Universitą degli studi di Pavia
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Courses 2014
Curriculum: Chemistry
Photochemical pathways for C-C bond formation (6 credits)
Prof. Maurizio Fagnoni
Contents: The course will start with a brief introduction on the main concepts of the photochemistry and the importance of such a discipline in the frame of organic synthesis. The effects of the light on the reactivity of organic compounds will be briefly introduced with particular regard to the photomediated hydrogen abstraction and photoinduced electron transfer mechanisms. The synthetic applications devoted to the formation of C-C bonds will follow. Main topics will be the photocatalytic processes (where a photocatalyst is the absorbing species) and the photoinduced functionalization of aromatic rings via arylation and nucleophilic aromatic substitution reactions. The use of visible light to promote organic reactions will complete the program. In some cases the photochemical approach will be confronted with thermal analogues regarding the efficiency of the process and its environmental impact.
Chirality Transfer in Organic Synthesis (6 credits)
Prof. Giuseppe Faita
Contents: The course is focused on the asymmetric synthesis. After a general introduction, it will be inferred the potentialities of the different synthetic approaches (use of chiral auxiliaries, chiral catalysts, and organocatalysts) in the enantiocontrolled formation of new C-C and C-X bonds. Specific deepening will be devoted to the use of bis(oxazolines) as chiral ligands in the asymmetric catalysis of both the Diels-Alder reactions and the 1,3-dipolar cycloadditions.
History of Chemistry in the XX century (6CFU).
Prof: P. Ferloni, G.G. Mellerio
The course will deal with selected topics in the development of Chemistry in the XX century. An interdisciplinary approach will be used in the systematic exposition of the subjects. The lectures will be held from 4 to 6 p.m. in a small lecture hall in the General Chemistry building, 1st floor. The timetable and programme are as follows: Foreword. Historical methods and tools. Chemistry between Botanics and Pharmacy Chemistry in the research of Camillo Golgi Topics in the classical chemistry of the XX century The development of the Italian chemical industry Remarkable industrial syntheses Electrochemistry The fate of some organic molecules in the XX century The fate of some organic molecules in the XX century Concluding remarks Guided tour, Museum for the History of the University
Suggested reading: Luigi Cerruti, Bella e potente, Editori Riuniti, Roma 2003 Final evaluation: oral exam.
Curriculum: Pharmaceutical Sciences
DOE: Application to pharmaceutical formulations (2 Credits)
Prof. Maria Cristina Bonferoni
Contents: The first part of the course will consider factorial and screening designs aimed at finding critical variables of methods, processes and formulations. The second part will deal with optimization methods. Response surface designs and mixture designs will be considered to find the region where optimal response can be obtained. Different examples of pharmaceutical applications will be studied. Attention will be paid to the application of DOE in the more recent regulatory approach to the pharmaceutical quality. Some examples will be analyzed with a computer specific software. Learning check: discussion of a report on two case studies.
Innovative analytical methods in drug discovery (4 Credits)
Prof. Enrica Calleri
Contents: Study of the most important and innovative analytical techniques used in drug discovery for the determination and characterization of drug-protein binding (separative and non-separative methods). Objectives of the course are: 1) make the students familiar with the theoretical basis of the most recent techniques and analytical methodologies used in the different steps of the drug discovery process (bioaffinity methods, methods based on mass spectrometry, ITC methods, luminescence methods etc.). 2) case studies presentation. Seminars will be also organized and given by experts operating in the drug discovery field. Learning check: written tests.
Production and characterization of active pharmaceutical ingredients and excipients (4 credits)
Prof. Carla M. Caramella
Contents: Drug Master File (DMF): how to present information on Active Pharmaceutical Ingredients (API)). API and excipients reported in the European Phamacopoeia: the certificate of compliance (CEP) to the Pharmacopoeia. API synthesis: the problem of raw materials and impurities.. Excipients and impurities. Production of API and Good Manufacturing Practices. Production of sterile APIs. Learning check: written examination.
From hit identification to lead optimization (4 Credits)
Prof. Simona Collina
Contents: This two-days course focuses on the drug discovery process, from the identification of novel drug targets to the identification of a drug candidate. The drug discovery process starts with the identification of compounds (one or more, name hit compounds), with either natural or synthetic origin, endowed with promising biological properties. Such compounds will successively undergo further studies aimed at turning hit into lead (hit-to-lead process). In this phase hit(s) are structurally modified in order to improve their pharmacodynamic, pharmacokinetic and toxicological profiles. The final output of hit-to-lead process is the drug candidate. Theoretical lessons are combined with practical case studies. Learning check: written examination.
Manufacturing of sterile pharmaceutical products (4 credits)
Prof. Bice Conti
Contents: General aspects of sterile pharmaceutical products. Sterility assurance: design and qualification of aseptic areas in compliance with regulatory requirements (GMP). Technology transfer of sterile pharmaceutical products. Risk assessment in sterility assurance. Microbiologic control assessment. “Process simulation testing” applied to aseptic processes. Isolators and containment. Learning check: written examination.
