·         The Structure of methane, ethane, Ethylene, and the Ethyne Sp³,SP², and SP³– orbital hybridization.

·         Restricted rotation and double bond, cis-trans E, Z -isomers, conformational analysis of ethane, butane, and cyclohexane, relative stabilities of cycloalkanes ; Ring strain

·         Nomenclature of alkanes, alkenes, alkynes, cycloalkanes and cycloalkenes, bicyclic and Spiro compounds.

·         Physical properties of alkanes and cycloalkanes

·         Isomerism.

·         Enantiomers and chiral molecules, nomenclature of Enantiomers, properties of enantiomers; optical activity

·         Introduction, physical properties of organic halides, reaction

·         mechanisms S1 and S2 reactions and the stereochemistry of S1 reactions.

·         Molecules with more than one stereocenter, stereoisomerism of cyclic compounds, resolution of enantiomers, and Fischer projection.

·         Dehdrohalogenation of alkyl halides, Dehydration of alcohol and its

·         mechanism, and Dehalogenation of vic-dibromides ,Hydrogenation of alkynes ,.

·         Additions reaction: Hydrogenation, Halogenation.

·         Addition of HX and oxidation

Assessment

·         Structure and nomenclature, physical properties of alcohols and ethers.

·         Synthesis of alcohols from alkenes, hydration of alkenes, through oxymercuration-demercuration, through hydroboration –oxidation.

·         Reaction of alcohols: with HX, PBr3, SOCl2.

·         Reaction of alcohols: with HX, PBr3, SOCl2.

·         Alcohols from carbonyl compounds: Oxidation- Reduction and organometallic compounds, oxidation of alcohols, preparation of organ lithium and organ magnesium.

·         Reaction of organ lithium and organ magnesium compounds

·         Nomenclature of benzene derivatives, the Kekule structure for benzene, the stability of benzene, aromatic, antiaromatic, nonaromatic, the annulenes aromatic ions , and benzeneoid aromatic compounds.

·         Theory of substituent effects on orientation and reactivity in electrophilic aromatic substitution, synthetic applications

·         Nomenclature of aldehydes and ketones, physicalproperties, synthesis of aldehydes, synthesis of ketones.

·         Nucleophilic addition to the carbon-oxygen double bond, the addition of water and alcohols, acetals and ketals , hemiacetals and hemi ketal and cyclic ketals .

·         Oxidation of aldehydes and ketones, TheBaeyr-Villger oxidation.

·         Nomenclature and physical properties, acidity of carboxylic acids, dicarboxylicacids, esters, carboxylicanhydrides, acyl chlorides amides and nitriles.

·         Nomenclature, physical properties and structure of amines, basicity of amines, amines as resolving agents,

·         Replacement reaction of arendiazonium salts, synthesis using diazonium salts.

·         Determination of melting points

·         Determination of boiling points

·         Crystallization

·         Sublimation

·         Simple and fractional distillation

·         Vacuum and steam distillation. 8-Extraction with solvents.

·         Functional group identification, alcohols, aldehydes and ketones, esters , carboxylic acids , and phenols

Content BreakdownWeek

Topical Coverage

Session 1 (Week 1)

I. Introduction

·         What is Analytical Chemistry?

·         Qualitative and Quantitative analysis.

·         The function of Analytical Chemistry.

Session 2 (Week 2)

·         MethodsofAnalysis.

·         Stereochemistry

·         Percentage concentration (Weight per weight- volume per volume)

Session 3 (Week 3)

·         Molar and formal concentration (Molarity and formality).

·         Normal concentration (Normality).

Session 4 (Week 4)

·         Conversion from one concentration to another.

·         Problems and calculations.

Session 5 (Week 5)

Volumetric quantitative methods of analysis

·         General principles (Titrimetric analysis, Titrate&Titrant).

·         Types of titrimetric analysis (direct and back titration).

Session 6 (Week 6)

Standards (primary & secondary substances).

•         Preparation of standard solutions by direct & indirect methods

Session 7 (Week 7)

Specific chemical reactions in analytical chemistry.

•         Equilibrium concept.

Session 8 (Week 8)

II. Neutralization in analytical chemistry

·         Introduction.

·         Acid – base theories.

·         Acid – base strength.

·         Leveling effect.

Session 9 (Week 9)

Acidity of solutions pH.

•         Calculation the pH of solution of strong acid and strong base.

•         The ionic product of water.

•         Calculation the pH of solutions of weak acid and weak base.

•         Calculation the pH during titration.

Session 10 (Week 10)

•         Ionization of polyprotic acids.

•         Hydrolysis of salt.

•         Buffer solutions.

•         Calculation of pH of Buffer (Henderson equation).

•         Problems and calculation.

