Decreased Penetration Mechanism of Ranitidine Due to Application of Sodium Sulfobutyl Ether-β-Cyclodextrin
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...
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| Main Authors: | , , , , , |
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| Format: | Book |
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MDPI AG,
2023-11-01T00:00:00Z.
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| Summary: | 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<sup>−5</sup>, 4.5 × 10<sup>−5</sup>, 3.61 × 10<sup>−5</sup> and 1.08 × 10<sup>−5</sup> 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. |
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| Item Description: | 10.3390/pharmaceutics15112593 1999-4923 |