PHARMACEUTICAL TECHNOLOGY AND LABORATORY

Alphabetic division AC-DL-MQ-RZ

Course Sheet

Course code:

TFL010

Academic Year of enrolment:

2019

Year of supply:

2022/2023

Divisions:

Cognomi A-G

Type of Course:

Characterising

Degree:

Course of Single Cycle Degree 5 years in PHARMACY

Disciplinary Sector:

Applied Technological Pharmaceutics

Is part of:

PHARMACEUTICAL TECHNOLOGY AND LABORATORY

Location:

CHIETI

Credits:

Programme Year:

Professor and Collaborators:

CELIA Christian

Cycle:

First semester

Obligatory attendance:

Yes

Minimum hours of attendance:

Hours of classroom activity:

136

Individual study hours:

214

Prerequisites:

Pharmaceutical Chemistry and Toxicology I

Objectives

The course offers an overview for the preparation, characterization, and procedures of conventional and innovative pharmaceutical dosage forms. Students will acquire the basic knowledges for the production of galenic formulations and the relative information for managing the best practice in pharmacy.

Contents

FUNDAMENTALS OF PHARMACEUTICS:
Historical evolution of pharmacy and pharmaceutical technology. Drugs and pharmaceutical dosage forms. Formulations in pharmacy and industrial pharmacy. The Official Italian Pharmacopoeia (FUI), its legal aspects and impact for pharmacists. Common aspects, relationship, and similarity of F.U.I. with the most important foreign pharmacopoeias (USP, BP, International) and particularly with the European Pharmacopoeia. Drug formularies: legislation, legal responsibility, ethics, and warning, shifting responsibility and distribution of prescriptions. Side effects of prescriptions. National Fare of Medicines.

PHARMACEUTICAL and TECHNOLOGICAL PROPERTIES:
Pharmaceutical manufacturing: Dissolution and solubility. Filtration. Evaporation. Concentration. Drying. Freeze-drying. Grinding. Sterilization.
Excipients: Fundamentals. Technology use. Interaction between drugs, excipients, and devices.
Additives: Coloring agents. Flavoring agents. Flavoring agents and preservatives (antioxidant, antibacterial and antifungal compounds). Stability, stabilization, and storage of medicines. Standards for storage medicines.
Packaging materials: Primary and secondary packaging. Aim and properties of the primary and secondary packaging of pharmaceutics. Technological properties and controls of raw materials for medicines (glass, plastics, silicones, elastomers, aluminum, paper).
Rheology properties of pharmaceutics.

ORAL SOLID DOSAGE FORMS:
Powders: Fundamentals and classification according to F.U.I. Grinding and particle size-reduction of powders. Particle size analysis: sieving, sedimentation, optical and electron microscopy, coulter counter. Rheological properties of powders and rate angle. True and apparent density, shaking and mixing densities. Mixing of the powders. Bulk and F.U.I. powder tests. Powders for pharmaceutical use: simple and composite powders, Selling of powder medicines.
Granules: Fundamentals. Dry and wet granulation processes. Advantages and disadvantages of processes. Pharmaceutical granulation equipment. Granulates as pharmaceutical dosage form or product to make tablets and capsules.
Tablets: Fundamental and introduction. Main and secondary excipients to make tablets. Technological properties of the excipients to make tablets. Classification of tablets according to the F.U.I: coating, enteric and controlled release tablets. Film and sugar coating of compressed tablets. Coating procedures and equipment. F.U.I. tests for tablets.
Capsules: Fundamental and introduction. Classification of capsules: hard and soft capsules. Capsule procedure and equipment. Classification of gelatin. Film-coating of capsules. F.U.I. tests for capsules.