Session 11 (Week 11)

Midterm Assessment

Session 12 (Week 12)

Session 13 (Week 13)

Session 14 (Week 14)

Session 15 (Week 15)

Acid – Base Titration,

·         Titration curves,

·         Acid – base Indicators.

·         Preparation of standard solutions of acid & base.

·         End point detection.

Session 16 (Week 16)

Acid-base Applications.

·         Determination of carbonate in a mixture of carbonate and bicarbonate.

·         Determination of carbonate in a mixture of carbonate and hydroxide.

·         Determination of carbon dioxide in the atmosphere.

·         Determination of nitrogen.

·         Determination the original boric acid in a mixture of Boric and Borax.

Session 17 (Week 17)

Acid-base titration in non-aqueous solvents:

·         Introduction.

·         Solvents.

·         Choosing a solvent.

·         End point detection.

Session 18 (Week 18)

III. Oxidation – Reduction

·         Oxidation – Reduction reactions.

·         Electro chemical cells.

·         Cell calculation.

·         Electrode potentials.

·         Factors affecting oxidation potentials

Session 19 (Week 19)

Titration curves.

·         Oxidation – Reduction indicators, Oxidation – Reduction titration, Oxidation and Reduction Agents.

·         The gram equivalent weight of an oxidizing Agent.

·         Potassium permanganate titration.

·         Preparation of standard solution.

·         Determination of ferrous sulphate using potassium permanganate.

·         Potassium dichromate titration.

·         Ceric titrations.

Session 20 (Week 20)

Methods of titration involving Iodine (Iodimetry and Iodometryreactions).

•         Iodine and sodium thiosulphate exercises.

Session 21 (Week 21)

IV. Precipitimetry

·         Introduction,

·         Solubility product.

·         Formation of a precipitate, Types of precipitates, Types of precipitating reagents.

·         Calculation of the solubility product from solubility.

·         Calculation of the solubility from the solubility product.

·         Factors affecting on the formation of a precipitate

Session 22(Week 22)

Argentometric titration

·         Preparation of standard solution of silver nitrate and sodium chloride.

·         End point detection.

·         Mohrs method for halides.

·         Fajan’s method for halides by using adsorption indicators.

·         Volhard method for halides (indirect method).   

Session 23 (Week 23)

Applications

·         Estimation of chloride anion.

·         Estimation of chloride in presence of iodide and bromide.

·         Estimation of chloride in presence of CN.

·         Estimation of Bromide and iodide.

Session 24 (Week 24)

V. Gravimetry

·         Gravimetric analysis,

·         Precipitation,

·         Post precipitation.

·         Co-precipitation,

·         Homogeneous

·         Calculation of gravimetric analysis

Session 25 (Week 25)

Applications:

·         Determination of Chloride,

·         Determination of Aluminum.

·         Determination of Sulphate,

·         Determination of Magnesium.

Session 26 (Week 26)

VI. Complexometry

·         Formation of complexes.

·         Chelating agents.

·         Stability of metal complexes.

·         Effect of pH on complex formations.

·         Solubility of complexes. Complex formation titrations

Session 27 (Week 27)

·         Ethylene – diamine – tetra – acetic acid (EDTA).

·         Titration of metal ions using EDTA.

·         End point detection by using metalo-chromic indicators.

·         Types of EDTA titrations:

·         – Direct titration.

Session 28 (Week 28)

Indirect titration.

·         Replacement titration.

·         Alkalimetric methods.

·         Titration of mixtures of metal ions.

·         Determination of hardness in water.

·         Masking and demasking agents.

Practical Work

General laboratory techniques:

·         Laboratory notebook (laboratory), Mass measurement,

·         how precision works in determining mass, and Size measurement

·         Adjustment in volume determination, pipette, calibration, burette calibration, quantitative transfer – sediment intake, moisture control, reagents, sampling, evaporative

·         Methods of weighing: Determination of chloride in a dissolved sample, Determination of nickel in steel, Determination of tin in zero (lead),

·         Determination of sulfur in a dissolved sample, Determination of iron (homogeneous precipitation), Determination of copper and nickel in Monbel (electrical weight)

·         Volumetric Methods: Preparation & Standardization From solid and liquid

·         Titration of Sodium Carbonate with Hydrochloric acid (Acid – Base Titration)

·         Titration of Sodium Hydroxide with Hydrochloric acid (Acid – Base Titration)

·         Standardization of potassium permanganate using oxalic acid (Reduction-Oxidation Titration)

·         Silver nitrate titrations by Mohrmethod (Precipitation titration)

·         Complex-formation titration (Water hardness)

·         Determination of iodine (Iodimetry titration).