Multivariate statistical analysis (2 Credits)
Prof. Maria Daglia
Contents: 1) Design of Experiment (DOE) as the best strategy for efficient experimentation; applications in the formulation development and analytical control of nutraceuticals. 2) Experimental design for a selection of homogeneous samples for a study of shelf-life. Multivariate statistical methods for analysis of chemical, physical and sensorial responses sampled in time; 3) Innovative approaches for the determination of the characteristics of nutraceuticals, with particular attention to metabolomic studies through LC/MS and NMR. 4) In silico models for the study of nutraceutical biological activities. 5) Multivariate Statistical Process Control (MSPC). Learning check: written examination.
Physical properties of powders (2 Credits)
Prof. Franca Ferrari
Contents: The characterization of particle size distribution of a multiparticulate system is of interest to many branches of learning: chemistry, pharmaceutical technology, chemical engineering. As for the pharmaceutical field, such a characterization it is important in three different moments: preformulation studies, manufacturing processes, biopharmaceutical properties of dosage forms. The course deals with fundamental (size, shape, surface area) and derived (packing, flow) properties of powders and the relevant analytical techniques. Theoretical lessons are implemented by many case studies. Learning check: written examination.
Rational drug design (4 credits)
Prof. Daniela Rossi
Contents: This two-days course is concerned with enabling students to molecular modeling techniques useful for the rational design of biologically active molecules (Computer Aided Drug Design - CADD). The course focus on both ligand-based (QSAR, pharmacophore modeling) and structure-based (molecular docking, homology modeling and virtual screening) drug design methodologies. Additionally, in silico prediction of ADMET properties is considered. The course is composed by theoretical lessons (2CFU) combined with hand-on section Learning check: written examination.
Technological controls of drug delivery systems (2 Credits)
Prof. Silvia Rossi
Contents: The course aims at providing an advanced knowledge of the technological controls of drug delivery systems with particular attention to liquid and semisolid formulations. Great importance will be devoted to viscosity and viscoelastic measurements, functional to characterization and formulation development of the above mentioned formulations. Suitable tests employed to evaluate mechanical and biopharmaceutical properties of liquid and semisolid formulations will also be treated. The theoretical explanation of the topics will be accompanied by the discussion of case studies. Learning check: oral examination.
Photochemical pathways for C-C bond formation (6 credits)
Prof. Maurizio Fagnoni
Contents: The course will start with a brief introduction on the main concepts of the photochemistry and the importance of such a discipline in the frame of organic synthesis. The effects of the light on the reactivity of organic compounds will be briefly introduced with particular regard to the photomediated hydrogen abstraction and photoinduced electron transfer mechanisms. The synthetic applications devoted to the formation of C-C bonds will follow. Main topics will be the photocatalytic processes (where a photocatalyst is the absorbing species) and the photoinduced functionalization of aromatic rings via arylation and nucleophilic aromatic substitution reactions. The use of visible light to promote organic reactions will complete the program. In some cases the photochemical approach will be confronted with thermal analogues regarding the efficiency of the process and its environmental impact.
Chirality Transfer in Organic Synthesis (6 credits)
Prof. Giuseppe Faita
Contents: The course is focused on the asymmetric synthesis. After a general introduction, it will be inferred the potentialities of the different synthetic approaches (use of chiral auxiliaries, chiral catalysts, and organocatalysts) in the enantiocontrolled formation of new C-C and C-X bonds. Specific deepening will be devoted to the use of bis(oxazolines) as chiral ligands in the asymmetric catalysis of both the Diels-Alder reactions and the 1,3-dipolar cycloadditions.
History of Chemistry in the XX century (6CFU).
Prof: P. Ferloni, G.G. Mellerio
The course will deal with selected topics in the development of Chemistry in the XX century. An interdisciplinary approach will be used in the systematic exposition of the subjects. The lectures will be held from 4 to 6 p.m. in a small lecture hall in the General Chemistry building, 1st floor. The timetable and programme are as follows: Foreword. Historical methods and tools. Chemistry between Botanics and Pharmacy Chemistry in the research of Camillo Golgi Topics in the classical chemistry of the XX century The development of the Italian chemical industry Remarkable industrial syntheses Electrochemistry The fate of some organic molecules in the XX century The fate of some organic molecules in the XX century Concluding remarks Guided tour, Museum for the History of the University
Suggested reading: Luigi Cerruti, Bella e potente, Editori Riuniti, Roma 2003 Final evaluation: oral exam.
