Poc-final-syllabus-sem-3-4

SYLLABUS
Saurashtra University
Master of Science
PHARMA. ORGANIC CHEMISTRY
(UGC Innovative Program sanctions No.F.14-30(A)/2012 (Inno /ASIST) Dt. 14-01-2012 to Shree M. & N. Virani Science College, Rajkot.) M.Sc. Semester III-IV
Choice Based Credit System (CBCS)
Effective from June 2012-13
Shree M & N Virani Science College, Rajkot
Course Information
M.Sc. Pharmaceutical Organic Chemistry
(Saurashtra University)
Semester - III
PHARMACEUTICAL ORGANIC CHEMISTRY
Course Information
M.Sc. Pharmaceutical Organic Chemistry
Faculty Name
Duration / Semester
Program Name
Max. duration / Semester 510 hrs
Faculty Code
Total Semester
Semester
Course Code
Total Credits
M.Sc. -PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER III
POC-301: Pharmaceutical Technology
1. Tablet
(a) Definition, Advantages and disadvantages, Introduction to types of tablets,
formulation of different types of tablets; excipients, granulation techniques, machinery for
large scale granulation and compression, physics of tablet making, In process controls,
processing problems and remedies,
(b) Evaluation (Pharmacopoeial and nonpharmacopoeial test) and equipment. Brief
outline on manufacturing method and evaluation of mouth dissolving tablets, buccal
tablets, floating tablets, tablets of colon drug delivery, matrix tablets.
(C) Coating Of Tablets: objectives, types of coating, film forming materials,
formulations of coating solution, equipment for coating, coating process, evaluation of
coated tablets, coating defects.
2. Capsules
Hard Capsules:
Definitions, Advantages, disadvantages, Ideal requirements, Production of Hard capsules
(Gelatin and nongelatin e.g. vegetable), Capsule storage, size of capsules, formulation and
methods of capsule filling, problems and remedies, quality control.
Soft Gelatin Capsules:
Formulation of shell and capsule coat, quality control with special emphasis on current
dissolution testing.
3. Sterile dosage forms:
Definitions, Advantages, Disadvantages, Ideal requirements and Formulation of sterile dosage forms, Water for injection-Preparation and quality control, Design and requirements for production area- Aseptic techniques, sources of contamination and methods of prevention, design of aseptic area, laminar flow benches, services and maintenance, containers and closures, methods of filling including form fill and seal technology. Evaluation of sterile dosage forms. 4. Cosmeticology and cosmetic preparations:
Fundamentals of cosmetic science, formulation, preparation and packaging of cosmetics for skin - Sunscreen, moisturizers, cold cream, and vanishing cream, hair - Shampoo and conditioners, dentifrice- powders, gels, paste and manicure preparations like- nail polish, lipsticks, eye lashes, brief introduction to cosmaceuticals, baby care products, shaving cream, hygienic products 5. Liquid dosage forms:
Introduction, advantages and disadvantages, types of additives used vehicles, stabilizers, preservatives, suspending agents, emulsifying agents, solubilizers, colors, flavors, etc. Reference Books
1. The Theory and Practice of Industrial Pharmacy by L Lachman, H Lieberman and J 2. Kanig. Gennaro, Alfonso R., Remington: The Science and Practice of Pharmacy, Vol- I & II, Lippincott Williams & Wilkins, New York. 3. Pharmaceutical Dosage Forms and Drug Delivery Systems by Ansel & others. 4. Pharmaceutics: The Science of Dosage Form Design by Michael E. Aulton M.Sc. PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER III
POC-302: Medicinal Chemistry I
1. Drug Design:
(i) Introduction to drug design & development, strategies for new lead findings, pharmacophore, structure activity relationship (SAR), Lead modification including homologation, isosterism & bioisosterism, ring transformation and prodrug concept. (ii) Quantitative Structure Activity Relationship (QSAR)- History and development of QSAR, Physicochemical parameters: lipophilicity, electronic and steric. Study on Hansch LFER model, The Craig plot, the topliss scheme, Free Wilson analysis and mixed approach, CADD. 2. Pharmacokinetics:
Introduction, Route of drug absorption, Factor influencing distribution of drug, Biotransformation of the drug, Drug excretion. 3. Pharmacodynamics:
Introduction, Concept of drug receptor interactions, Study of LD50, ED50, MIC and MEC etc. 4. Combinatorial Chemistry:
The Principle and design of combinatorial chemistry, Pool and split method for peptide synthesis, Parallel synthesis, Furka’s mix and split technique, Solid support method. 5. Introduction, classification, mechanism of action, adverse effects, therapeutic uses,
structure activity relationship (SAR)* and synthetic procedures* of selected drugs of
following categories to be covered.
