Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Decreased Penetration Mechanism of Ranitidine Due to Application of Sodium Sulfobutyl Ether-β-Cyclodextrin

Version 1 : Received: 11 October 2023 / Approved: 11 October 2023 / Online: 12 October 2023 (20:13:47 CEST)

A peer-reviewed article of this Preprint also exists.

Yang, R.; Zhang, J.; Huang, J.; Wang, X.; Yang, H.; Jin, Q. Decreased Penetration Mechanism of Ranitidine Due to Application of Sodium Sulfobutyl Ether-β-Cyclodextrin. Pharmaceutics 2023, 15, 2593. Yang, R.; Zhang, J.; Huang, J.; Wang, X.; Yang, H.; Jin, Q. Decreased Penetration Mechanism of Ranitidine Due to Application of Sodium Sulfobutyl Ether-β-Cyclodextrin. Pharmaceutics 2023, 15, 2593.

Abstract

Permeability has an important effect on drug absorption. In this study, the effect of different concentrations of sodium sulfobutyl ether-β-cyclodextrin (SBE-β-CD) on the absorption of ranitidine was investigated to examine the mechanism of permeability changes. The results of parallel artificial membrane permeability assay (PAMPA) showed that increasing the concentration of sodium sulfobutyl ether-β-cyclodextrin, 0, 0.12% (w/v), 0.36% (w/v) and 3.6% (w/v), respectively, the apparent permeability coefficient of ranitidine decreased to 4.62×10-5 , 4.5×10-5 , 3.61×10-5 and 1.08×10-5 in Caco-2 cells, respectively. The same results were obtained from oral pharmacokinetic study in rats; Further studies indicated that SBE-β-CD significantly increased the zeta potential of ranitidine. SBE-β-CD interacted with ranitidine charges to form a complex that reduced ranitidine permeability, and SBE-β-CD should be chosen with caution for drugs with poor permeability.

Keywords

sodium sulfobutyl ether-β-cyclodextrin; ranitidine; apparent permeability coefficient; permeability; inhibition

Subject

Medicine and Pharmacology, Medicine and Pharmacology

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