; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage* / Q000737:chemistry; D016062:Porosity; D012995:Solubility; D013607:Tablets; D013777:Tetrazoles / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D001993:Bronchodilator Agents; D005079:Excipients; D005227:Fatty Acids; D010975:Platelet Aggregation Inhibitors; D013607:Tablets; D013777:Tetrazoles; C086409:glyceryl behenate; D000077407:Cilostazol
keywords: Floating; cilostazol; gastroretentive; glyceryl behenate; porous; sintering