Universitą degli studi di Pavia
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Courses 2015
Curriculum: Chemistry
Advanced Diffraction Techniques for Structural Investigation in Material Science (6 credits)
Prof: D. Capsoni, L. Malavasi
Contents: Aim of this course is to give an overview about the advanced techniques for the structural characterization of different classes of materials. We will first give an introduction about diffraction methods and then we will focus on more specific topics. These will include: combined x-ray and neutron diffraction collection; ab-initio structural determination from powder diffraction data; magnetic structure determination; in-situ and time-resolved techniques; local structure determination from total scattering data. The different topics will be presented with basic theoretical information while a more detailed description will be given regarding the capabilities of each method, considerable “practical” details about data collection and analysis, and with a large choice of examples. Some “hands-on” sessions on data analysis methods of diffraction data are also planned.
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 XVIII and XIX centuries (6 Credits)
Prof. G.G. Mellerio, P. Ferloni, F. Sartori
Objectives: To realize the importance of chemistry in modern civilization, to appreciate the history of development of chemistry. In the first part of the course, the history of mankind is considered from the point of view of chemistry. It is shown as artisans of different kinds, smiths, potters, painters, healers, did practice chemistry in the past, thus contributing to its improvement and progress. The rise and development of the major chemical concepts and ideas are discussed in two great periods. They are delivered in two academic years: course I and course II, respectively. This year 2014-2015 should be Course I. Selected topics of the history of chemistry in the XVIII and XIX centuries will be presented and discussed. Theories and experiments will be illustrated with an interdisciplinary approach taking into account scientific fields related to chemistry, namely the history of botany and the history of the biological and medical sciences in the Enlightenment age and in the University of Pavia.
Suggested readings: Salvatore Califano, Storia della Chimica. Vol. I. Dall’ alchimia alla chimica del sec. XIX, pp. 434, Bollati Boringhieri, Torino 2010. Edward Thorpe, Storia della Chimica, traduzione di Rinaldo Pitoni, pp. 325, S.T.E.N., Torino 1911 http://www.liberliber.it/mediateca/libri/t/thorpe/storia_della_chimica/pdf/thorpe_storia_della_chimica.pdf. In English, see e.g.: Sir Thomas Edward Thorpe, History of chemistry, Watts & Co., London 1921. Final exam: oral presentation of a subject chosen by the candidate in accord with the lecturers. Handouts and lecture slides are available from the teachers
Understanding Mass Spectra: a Basic Approach (6 credits)
Prof. G.G. Mellerio
Objectives: This course seeks to provide a basic familiarity with interpreting data of mass spectrometry. The course introduces one of the key disciplines of organic mass spectrometry: the common fragmentation pathways of organic ions and the resulting methodology for the interpretation of electron ionization (EI) mass spectra. Intended as a systematic introduction to the topic the course emphasizes the most important fragmentation pathways rather than dwelling on compounds. Basic skills are provided as a guideline for extracting structural information from mass spectra: tools and rules. As a prerequisite some knowledge on general concept of mass spectrometry, tandem mass spectrometry, isotopic mass and isotopic distributions are provided. The occurrence of common fragmentation pathways is not restricted to EI technique. All of modern ionization methods (e.g. ESI) are used for producing protonated (or deprotonated) molecules, as well as adduct ions, yielding, by the dearth of fragment ions, a simplification of mass spectra useful for analytical purposes. However, such even-electron molecular species are of varying stability in accordance with their chemical nature (positive vs negative species) and their internal energies that orient their respective dissociation toward competitive and/or consecutive prompt dissociation displayed in mass spectra. Some examples of dissociation of even-electron species will be reported (only for singly charged systems).
Recommended readings: J. H. Gross, Mass Spectrometry. A Textbook, 2nd ed., Berlin – Heidelberg, Springer Verlag, 2011, Hardcover ISBN: 978-3-642-10709-2. F.W. McLafferty and F. Tureček, Interpretation of Mass Spectra, 4th edition, Mill Valley, University Science Books, 1993, ISBN 0-935702-25-3. Final exam: oral Pre-requisite: basic analytical and organic chemistry Handouts and lecture slides are available from the teacher.
Modern NMR spectroscopy in Organic Chemistry (Two Modules, 3+3 credits)
Prof: Mariella Mella
The course will be divided into two modules Module A: Brief introduction on the general principles of high-resolution NMR, practical aspects and one-dimensional techniques , examples and experimental methods Module B: Main two-dimensional experiments. Homo and hetero correlations through the chemical bond; correlations through space: Examples and some practical applications 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.