Drugs acting on Cardiovascular System
1. Cardiotonic Agents
SAR: Cardiac glycosides
Synthesis: Dobutamine,
2. Antihypertensive Agents
SAR: ACE Inhibitors, Dihydropyridnes
Synthesis: Nifedipine, Amlodipine, Atenolol, Metoprolol, Carvediol, Captopril,
Hydralazine.
3. Antiarrhythmic Agents,
4. Antianginal Agents,
Synthesis: Glyceryl trinitrate, Isosorbide dinitrate 5. Antihyperlipidemic agents,
SAR: HMG CoA Reductase inhibitors
Synthesis: Clofibrate
6. Coagulants and Anticoagulants
Synthesis: warfarin
7. Miscellaneous
Diuretics
SAR: Thiazide diuretics
Synthesis: Hydrochlorthiazide, Acetazolamide, Furosemide, Dihydroflumethiazide,
Ethacrinic acid
Antidiabetic agents
Synthesis: Glipizide, Metformin, Pioglitazone, Tolbutamide, Glimipride.
Reference Books
1. Introduction to Medicinal Chemistry, A Gringuage, Wiley-VCH. 2. Wilson and Gisvold’s Text Book of Organic Medicinal and Pharmaceutical 3. An Introduction to Drug Design, S.S. Pandey and J.R. Dimmock, New Age 4. Burger’s Medicinal Chemistry and Drug Discovery, Sixth Edition, Ed.M.E.vWolff, 5. Goodman and Gilman’s Pharmacological Basis of Therapeutics, McGraw-Hill. 6. The Organic Chemistry of Drug Design and Drug Action, R.B. Silverman, Academic 7. Strategies for Organic Drug Synthesis and Design, D. Lednicer, John Wiley. 8. Pharmaceutical Substances., Kleemann, Vol-I & II., Fourth edition., Thieme. M.Sc. PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER III
POC-303: Separation Techniques
Adsorption & Partition Chromatography: Classification, Definition of
terms; Principle, Basic theory, Technique & Applications of following:
1. Column, Ion-exchange and Affinity chromatography.
2. Paper Chromatography: AC, DC, CC, 2D-AC
3. Thin Layer chromatography: TLC, 2D-TLC & HP-TLC
Modern Separation Techniques: Instrumentation, Working and Applications
of following:
4. HPLC & LC-MS
5. GC & GC-MS
Band broadening & Column efficiency: Definition of terms, Factors
affecting, Plate theory & Rate theory of chromatography, Limitations of
theory
Reference Books
1. Thin layer chromatography, E. Stahl. 2. Chromatography, Heptman. 3. HPTLC, Dr.P.D. Sethi. 4. High Performance liquid chromatography, Dr.P.D. Sethi 5. Principles of Instrumental Analysis, D.A. Skoog and J.L. Loary, W.B. Saunders. 6. Fundamentals of Analytical Chemistry, D.A. Skoog, D.M. West and F.J. Holler, W.B. 7. Principles of Instrumental analysis, D.A. Skoog and W.B. Saunders. M.Sc. PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER III
POC-304: Stereochemistry
1. Fundamental
Stereochemistry:
stereoisomerism, Optical isomerism, Conventions for D, L and R, S- system, Interconversion between Fischer and Three-dimensional formulas with one stereocenter, Stereoisomerism for more than one stereogenic unit, Threo & Erythro, Geometrical isomerism, Cis/Trans, E-Z isomerism resulting from double bonds, Oximes, Racemic mixtures and Racemization, Resolution of racemic mixtures, Optical purity & Enantiomeric excess, Formation of diasteromers, Stereoselective and stereospecific reactions, Epimers, Anomers and Epimerization, Stereoisomerism without a stereogenic carbon (axial chirality), Planar chirality, Helicity and Molecular stereoisomerism. 2. Prochirality and Asymmetric Synthesis: Introduction, Homotopic & Heterotopic
ligands and faces, Enantiotopic ligands & faces, Asymmetric synthesis. 3. Conformational Analysis & Reactivity: Restricted rotation around single bonds-
confirmations of ethane & butane, Origin of conformational energy, Conformations and chemical reactivity of acyclic system, Cycloalkane ring other than cyclohexane, Conformations of substituted cyclohexane, Stereoisomerism in di-substituted cyclohexanes, Effect of confirmations on reactivity-cyclic system, Conformation of heterocycles, Conformation of sugars and Anomeric effect. 4. Stereochemistry of Aliphatic Nucleophilic Substitution Reactions: Introduction,
Stereochemistry of SN1 & SN2 reaction mechanism, The SNi mechanism, Mixed SN1 & SN2 reaction, ambient nucleophile, Regioselectivity, Neighbouring group participation. 5. Stereochemistry of Elimination Reactions: Introduction, Mechanism E1, E2 and
E1cB, Stereochemistry of E2-anti-ellimination reaction, E2-syn-elimination, Orientation of the double bond, Pyrolytic elimination. 6. Stereochemistry of Addition Reactions to Carbon-Hetero multiple bonds:
Introduction, Stereo chemical aspects of addition to carbonyl compounds, Stereochemistry of metal hydride reduction, Cannizzaro reaction, Meerwein-ponndorf reduction, Addition of organometallic compounds, Conjugate addition of organocopper reagents, Condensation reactions involving enolates, Hydrolysis of amides. Reference Books
1. Organic chemistry - I.L. Finar
2. Stereochemistry -Conformation and mechanism- P.S.Kalsi.
3. Stereochemistry - D. Nasipuri
4. Organic Chemistry-J.Clayden
5. Stereochemistry-Eliel
6. Stereochemistry of organic compounds - P.S. Kalsi.
7. Stereoselective synthesis : A practical approach, - M. Nogradi, VCH
M.Sc. -PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER III
POC-305 & 306: PRACTICALS
POC-305: Practical
1. Pharmaceutical Technology:
Preparation and evaluation of effervescent tablet, ferrous sulphate tablet,
Paracetamol tablet.
Preparation and evaluation of tablets employing direct compression, wet granulation, dry granulation (slugging), compression coating. Filling of powder/ granules/ pellets in hard gelatin capsule and its evaluation.
Perform pharmacopoeial test for given sample of glass vial / ampoule.
Preparation and evaluation of face powder, lipstick, cold cream, vanishing cream, tooth paste/ tooth powder. Formulation and evaluation of syrup, emulsion (o/w, w/o), turpentine liniment,
calamine lotion.
