Special Issue "Pharmacokinetics of Orally Administered Drugs, 2nd Edition"

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmacokinetics and Pharmacodynamics".

Deadline for manuscript submissions: 20 June 2023 | Viewed by 810

Special Issue Editors

Research Unit for Inland Development (UDI), Polytechnic Institute of Guarda, Av. Dr. Francisco Sá Carneiro, 50, 6300-559 Guarda, Portugal
Interests: pharmacology; pharmacokinetics; bioanalysis; bioavailability; drug delivery; preclinical studies
Special Issues, Collections and Topics in MDPI journals
CICS-UBI—Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal
Interests: pharmacokinetics; ADME; bioavailability; drug evaluation; drug delivery; systemic drug exposure
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Oral administration has been the most common route of administration of medicines since it offers the greatest convenience to the patients. Even during the drug discovery process, a frequent requirement is that compounds should enable an adequate systemic exposure via the oral route. However, there are several factors that limit its oral bioavailability, such as poor aqueous solubility, hydrolysis of the drug in the gastrointestinal tract, limited permeability, particle size, extensive intestinal and hepatic first-pass metabolism, high affinity for efflux transporters, and the food effect, among others. To overcome these issues, several strategies have been explored to enhance oral bioavailability and thus systemic drug exposure, but further developments are needed. Therefore, the main goal of this editorial issue is to gather scientific information regarding the latest evidence and recent advances in this field, including the (nano)pharmaceutical approaches that have been explored to improve the bioavailability and pharmacokinetic profile of orally administered drugs.

Prof. Dr. Márcio Rodrigues
Prof. Dr. Gilberto Alves
Guest Editors

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  • oral bioavailability
  • absorption
  • pharmacokinetics
  • drug delivery
  • formulation

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Pharmacokinetic Feasibility of Stability-Enhanced Solid-State (SESS) Tenofovir Disoproxil Free Base Crystal
Pharmaceutics 2023, 15(5), 1392; https://doi.org/10.3390/pharmaceutics15051392 - 01 May 2023
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Tenofovir (TEV) is a nucleotide reverse transcriptase inhibitor used against human immunodeficiency virus (HIV) reverse transcriptase. To improve the poor bioavailability of TEV, TEV disoproxil (TD), an ester prodrug of TEV, was developed, and TD fumarate (TDF; Viread®) has been marketed [...] Read more.
Tenofovir (TEV) is a nucleotide reverse transcriptase inhibitor used against human immunodeficiency virus (HIV) reverse transcriptase. To improve the poor bioavailability of TEV, TEV disoproxil (TD), an ester prodrug of TEV, was developed, and TD fumarate (TDF; Viread®) has been marketed due to the hydrolysis of TD in moisture. Recently, a stability-enhanced solid-state TD free base crystal (SESS-TD crystal) was developed with improved solubility (192% of TEV) under gastrointestinal pH condition and stability under accelerated conditions (40 °C, RH 75%) for 30 days. However, its pharmacokinetic property has not been evaluated yet. Therefore, this study aimed to evaluate the pharmacokinetic feasibility of SESS-TD crystal and to determine whether the pharmacokinetic profile of TEV remained unchanged when administering SESS-TD crystal stored for 12 months. In our results, the F and systemic exposure (i.e., AUC and Cmax) of TEV in the SESS-TD crystal and TDF groups were increased compared to those in the TEV group. The pharmacokinetic profiles of TEV between the SESS-TD and TDF groups were comparable. Moreover, the pharmacokinetic profiles of TEV remained unchanged even after the administration of the SESS-TD crystal and TDF stored for 12 months. Based on the improved F after the SESS-TD crystal administration and the stable condition of the SESS-TD crystal after 12 months, SESS-TD crystal may have enough pharmacokinetic feasibility to replace TDF. Full article
(This article belongs to the Special Issue Pharmacokinetics of Orally Administered Drugs, 2nd Edition)
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