title: Design and in vivo evaluation of oxycodone once-a-day controlled-release tablets.
abstract: The aim of present study was to design oxycodone once-a-day controlled-release (CR) tablets and to perform in vitro/in vivo characterizations. Release profiles to achieve desired plasma concentration versus time curves were established by using simulation software and reported pharmacokinetic parameters of the drug. Hydroxypropyl methylcellulose (HPMC) 100,000 mPa·s was used as a release modifier because the polymer was found to be resistant to changes in conditions of the release study, including rotation speed of paddle and ion strength. The burst release of the drug from the CR tablets could be suppressed by applying an additional HPMC layer as a physical barrier. Finally, the oxycodone once-a-day tablet was comprised of two layers, an inert HPMC layer and a CR layer containing drug and HPMC. Commercial products, either 10 mg bis in die (bid [twice a day]) or once-a-day CR tablets (20 mg) were administered to healthy volunteers, and calculated pharmacokinetic parameters indicated bioequivalence of the two different treatments. The findings of the present study emphasize the potential of oxycodone once-a-day CR tablets for improved patient compliance, safety, and efficacy, which could help researchers to develop new CR dosage forms of oxycodone.
authors: College of Pharmacy, Woosuk University, Wanju-gun, Republic of Korea.
authors: Ju-Young
authors: JY
authors: Kim
authors: School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea ; GL Pharmtech, Seongnam, Republic of Korea.
authors: Sung-Hoon
authors: SH
authors: Lee
authors: College of Pharmacy, Chungbuk National University, Cheongju, Republic of Korea.
authors: Chun-Woong
authors: CW
authors: Park
authors: College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju, Republic of Korea.
authors: Yun-Seok
authors: YS
authors: Rhee
authors: Department of Pharmaceutical Engineering, Cheongju University, Cheongju, Republic of Korea.
authors: Dong-Wook
authors: DW
authors: Kim
authors: GL Pharmtech, Seongnam, Republic of Korea.
authors: Junsang
authors: J
authors: Park
authors: GL Pharmtech, Seongnam, Republic of Korea.
authors: Moonseok
authors: M
authors: Lee
authors: School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea.
authors: Jeong-Woong
authors: JW
authors: Seo
authors: School of Pharmacy, Sungkyunkwan University, Suwon, Republic of Korea.
authors: Eun-Seok
authors: ES
authors: Park
mesh_terms: D000284:Administration, Oral; D000701:Analgesics, Opioid / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D004334:Drug Administration Schedule; D064368:Healthy Volunteers; D006801:Humans; D065347:Hypromellose Derivatives / Q000737:chemistry; D008297:Male; D010098:Oxycodone / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D012995:Solubility; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods; D013810:Therapeutic Equivalency
chemical_list: D000701:Analgesics, Opioid; D003692:Delayed-Action Preparations; D013607:Tablets; D065347:Hypromellose Derivatives; D010098:Oxycodone
keywords: double-layer tablet; in vitro–in vivo correlation; oral delivery; pharmacokinetics