32046 - Pharmaceutical Technology and Law II (G.B.)

Learning outcomes

At the end of the course the student will be able to know the differences between the different pharmaceutical formulations in relation to the characteristics of the excipients and the preparation methods, the correlations between the drug release and the administration environment, the evaluation methods of drug release and bioavailability. The student will be able moreover to prepare and evaluate innovative pharmaceutical formulations such as liposomes, micro and nanoparticulate systems , micellar and macromolecular carriers.

Course contents

1st Module  Prof. I. Orienti
Bioavailability and pharmacokinetics
Pharmaceutical dosage forms and pharmaceutical systems. Factors influencing drug absorption and drug availability. Pharmacokinetics. Plasma concentration –time curves. Absolute bioavailability. Relative bioavailability. Bioequivalence. Dose size and frequency of administration. 
Physico-chemical processes that control drug release and drug absorption. Passive diffusion through a membrane. Partition coefficient. Dissolution. Solubility. Thermodynamic parameters. Enhanced solubility. Micellisation. Salification. Complexation.
 Conventional drug delivery systems. Formulative and preparative aspects correlable with the administration route and the release characteristics. Characteristics of the excipients. Powders, Granules, Tablets, Capsules, Solutions, Suspensions, Emulsions, Ointments, Hydrogels, Lipogels, Pastes.
 Controlled drug delivery systems. Physico-chemical properties of the excipients correlable with the release characteristics.
Diffusion controlled devices. Characteristics of the excipients. Monolithic devices. Reservoir devices. Solvent controlled devices. Osmotically controlled devices. Swelling controlled devices. Chemically controlled devices.

Nanosystems for drug targeting
 Drug targeting. Passive targeting. Active targeting. Physical targeting. Polymeric nanoparticulate systems, solid lipid nanoparticles dendrimers, liposomes, macromolecular systems and self-assembling polymers. Gene-delivery systems. Physico-chemical characteristics of the drug-delivery systems, preparation technology and functiona characteristics.

 

2nd module  Dott.ssa  Cristina Cavallari

The pharmaceutical technologist. Development of a pharmaceutical form. Good practices for pharmaceutical development. Laboratory of Pharmaceutical development.
pre-formulative Developments. Chemical stability. compatibility and interactions.
Nature of the physical state of drugs and excipients
The polymorph state. The amorphous state. The glass transition temperature. Stabilizing the amorphous state.
Analysis of the solid state: Thermal analysis: DSC, TGA, and HSM. X-ray diffraction
Routes of administration of drugs. Pharmaceutical forms for oral use: pellets (production methods and technologies), capsules and effervescent tablets. . Preparations for parenteral use.
Pharmaceutical forms can be administered by transmucosal: prepared for nasal administration, pulmonary, ocular, buccal and vaginal
Gastro-resistant pharmaceutical forms: Examples and materials used
Release oral pharmaceutical forms: colon-specific systems
Route of administration of ophthalmic drugs.
The inhalation of dust and aerosols.
The orodispersible formulations.
The vaginal preparations
Polymers of pharmaceutical interest: Polyvinylpirrolidone (PVP), Polyethylenglicols (PEG), poloxamers; acrylic polymers (Carbopol and EUDRAGIT).
Polysaccharide polymers: cellulose, derivatives (HPMC) and chitosan.
Taste masking of oral pharmaceutical forms.
Freeze drying: process description, formulation and development.

3th Module Laboratory

1: Preparing a mucilage base

    Preparation of a wet granulate; using granulator

    Preparing oleogel and hydrogel

    Uniformity of weight of tablets

 

2: Dimensional analysis using sieves, vibrating screen

     Measuring angle of repose of a granular material

     Prepare a paste and demonstration of the Refiner

     Preparing emulgel

 

3: Measurement of the density of a powder with a hydrometer

     Monsanto hardness tester

     Friabilometer

     De-aggregator

     Preparation of an emulsion and analysis using Microscope

     Suppositories with the method of the double fusion

    

4: Manual Capsule filling machine (and uniformity of mass on the capsules)

     Demonstration and explanation of the operation of the tabletting machine

     Measurement of the content of a tablet using spectrophotometer

Readings/Bibliography

1) SWARBRICK, BOYLAN, Encyclopedia of Pharmaceutical Technology, Dekker, 1999-2005. 2) Edizioni in vigore delle Farmacopee Italiana e Europea.

Teaching methods

lessons and laboratory activity

Assessment methods

1st Module

The Assessment of the first module occurs only with the final exam, which ensures the acquisition of knowledge and skills expected by conducting a written test lasting 1 hour. 
The final exam test is intended to verify the achievement of the following objectives:

Knowledge of the  main functional differences among the different pharmaceutical formulations in relation to the physico-chemical characteristics of the excipients and the preparative methods. Correlations between drug release and administration environment. Evaluation methods for drug release. Correlations between release kinetics and bioavailability. Methods to improve bioavailability. Preparative methods for micro/nano particulate drug delivery systems and their functional evaluation.

The written test will consist of 14 questions with multiple choice answer and 1 question with free answer. It will last 1 hour.

2nd Module 

The written test will consist of 5 questions with multiple choice answer and 2 question with free answer. It will last 2 hour.

Teaching tools

power point

Office hours

See the website of Isabella Orienti

See the website of Cristina Cavallari

See the website of Cristina Cavallari