Formulation of Tablets
Session 16: Formulation of Tablets
Total Session Time: 120 minutes
Pre-requisites
Learning Tasks
By the end of this session students are expected to be able to:
Resources Needed:
SESSION OVERVIEW
|Step |Time |Activity/ |Content |
| | |Method | |
|1 |05 minutes|Presentation |Introduction, Learning Tasks |
|2 |30 minutes|Presentation |Formulation of Tablets |
|3 |25 minutes|Buzzing |Ingredients used in Tablet Production |
| | |Presentation | |
|4 |50 minutes|Presentation |Classification, Properties and Roles of |
| | | |Excipients |
|5 |05 minutes|Presentation |Key Points |
|6 |05 minutes|Presentation |Evaluation |
SESSION CONTENTS
STEP 1: Presentation of Session Title and Learning Tasks (5 minutes)
READ or ASK students to read the learning tasks and clarify
ASK students if they have any questions before continuing
STEP 1: Formulation of Tablets (30 minutes)
ingredient(s) (APIs) and excipients are combined to produce a tablet
o The type and amounts of each ingredient i.e. the medicament(s) and the
excipients are known prior to manufacturing process
o Formulation must ensure that the dosage form formed is stable
acceptable to the patient who will use it
o In formulation the variety of ingredients used (including the drug
itself) must be compatible with each other
o Therefore it is very important to do a lot of formulation studies in
order to detect the point of compatibility
o Formulation studies must focus on other factors like particle size,
polymorphism, pH and solubility, in order to check whether these
factors will effect on bioavailability of the drug or not
o Oral formulations such as tablets and capsules must be formulated in
such as way to ensure that they release the drug(s) in a constant and
predictable manner
o A formula for tablet production
o A formally authorized Master Formula Record or Master Production
Record should exist for each product and batch size to be manufactured
quantities and packaging materials, together with a description of
the procedures and precautions required to produce a specific
quantity of a finished product as well as the processing
instructions including the in-process controls
STEP 2: Ingredients Used in Tablet Production (25 minutes)
o Active Pharmaceutical Ingredients (APIs)
diclofenac, amoxicillin etc.
action upon administration of the tablet
o Excipients/Pharmaceutical aids
improving the quality of the tablets or facilitating
manufacturing process
|Activity: Small Group Discussion ( 10 minutes) |
| |
|DIVIDE students into small manageable groups |
| |
|ASK students to discuss on the following question |
|What are the functions of excipients in tablets? |
| |
|ALLOW students to discuss for 10 minutes |
| |
|ALLOW few groups to present and the rest to add points not mentioned |
| |
|CLARIFY and SUMMARIZE by using the contents below |
o Impart weight, accuracy and volume
o Ensure accuracy of the dose
o Improve solubility
o Increase stability
o Enhance bioavailability
o Modify drug release pattern
o Assist product identification
o Increase patient acceptability
o Facilitate dosage form design
STEP 5: Classification, Properties and Roles of Excipients (50 minutes)
o Diluents/filler/bulking agents
o Binders and adhesives
o Disintegrants
o Lubricants and glidants
o Colouring agents
o Flavouring agents
o Sweetening agents
o Adsorbent
o They are fillers and make required bulk when the drug(s) is/are not
adequate to make the bulk
o They also help improve cohesion and permit use of direct compression
manufacturing or to promote flow
o Some commonly used diluents are Microcrystalline cellulose, Mannitol,
Dextrose, Sorbitol, Lactose anhydrous and Starch
o Diluents should have the following properties;
combination with the drug(s)
o They are materials added to form granules or to form cohesive compacts
for directly compressed tablets
o Binders are classified into two groups
gelatin
(PEG)
o Some commonly used binders are acacia, tragacanth, cellulose
derivatives (methyl cellulose, hydroxymethyl cellulose, hydroxyproply
cellulose), gelatine, glucose, polyvinyl pyrolidone (PVP), starch,
sodium alginate, sorbitol
o Are materials added in tablet formulation to facilitate its breaking
down when it contacts water in the gastrointestinal tract
o They are added before granulation and before compression
o Some commonly used disintegrants include starch; starch derivatives
(e.g. primogel); clays e.g. veegum, bentonite; cellulose; cellulose
derivatives e.g. sodium carboxymethyl cellulose; alginate and
polyvinyl pyrolidone cross-linked
o Super disintegrants
contacting water
linked cellulose), crospovidone, sodium starch glycolate
o Lubricants
when introduced as a film between solid surfaces
dies and punches thereby reducing interparticle friction
(e.g. magenisum stearate), talc, polyethylene glycol (PEG),
surfactants
o Glidants
flow
e.g. colloidal silica
o These are colours and dyes used for;
distinctive appearance to the tablets
o All colouring agents must be approved and certified by competent
authority e.g. TFDA
o These excipients are added in solution or in dry form
o Two classes of colouring agents are used in tablet production
cosmetics)
o Commonly colouring agents used in tablet production are white, sunset
yellow, tartrazine, fast green, brilliant blue, erythrosine and indigo
carmine
o Ideal characteristics of colouring agents
quantities are used
and microorganisms i.e. stable on storage
cosmetics i.e. FD and C colouring agents
o Flavouring agents
o Sweetening agents
–sweeter than sugar, has one disadvantage –bitter after taste and
carcinogenic; aspartame (artificial) –not stable in presence of
moisture
STEP 4: Key Points (5 minutes)
ingredient(s) (APIs) and excipients are combined to produce a tablet
acceptable to the patient who will use it
pharmaceutical ingredient(s) and the excipients
adhesives, disintegrants, lubricants and glidants, colouring agents,
flavouring agents and sweetening agents
STEP 5: Evaluation (5 minutes)
References
Aulton M.E & Kevin M.G, Eds: (2013) Pharmaceutics: The design and
manufacture of medicines, (4th ed.) Churchill Livingstone
Handbook of pharmaceutical excipients, Edition sixth, Edited by Raymond
Crow, Paul J Shekey and Marian E. Quinn, Publisher –Pharmaceutical
Press
Hugo and Russell (2011), Pharmaceutical Microbiology (8th ed.), Willey-
Blackwel publications
Gennaro, R. A, et al. (Eds) (1995) Remington: The Science and Practice of
Pharmacy, Volume I & II, (19th ed.): Mack Publishing Company, Easton,
Pennsylvania 18042
Liebsch, B et al (1988): Tanzania Pharmaceutical Handbook, Dar es Salaam
University Press.
Lund, W. Editor (1994). The Pharmaceutical Codex, Principles and Practice
of Pharmaceutics (12th ed.): The Pharmaceutical Press, London
Polderman, J (1990) Introduction to Pharmaceutical Production: Novib, The
Hague
Rawlins E.A, Editor: (1977) Bentley’s Textbook of Pharmaceutics, (8th ed.)
Baillie're Tindall. London Kamm, G. and Kohler, B. Editors: (1995)
Manual for Decentralized Infusion Production, Infusion Unit Project
Tanzania
Schmidt, O. (ed) (2000) Pharmaceutical Quality systems, Interpharm Press,
Colorado.
Shayne C et al (2008), Pharmaceutical Manufacturing Handbook: Production
and processes, John Wiley & Sons
Watson, D. G (1999) Pharmaceutical Analysis: A Textbook for Pharmacy
Students and Pharmaceutical Chemists: Churchill Livingstone,
Edinburgh.
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