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. 2023 Nov 6;15(11):2593.
doi: 10.3390/pharmaceutics15112593.

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

Rui Yang  1 , Jing Zhang  1 , Jiaqi Huang  1 , Xiaofeng Wang  1 , Huiying Yang  1 , Qingri Jin  2
Affiliations

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

Rui Yang et al. Pharmaceutics. .

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 a 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, 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.

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

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
SBE-β-CD and ranitidine form a complex to reduce permeability.
Figure 2
Figure 2
Effect of different concentrations of SBE-β-CD on ranitidine permeability in PAMPA test. (A): Different concentrations of SBE-β-CD on ranitidine permeability, (B): the ANOVA test of ranitidine Papp value. *** p < 0.001.
Figure 3
Figure 3
Effect of different concentrations of SBE-β-CD on ranitidine permeability in Caco-2 cell analysis. *** p < 0.001.
Figure 4
Figure 4
Ranitidine plasma concentration–time curve in rats.
Figure 5
Figure 5
The zeta potential curves of different concentrations of SBE-β-CD solutions and mixed solutions of SBE-β-CD and ranitidine. ** p < 0.01.
See this image and copyright information in PMC

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