Content BreakdownWeek

Topical Coverage

Session 1 (Week 1)

Unit one: Chemistry of Heterocyclic Compounds:

•         Nomenclature including IUPAC and trivial names still used by the chemical abstracts.

Session 2 (Week 2)

•         Nomenclature including IUPAC and trivial names still used by the chemical abstracts.

Session 3 (Week 3)

Chemistry: Including

•         The aromatic properties in terms of MO and resonance, the resonance theories, chemical reaction, and the properties such as behavior towards electrophilic and nucleophilic reagents, basic and acidic properties, oxidation, reduction.

Session 4 (Week 4)

Chemistry: Including

•         The aromatic properties in terms of MO and resonance, the resonance theories, chemical reaction, and the properties such as behavior towards electrophilic and nucleophilic reagents, basic and acidic properties, oxidation, reduction.

Session 5 (Week 5)

·         Methods of synthesis of following:

Heterocyclic five membered rings with one heteroatom (pyrrole, thiophene and furan).

Session 6 (Week 6)

•         Heterocyclic six membered with one heteroatom (pyridine).

Session 7 (Week 7)

•         Fused heterocycles containioline and isoquinng five membered ring (indol, benzothiophene and benzofuran).

Session 8 (Week 8)

•         Fused heterocycles containing six membered rings (quinoline and isoquinoline).

Session 9 (Week 9)

•         Five membered rings with two heteroatoms (pyrazole, imidazole, oxazole and thiazole).

Session 10 (Week 10)

•         Six membered rings with two nitrogen atoms (pyrimidine, pyridazine and pyridazine and pyrazine).

Session 11 (Week 11)

Midterm Assessment

Session 12 (Week 12)

Session 13 (Week 13)

Session 14 (Week 14)

Session 15 (Week 15)

Unit two: Chemistry of Carbohydrates:

•         Classifications, synthesis (descending, ascending and interoconversion)  structure e and physical properties (optical activity and mutarotation) chemical reaction.

Session 16 (Week 16)

•         Classifications, synthesis (descending, ascending and interoconversion) structure e and physical properties (optical activity and mutarotation) chemical reaction.

Session 17 (Week 17)

•         Classifications, synthesis (descending, ascending and interoconversion) structure e and physical properties (optical activity and mutarotation) chemical reaction.

Session 18 (Week 18)

•         Classifications, synthesis (descending, ascending and interoconversion) structure e and physical properties (optical activity and mutarotation) chemical reaction.

Session 19 (Week 19)

•         Vitamin C synthesis with special reference to biological significance of deoxy and amino sugars.

Session 20 (Week 20)

•         Vitamin C synthesis with special reference to biological significance of deoxy          and amino sugars.

Session 21 (Week 21)

Unit three: Polynuclear Compounds:

·         Fused ring aromatic compounds, naphthalene.

·         Nomenclature of naphthalene.

·       Reactions of naphthalene.

Session 22 (Week 22)

·         Oxidation of naphthalene.

·         Reduction of naphthalene.

·         Dehydrogenation of hydraromatic compounds, aromatiztion.

Session 23 (Week 23)

·         Nitration and halogenations of naphthalene.

·         Orientation of electrophilic substitution in naphthalene.

·         Friedel-Crafts acylation of naphthalene.

Session 24 (Week 24)

·         Sulfonation of naphthalene.

·         Napthols.

·       Orientation of electrophilic substitution in naphthalene derivatives.

Session 25 (Week 25)

·         Synthesis of naphthalene derivatives by ring closure. The Hawoth synthesis.

·         Anthracene and phenanthrene, nomenclature.

·         Structure of anthracene and phenanthrene.

Session 26 (Week 26)

·         Reactions of anthracene derivatives by ring closer, anthraquinone.

·         Preparation of phenanthrene derivatives by ring closer.

·         Carcinogenic hydrocarbons, arene oxides.

Session 27 (Week 27)

Review

Session 27 (Week 28)

Review

Practical Part:

•         Single step synthesis and preparations-(with reaction mechanism, determination of physical constants and calculation of percentage yield of the following:

–          Synthesis of Aspirin.

–          Acetylation.

–          Preparation of Acetanilide.

–          Nitration.

–          Preparation of Para nitro acetanilide.

–          hydrolysis.

–          Preparation of para nitro aniline

–          Benzoylation.

–          preparation of 2-Naphthyl benzoate.

–          Esterification.

–          preparation of Methyl salicylate

–          Condensation reactions.

–          preparation of Dibenzal acetone.

–          preparation of Barbituric acid.

•         Separation of binary and tertiary organic mixtures of compounds: (Reactions and principle, procedures, and pilot separations).

•         Separation of organic mixtures of (carboxylic acid, Hydrocarbons, Phenols, Amines, and Neutral organic compounds).

