37259 - Modified Release Pharmaceutical Systems

Course Unit Page

Academic Year 2018/2019

Course contents

MODIFIED DRUG RELEASE - 4 cfu (Prof. B. Luppi)

Bioavailability and Modified drug release

Immediate release systems and modified release systems: definition, biopharmaceutical, clinical and indutrial aim. The concept of biopharmaceutics. LADME. Bioequivalence. Important factors influencing steady-state plasma concentration of a drug. Repeat action versus sustained action drug therapy.

Diffusion in polymeric systems

Polymeric systems and main mechanism of drug release. Theory of mass transfert. Fick's First and Second Lows.  Diffusion coefficient. Partition coefficient. Stagnant diffusion layer. Macroporous systems, microporous systems and unporous systems. Diffusion through hydrate polymers. Solubility and partition coefficient.

Modified drug delivery systems

Controlled release kinetics. A) Diffusion controlled devices. I) Monolithic devices. II) Reservoir devices. B) Chemically controlled devices. C) Solvent controlled devices: I) Osmotically controlled devices. II) Swelling controlled devices. D) Pulsatile systems and intelligent systems.

 

DRUG DELIVERY - 4 cfu (Prof. B. Luppi)

 

Enhancement of solubility and dissolution rate

Dissolution and Noyes-Whitney Law. Thermodynamic parameters (Gibbs equation and Van't Hoff equation). Solubility enhancement strategies. Micellation. Complexation. Cyclodextrins and phase-solubility diagrams. Salification.

Pharmaceutical polymers

Classification. Crystalline and amorphous polymers. Polymer synthesis: addition polymerization and condensation polymerization. Water-soluble polymers. Water-insoluble polymers. Biocompatible and biodegradable polymers. Examples of pharmaceutical polymers.

Drug targeting and site-specific delivery

Main mechanisms of spatial controlled drug release: drug targeting and site-specific delivery. Passive targeting. Physical targeting. Active targeting. Pharmaceutical carries. Micro and nanoparticulate carriers (spheres, capsules, liposomes, niosomes, polymeric micelles, solid lipid nanoparticles), macromolecular carriers and cellular carriers.

Readings/Bibliography

A.T. Florence, D. Attwood, Physicochemical Principles of Pharmacy, Pharmaceutical Press, 2011

P. Colombo et al., Principi e Tecnologie Farmaceutiche, casa Editrice Ambrosiana, Milano, II Ed. 2015

Slides discussed during the course

Teaching methods

Theoretical lectures. Multiple choise test to be discussed in class.

Assessment methods

Oral examination. For the oral examination, registration by AlmaEsami list is required.

Teaching tools

Video-projector and PC.

Office hours

See the website of Barbara Luppi