SOLUTION AS PHARMACEUTICAL DOSAGE FORMS:
Fundamentals: Physical bases of dissolution process. Principles of dissolution. Dissolution process and analysis. Solubility measurements. Procedures to evaluate the solubility and concentration of solutions.
Water: Water for pharmaceutical use (deionized water, sterile water, water for injection, sterile water for injection). Procedures for water fabrication: filtration, ion-exchange, distillation, reverse and direct osmosis.
Solutions or colloidal suspensions: Fundamental and properties. Lyophilic and lyophobic colloids. Hydrophilic colloids or mucilage. Natural, semisynthetic, and synthetic products forming hydrophilic colloids.
Gels: Fundamentals. Rheological properties. Physicochemical and pharmaceutical properties of gels.
Emulsions: Liquid-liquid systems. Surface-active agents. Classification of emulsions (W/O and O/W). Surfactants: properties, classification, and choice of surfactants (Bancroft, HLB and its determination). Methods for preparation of the emulsions. Identification of emulsions. Physical factors affecting emulsion stability: creaming, flocculation, and coalescence. Accelerated stability tests. Stokes' law and physical stability of emulsions. Application of emulsions. Micro-emulsions.
Suspensions: Physical and chemical characteristics of suspensions. Flocculated and deflocculated suspensions. Zeta potential and its role in the stability of suspensions. Preparation of suspensions and surfactant agents. Stability of suspensions. Fundamentals of pharmaceutical suspensions: oral, parenteral, and topical application.
Syrups: Fundamentals and general properties. Syrups of F.U.I. Classification of syrups: regular, flavored, and medicated. Modification of syrups for pharmaceutical use: sorbitol and saccharin. Procedures and equipment to make syrups: advantages and disadvantages of different methods. Storage and tests of syrups.

SEMISOLID PHARMACEUTICAL DOSAGE FORMS:
Epidermal and transdermal drug delivery: Anatomical and physiological features of the skin. Percutaneous absorption of drugs. Classifications: ointments, creams, pastes, and gels. Physicochemical properties and fundamentals of hydrophilic and lipophilic excipients.

RECTAL AND VAGINAL DRUG DELIVERY:
Rectal and vaginal drug delivery: Introduction. Fundamentals. Physicochemical properties. Classification of excipients and related properties. Therapeutic use.
Suppositories and capsules for rectal delivery: Introduction. Fundamentals. Physicochemical properties. Lipophilic, water-dispersible, and water-soluble excipients. Classification of excipients. Production and preparation methods of suppositories. Rectal adsorption of drugs.
Pessaries and vaginal tablets: Introduction. Fundamentals. Physicochemical properties. Classification of excipients. Vaginal adsorptions of drugs.
Urethral glow plugs: Introduction. Fundamentals. Physicochemical properties. Classification of excipients.
PARENTERAL DOSAGE FORMS:
Fundamentals. Classification of parenteral dosage forms according to F.U.I. Intravenous administration: fundamentals, preparation, vehicles (water and natural oil), glass and plastic containers. Piggyback parenteral perfusion. Lyophilized powders for injection.

OPHTHALMIC DOSAGE FORMS:
Anatomy and physiology of the eye. Bioavailability and adsorption of drugs through the eye. Types of ophthalmic products: eye drops, ophthalmic solutions, ophthalmic suspensions, ophthalmic ointments, ocular insert, intraocular solution. Fundamentals, physicochemical properties, and preparation methods. Osmolarity and relative determination.

NASAL DRUG DELIVERY:
Anatomy and physiology of the nose. Physicochemical factors influencing drug absorption in the nasal cavity. Strategy for improving drug availability in nasal administration. Nasal delivery systems and their formulations.
Aerosol: Fundamentals. Introduction. Adsorption of drugs through the nasal mucosa. Trans-mucosal adsorption. Mechanisms of adsorption through the nasal mucosa. Containers for the nasal drug delivery. Classification of the nasal dosage forms: liquid nasal dosage forms, squeeze-bottles nasal dosage forms, metered-dose pump systems, nasal powders.

PULMONARY DRUG DELIVERY:
Lung anatomy and physiology.
Biopharmaceutics of inhaled drug delivery: Size. Density. Shape. Influence of environmental humidity on particle size. Particle deposition in the airways.
Classification of pulmonary drug delivery: Fundamentals. Introduction. Excipients for inhaled drug delivery. Physicochemical properties. Classification and synthesis of inhaled drug delivery.
Nebulized drug delivery: Nebulizers, jet nebulizers, ultrasonic nebulizers, dry powder inhaler, formulating nebulizer fluids.
Metered dose inhaler: containers, propellants, metering valve, formulating metered-dose inhaler, filling metered-dose inhaler canisters, spacers, and breath-actuated metered dose-dose inhalers.

