Pharmaceutical Application Tablets and Capsules

CE457_527 Colloid and Surface Phenomena Spring 2004

Yoshiko Katori

Overview
Introduction Tablets and capsules Composition and Manufacture Process Applications

Tablets and Capsules

Pharmaceutical market over $280 billion Supplements market $17.7 billions

http://www.concerta.net

How the medicine works

Ingest tablets or capsules from the mouth Mouth Dissolve in the stomach or the small intestine Absorb into the blood stream via small intestines Stomach Go through the entire body It only works where the pain is.
Small Intestine

Tablets and Capsules

Tablets Regular Chewable Dissolvable in water Capsules Hard capsules Soft capsules
www.aspirin.com, www.advil.com

Tablets
Active substance Surfactant (SDS, Pluronic) Binder
(Polyvinilpyrrolidone)

0.1-20% 1-10%

Manufacture Process Tablets

Punch Die Punch Tablet

Filling

Compression

Ejection

coating

http://www.dekker.com

Hard Capsule
Gelatin Water Dye Surfactants (sodium docusate
Sodium lauryl sulfate)

30% 65% 5% 0.1-0.5% 1-2%

Speed up Dissolution By increasing the wetting of powder

Manufacture Process Hard Capsules

Dipped into gelatin solution

Dried

Stripped off

Combined

Filling is a separate process.

http://www.rjengineering.com

Soft capsule
Gelatin Water Dye Plasticizer
Propylene glycol, sorbitol, glycerin

40-45% 20-30% 5% 30-35%

Manufacture Process Soft Capsules

1. 2. 3. 4. 5. 6.

Gelatin Ribbon Rotary die Filling capsule Filled capsule Webbing Pumping mechanism

http://www.asojsoftcaps.com/technology.htm

Comparison
Tablets Easy to swallow Price Bioavailability Stability Yes Cheap Poor Relatively stable Layers possible Hard Capsules Yes Costly Good Brittle or get sticky humidity control required Easy to have mixtures Soft Capsules Yes Costly Good Stable Less impurities Not adaptable to incorporate mixtures

Fill

Applications

Controlled Drug Delivery System Solvent controlled

Delivery orifice Rate Controlling Membrane Hard Capsule Drug solution Barrier Layer Push Layer

Controlled Drug Delivery System Solvent controlled

Delivery orifice Rate controlling Membrane Osmotic Layer Inner Layer Liquid drug formulation Soft gelatin Capsule

Rate controlling membrane: semi-permeable homopolymer, copolymer or polymer blend Push layer: Expandable hydrophilic polymer poly(hydroxyl-alkyl methyl methacrylates) Poly(vinyl pyrrolidone), poly(vinyl alcohol) etc.

Delivery Profiles

Examples of Delivery Profiles possible with OROS technology

Delayed Drug Release

For pH sensitive drug Enteric coating Not deliver drug in the stomach Absorb in the small intestine

placebo Placebo Time delayed by placebo Adsorbed in the small intestine

Capsules for Vegetarians

Mad-cow disease Fear Religious Personal preference Non-animal origin Odorless, tasteless Low moisture content Resists physical changes at low humidity Excellent dissolution Chemically stable Resistant to cross-linking Three-year shelf life

HPMC
Hydroxypropylmethyl cellulose