title: Formulation of controlled-release pelubiprofen tablet using Kollidon(®) SR.
abstract: To develop a matrix-type, controlled-release tablet formulation of pelubiprofen (PLB), a recently developed non-steroidal anti-inflammatory drug, polymeric excipients including hypromellose, hydroxypropylcellulose, Eudragit(®) RS PO, and Kollidon(®) SR were screened. A formulation containing 12.4% w/w Kollidon(®) SR (K2 tablet) was found to be the most promising and stable for 6 months in an accelerated stability test. PLB release from K2 tablet was limited at pH 1.2, but gradually increased at pH 6.8 with a surface-erosion, resulting in the best fit to Hixson-Crowell equation. Comparative human PK studies were performed using a randomized, 2-way crossover design. LC-MS/MS assay revealed that the plasma level of PLB-transOH, an active metabolite, was significantly higher than that of PLB. After multiple dosing of immediate-release tablet (R) and K2 tablet (T), the T/R ratios of AUC were 1.02 and 1.04 for PLB and PLB-transOH, respectively. Level A in vitro-in vivo correlation was established for the K2 tablet-administered group. PK profile of PLB-transOH was not influenced by food intake, while that of PLB was altered. We suggest that K2 tablet could be administered twice a day without being affected by food intake, thereby enhancing patient compliance.
authors: Daewon Pharm. Co., Ltd., 520 Cheonhodae-ro, Gwangjin-gu, Seoul 04994, Republic of Korea. Electronic address: 208058@daewonpharm.com.
authors: Seh Hyon
authors: SH
authors: Song
authors: Daewon Pharm. Co., Ltd., 520 Cheonhodae-ro, Gwangjin-gu, Seoul 04994, Republic of Korea. Electronic address: hifyram@daewonpharm.com.
authors: Bo Ram
authors: BR
authors: Chae
authors: Daewon Pharm. Co., Ltd., 520 Cheonhodae-ro, Gwangjin-gu, Seoul 04994, Republic of Korea. Electronic address: sisohn@daewonpharm.com.
authors: Se Il
authors: SI
authors: Sohn
authors: College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul 06974, Republic of Korea. Electronic address: yeompd@naver.com.
authors: Dong Woo
authors: DW
authors: Yeom
authors: College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul 06974, Republic of Korea. Electronic address: lakers0204@naver.com.
authors: Ho Yong
authors: HY
authors: Son
authors: College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul 06974, Republic of Korea. Electronic address: jinhan8910@daum.net.
authors: Jin Han
authors: JH
authors: Kim
authors: College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul 06974, Republic of Korea. Electronic address: kimsrkr@naver.com.
authors: Sung Rae
authors: SR
authors: Kim
authors: College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul 06974, Republic of Korea. Electronic address: idealgon@gmail.com.
authors: Sang Gon
authors: SG
authors: Lee
authors: College of Pharmacy, Chung-Ang University, 84 Heuksuk-ro, Dongjak-gu, Seoul 06974, Republic of Korea. Electronic address: ywchoi@cau.ac.kr.
authors: Young Wook
authors: YW
authors: Choi
mesh_terms: D000328:Adult; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D065546:Drug Liberation; D004355:Drug Stability; D004435:Eating; D005079:Excipients / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D010666:Phenylpropionates / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility; D013607:Tablets / Q000737:chemistry / Q000493:pharmacokinetics; D055815:Young Adult
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D010666:Phenylpropionates; D013607:Tablets; C040375:pelubiprofen
keywords: Controlled release; Food effect; Kollidon(®) SR; Matrix tablet; Pelubiprofen; Pharmacokinetic