PHARMACEUTICAL DOSAGE FORMS FOR ALTERNATIVE THERAPY:
Homeopathy: Fundamentals. Introduction. Physicochemical and technological properties. Management and law governing the production and distribution of homeopathy drug.
Plant and phytochemical drugs: Fundamentals. Introduction. Physicochemical and technological properties. Management and law governing the production and distribution of plant and phytochemical drugs.
Medical devices and latexes: Fundamentals. Introduction. Physicochemical and technological properties. Management and law governing the production and distribution of medical devices and latexes.
Veterinary drugs: Fundamentals. Introduction. Physicochemical and technological properties. Management and law governing the production and distribution of veterinary drugs.

BIOPHARMACEUTICS:
Release Adsorption Distribution Metabolism and Elimination (LADME): Fundamentals. Introduction. Drug adsorption. Drug delivery across the biological barriers. Administration routes and physiological factors that affect the drug absorption. Release of drug from delivery systems. Bioavailability: Fundamentals. Introduction. Plasmatic and urinary curve analysis. Multiple dose studies. Bioequivalence. Experimental protocols. Pre-formulation studies for innovative drug delivery.

DRUG DELIVERY SYSTEMS:
Fundamentals: Differences between drug delivery systems and conventional drug dosage form. Transport equations. Diffusion or transport of the substance: flow and Fick's first law, Fick's second law, diffusion in different media. Solubility and partition coefficient. Classification of drug delivery systems and relative mechanisms. Application of drug delivery systems.
Polymers: Silicones; polyvinylchloride; polyethylene vinyl acetate; polyesters; polyamides; cellulose; polyurethanes; polyacrylates; polyethylene glycol. Analytical methods used for the characterization of polymers. Hydrogels. Therapeutic applications of drug delivery systems.
Dermal and transdermal patches: Fundamental. Introduction. Physicochemical and technological properties. Classifications. Mechanisms of drug delivery systems. Physicochemical properties of drug delivery systems. Pharmaceutical applications. Samples of transdermal patches: Nitroderm® and Transcop®.
Subcutaneous implants: Fundamentals. Introduction. Physicochemical and technological properties. Classifications. Mechanisms of drug delivery systems. Physicochemical properties of drug delivery systems. Pharmaceutical applications. Samples of intrauterine drug delivery systems: spirals, implants, intrauterine systems.

OSMOTIC DRUG DELIVERY SYSTEMS:
Fundamentals. Introduction. Mechanisms regulating the release of drugs. Physicochemical and technological properties of osmotic drug delivery systems. Classification: osmotic systems with single compartment (elementary osmotic systems and controlled osmotic systems); multicompartment osmotic systems (push-pull). Therapeutic applications of osmotic systems.

LIPID AND POLYMERIC BASED NANOPARTICLES:
Polymeric nanoparticles for oral administration: Fundamentals. Introduction. Physicochemical and technological properties. Physicochemical properties of payloads. Formulations based polymeric nanoparticles for oral administration.
Polymeric nanoparticles for trans-mucosal administration: Fundamentals. Introduction. Physicochemical and technological properties. Physicochemical properties of payloads. Formulations based polymeric nanoparticles for trans-mucosal administration.
Micro- and nano- particles: Polymeric micro- and nano- particles, solid lipid nanoparticles, nanostructured lipid carrier systems. Synthesis and physicochemical characterization. Preparation procedures. Stability. Mechanisms of interaction with biological models. Route of administration. Therapeutic applications.
Vesicular nanocarriers: Fundamentals. Introduction. Classification of vesicular nanocarriers based on composition, size, shape, and physical properties. Excipients used to make vesicular nanocarriers. Synthesis and physicochemical characterization. Preparation procedures. Stability. Mechanisms of interaction with biological models. Route of administration. Passive and active targeting strategies. Therapeutic applications of vesicular nanocarriers: liposomes, niosomes, transfersomes, ethosomes.

SUPRAMOLECULAR CARRIERS:
Pro-drugs: Fundamentals. Introduction. Physicochemical and technological properties to improve the delivery of payloads. Mechanisms of release.
Cyclodextrins: Fundamentals. Introduction. Physicochemical and technological properties of cyclodextrins. Classification of cyclodextrins (α, β, γ). Natural and synthetic cyclodextrins. Classification of preparation procedures to make the complex between drug and cyclodextrins. Physicochemical characterization of cyclodextrins: solid and liquid state procedures (differential scanning calorimetry, X-ray diffraction, circular dichroism, UV-Vis spectroscopy, nuclear magnetic resonance). Dissolution tests on cyclodextrin. Solubility studies of cyclodextrins. Active targeting of cyclodextrins.

