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Summary Tablet formulation

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Industrial pharmacy - 2nd semester Includes bullet points, key diagrams and images

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  • June 8, 2023
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  • 2019/2020
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Tablet Formulation

Conventional Compressed Tablets

 Rapid disintegration and release of drug in GIT
 Compression of granules or powder

Multiple Compressed Tablets

 Multiple layered formulation- light compression of drug powder/granules to
form layer. Next layer is formed by compressing mixture on top of previous layer
 Multiple compressed formulation- light compression of first drug layer. Tablet is
added to mix of second powder and then compressed so encasing the first tablet
 Drugs may be incompatible so separate layers used
 API can be delivered at different rates to different sites in GIT
 Mask taste or prevent degradation in stomach

Enteric Coated

 Polymer coating that dissolve under alkaline pH but not acidic
 Protection against degradation or prevent irritation
 Polymer dissolves in lower intestine which releases drug
 Cellulose acetate/phthalate/butyrate- esters that dissolve at above pH 6
 Hydroxypropylmethyl cellulose succinate/acetate- esters which dissolve in the
intestine
 Methacrylic acid copolymer (Eudragit)- ethyl/methyl/butyl/dimethylamino
methacrylate
 Eudragit L100- poly(methycrylate- co-methylacrylate) in a 1:1 molar ratio is
soluble at above pH 5.5
 Eudrgait S100- poly(methycrylate- co-methylacrylate) in a 1:2 molar ratio is
soluble from pH 7




Sugar Coated Tablets

 Compressed tablets coated in >50% sugar solution
 Masks bitter taste of API

Film Coated Tablets

 Can target different parts of GIT with polymer composition
 Polymers are insoluble so drug diffuses through
 Are soluble at some pHs
 Hydroxypropylmethylcellulose
 Hydroxypropylcellulose

,  Eudragit E100 co-polymer of butylmethacrylate, 2-
dimethylaminoethylmethacrylate and methylmethacrylate in a 1:2:1 molar ratio
 Are insoluble at all pHs
 Ethylcellulose
 Eudragit RL- ethylacrylate- co methyl methacrylate and co
triethylaminoethylmethacrylate chloride in a 1:2:0.2 molar ratio so is more
permeable than RS
 Same as RS but 1:2:0.1 molar ratio

Chewable Tablets

 For people who have trouble swallowing
 If tablet is too large

Effervescent Tablets

 Rapidly disintegrate forming a solution or suspension
 Reaction between citric acid and sodium bicarbonate
 API is rapidly absorbed
 Need moisture free packaging

Buccal and Sublingual Tablets

 Slowly dissolve into systemic circulation
 Avoids first pass metabolism

Manufacturing Tablets

 Wet granulation
 Dry granulation
 Direct compression
 Roller compaction (chilsonation)
 Choice dependant on: compression properties of API, particle size, types of
excipients and chemical stability
 General steps: mixing API with excipients, granulation of mixed powder, mixing
of powder with other excipients and compression of powder into tablet




Diluent/fillers

 Increases the mass of the tablet
 Must have good compression properties

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