Content BreakdownWeek

Topical Coverage

Session 1 (Week 1)

Pharmaceutical analysis

•         Definition

•         Identify the difference between qualification and quantification Classification of pharmaceutical analysis

•         Different mechanisms used in pharmaceutical analysis Aim of pharmaceutical analysis

Session 2 (Week 2)

Spectroscopy:(Spectral analysis)

•         Definition

•         Different instruments used in spectral analysis

•         Ultra-violet spectroscopy

•         Definition

•         Principle of UV spectra

Session 3 (Week 3)

Ultra-violet spectrophotometer

•         Application of UV spectroscopy

Session 4 (Week 4)

Infrared spectroscopy

•         Definition

•         Theory of IR

Session 5 (Week 5)

•         IR – spectrophotometer (device)

•         Application of IR spectra

Session 6 (Week 6)

Atomic spectroscopy

•         Atomic absorption and fluorescence

Session 7 (Week 7)

•         Theory of atomic absorption spectroscopy (AAS) Atomic absorption (instrument)

Session 8 (Week 8)

Atomic spectroscopy (flame spectroscopy)

•         Atomic emission and fluorescence

•         Theory of atomic emission spectroscopy (AES)

•         Atomic Emission (instrument)

Session 9 (Week 9)

Molecular Spectroscopy – Nuclear transitions NMR,

•         introduction, theory, instrumentation, applications.

Session 10 (Week 10)

Mass spectrophotometery:

•         Introduction, theory, instrumentation, limitation, applications.

•         Fourier Transform Mass Spectrometry.

Session 11 (Week 11)

Midterm Assessment

Session 12 (Week 12)

Session 13 (Week 13)

Session 14 (Week 14)

Session 15 (Week 15)

Non-spectroscopic analysis

Tubidemetry

Session 16 (Week 16)

Separation techniques:

•         Chromatographic Analysis

•         General chromatographic techniques HPLC

•         Theory of HPLC

Session 17 (Week 17)

•         Basic information for the different mechanism of HPLC HPLC instrument

•         Application of HPLC

Session 18 (Week 18)

GAS chromatography

•         Theory of GAS chromatography

•         GAS chromatography instrument

•         Application of GAS chromatography

Session 19 (Week 19)

Ion chromatography

Session 20 (Week 20)

Electrophoresis

Session 21 (Week 21)

Electrochemical analysis:

•         Introduction.

Session 22(Week 22)

Potentiometry

•         Theory of potentiometry Potentiometer (device)

•         Application of Potentiometry

Session 23 (Week 23)

Polarography

•         Theory of polarography

•         Polarography (device)

•         Application of polarography

Session 24 (Week 24)

Conductometry

•         Theory of conductometry Conductometric titrations

•         Application of conductumetry

Session 25 (Week 25)

Amperometry

•         Theory of amperomtry Amperometry (device)

•         Application of amperometric titration

Session 26 (Week 26)

Electrogravimetry

Columetry

Flourometry

Session 27 (Week 27)

Coulometry:

•         Introduction, types of coulometery, parameters in coulometric analysis,

•         applications.

Session 28 (Week 28)

Thermal analysis:

•         Introduction, thermogravimetry (TG), differential thermal analysis (DTA), differential scanning calorimetry (DSC), factors affecting DTA and DSC

•         results, instruments for thermal analysis, applications.

Practical work

•         Identify Ultra -violet instrument components

•         Effect of solvent in Lmda max using phenol

•         Identify Infrared instrument components

•         Determination of Lasix

•         Identify AAS instruments components

•         Assay some metals by AAS instrument

•         Identify HPLC instrument

•         Identify GAS chromatographic instruments

•         Assay quality of some medicines by using different pharmaceutical

•         techniques according to BP

•         Calibration curve using of UV of unknown concentration.

Content BreakdownWeek

Topical Coverage

Session 1 (Week 1)

Unit I: Introduction:

·         Processesofdrugdiscovery

·         Modern drug discovery

·  Biotechnology and Drug Discovery

Session 2 (Week 2)

Physicochemical Properties and biological activity:

•         Solubility and partition coefficient

•         Ionized and unionized species (ionization constant)

•         Surface activity (nature of receptor site)

•         Hydrogen bonding and chelation

Session 3 (Week 3)

Receptor and drug-receptor interaction Concepts of:

·         Nonspecific and specific drugs,

·         Prodrugs and soft drugs,

·         Isosters and bioisosters)

Session 4 (Week 4)

Unit II: Drug metabolism:

•         General pathways of drug metabolism (Phase Iand II).

