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Updated: May 11, 2026
10:22
In Vitro and In Vivo Approaches to Determine Intestinal Epithelial Cell Permeability
Published on: October 19, 2018
Intestinal permeability of Lamivudine using single pass intestinal perfusion
1Pharmacology Department, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM's NMIMS, Mithibai College, Mumbai-400 056, India.
Indian Journal of Pharmaceutical Sciences
|May 30, 2013
Summary
Lamivudine, a key HIV medication, demonstrates high intestinal permeability in rats, suggesting excellent absorption. This finding supports its classification as a Biopharmaceutics Classification System Class I drug.
Area of Science:
- Pharmacokinetics
- Drug Absorption
- Gastrointestinal Physiology
Background:
- Lamivudine is a crucial nucleotide reverse transcriptase inhibitor used in HIV treatment.
- Understanding its intestinal transport is vital for optimizing drug efficacy.
- Previous studies may not have fully elucidated its absorption characteristics across the small intestine.
Purpose of the Study:
- To investigate the intestinal transport and permeability of lamivudine in a preclinical model.
- To determine the effective intestinal permeability (Peff) of lamivudine.
- To assess lamivudine's suitability for Biopharmaceutics Classification System (BCS)-based biowaivers.
Main Methods:
- Utilized the single-pass intestinal perfusion (SPIP) technique in male Wistar rats.
- Administered lamivudine through the small intestine at a controlled flow rate of 0.20 ml/min.
- Measured lamivudine's effective permeability (Peff) to assess its absorption.
Main Results:
- Lamivudine exhibited high intestinal permeability throughout the small intestine.
- The measured Peff values indicate that lamivudine is readily absorbed.
- Results align with drugs possessing high intestinal permeability and high fraction of dose absorbed.
Conclusions:
- Lamivudine demonstrates favorable intestinal absorption characteristics.
- The drug is a strong candidate for Biopharmaceutics Classification System Class I designation.
- The permeability data can inform exposure assessment models and support biowaiver strategies.
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