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A thorough analysis of the effect of surfactant/s on the solubility and pharmacokinetics of (S)-zaltoprofen by Cuong Viet Pham; Jong-Suep Baek; Jong-Hun Park; Sang-Hun Jung; Jong-Seong Kang; Cheong-Weon Cho is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.
What is A thorough analysis of the effect of surfactant/s on the solubility and pharmacokinetics of (S)-zaltoprofen about?
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-βcyclodextrin (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 μg h/ml) in comparison with AUC 0-24 h in the HPCD group (595.57 ± 71.76 μg h/ml) and water group (465.57 ± 90.89 μg 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 o
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- Author
- Cuong Viet Pham; Jong-Suep Baek; Jong-Hun Park; Sang-Hun Jung; Jong-Seong Kang; Cheong-Weon Cho
- Publisher
- Elsevier BV
- Published
- 2018
- Language
- EN
- Field
- Pharmacology, Toxicology and Pharmaceutics (Life Sciences)