•         Sites of drug biotransformation

•         Factors Affecting Metabolism

•         Drug Biotransformation Pathway (Phase 1), Monooxygenase, Human Hepatic Cytochrome P450 Enzyme System

•         Drug Conjugation Pathways (Phase 2)

•         Elimination Pathways

Session 5 (Week 5)

•         Drug Metabolism and Age

•         Genetic Polymorphism

•         Oral Bioavailability

•         Extrahepatic Metabolism

•         Stereochemical Aspects of Drug Metabolism

•         Structure-activity relationship, specific use and adverse effect.

Session 6 (Week 6)

Unit III: Drugs acting on the autonomic nervous system:

Introduction to ANS , Cholinergic Drugs:

•         Direct acting cholinergic agonists.

Session 7 (Week 7)

•         Indirect acting cholinergic agonists.

•         Cholinesterase inhibitors: synthesis of Carbachol, neostigmine bromide and Isofurophate.

Session 8 (Week 8)

Anticholinergic Drugs or cholinergic blocking agents:

•         Parasympathetic postcholinergic – blocking agents (solanaceous alkaloids “and synthetic analogous”, aminoalcohol ether, aminoalcohol ester, aminoamides, papaveracous alkaloids and their synthetic analogies).

•         Ganglionic   blocking    agents    (curares    “and    related    compound”,

•         succinylcholine, decamethonium. Gallamin, and hexafluorinium bromide)

•         Synthesis of succinylcholine chloride.

Session 9 (Week 9)

Adrenergic Drugs

·         Direct  sympathomimetic agent. indirect sympathomimetic agent

•         Adrenergic Blockers: α-Adrenergic Blockers. β-Adrenergic Blockers.

•         Synthesis of Phenylepherine, Prazocin HCL and Atenolol.

Session 10 (Week 10)

Unit IV: Diuretics:

Introduction of nephrons

·         Site 1 diuretics carbonic anhydrase inhibitors

·         Site 2 diuretics thiazide and thiazide-like drugs

·         Site 3 diuretics high-ceiling or loop diuretics

·         Site 4 diuretics potassium-sparing diuretics

·         Miscellaneous diuretics.

Session 11 (Week 11)

Midterm Assessment

Session 12 (Week 12)

Session 13 (Week 13)

Session 14 (Week 14)

Session 15 (Week 15)

Unit V: Drugs acting on cardiovascular system:

Cardiotonic agents

Antianginal and vasodilators:

·         Ester of nitrous and nitric acids.

·         Calcium antagonist: synthesis of Nifedipine and Diltiazem.

·         Antiarrhythmic

Session 16 (Week 16)

Antihypertensive agents

·         Agents affecting peripheral sympathetic nerve

·         Centrally acting adrenergic drugs

·         Drugs acting directly on smooth muscles (vasodilators):

·         Angiotensin-converting enzyme inhibitors.

·         synthesis of hydralazine, Captopril and Methyldopa.

Session 17 (Week 17)

Antihyperlipidemics: Synthesis of Clofibrate.

Anticoagulants

Session 18 (Week 18)

Unit VI: Antihistaminic agent:

·         H1-antagonist; synthesis of diphenhydramine, tripelenamine, and chlorpheniramine

·         H1-antagonist; synthesis of cimetidine and ranitidine.

·         Proton pump inhibitors

Session 19 (Week 19)

Unit VII: Local anesthetics:

·         Synthesis of procaine, benzocaine, and lidocaine

Session 20 (Week 20)

Unit VIII: Anti- diabetic drugs:

·         Insulin and its preparations.

·         Oral hypoglycemic agents: Synthesis of Tolbutamide, Glyubenclamide and Phenformin HCL.

Session 21 (Week 21)

Unit V: Antineoplastic and Immunoactive drugs:

·         Types of neoplasms

·         Metastasis

·         Synthesis of chlorambucil, thiotepa,

Session 22(Week 22)

·         Synthesis of cyclophosphamide, methotrexate.

Session 23 (Week 23)

·         Synthesis of 6-mercaptopurine, and 5-fluorouracil.

Session 24 (Week 24)

·         Immunoactive drugs:

Session 25 (Week 25)

Unit VIII: Diagnostic agents: Contrast media:

·         Barium sulphate

Session 26 (Week 26)

·         Iodine compounds

Session 27 (Week 27)

·         Review

Session 28 (Week 28)

·         Review

Practical work (one/week)

·         Identification of some drugs: To carry out characteristic chemical tests for identification of some studied in theory, as specified in the BP 1993 (VOL I & II).

·         Assay of some drugs (with emphasis on the functional group analysis): To carry out the assay (estimation and % purity) of some drugs studied in theory by following the procedures given in BP 1993 (VOL I & II) and emphasis will be given on the functional group wherever applicable.

