91047 - Pharmaceutics I

Learning outcomes

The course provides a comprehensive understanding of the process of converting an active pharmaceutical ingredient into a medicinal product that can be safely and effectively administered to patients. On completion of the course, the student will have an in-depth knowledge of: - the correlation between physico-chemical properties of the active pharmaceutical ingredient, dosage form, route of administration and therapeutic outcome; - the formulation of solid, semi-solid and liquid dosage forms; - the role and application of excipients in the development of dosage forms; - the principles that govern stability improvement and quality assessment of dosage forms; - the technologies and equipment used in manufacturing processes. The course also provides practical skills related to pharmaceutical compounding.

Course contents

Module 1

Introduction. Definitions of drug, excipient and dosage form. Rule of excipients in dosage forms. Classification of dosage forms according to physical state, route of administration and drug release.

Biopharmaceutical factors affecting drug bioavailability. Introduction to biopharmaceutics. Bioavailability. Gastrointestinal tract and absorption. Factors affecting drug release and absorption. Dissolution and solubility.

Particle science and powder technology. Particle size and particle size analysis. Particle size reduction and size separation. Mixing. Powder flow. Drying.

Solid dosage forms. Powders and granules. Powdered and granulated products as dosage forms. Granules as intermediate in tablet manufacture. Pharmaceutical technology of granule production. Granulation mechanisms. Pharmaceutical granulation equipment and processes. Tablets. Quality attributes of tablets. Tablet types. Tablet manufacturing. Tablet excipients. Fundamental aspects of the compression of powders. Fundamental aspects of the compaction of powders. Relationships between material properties and tablet strength. Coated oral dosage forms. Reasons for coating dosage forms. Starting material. Sugar coating. Film coating. Compression coating. Capsules. Hard capsules. Soft capsules. Raw materials and manufacturing processes. Rectal and vaginal suppositories. Anatomy and physiology of the rectum and vagina. Absorption of drugs from the rectum and vagina. Requirements of suppositories. Suppository bases. Formulation principles and manufacturing processes.

Semi-solid dosage forms. Skin structure and function. Transport through the skin. Classification of semi-solid preparations for cutaneous application: ointments, creams, gels and pastes. Requirements of preparations with semi-solid properties. Formulation principles and manufacturing technology.

Liquid dosage forms. Solutions. Pharmaceutical solutions. Formulation and manufacturing processes. Solution stability. Enhancement of drug solubility: pH adjustment, cosolvents, complexation with cyclodextrins, surfactants and micelles. Emulsions. Emulsion types. Formulation of pharmaceutical emulsions. Instability phenomena and stabilizing principles. Emulsifying agents. Preparation technology. Suspensions. Definition. Solid particle-liquid vehicle interactions. Particle movement in suspensions. Dispersibility issues and surface wetting. Stability. Formulation and manufacturing technology.

Parenteral formulations. General introduction. Routes of parenteral administration. Pharmacopoeial requirements. Excipients. Preparation of solutions and suspensions for injection. Parenteral depot drug formulations. Pharmaceutical sterilization.

Module 2 (Pharmaceutical compounding laboratory)

Small-scale manufacturing (compounding), packaging and labelling of powders, capsules, solutions, suspensions, liquid emulsions, creams, ointments, gels, pastes and suppositories.

Readings/Bibliography

A. Fahr; G.L. Scherphof, Voigt's Pharmaceutical Technology, Wiley, New York (Twelfth Edition, 2018).

M.E. Aulton, K.M.G. Taylor, Aulton's Pharmaceutics - The Design and Manufacture of Medicines, Elsevier, Amsterdam (Sixth Edition, 2022).

 

Teaching methods

The course is divided into two parts, 56 hours (7 ECTS Credits) of lessons and 60 hours (4 ECTS Credits) of laboratory practice. Laboratory practical is carried out individually, with a final test.

The obligation to attend the didactic activities is considered to be fulfilled attending at least 80% of the laboratory activities and 70% of lessons.

Prerequisite: Medicinal and toxicological chemistry I and Physics, Elements of mathematics (I.C.).

As concerns the teaching methods of this course unit, all students must attend Module 1, 2 [https://www.unibo.it/en/services-and-opportunities/health-and-assistance/health-and-safety/online-course-on-health-and-safety-in-study-and-internship-areas] online, while Module 3 on health and safety is to be attended in class. Information about Module 3 attendance schedule is available on the website of your degree programme.

Assessment methods

The examination is divided into two parts: a practical examination concerning the preparation of a formulation, calculation of price, packaging and labelling and an oral examination consisting of 3-5 open questions on the arguments of the program.

Teaching tools

The theoretical lessons will be held by using common audio-visual means.

Practical activities will be carried out in laboratories equipped with all necessary chemicals, equipment and texts (European Pharmacopoeia and Official Pharmacopoeia of the Italian Republic).

The material used for lectures (power-point presentations, laboratory manual) will be made available to students on the Virtuale website.

Office hours

See the website of Federica Bigucci