FaF:FACF1_15 Chemistry of Pharmaceutical Ex - Course Information
FACF1_15 Chemistry of Pharmaceutical Excipients
Faculty of PharmacySpring 2022
- Extent and Intensity
- 1/1/0. 3 credit(s). Type of Completion: zk (examination).
Taught in person. - Teacher(s)
- doc. PharmDr. Oldřich Farsa, Ph.D. (lecturer)
doc. PharmDr. Oldřich Farsa, Ph.D. (seminar tutor) - Guaranteed by
- doc. PharmDr. Oldřich Farsa, Ph.D.
Department of Chemical Drugs – Departments – Faculty of Pharmacy - Timetable
- each odd Tuesday 13:00–14:40 44–037
- Timetable of Seminar Groups:
- Prerequisites
- The discipline is prinarilly intended for students of the 3rd year od study. Despite of it, all who have successfully passed exams in general and inorganic and organic chemistry can pass through this discipline without major problems.
- Course Enrolment Limitations
- The course is only offered to the students of the study fields the course is directly associated with.
The capacity limit for the course is 24 student(s).
Current registration and enrolment status: enrolled: 0/24, only registered: 0/24 - fields of study / plans the course is directly associated with
- Multidisciplinary studies at Faculty of Pharmacy (programme CST, KOS)
- Pharmacy (programme FaF, M-FARMA)
- Course objectives
- Pharmaceutical excipients are inorganic or organic compounds, which are necessary
for formulation of medicinal preparations suitable for direct aplication to a
patient, although, they are not holders of any pharmacological activity. In the study
program of pharmacy in the Czech Republic, such substances are the matter of interest
predominantly from the point of view of their use in application forms, and from
the point of view of physico-chemical properties related to it. Pharmaceutics, in the
middle Europe often called pharmaceutical technology or galenic pharmacy, is the
discipline which deals with them applying such approaches. Medicinal chemistry had
been marginally interested in structures, syntheses and partially structure-activity relationships
of some selected classes of excipients like preservatives, colorants and
sweeteners and appropriate chapters in older textbooks of medicinal chemistry had
been also devoted to them but increasing number of chemical drugs crowded out
stepwisely these topics. Indeed, neither any of these above mentioned nor other discipline
offers a comprehensive view to chemical structures, synthetic ways and typical
analytical procedures of these compounds. It is in contradiction to the fact that most
of modern pharmacopeias have for excipients the same requierements on purity as
for active ingredients. Chemistry of pharmaceutical excipients could be a discipline
capable to fill out this blank and build a bridge between pharmaceutics on one side and medicinal chemistry together with pharmaceutical analysis on another one. It will also
have a small overlap with margins of pharmacognosy in fields of natural sweeteners,
dyes and antioxidants. - Learning outcomes
- A student will capable after passing the subject:
-to know main groups of pharmaceutical excipients from the point of view of both function and chemical structure
-to know structures and important propreties of several main representatives of each group
-to distinguish between excipients with a quatifiable activity and without it
-to know and describe quantities which are possible to use for such a activity quantification
-to know and express syntheses and mechanisms of activity of selected excipients - Syllabus
- The topics of 6 two hours lectures are as follows:
1. Circumscription of the concept of pharmaceutical excipients. Their fundamental
division from the points of view of their usage and structure. Compounds
at the border between drugs and excipients.
2. Compounds enhancing the disintegration of tablets. Stabilizers of physico-chemical
properties of dispersion systems: viscosity-increasing, emulsifying and suspending
agents. Oligo- and polysaccharides and their semisynthetic derivatives.
(Starch, alkylated starches, cellulose, cellulose ethers and esters,
cyclodextrines). Specific methods of their pharmacopeial analysis including
applications of NMR spectroscopy. (Determination of substitution grade of
hydroxypropylbetadex, i.e. hydroxypropyl- alpha-cyclodextrine according to European
and Czech pharmacopeias.
3. Stabilizers of chemical composition of medicinal preparations: antioxidants
(inorganic and organic compounds suitable for either hydrophilic or hydrophobic media), antimicrobial and antifungal preservatives (organic compounds
containing heavy metals in their molecules, phenolic compounds including a
homologic series of parabens (nipagins), carboxylic acids, quarternary ammonium
salts, aldehydes and their precursors). Dependence of activity of
preservatives on pH. Structure-activity relationships including selected QSAR regression models, syntheses of principal compounds.
4. Selected compounds controling bioavailability of drugs. Transdermal, buccal
and gastro-intestinal penetration enhancers. (Percutaneous permeation
accelerants, which have been beeing most widely studied, are accentuated.)
Overview of basic structural groups, proposed and particularly evidenced
mechanisms of their actions, special demands of enhancers used in topical
application forms, methods of determination and quantitative expression of
their activity.
5. Compounds triming taste and flavour of medicinal preparations.
Sweeteners of natural origin: carbohydrates, alcoholic sugars, glycosides useful
as sweeteners. Alternate sweeteners: basic structural types, their toxicity,
syntheses of some principal compounds. Quantitative expression of sweetening ability, its relationship to structure. Volatile compounds of both natural and
synthetic origin suitable as odour regulating agents.
6. Colour corrigents: pharmaceutical dyes and colouring agents. Specific methods of analysis of colour substances. Quantitative description of a colour in
CIE L*a*b* system and similar systems according to USP Chapter 1061,
"Color ? instrumental measurement."3) Overview of approved dyes of both
natural and synthetic origin, their toxicity, lipohilicity and spectral properties
(absorption extremes). Structure-colour relationships of anthocyanines.
The topics of two 4-hours sections of laboratory are as follows:
1. Synthesis of an antimicrobial preservative ? paraben with longer and/or branched
alkyl chain. (Alternative: synthesis of an artificial sweetener ? sacharine.)
2. Analysis of pharmaceutical colorants. Quantitative description of a colour in
CIE L*a*b* system and evaluation of purity and
homogenity of colour substances (for better exploitation of time, the work on
both topics overlaps).
- The topics of 6 two hours lectures are as follows:
- Literature
- required literature
- Rowe R. et al. Handbook of pharmaceutical excipients. London, 2005. info
- Teaching methods
- Lectures, seminar devoted to QSAR or similar calculations, or a single practical class or more such classes devoted to the analysis of substituted polysaccharides.
- Assessment methods
- Written quiz.
- Language of instruction
- English
- Further comments (probably available only in Czech)
- Study Materials
The course can also be completed outside the examination period. - Teacher's information
- Attendance in all practical classes, passing of syntheses products on, processing of all topics of practical classes in the form of laboratory reports ("protocols"), knowledge of the contents of lectures.
- Enrolment Statistics (Spring 2022, recent)
- Permalink: https://is.muni.cz/course/pharm/spring2022/FACF1_15