·         Phenols (or Chlorocresol or Chloroxylenol), Hydrogen peroxide, Formaldehyde, Methyl salicylate, Cephalexin, INH, Fusidic acid, Sulphur ointment, Benzoic acid and Salicylic acid ointment, Nicotinamide, Ascorbic acid, Diphenhydramine HCl, CPM, Chloroquine phosphate, Chlorambucil, Lidocaine HCl, Sulpha drugs (Sulphanilamide or Sulphacetamide sodium).

·         Synthesis of some representative drugs: (Sulphanilamide, Sulphacetamide, Benzocaine)

·         Note: In addition to determination of the percentage purity of drug, the principle of calculations involved in the functional groups have to be studied during the assay of the drugs containing a distinct mono-functional group.

Content BreakdownWeek

Topical Coverage

Session 1 (Week 1)

Unit I: Chemotherapy:

Antiseptic and disinfectants: preparation, action, uses:

·         Benzalkonium chloride: structure, action and uses

·         Alcohols: Ethanol, Synthesis, concentration, uses as antiseptic

·         Isoprpoyl alcohol: structure, uses, preparation

·         Ethylene oxide: method of preparation, uses as antiseptics.

·         Formalin: structure, method of preparation, uses

Session 2 (Week 2)

·         Boric acid: structure and uses

·         Gentain violet: structure, method of preparation, uses.

·         Phenol: preparation, mechanism of action, uses.

·         Cresol: Orth, meta, para, uses

·         Hydrogen peroxide: composition, mechanism of action as an oxidizing agent, uses.

·         Chlorothymol: preparation, uses.

·         Chloroxylenol (Dettol®): structure, uses.

·         Potassium permanganate: as an oxidizing agent, concentration, uses.

·         Iodine: solubility, concentration, mechanism of action.

·         Silver nitrate: medical uses.

·         Organic halogenated compounds as chloramine and Chloramine T: action, structure, uses.

·         Mercurochrome: structure, uses

Session 3 (Week 3)

Preservatives:

·         Benzyl alcohol: composition, preparation, and methods of uses.

·         Beta-phenyl alcohol: composition, preparation, and methods of uses.

·         Sodium benzoate: composition, preparation, and methods of uses.

Session 4 (Week 4)

Antimicrobial and antibiotics:

·         Sulpha drugs and miscellaneous antibacterial, general method of synthesis of sulph drugs; trimethoprim and its synthesis

Session 5 (Week 5)

Antibiotics:

·         Beta-lactam antibiotic: penicillin, cephalosporin, and beta-lactamase inhibitors.

·         Chloramphenicol including stereochemistry.

·         Tetracycline

·         Polypeptide inhibitors: Bacitracin and polymycin B (as representatives).

·         Macrolide antibiotics: erythromycin (as representatives).

·         Miscellaneous antibiotics: Fusidic acid, lincomycin and novobiocin

Session 6 (Week 6)

Antimycobacterial agent

concepts of multi-drug therapy (MDT)

•         Antitubercular agents: synthesis of PAS, INH, and ethambutol.

•         Antileprotic drug: synthesis of dapsone

Session 7 (Week 7)

Antifungal agents: synthesis of miconazole.

Session 8 (Week 8)

Antiviral agents and an introduction of current anti-AIDS therapy

Session 9 (Week 9)

Antimalarial agents: synthesis of chloroquine and primaquine

Anthelmintics: synthesis of diethylcarbamazine citrate, pyrantel pamoate, and mebendazole

Session 10 (Week 10)

Antiamoebics: synthesis of metronidazole and diloxanide furoate

Session 11 (Week 11)

Midterm Assessment

Session 12 (Week 12)

Session 13 (Week 13)

Session 14 (Week 14)

Session 15 (Week 15)

Unit II: Central nervous system depressant:

General anesthesia

Anxiolytic, Sedative, and hypnotic agent (synthesis of phenobarbital, diazepam, and gluethimide)

·         Benzodiazepines, Barbiturates

·         Miscellaneous sedative Hypnotics:

a)       Amides and imides

b)      Alcohol and their carbamate derivatives

c)       Aldehydes and their derivative

Session 16 (Week 16)

Antipsychotics

·         Synthesis of chlorpromazine, and haloperidol

·         Phenothiazine

·         Ring analogies of phenothiazines (Thioxanthines, Dibenzoxazepines, and Dibenzodiazepines).

