Biopharmaceutics

The main objective of the course is the complete presentation of the effects on the therapeutic efficacy and safety of pharmaceutical products due to formulation factors (manufacturing methods and conditions) as well as the routes of administration combined with the effects of the physicochemical properties of the active substances. In order to achieve the above objective a prerequisite is the understanding of the action of the following factors and mechanisms: (1) the mechanism of drug release from the formulation into gastrointestinal fluids (GΙΤ), and the technological methods of modifying it; 2) (3) factors that cause bioconversion of the drug such as pre-systemic metabolism in the different physiological settings of the GΙΤ, a phenomenon οf the gastrointestinal epithelium, the absorption in the general circulation, tissue distribution, and the possible association of the drug with the plasma proteins; 5) mechanisms for removing the drug from the body such as Excretion and metabolism, as well as the concept of renal and hepatic clearance. 6) Absorption mechanisms via alternative routes of administration beyond oral administration. Laboratory classes complementing theater lectures help students to familiarize with the above processes. The main objective of the course is the complete presentation of the effects on the therapeutic efficacy and safety of pharmaceutical products due to formulation factors (manufacturing methods and conditions) as well as the routes of administration combined with the effects of the physicochemical properties of the active substances. In order to achieve the above objective, a prerequisite is to understand the mechanism of action of the drug release from the formulation in gastrointestinal tract fluids (GΙΤ), biotransforming agents and biotransformation agents as well as uptake mechanisms.

Introduction-Definitions. Pharmacokinetic parameters and patterns of drug absorption, distribution, metabolism and excretion. Bioavailability and bioequivalence of formulations and active substances. Drug route from drug to environmental fluid (direct and modified release forms, mechanisms, mathematical expression and modes of study of release). Movement of pharmacopoeias in the gastrointestinal tract (anatomy and gastrointestinal tract physiology, biological barriers and mechanisms for the transport and absorption of drugs, physiological and pharmacological factors affecting the bioavailability of per os administered formulations). Other routes of drug delivery (oral cavity, skin, muscle, rectum, nasal cavity, lungs, etc.). The drug after arrival in the general circulation (distribution, protein binding and removal). Elimination and metabolism of drugs (renal and hepatic clearance, hepatotoxic excretion and enterohepatic circulation). First-pass phenomenon (factors affecting its manifestation and effects on the bioavailability of drugs). Dosage in special cases of drugs and illnesses. Laboratory exercises of pharmacokinetic simulation and computation of pharmacokinetic parameters with the help of computers and interactive self-study programs. In Vivo - In Vivo Pharmacokinetic Relationship Relationships of Pharmaceutical Formulations and Active Substances.

04-05-2020