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Pharmacokinetics and Quantitative Structure-Pharmacokinetics Relationship Study of Xanthine Derivatives with Antidepressant, Anti-Inflammatory, and Analgesic Activity in Rats.
Pharmaceutics
November 2024
Department of Pharmacokinetics and Physical Pharmacy, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland.
Objective: The aim of this study was to develop quantitative structure-pharmacokinetics relationship (QSPKR) models for a group of xanthine derivatives with proven pharmacological activity and to investigate its applicability for the prediction of the pharmacokinetics of these compounds.
Methods: The SYBYL-X, KowWin, and MarvinSketch programs were employed to generate a total of fourteen descriptor variables for a series of new compounds: 7- and 7,8-substituted theophylline derivatives (GR-1-GR-8) and three well-known methylxanthines. Pharmacokinetic profiles of all compounds were determined after intravenous administration of studied compounds to cannulated male rats.
FDA and EMA Oversight of Disruptive Science on Application of Finite Absorption Time (F.A.T.) Concept in Oral Drug Absorption: Time for Scientific and Regulatory Changes.
Pharmaceutics
November 2024
Faculty of Pharmacy, National and Kapodistrian University of Athens, 15784 Athens, Greece.
It has been demonstrated that the concept of infinite absorption time, associated with the absorption rate constant, which drives a drug's gastrointestinal absorption rate, is not physiologically sound. The recent analysis of oral drug absorption data based on the finite absorption time (F.A.
View Article and Find Full Text PDFEvaluating Pharmacists' Knowledge of Food-Drug Interactions in Croatia: Identifying Gaps and Opportunities.
Pharmacy (Basel)
November 2024
Department of Pharmacy, University of Split School of Medicine, 21000 Split, Croatia.
Food-drug interactions (FDIs) are pharmacokinetic or pharmacodynamic changes in drug effects caused by the presence of specific foods. To identify and prevent FDIs, pharmacists, alongside other healthcare professionals, should possess a certain level of knowledge. This study aimed to assess knowledge of FDIs among Croatian pharmacists.
View Article and Find Full Text PDFNarrow Therapeutic Index Drugs: FDA Experience, Views, and Operations.
Clin Pharmacol Ther
January 2025
Division of Quantitative Methods and Modeling (DQMM), Office of Research and Standards (ORS), Office of Generic Drugs (OGD), Center for Drug Evaluation and Research (CDER), U.S. Food and Drug Administration (FDA), Silver Spring, Maryland, USA.
The U.S. Food and Drug Administration (FDA) has defined narrow therapeutic index (NTI) drugs as "those drugs where small differences in dose or blood concentration may lead to serious therapeutic failures and/or adverse drug reactions that are life-threatening or result in persistent or significant disability or incapacity.
View Article and Find Full Text PDFInvestigations on the Impacts of Drugs or Excipients with Different Physicochemical and Compaction Properties on the Disintegration Behavior of Kollidon®SR-Based Binary Controlled Release Matrix Tablets.
AAPS PharmSciTech
October 2024
Jerash University-Faculty of Pharmacy, Department of Pharmaceutical Sciences, Jerash, Jordan.
The objective of this study was to examine the impact of the physicochemical properties of the loaded drug or excipient, the concentration of Kollidon®SR (KSR), and the mechanical characteristics of KSR compacts on their disintegration times. Using disintegration apparatus, a two-hour constraint was chosen as the process's end point. Lactose-KSR compacts subjected to the highest compression pressure and Microcrystalline cellulose-KSR compacts with KSR concentrations exceeding 30% exhibited disintegration times of less than ten minutes.
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