Contact
    Start Publications A thorough analysis of the effect of surfactant/s on the ...
    ←  Publication Finder
    Attension

    A thorough analysis of the effect of surfactant/s on the solubility and pharmacokinetics of (S)-zaltoprofen

    Year: 2019

    Journal: Asian J. Pharm. Sci., Volume 14, JUL, page 435–444

    Authors: Cuong Viet Pham; Baek, Jong-Suep; Park, Jong-Hun; Jung, Sang-Hun; Kang, Jong-Seong; Cho, Cheong-Weon

    Organizations: Basic Science Research Program through the National Research Foundation of Korea (NRF) - Ministry of Education, Science and Technology [2016R1A2B4011294]

    Keywords: (S)-zaltoprofen; Solubility; Bioavailability; D-alpha tocopheryl polyethylene glycol 1000 succinate; 2-hydroxypropyl-beta-cyclodextrin

    Until now, there are no publications about the preformulation studies on (S)-zaltoprofen ((S)-ZPF). Hence, we first investigated the solubility of (S)-ZPF, screened solubilizers and performed the pharmacokinetic study of (S)-ZPF in the presence of the solubilizers. The measurement of the solubility of (S)-ZPF in 26 different solvents was carried out, including D-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS), 2-hydroxypropyl-beta-cyclodextrin (HPCD), and mixtures of individual solvent. The plasma concentration of (S)-ZPF and the amount of (S)-ZPF retained in stomach were determined after oral (35.0 mg/kg) and intravenous (5.0 mg/kg) administration. The solubility of (S)-ZPF showed an increase of 484-fold in TPGS compared to its aqueous solubility. There was a significant increase of AUC(0-24 h) for pure (S)-ZPF in the TPGS group (813.59 +/- 64.17 mu g.h/ml) in comparison with AUC(0-24 h) in the HPCD group (595.57 +/- 71.76 mu g.h/ml) and water group (465.57 +/- 90.89 mu g.h/ml). In addition, the T-max of (S)-ZPF in the TPGS group was 2 h, much faster than that in the HPCD or water groups (5.50 or 5.67 h, respectively). This suggested that TPGS played a significant role in the increase of solubility and bioavailability of (S)-ZPF. (C) 2018 Shenyang Pharmaceutical University. Published by Elsevier B.V.
    View publication