Curriculum: Pharmaceutical Sciences
DOE: Application to pharmaceutical formulations (2 Credits)
Prof. Maria Cristina Bonferoni
Contents: The first part of the course will consider factorial and screening designs aimed at finding critical variables of methods, processes and formulations. The second part will deal with optimization methods. Response surface designs and mixture designs will be considered to find the region where optimal response can be obtained. Different examples of pharmaceutical applications will be studied. Attention will be paid to the application of DOE in the more recent regulatory approach to the pharmaceutical quality. Some examples will be analyzed with a computer specific software. Learning check: discussion of a report on two case studies.
Innovative analytical methods in drug discovery (4 Credits)
Prof. Enrica Calleri
Contents: Study of the most important and innovative analytical techniques used in drug discovery for the determination and characterization of drug-protein binding (separative and non-separative methods). Objectives of the course are: 1) make the students familiar with the theoretical basis of the most recent techniques and analytical methodologies used in the different steps of the drug discovery process (bioaffinity methods, methods based on mass spectrometry, ITC methods, luminescence methods etc.). 2) case studies presentation. Seminars will be also organized and given by experts operating in the drug discovery field. Learning check: written tests.
Production and characterization of active pharmaceutical ingredients and excipients (4 credits)
Prof. Carla M. Caramella
Contents: Drug Master File (DMF): how to present information on Active Pharmaceutical Ingredients (API)). API and excipients reported in the European Phamacopoeia: the certificate of compliance (CEP) to the Pharmacopoeia. API synthesis: the problem of raw materials and impurities.. Excipients and impurities. Production of API and Good Manufacturing Practices. Production of sterile APIs. Learning check: written examination.
From hit identification to lead optimization (4 Credits)
Prof. Simona Collina
Contents: This two-days course focuses on the drug discovery process, from the identification of novel drug targets to the identification of a drug candidate. The drug discovery process starts with the identification of compounds (one or more, name hit compounds), with either natural or synthetic origin, endowed with promising biological properties. Such compounds will successively undergo further studies aimed at turning hit into lead (hit-to-lead process). In this phase hit(s) are structurally modified in order to improve their pharmacodynamic, pharmacokinetic and toxicological profiles. The final output of hit-to-lead process is the drug candidate. Theoretical lessons are combined with practical case studies. Learning check: written examination.
Manufacturing of sterile pharmaceutical products (4 credits)
Prof. Bice Conti
Contents: General aspects of sterile pharmaceutical products. Sterility assurance: design and qualification of aseptic areas in compliance with regulatory requirements (GMP). Technology transfer of sterile pharmaceutical products. Risk assessment in sterility assurance. Microbiologic control assessment. “Process simulation testing” applied to aseptic processes. Isolators and containment. Learning check: written examination.
Multivariate statistical analysis (2 Credits)
Prof. Maria Daglia
Contents: 1) Design of Experiment (DOE) as the best strategy for efficient experimentation; applications in the formulation development and analytical control of nutraceuticals. 2) Experimental design for a selection of homogeneous samples for a study of shelf-life. Multivariate statistical methods for analysis of chemical, physical and sensorial responses sampled in time; 3) Innovative approaches for the determination of the characteristics of nutraceuticals, with particular attention to metabolomic studies through LC/MS and NMR. 4) In silico models for the study of nutraceutical biological activities. 5) Multivariate Statistical Process Control (MSPC). Learning check: written examination.
Physical properties of powders (2 Credits)
Prof. Franca Ferrari
Contents: The characterization of particle size distribution of a multiparticulate system is of interest to many branches of learning: chemistry, pharmaceutical technology, chemical engineering. As for the pharmaceutical field, such a characterization it is important in three different moments: preformulation studies, manufacturing processes, biopharmaceutical properties of dosage forms. The course deals with fundamental (size, shape, surface area) and derived (packing, flow) properties of powders and the relevant analytical techniques. Theoretical lessons are implemented by many case studies. Learning check: written examination.
Rational drug design (4 credits)
Prof. Daniela Rossi
Contents: This two-days course is concerned with enabling students to molecular modeling techniques useful for the rational design of biologically active molecules (Computer Aided Drug Design - CADD). The course focus on both ligand-based (QSAR, pharmacophore modeling) and structure-based (molecular docking, homology modeling and virtual screening) drug design methodologies. Additionally, in silico prediction of ADMET properties is considered. The course is composed by theoretical lessons (2CFU) combined with hand-on section Learning check: written examination.
Technological controls of drug delivery systems (2 Credits)
Prof. Silvia Rossi
Contents: The course aims at providing an advanced knowledge of the technological controls of drug delivery systems with particular attention to liquid and semisolid formulations. Great importance will be devoted to viscosity and viscoelastic measurements, functional to characterization and formulation development of the above mentioned formulations. Suitable tests employed to evaluate mechanical and biopharmaceutical properties of liquid and semisolid formulations will also be treated. The theoretical explanation of the topics will be accompanied by the discussion of case studies. Learning check: oral examination.
