Multi-Segmental Evaluation of Intestinal Permeability of Amlodipine at Two Dose Levels

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dc.contributor.authorAtes, Muge
dc.contributor.authorStelmasinska, Agata Bogacz
dc.contributor.authorStelmasinska, Michal
dc.contributor.authorBarre, Liban
dc.contributor.authorBuyuktuncel, Ebru
dc.contributor.authorKaynak, Mustafa Sinan
dc.contributor.authorSahin, Selma
dc.date.accessioned2026-04-04T13:32:56Z
dc.date.available2026-04-04T13:32:56Z
dc.date.issued2025
dc.departmentİnönü Üniversitesi
dc.description.abstractBackground Intestinal permeability plays a crucial role in drug absorption, as it varies across different gastrointestinal regions, affecting the bioavailability of orally administered drugs. This variability, combined with dose-dependent absorption, influences the overall efficacy and pharmacokinetics of the drug.Objective This study aimed to investigate the impact of three intestinal regions (jejunum, ileum, and colon) along with two different doses of amlodipine (AML) (5 mg and 10 mg) on its permeability.Methods An optimized HPLC method was developed and validated for the simultaneous quantification of AML, metoprolol (MTP), and phenol red (PR), while a modified single-pass intestinal perfusion (SPIP) was used to assess AML permeability across different intestinal segments.Results Net Water Flux (NWF) showed significant fluctuations, with high positive values in the colon, indicating distinct physiological responses in this region. The effective permeability (Peff) of AML varied across different intestinal segments and doses. In the jejunum and ileum, the Peff of AML decreased with increasing doses from 5 mg to 10 mg, while in the colon, Peff remained relatively stable. Peff values ranged from 3.50 x 10-4 cm/s for the 5 mg dose to 1.80 x 10-4 cm/s for the 10 mg dose in the jejunum, from 3.30 x 10-4 cm/s (5 mg) to 2.41 x 10-4 cm/s (10 mg) in the ileum, and from 6.65 x 10-4 cm/s (5 mg) to 6.79 x 10-4 cm/s (10 mg) in the colon.Conclusion This study demonstrated significant segmental and dose-dependent variations in the intestinal permeability of AML using the SPIP model in rats.
dc.identifier.doi10.2174/0113816128381339250422080602
dc.identifier.issn1381-6128
dc.identifier.issn1873-4286
dc.identifier.orcid0000-0001-8075-6622
dc.identifier.orcid0000-0001-5736-5906
dc.identifier.pmid41334613
dc.identifier.scopus2-s2.0-105023584720
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.2174/0113816128381339250422080602
dc.identifier.urihttps://hdl.handle.net/11616/108805
dc.identifier.wosWOS:001629229300001
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherBentham Science Publ Ltd
dc.relation.ispartofCurrent Pharmaceutical Design
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.snmzKA_WOS_20250329
dc.subjectAmlodipine
dc.subjectintestinal permeability
dc.subjectPerfusion coefficient
dc.subjectileum
dc.subjectdrug absorption
dc.subjectSPIP
dc.titleMulti-Segmental Evaluation of Intestinal Permeability of Amlodipine at Two Dose Levels
dc.typeArticle

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