CHIMICA FARMACEUTICA APPLICATA

The course aims to provide the methodological basis and the knowledge necessary for the "Study of the release and direction of drugs", through the deepening of chemical, physical and technological methods capable of conditioning liberation, absorption, distribution, directing and eliminating drugs. Provide the knowledge of the pharmacokinetic study of a drug. Provide the knowledge of innovative pharmaceutical forms.

The course will be carried out through frontal lessons with the help of PowerPoint presentations and through experiences carried out in the laboratory by students group on specific topics as reported in the program on calorimetric techniques and surface potential measurements

http://www.dsf.unict.it/sites/default/files/files/ORARIO%20CDLS%20CTF%20I.pdf

COURSE PROGRAM

With an asterisk *, the less necessary subjects for passing the exam are indicated.

- Bioavailability and Bioequivalence. - Chemical Kinetics: kinetics of the decomposition of drugs. Reaction speed, order of reaction. Zero-order degradation reactions; half-life and t90%. Kinetics of the decomposition of the first order. Pseudo-first order reactions. Second order reactions *. Complex reactions *. Methods for determining the order of a reaction. Dependency of the reaction speed from the temperature; Arrhenius equation. Calculation of the expiration date of a drug. Biopharmaceutical and drug transfer kinetics models: one-compartment model, two-compartment model closed *, two-compartment model open, multi-compartmental models *. The transport of drugs, passive diffusion and its laws. Time trend of the quantity of a drug in the various compartments. Blood levels and bioavailability curves. Parameters that influence bioavailability. Dosage regimes Intravenous Infusion and Clearance Preformulation studies: Chemical and / or physical properties of the active substance: (solubility, dissolution and influencing factors, crystallinity, polymorphism, particle size). Thermal analysis Partition coefficient. Lipophilicity. Interface phenomena: Surface tension; Film-balance; micellization; Liquid crystals Electrical properties of the interfaces: Zeta potential; Dispersed systems and their properties Ionization and prediction of the absorption in function: of the pH of the medium, of the pKa and of the partition coefficient of the active ingredient. Prodrug and release systems *.

- Natural and synthetic polymers (structure, chemical-physical properties, binding methods).

- Polymers in solution.
Controlled Release Polymer Systems: Deposit Systems; Homogeneous matrix systems with dissolved active ingredient; Homogeneous matrix systems with dispersed active principle; Methods to condition the release or to convey and direct the active ingredients.

a) Polymer-related drugs - Drugs incorporated into biodegradable polymers.

b) Therapeutic systems with general action: osmotic micro-pumps, implants,

c) Transdermal systems.

d) Therapeutic tank systems with localized action: ophthalmic systems and gynecological systems *.

e) Nanoparticulate therapeutic systems: microcapsules, vesicular forms (liposomes, nanoparticles, SLN and NLC).

Stability and stabilization *. Chemical factors of drug instability *. Reactions of hydrolysis, oxidation, polymerization and photodegradation *. Prevention methods *. Freeze drying *. Antioxidants and antioxidant synergists *. Bacterial pollution of pharmaceutical forms and its prevention *. Antimicrobials *. Kinetics of the decomposition of solid forms Drug interactions and incompatibilities

1. R. Notari, Biofarmaceutica e Farmacocinetica, Piccin Ed.
2. P. Buri, F. Puisieux, E. Doelker e J.P. Benoit, Formes Farmaceutiques Nouvelles, Rec e Doc, Paris (1985).
3. A.N. Martin, J. Swarbrik, A. Cammarata, Physical Pharmacy, Lea and Febiger, Philadelphia.
4. A.T. Florence, D.T. Attwood, Le Basi Chimico-Fisiche della Tecnologia Farmaceutica, EdiSES,Napoli (2002).
5. M. Amorosa, Principi di Tecnica Farmaceutica, Libreria Universale L. Tinarelli - Bologna (1989).
6. Remington's, Pharmaceutical Sciences, Mack Publishing Company.
7. L. Shargel and A.B.C. Yu, Applied Biopharmaceutics and Pharmacokinetics, Appleton&Lange, USA VI EDIZIONE.
8. P. Colombo, P.L. Catellani, A. Cazzaniga, E. Menegatti, E. Vidale, Principi di Tecnologie Farmaceutiche, Casa Editrice Ambrosiana.