Release kinetics of highly porous floating tablets containing cilostazol

  • Hwang, Kyu-Mok; 
  • Cho, Cheol-Hee; 
  • Nguyen-Thach Tung; 
  • Kim, Ju-Young; 
  • Rhee, Yun-Seok; 
  • 외 1명
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초록

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. (C) 2017 Elsevier B.V. All rights reserved.

키워드

Cilostazol; Floating; Porous; Release kinetics; Gastroretentive; Hydrophobic; Percolation threshold; Powder rheometer; HYDROPHILIC MATRIX TABLETS; DRUG-DELIVERY SYSTEMS; WATER-SOLUBLE DRUG; HYDROXYPROPYLMETHYLCELLULOSE HPMC; SUSTAINED-RELEASE; FLOW PROPERTIES; PARTICLE-SIZE; GEL-LAYER; DISSOLUTION; EROSION
제목
Release kinetics of highly porous floating tablets containing cilostazol
저자
Hwang, Kyu-Mok; Cho, Cheol-Hee; Nguyen-Thach Tung; Kim, Ju-Young; Rhee, Yun-Seok; Park, Eun-Seok
DOI
10.1016/j.ejpb.2017.01.027
발행일
2017-06
유형
Article
저널명
European Journal of Pharmaceutics and Biopharmaceutics
권
115
페이지
39 ~ 51