title: Release kinetics of highly porous floating tablets containing cilostazol.
abstract: This study focuses on developing a highly porous floating tablet containing cilostazol. The underlying release mechanism of cilostazol from porous and floating tablets in dissolution media containing surfactants was investigated. The tablets were prepared by compressing granules and excipients with a sublimating agent, followed by sublimation under vacuum. The volatile material for the sublimating agent was chosen based on its flow properties using conventional methods as well as the twisted blade method. Resultant tablets could float immediately and had significantly higher tensile strengths than conventional tablets of similar porosities, holding a promising potential for increasing gastroretentive properties. Fitting the release profiles to the Korsmeyer-Peppas equation indicated Super Case II, Case II and non-Fickian kinetics, which implied that the release was affected by both floating behavior and matrix erosion. Abrupt changes in release kinetic parameters and erosional behaviors were found between the tablets containing different amounts of HPMC, indicating the existence of an excipient percolation threshold. Neither the surfactant in the media nor the porosity affected the dominant release mechanism, which was matrix erosion. Understanding the dominant release mechanism and percolation threshold allows for tuning the formulation to obtain various release profiles.
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
authors.forename: Kyu-Mok
authors.initials: KM
authors.lastname: Hwang
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
authors.forename: Cheol-Hee
authors.initials: CH
authors.lastname: Cho
authors.affiliation: Department of Pharmaceutics, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem, Ha Noi, Viet Nam.
authors.forename: Nguyen-Thach
authors.initials: NT
authors.lastname: Tung
authors.affiliation: College of Pharmacy, Woosuk University, Wanju-gun 55338, Republic of Korea.
authors.forename: Ju-Young
authors.initials: JY
authors.lastname: Kim
authors.affiliation: College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju 52828, Republic of Korea.
authors.forename: Yun-Seok
authors.initials: YS
authors.lastname: Rhee
authors.affiliation: School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea. Electronic address: espark@skku.edu.
authors.forename: Eun-Seok
authors.initials: ES
authors.lastname: Park
mesh_terms: D002626:Chemistry, Pharmaceutical / Q000379:methods; D000077407:Cilostazol; D003692:Delayed-Action Preparations / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005079:Excipients / Q000737:chemistry; D007700:Kinetics; D007785:Lactose / Q000031:analogs & derivatives / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D016062:Porosity; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013607:Tablets / Q000737:chemistry*; D013777:Tetrazoles / Q000737:chemistry*
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D013501:Surface-Active Agents; D013607:Tablets; D013777:Tetrazoles; C509290:hydroxypropylmethylcellulose-lactose matrix; D008747:Methylcellulose; D007785:Lactose; D000077407:Cilostazol
keywords: Cilostazol; Floating; Gastroretentive; Hydrophobic; Percolation threshold; Porous; Powder rheometer; Release kinetics