Pharmaceutical ApplicationTablets and Capsules

Yoshiko Katori

CE457_527

Colloid and Surface Phenomena

Spring 2004

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

Mouth

Stomach

Small Intestine

• Ingest tablets or capsules from the mouth

• Dissolve in the stomach or the small intestine

• Absorb into the blood stream via small intestines

• Go through the entire body• It only works where the pain is.

Tablets and Capsules

• Tablets• Regular • Chewable• Dissolvable in water

• Capsules• Hard capsules• Soft capsules

www.aspirin.com, www.advil.com

Tablets

1-10%Binder(Polyvinilpyrrolidone)

0.1-20%Surfactant(SDS, Pluronic)

Active substance

Manufacture ProcessTablets

http://www.dekker.com

Filling

Punch

Die

Compression

Punch

Ejection

Tablet

coating

Hard Capsule

30%Gelatin

65%Water

5%Dye

0.1-0.5%1-2%

Surfactants(sodium docusateSodium lauryl sulfate)

Speed up DissolutionBy increasing the wetting of powder

Manufacture ProcessHard Capsules

Dipped into gelatin solution Dried Stripped off Combined

http://www.rjengineering.com

Filling is a separate process.

Soft capsule

40-45%Gelatin

20-30%Water

5%Dye

30-35%PlasticizerPropylene glycol, sorbitol, glycerin

Manufacture ProcessSoft Capsules

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

1. Gelatin Ribbon2. Rotary die3. Filling capsule4. Filled capsule5. Webbing6. Pumping mechanism

Comparison

YesYesYesEasy to swallow

GoodGoodPoorBioavailability

CostlyCostlyCheapPrice

StableLess impurities

Brittle or get stickyhumidity control required

Relatively stable

Stability

Not adaptable to incorporate mixtures

Easy to have mixtures

Layers possible

Fill

Soft CapsulesHard CapsulesTablets

Applications

Controlled Drug Delivery SystemSolvent controlled

Push Layer

Barrier Layer

Drug solution

Hard Capsule

Rate Controlling Membrane

Delivery orifice

Controlled Drug Delivery SystemSolvent controlled

Inner Layer

Osmotic Layer

Rate controlling Membrane

Delivery orifice

Soft gelatin Capsule

Liquid drug formulation

Rate controlling membrane:semi-permeable homopolymer, copolymer or polymer blend

Push layer: Expandable hydrophilic polymerpoly(hydroxyl-alkyl methyl methacrylates)Poly(vinyl pyrrolidone), poly(vinyl alcohol) etc.

Examples of Delivery Profiles possible with OROS® technology

Delivery Profiles

Delayed Drug Release

For pH sensitive drug

Enteric coating

•Not deliver drug in the stomach

• Absorb in the small intestine

PlaceboTime delayed by placeboAdsorbed in the small intestine

placebo

Capsules for Vegetarians

HPMCHydroxypropylmethyl cellulose

• 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

Mad-cow disease FearReligiousPersonal preference