Formulation and evaluation of milk of magnesia/aluminum hydroxide gel antacid suspension. Formulation and evaluation of dry suspension. Formulation and evaluation of diclofenac sodium gel. 10) Formulation and evaluation of transdermal spray. 11) Formulation and evaluation of calcium gluconate injection, dextrose injection, NaCl injection, dextrose saline injection, menadion injection. 12) Formulation and evaluation of eye drops. 13) Formulation and evaluation of multidose injection of chloroquine phosphate. 14) Formulation and evaluation of metronidazole infusion. 2. Organic Separation of Ternary Mixtures*:
a. Liquid + Solid b. Liquid + Liquid
3. Analytical Techniques:
Extraction of Natural Products & separation of specific components
Chromatography: TLC, Column, Paper chromatography
UV-Visible Spectroscopy: Analysis and Estimation
4. Medicinal Chemistry:
Synthesis of privileged scaffolds using Conventional & Green synthetic methods: Single
/ Multi-step synthesis of organic compounds, TLC monitoring & spectral study. Green methods such as Microwave / Mortar pastel / Ionic Liquid / Water mediated / Solid 5. Demonstrative Practical:
• HPLC analysis of Active Pharmaceutical Ingredients
• Moisture analysis using KaFi Auto Titrator
• IR spectral study of selected APIs
• Pilot Plant Production of raw materials/ intermediates for APIs.
POC - 306: Viva Voce examination
Course Information
M.Sc. Pharmaceutical Organic Chemistry
(Saurashtra University)
Semester – IV
PHARMACEUTICAL ORGANIC CHEMISTRY
Course Information
M.Sc. Pharmaceutical Organic Chemistry
Faculty Name
Duration / Semester
Program Name
Max. duration/ Semester
Faculty Code
Total Semester
Semester
Course Code
Total Credits
M.Sc. PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER IV
POC-401: Heterocyclic Chemistry
1. Nomenclature of Heterocyclic compounds.
2. Heterocyclic Analogues of Cyclopropane:
Preparation and properties of aziridine, oxirane, thiirane. 3. Heterocyclic Analogues of Cyclobutane:
a. Preparation and properties of azetidine, oxetane, thietane, b. Preparation of 1,2-diazetidine, 1,2-dioxetane, 1,3-dithietane. 4. Heterocyclic Analogues of Cyclopentane:
a. Preparation and properties of pyrrole, furan, thiophene. b. Preparation and properties of indole, benzofuran, benzothiophene. c. Preparation of isoindole, indolizine, isatin. 5. Heterocyclic Analogues of Benzene:
a. Preparation and properties of pyridine and pyran. b. Preparation of α & γ -pyridones and α & γ -pyrones. 6. Heterocyclic Analogues of Naphthalene:
a. Preparation and properties of quinoline, isoquinoline, acridine. b. Preparation of benzopyran, benzopyran-2-one and benzopyran-4-one. 7. Compounds with two Heteroatoms in a Five Membered Ring:
a. Preparation & properties of pyrazole, oxazole, thiazole b. Preparation of, imidazole, isoxazole, isothiazole. 8. Compounds with Two Heteroatoms in a Six Membered Ring:
Preparation of pyridazine, pyrimidine, pyrazine, oxazine, thiazine, dioxane, Morpholine, phthalazine, quinazoline, quinaxoline, phenothiazine. 9. Compounds containing more than Two Heteroatoms:
Preparation of triazole, oxadiazole, thiadiazole, triazenes. 10. Heteroatoms in seven & eight membered ring:
Reference Books
1. Heterocyclic chemistry-R.K. Bansal 2. An introduction to the chemistry of Heterocyclic compds. - R.H.Acheson 3. Chemistry of Heterocyclic compounds-J.J. Trivedi 4. Heterocyclic chemistry-R.R. Gupta, M.Kumar & V. Gupta, Springer 5. The chemistry of Heterocycles - T. Eicher & S. Hauptmann 6. Heterocyclic chemistry - J.A. Joule, K. Mills & G.F. Smith 7. Comprehensive Heterocyclic chemistry - A. R. Katritzky & C. W. Rees 8. Heterocyclic chemistry - T. L. Gilchrist M.Sc. PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER IV
POC-402: Medicinal Chemistry-II
Introduction, classification, mechanism of action, adverse effects, therapeutic
uses, structure activity relationship (SAR)* and synthetic procedures* of selected
drugs of following categories to be covered.
