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

• Main Authors: Rui Yang (Author), Jing Zhang (Author), Jiaqi Huang (Author), Xiaofeng Wang (Author), Huiying Yang (Author), Qingri Jin (Author)
• Format: Book
• Published: MDPI AG, 2023-11-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/pharmaceutics15112593; 1999-4923
• Keywords: sodium sulfobutyl ether-β-cyclodextrin; ranitidine; apparent permeability coefficient; permeability; inhibition; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 15, Iss 11, p 2593 (2023)

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 a parallel artificial membrane permeability assay (PAMPA) showed that increasing the concentration of sodium sulfobutyl ether-β-cyclodextrin, 0, 0.12% (<i>w</i>/<i>v</i>), 0.36% (<i>w/v</i>) and 3.6% (<i>w/v</i>), respectively, caused the apparent permeability coefficient of ranitidine to decrease 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 an 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.