Session 17 (Week 17)

·         Fluorobutyrophenones

·         β-Aminoketones

·         Benzamides

·         Antimanic agents

Session 18 (Week 18)

Anticonvulsant or Antiepileptic drugs (synthesis of phenytoin, ethosuximide, carbamazepine, and valproic)

·         Barbiturates

·         Oxazolidinones

·         Succinimides

·         Benzodiazepines

·         Ureas and monoacylureas (Phenacemide)

·         Miscellaneous agents (primidone)

Session 19 (Week 19)

CNS depressant with skeletal muscle relaxant properties

·         Agents used in acute muscle spasm

·         Drugs used in spasticity

Session 20 (Week 20)

Unit III: CNS Stimulants

·         Analeptics

·         Methylxanthines

·         Central sympathomimetic agents (Psychomotor stimulants)

·         Monoamine oxidase inhibitors

·         Tricyclic antidepressant compound

Session 21 (Week 21)

Psychedelics

·         Indolethylamines

·         2-Phenylethylamines

·         Agents possessing both indolethylamines and a phenylethylamines moiety

·         Dissociative agents

·         Depressant – intoxicants

Session 22(Week 22)

Unit VI: Analgesic and NSAID

Narcotic analgesics

·         Morphine derivatives

·         Morphinans and benzomorphinons

·         Meperidine derivatives

Antitussive agents

Session 23 (Week 23)

Non-narcotic analgesics (NSAID)

·         Salicylates

·         Arylacetic acid derivatives

·         Aniline and p-aminophenol derivatives

·         Pyrazolone and pyrazolidinone derivative

Session 24 (Week 24)

Unit VII: Hormones:

Steroidal hormones (sex hormones)

·         Male sex hormones

·         Female sex hormones

·         Contraceptives

Session 25 (Week 25)

·         Adrenocorticoids

·         Mineralocorticoids

Other hormones

·         Thyroid hormone

·         Pancreatic hormones

·         Adrenal medulla hormones

·         Pituitary gland hormones and hypothalamic hormones

Session 26 (Week 26)

IX: Development of drugs (drug design):

·         Genesis of drugs (natural sources, semisynthetic drugs, and synthetic drugs)

·         Serendipity (accidental discovery)

·         Random screening

·         Rationally directed random screening

·         Rationally directed metabolite approach

·         General processes (simplification “disjunction”, replication, hybridization, and addition)

·         Special processes

Session 27 (Week 27)

Special processes

·         Vinylogy principle

·         Increase or decrease of the alkyl chain

·         Isosteric substitution (isosteres and bioisosters)

·         Introduction of bulky group

·         Electron withdrawing and electron donating groups

·         Others

Session 28 (Week 28)

Soft and hard drugs

·         Methods of lead optimization (topless sequential methods “pi, sigma, es”)

·         Drug latentiation (Prodrugs, bioprecursors, and targeted drugs)

·         Antimetabolite approach

·         Molecular modelling (docking small molecule, homology modelling and molecular dynamic)

Practical work

A. Analysis of different examples of pharmaceutical chemicals and pharmaceutical dosage forms according to the official methods

·         Anti-inflammatory: (Methyl salicylate, Naproxen, Phenazone, Phenylbutazone, Indomethacin, and Aspirin)

·         Antibiotics: (Amoxicillin, Penicillin, Benzyl penicillin, Cephalexin, Fusidic acid, and Cycloserine)

·         Diuretics: (Ethacrynic acid, and Furosemide)

·         Oral contraceptive: (Ethinylestradiol, Ethisterone, and Mestranol)

·          Antineoplastic (Melphalan, Lomustine, and Chlorambucil)

·         Hypoglycemic (Chlorpropamide, and Tolazamide)

·         Antituberculosis (Isoniazid, and Pyrazinamide)

·         Antihistaminic (Dimethydrinate, and Chlorpheniramine)

·         Sedative hypnotics (Chloral hydrate, Glutethimide, and mebrobamate)

·         Antiseptics (Mercurochrome, and Resorcinol)

B. Analysis of active constituents of different pharmaceutical dosage forms

·         Aerosol inhalations: Isoprenalions sulphate inhalation: ferrous chelate formation “spectrophotometry”. Albuterol inhalation: colored derivative with p-dimethylaminoaniline “spectrophotometry”.

·         Creams (analysis of triamcinolone cream by isoniazid method “spectrophotometry”

·         Ointments: Sulphur ointment: by oxidation to thiosulphate (titration method). Benzoic and salicylic acid ointments by acid-base titration

·         Suppositories: Glycerin suppositories: determination of glycerol content by oxidation with sodium metaperiodate by titration method. Neo-haemorrhan suppositories containing (Prednisolone acetate by phenyltetrazole method “spectrophotometry”. Lignocaine (xylocaine) by acid-dye method: methyl orange or bromocresol purple by spectrophotometry. Zinc oxide and aluminum acetate by Compleximetric method). Docking programs (MOE, autodock and Schrodinger), homology modeling and molecular dynamics.

