Investigation of the Permeability of Antiretroviral Drugs Lamivudine and Valganciclovir <i>via</i> Single-Pass Intestinal Perfusion (SPIP) Method


ŞANLI S., KAYNAK M. S., Sanli N., Balta E. E.

CURRENT PHARMACEUTICAL ANALYSIS, 2024 (SCI-Expanded) identifier

Abstract

Introduction: Antiretroviral medications are widely used to treat HIV infections. Lamivudine (3TC) is prescribed for HIV-1 infection management in adults and pediatrics, while valganciclovir (VGC) is a prodrug of ganciclovir derived from valine. Method: The Biopharmaceutics Classification System (BCS) estimates the contributions of intestinal permeability, dissolution, and solubility in oral drug absorption. Intestinal permeability refers to a substance's capacity to pass through the protective layer of cells in the intestine. The intestinal permeability of 3TC and VGC was analyzed and categorized using the single-pass intestinal perfusion technique according to the BCS in male Sprague Dawley rats, and a reversed-phase HPLC method was validated for precise and accurate measurement. Result: According to the BCS, 3TC and VGC have been classified as having low permeability when compared to metoprolol tartrate, which is classified as Class I with good permeability and resolution. Conclusion: The permeability values derived from this work can be valuable in exposure assessment models.