1. Drugs acting on gastrointestinal tract:
• Antacids, Antisecretary, Antidiarrheals, Laxatives
Synthesis: Ranitidine, Omeprazole
2. Drugs Acting on CNS:
• CNS stimulants: Analeptics, Antidepressants
SAR: Tricyclic antidepressants
Synthesis: Amphetamine, Nikethamine, Imipramine.
• CNS Depressants: General and local anesthetics, Sedative and hypnotics,
Antiepileptics, Antipsychotics
SAR: Benzoic acid derivatives, Barbiturates, Benzodiazepines, Phenothiazines
Synthesis:
Chlordiazepoxide, Meprobamate, Phenytoin, Sodium valproic acid, Carbamazepine, Chlopromazine, Trifluperazine 3. Chemotherapeutic Agents:
• Synthetic Antibacterial Agents / Antimicrobial Agents:
SAR: Sulfonamides, Quinolones
Synthesis:
• β-Lactam Antibiotics:
SAR: Cephalosporins, Penicillins
Synthesis: Penicillin-G
• Antimycobacterial Agents:
Synthesis: Ethambutol, Isoniazid, Pyrazinamide, Clofazimine, PAS.
• Antifungal Agents:
Synthesis: Clotrimazole, Ketoconazole, Fluconazole
• Antiprotozoal Agents: Antimalarial, Antiamoebic Agents
SAR: Quinolines
Synthesis: Metronidazole, Ornidazole, Chloroquine, Primaquine, Pyrimethamine.
• Anthelmintics:
Synthesis: Albendazole, Mebendazole.
• Antiviral and Anti-HIV Agents:
Synthesis: Amantadine
• Antineoplastic agents:
Synthesis: Chlorambucil, Cyclophosphamide, Methotrexate, Fluorouracil
4. Miscellaneous
• Antiparkinson’s agents,
• Alzheimer’s disease,
• Non Steroidal Anti-Inflammatory Agents
Synthesis: Diclofenac, Ibuprofen, Indomethacin, Mefenamic acid, Nimesulide
Reference Books
1. Wilson and Gisvsld’s Textbook of Organic Medicinal & Pharmaceutical Chemistry, 2. The Organic Chemistry of drug design and drug action, R. B. Silverman. 3. Strategies for organic drug synthesis & design, D. Lednicer John Wiley. 4. Principles of Medicinal Chemistry, William O. Foye, Lippincott, William and 5. Total synthesis of Natural products, Apsimon (Series). 6. Textbook of Medicinal Chemistry by A. Kar, Asian Age. Publication. 7. Pharmaceutical substances by A. Kaleemann & Engle. M.Sc. SEMESTER IV
PHARMACEUTICAL ORGANIC CHEMISTRY
POC-403: Modern Analytical Techniques-MAT
Introduction to Spectroscopic Techniques:
Types of Analytical techniques, Introduction of Instrumental methods and its classification,
Overview of spectroscopic methods based on wave length regions of Electromagnetic
radiation, Properties of Electromagnetic radiation.