Content BreakdownWeek

Topical Coverage

Session 1 (Week 1)

Unit I: Introduction:

•         Definitions

•         Drug quality control (QC), rules, QC lab. (Official and industry), lab records.

•         Quality assurance (QA), documentation, self-inspection and validation process of food and drug administration of USK.

•         Total quality management (TQM)

•         Different types of ISO

•         Organization dealing with drug legislations: FDA, European (EMEA), Japanese and ICH system.

Session 2 (Week 2)

Unit II: GMP, GLP, CGMP, ICH rules

Session 3 (Week 3)

•         GMP, GLP, CGMP, ICH rules

Session 4 (Week 4)

•         GMP, GLP, CGMP, ICH rules

Session 5 (Week 5)

Unit III: introduction of new drugs:

•         Drug registration: FDA, IVH, European and Libyan system of registration.

•         Stability testing for new drugs

•         Drug approval process.

Session 6 (Week 6)

Unit IV: Pharmaceutical quality control

•         Product specifications (reference standards, raw materials, recipient, in-process QC, finished product QC), batches recall, batch record.

Session 7 (Week 7)

Unit V: Analytical criteria for drug quality assessment

•         Types of criteria judging drug quality, pharmacopeial standards (USP, BP, IP) specification of quality.

Session 8 (Week 8)

Unit VI: Chemical purity and its control      

•         Drug impurities and limit tests, chiral purity

Session 9 (Week 9)

Unit VII: Procedures of QC

•         Logic sequence of QC

•         Quarantine

•         Sampling

•         Interpretation of statistical data

•         Integration of different results

•         Types of errors

•         Rejection of doubtful results

•         Certificate of analysis

•         Product release (raw materials, packaging materials and finished products)

Session 10 (Week 10)

Unit VIII: Stability studies         

·         Impurities and degradation products

Session 11 (Week 11)

Midterm Assessment

Session 12 (Week 12)

Session 13 (Week 13)

Session 14 (Week 14)

Session 15 (Week 15)

·         Strategies and predispose factors of bacterial resistance.

·         (Miss use & overuse of antibiotics, capsules, cell wall components, antigenic variation)

Session 16 (Week 16)

Unit IX: Dosage form analysis                                          

·         Inhaled dosage form, solids, semisolids, liquids, drops, injectable drugs, transdermal patches, medicated forms.

·         Multi-component dosage forms.

Session 17 (Week 17)

Unit X: Functional group analysis                                   

Session 18 (Week 18)

Functional group analysis

Session 19 (Week 19)

Functional group analysis

Session 20 (Week 20)

Unit XI: Titrimetric methods of drug analysis

·         Volumetric methods (acid-base, gravimetry, compleximetry, redox titration, ..etc.

Session 21 (Week 21)

·         Volumetric methods (acid-base, gravimetry, compleximetry, redox titration, ..etc.

Session 22(Week 22)

Unit XII: Instrumental methods of analysis  

·         UV-Visible, diodarry, flourimetry, spectroscopy (IR, FTIR, NMR, MS)

Session 23 (Week 23)

·         Electrochemical methods (polarography, potentiometry, conductimetry, ..etc

Session 24 (Week 24)

·         Separation techniques (TLC, UP, TLC, GC, HPLC, CE)

Session 25 (Week 25)

·         Treatment of chromatographic data: qualitative and quantitative analysis

·         Hyphenation of separation techniques with detection tools.

Session 26 (Week 26)

Unit XII: Automation in pharmaceutical analysis

Session 27 (Week 27)

Unit XIV: Assay of drugs and related substance in biological fluids

·         Sample preparation; separation, and purification

·         Extraction procedures

Session 28 (Week 28)

Unit XV: Radiopharmaceuticals           

·         Radiochemical methods, radioactive products, and radio labeling.

·         QC of radiopharmaceuticals.

Practical work

·         Analysis of different dosage form

·         Carrying out identification assay and physical parameters according to the official pharmacopeial methods and / or develop manufacturing companies’ methods:

·         Assay of aspirin tablets using UV-visible — BP 2013.

·         Assay of paracetamol tablets using UV-visible – BP 2013.

·         Assay of nalidixic acid suspension – BP 2013.

·         Assay of enalapril tablets by potentiometer titration.

·         Assay of sodium bicarbonate infusion by direct acid titration – BP 2013.

·         Assay of chloramphnicol eye drop by UV-visible – PB 2013.

·         Assay of pyridoxine tables by UV-visible.

·         Assay of ORS sachet by UV-visible.

·         Detection of Zn in insulin using atomic emission spectroscopy.

·         Assay of tretinoin (Retina A)® gel using UV-divisible—BP 2013. 11 Assay of Nifedipine tables using HPLC – BP 2013.