Patent low (2 Credits)
Teacher: Lauretta Maggi
Scheduled period: June–July Aim: provide a theoretical and practical guideline to patent an invention in the pharmaceutical chemical and biotechnological fields. Some possibilities for the technological transfer of the product will be considered. Spin-off and start-up. Content: Introduction on the intellectual property rights in the modern society. Patentability requirements of an invention. Evaluation of the potential costs and limitations of a patent. Search report and on-line database. Procedures to file a national or international patent. Procedures for examination, extension, possible opposition or patent infringement. Regional and international organizations: European Patent Office, Patent Cooperation Treaty, Word Intellectual Property Organization. Final evaluation: written
Advanced Diffraction Techniques for Structural Investigation in Material Science (6 credits)
Prof: D. Capsoni, L. Malavasi
Contents: Aim of this course is to give an overview about the advanced techniques for the structural characterization of different classes of materials. We will first give an introduction about diffraction methods and then we will focus on more specific topics. These will include: combined x-ray and neutron diffraction collection; ab-initio structural determination from powder diffraction data; magnetic structure determination; in-situ and time-resolved techniques; local structure determination from total scattering data. The different topics will be presented with basic theoretical information while a more detailed description will be given regarding the capabilities of each method, considerable “practical” details about data collection and analysis, and with a large choice of examples. Some “hands-on” sessions on data analysis methods of diffraction data are also planned.
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 XVIII and XIX centuries (6 Credits)
Prof. G.G. Mellerio, P. Ferloni, F. Sartori
Objectives: To realize the importance of chemistry in modern civilization, to appreciate the history of development of chemistry. In the first part of the course, the history of mankind is considered from the point of view of chemistry. It is shown as artisans of different kinds, smiths, potters, painters, healers, did practice chemistry in the past, thus contributing to its improvement and progress. The rise and development of the major chemical concepts and ideas are discussed in two great periods. They are delivered in two academic years: course I and course II, respectively. This year 2014-2015 should be Course I. Selected topics of the history of chemistry in the XVIII and XIX centuries will be presented and discussed. Theories and experiments will be illustrated with an interdisciplinary approach taking into account scientific fields related to chemistry, namely the history of botany and the history of the biological and medical sciences in the Enlightenment age and in the University of Pavia.
Suggested readings: Salvatore Califano, Storia della Chimica. Vol. I. Dall’ alchimia alla chimica del sec. XIX, pp. 434, Bollati Boringhieri, Torino 2010. Edward Thorpe, Storia della Chimica, traduzione di Rinaldo Pitoni, pp. 325, S.T.E.N., Torino 1911 http://www.liberliber.it/mediateca/libri/t/thorpe/storia_della_chimica/pdf/thorpe_storia_della_chimica.pdf. In English, see e.g.: Sir Thomas Edward Thorpe, History of chemistry, Watts & Co., London 1921. Final exam: oral presentation of a subject chosen by the candidate in accord with the lecturers. Handouts and lecture slides are available from the teachers
Understanding Mass Spectra: a Basic Approach (6 credits)
Prof. G.G. Mellerio
Objectives: This course seeks to provide a basic familiarity with interpreting data of mass spectrometry. The course introduces one of the key disciplines of organic mass spectrometry: the common fragmentation pathways of organic ions and the resulting methodology for the interpretation of electron ionization (EI) mass spectra. Intended as a systematic introduction to the topic the course emphasizes the most important fragmentation pathways rather than dwelling on compounds. Basic skills are provided as a guideline for extracting structural information from mass spectra: tools and rules. As a prerequisite some knowledge on general concept of mass spectrometry, tandem mass spectrometry, isotopic mass and isotopic distributions are provided. The occurrence of common fragmentation pathways is not restricted to EI technique. All of modern ionization methods (e.g. ESI) are used for producing protonated (or deprotonated) molecules, as well as adduct ions, yielding, by the dearth of fragment ions, a simplification of mass spectra useful for analytical purposes. However, such even-electron molecular species are of varying stability in accordance with their chemical nature (positive vs negative species) and their internal energies that orient their respective dissociation toward competitive and/or consecutive prompt dissociation displayed in mass spectra. Some examples of dissociation of even-electron species will be reported (only for singly charged systems).
Recommended readings: J. H. Gross, Mass Spectrometry. A Textbook, 2nd ed., Berlin – Heidelberg, Springer Verlag, 2011, Hardcover ISBN: 978-3-642-10709-2. F.W. McLafferty and F. Tureček, Interpretation of Mass Spectra, 4th edition, Mill Valley, University Science Books, 1993, ISBN 0-935702-25-3. Final exam: oral Pre-requisite: basic analytical and organic chemistry Handouts and lecture slides are available from the teacher.
Modern NMR spectroscopy in Organic Chemistry (Two Modules, 3+3 credits)
Prof: Mariella Mella
The course will be divided into two modules Module A: Brief introduction on the general principles of high-resolution NMR, practical aspects and one-dimensional techniques , examples and experimental methods Module B: Main two-dimensional experiments. Homo and hetero correlations through the chemical bond; correlations through space: Examples and some practical applications 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.
Patent low (2 Credits)
Teacher: Lauretta Maggi
Scheduled period: June–July Aim: provide a theoretical and practical guideline to patent an invention in the pharmaceutical chemical and biotechnological fields. Some possibilities for the technological transfer of the product will be considered. Spin-off and start-up. Content: Introduction on the intellectual property rights in the modern society. Patentability requirements of an invention. Evaluation of the potential costs and limitations of a patent. Search report and on-line database. Procedures to file a national or international patent. Procedures for examination, extension, possible opposition or patent infringement. Regional and international organizations: European Patent Office, Patent Cooperation Treaty, Word Intellectual Property Organization. Final evaluation: written
