IR (Immediate Release Tablets) - Lecture 5-6

The degree to which patient correctly follows medical advice

1. More economical - can make large commercial batches possible, and is also cheaper to manufacture
2. More stable- so longer shelf-life
3. Can be tailored to special needs (ie. controlled/modified release tablets) - enteric coating, protection for stability
4. Lots of resources available - technology and equipment, man power and expertise, raw material and packing material, contract manufacturing facilities

1. Immediate Release (IR)
2. Orally Disintegrating/Dispersable Tablet (ODT)
3. Chewable
4. Effervescent
5. Modified Release

In IR tablets, the drug is released quickly and completely in one shot. Must do multiple daily dosing!
Examples: acetominophen, aspirin tablets, ibuprofen

Tablet designed to disperse/disintegrate in the mouth or on tongue. Generally used for patients experiencing dysphasia (speech disorder) and compliance is an issue.
Example: donepezil for Alzheimers

Tablet often for ease of administration - pediatric (tablets suitable for children and infants) and also for quicker absorption.

These tablets are dispersed in water before administration. Often used for quick absorption and for ease of administration.

MR is designed to release medication in a predetermined manner and/or over an extended period of time.

The advantages include:
1) avoids peaks and troughs
2) less dosing frequency
3) patient compliance is improved

Categories of MR can be sub-divided into:
1) controlled release
2) sustained release
3) delayed release

Controlled release - these tablets are designed with a built-in mechanism where external conditions will not affect the tablet

Sustained release - prolonged release is generally not "zero order" and is often influenced by surrounding environment

Delayed release - tablet only will be released at a specific site (e.g. duodenum, colon). These tablets will often be enteric coated in order to avoid release in the stomach, since the stomach is highly acidic which can cause degradation. GI disturbance can also affect tablet if not enterically coated.

1) ER coated particles and beads
2) ER inert matrix
3) ER hydrophilic/eroding matrix
4) ER osmotic

Tablet must be disintegrated into granules, then be converted to fine particles through deaggregation. These particles can then be dissolved into solution and be absorbed.

1. The API (Drug) - the active pharmaceutical ingredient
2. Diluent - "inert filler to provide the properties of flow, necessary bulk, and compression properties to granules (e.g. lactose, microcrystalline cellulose, starch, dicalcium phosphate)
3. Binder - provides necessary adhesion of powders into granules to allow flow (e.g starch, methyl cellulose, povidone) - can also act as disintegrants when wetted
4. Disintegrant - makes tablet mass into smaller particles
-also superintegrants - more powerful and are crosslinked polymers
5. Lubricant - reduces friction during compression. Generally the LAST stop in tablet processing before compression. (e.g magnesium stearate, stearic acid)
6. Glidant - improves flow property
7. Film Coating - for protection
8. Polishing Agent - for attractive look
9. Opacifying agent - for opaque property

Most important is #1-5

1. Single stroke (punch) (R&D)
2. Rotary

There are multiple stations in the rotary tablet compression cycle. Each station has a set of die, upper, and lower punch. The steps are fill, compress, and eject. Filling involves the fill cam, weight-adjustment pull down cam, feed frame, and wipe off blade. Compression involves the pre-compression and compression cycles. Ejection involves the upper and lower cam, and ejector knob.

1. Dispensing (which includes milling, sieving, and weighing).
2. Granulation (multiple types)
3. Compression of tablets
4. Film coating
5. Packaging