1. Infrared Spectroscopy: Introduction to IR and FTIR, Principle & Theory of Infrared
absorption spectrometry, Infrared sources and transducers, Sample handling, Instrumentation, Interpretation of IR spectra, Applications and limitations of IR spectroscopy. 2. Mass Spectroscopy: Introduction, Principle, Theory and components of mass
spectrometers, Different ionization and detection techniques, Recording and resolution of mass spectrometer, Types of ions produced in mass spectrometer, Interpretation of Mass spectra of selected compounds /API, Applications of Mass spectrometry, Introduction to ICP-MS. 3. Emission Spectroscopy: Atomic emission spectroscopy, Principle, theory and
Instrumentation, Atomization techniques, Flame atomizer, Electrothermal atomizer and Inductively coupled plasma atomizer (ICPA). Flame emission spectroscopy: Principle, Instrumentation and applications, Fluorimetry: Principle, Instrumentation and application. 4. Nuclear Magnetic Resonance Spectroscopy: Introduction to Nuclear Magnetic
Resonance, NMR Spectrometer, Chemical shift, Applications of Nuclear magnetic resonance spectroscopy, Introduction, Principle, Theory, Application and Problems of C13 – NMR, Introduction to 2D NMR. 5. Polarimetry and Spectropolarimetry: Introduction, Polarized light, Optical activity,
Specific rotation measurement of rotatory power, Optical rotatory dispersion and circulardichroism, Instrumentation and applications, Saccharimetry. 6. Structure determination and distinction of various isomeric compounds through
Reference Books
1. Practical NMR Spectroscopy, M.L. Martin, J.J. Delpeuch and G.J. Martin, Heyden. 2. Specrometric identification of Organic Compounds, R. M. Silverstein, G. C. Bassler 3. Introduction to NMR Spectroscopy, R. J. Abraham, J. Fisher and P. Loftus, Wiley. 4. Application of Spectroscopy of Organic Compounds, J. R. Dyer, Prentice Hall. 5. Spectroscopy Methods in Organic Chemistry, D. H. Williams, I. Fleming, Tata 6. Spectroscopy of Organic Compounds, P. S. Kalsi, New Age International Ltd. M.Sc. PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER IV
POC-404: Dissertation
Dissertation:

• A student of M.Sc. POC will undertake a research dissertation in a group of 2-4 on full-time basis for a period of six months during semester- 4. The candidates will be given the option of selecting a research problem in a preferred area that falls within the disciplines of courses undertaken. The project could be conducted at the College. • At the end of the semester the candidates are required to present their results in the form of a dissertation thesis & oral presentation. • The evaluation (Presentation & Viva) of the dissertation work will be carried out during University practical examination. M.Sc. -PHARMACEUTICAL ORGANIC CHEMISTRY
SEMESTER III
POC-405 & 406: PRACTICALS
POC-405: Practical
1. Pharmaceutical Technology:
Preparation and evaluation of effervescent tablet, ferrous sulphate tablet,
Paracetamol tablet.
Preparation and evaluation of tablets employing direct compression, wet granulation, dry granulation (slugging), compression coating. Filling of powder/ granules/ pellets in hard gelatin capsule and its evaluation.
Perform pharmacopoeial test for given sample of glass vial / ampoule.
Preparation and evaluation of face powder, lipstick, cold cream, vanishing cream, tooth paste/ tooth powder. Formulation and evaluation of syrup, emulsion (o/w, w/o), turpentine liniment,
calamine lotion.
Formulation and evaluation of milk of magnesia/aluminum hydroxide gel antacid suspension. Formulation and evaluation of dry suspension. Formulation and evaluation of diclofenac sodium gel. 10) Formulation and evaluation of transdermal spray. 11) Formulation and evaluation of calcium gluconate injection, dextrose injection, NaCl injection, dextrose saline injection, menadion injection. 12) Formulation and evaluation of eye drops. 13) Formulation and evaluation of multidose injection of chloroquine phosphate. 14) Formulation and evaluation of metronidazole infusion. 2. Organic Separation of Ternary Mixtures*:
a. Liquid + Solid b. Liquid + Liquid
3. Analytical Techniques:
Extraction of Natural Products & separation of specific components
Chromatography: TLC, Column, Paper chromatography
UV-Visible Spectroscopy: Analysis and Estimation
4. Medicinal Chemistry:
Synthesis of privileged scaffolds using Conventional & Green synthetic methods: Single
/ Multi-step synthesis of organic compounds, TLC monitoring & spectral study. Green methods such as Microwave / Mortar pastel / Ionic Liquid / Water mediated / Solid 5. Demonstrative Practical:
• HPLC analysis of Active Pharmaceutical Ingredients
• Moisture analysis using KaFi Auto Titrator
• IR spectral study of selected APIs
• Pilot Plant Production of raw materials/ intermediates for APIs.
POC - 406: Viva Voce examination
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