GENE DELIVERY AND VACCINES:
Gene therapy: Aim of gene therapy. Design and production of gene vectors. Mechanism of action.
Antisense and anti-gene therapy: Design and synthesis of oligonucleotides. Mechanism of action. Anatomical structures and components involved in the transfection of genetic materials.
Vectors for gene delivery: viral and non-viral (cationic liposomes, polyplexes,
lipopolyplexes) vectors.
Vaccines based on genetic materials: Classification of vaccines based on genetic materials. Composition of vaccines based on genetic materials. Mechanisms of transfection and different composition of vaccines

ETHIC, SOCIO-ECONOMIC AND LEGAL IMPLICATIONS IN THE PRESCRIPTION AND DELIVERY OF MEDICINES:
Health system pharmacy. Professional activity in pharmacy. Delivery of medicines. Classifications of medical prescriptions. Management and delivery of toxic drugs. Mandatory records and equipment in pharmacy. Pharmaceutical care. Public and private pharmacy. Classification of pharmacies: urban, rural, rural with assistance, branch pharmacies, pharmaceutical dispensary, temporary pharmacy management. Ownership and management of private pharmacies. Organic plant and ordinary and extraordinary competition for pharmaceutical locations. Regulations relating to the management and delivery of drugs (D.P.R. 309/90) and relative amendments. Consolidated text of the laws on the subject of the regulation of narcotic drugs and psychotropic substances: purchase, possession, dispatch and possible destruction. Medicinal legislation. Classification of medicines: medicinal specialties, magisterial and industrial drugs, OTC, SOP, generics, and specialty copy. Anti-doping legislation. Presentation of medicines: label and leaflet. Italian Official Pharmacopoeia (F.U.I.). European Pharmacopoeia. Deontological code.

Extended Syllabus

Recommended Bibliography

F- Farmacopea Ufficiale Italiana (F.U.I.) XII Edizione. Farmacopea Europea. Preparati galenici per uso umano, Ultima edizione.
- RAGAZZI E., Principi di Tecnica Farmaceutica, Libreria Cortina, Padova, Ultima edizione.
- REMINGTON'S PHARMACEUTICAL SCIENCE, Ultima edizione.
- MEDICAMENTA, Cooperativa Farmaceutica, Milano, Ultima edizione.
- MARCHETTI M., MINGHETTI P., Legislazione Farmaceutica, Casa Ed. Ambrosiana, Ultima Edizione.
- COLOMBO P., CATELLANI P.L., GAZZANIGA A., MENEGATTI E., VIDALE E., Principi di tecnologie farmaceutiche, Ambrosiana, Milano, Ultima edizione. - AULTON Tecnologie Farmaceutiche, Progettazione e allestimento dei medicinali, Caviglioli G., Coviello T., De Rosa G., Modena T., Ultima edizione.
- A.T. FLORENCE, D. ATTWOOD Le basi chimico-fisiche della tecnologia farmaceutica. Edises Ultima edizione.

Teaching Methods

Interactive classes consisting of frontal lessons with students;
Individual Laboratory training for each student;
Preparation of medicines, description, healthcare registration, analysis and delivery;
Tutor for the student shall be selected with appointment from Department of Pharmacy year per year and depending on Institutional founds dedicated to the Integrative support for the Students.

Evaluation methods

Verification of learning:

The exam consists of working laboratory test concerning of preparation and evaluation of cost of galenic formulation. The test required maximum 4 hours maximum and give the opportunity to attend a class working that has not any effect on the final score. All students, who successfully pass the working laboratory, will have the access to the written test which consists of 3 exercises (5 points each) and the description and cost analysis of galenic formulation (15 points). The test is passed if a minimum score of 18 points is obtained. The written test does not affect the final score of the student, but it is mandatory to get access to the oral exam. The oral exam consists of at least 5 questions covering all topics of program. The exam is considered passed if the minimum score of 18/30 is reached during the oral exam. The written test must be repeated by students who do not pass the written test. The laboratory working exam will be made during the February and June calendar of the exams, except possible extensions provided by the Teacher, and it shell be valid for the full Academic Year. A supplementary laboratory exam shall be carried out during the summer season in the September.

Contacts/More Information

Individual laboratories activity.
Individual meetings after scheduled appointments and interactive discussion during teaching activities

Università degli Studi
"G. d'Annunzio"

Chieti - Pescara

Aree

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