1. free of defects

2. good mechanical strength

3.  easy to divide dose: grooved/scored

4.  stable:  chemically and physically stable

5.  reproducible:  good content uniformity

6.  predictable release charcteristics

1. systemic or local

2. sugar coated sct

3. multiple compressed mct

4. film coated fct

5. enteric coated ec

6. orally disintegrating

7. extended release er

1.  sublingual

2. buccal

3. lozenges

stick it next to the gumline

1.  progesterone/testosterone

candy w/medicine

1. pastilles:  molded

2.  troches:  compressed

1.  effervescent:  mask taste, buffering pH

2.  hypodermic:  parental use

1.  vaginal

2.  implantable

3.  diagnostic

1.  accurate dosing

2.  lower cost to mass produce

3.  compact

4.  stable

1.  mostly inflexible dose:  except scored tablets

2.  can be difficult to swallow

3.  less effective than liquid dosage forms bc of lag time to dissolve

4.  composition could change physical form

place on tongue and swallow w/a glass of water

- water is important bc without it, tablet can lodge in esophagus and may cause ulceration

- patients w/gastro esophageal reflux must take w/water and avoid reclining for 1 hour

1. diluents

2. binders and adhesives

3.  disintegrants

4. lubricants

5.  antiadherents

6. glidants

7. colors and dyes

8. flavorants and sweetners

9. adsorbents

- increasing compression gives a harder tablet

- increasing compression increases disintegration time

- increasing disintegrant decreases disintegration time

- reduce friction during the tablet compression process

- are lipophilic compounds

insoluble form of dyes

- dyes adhered to aluminum hydroxide

crystalline form

particle size and segregation

moisture content

crystalline forms

polymorphisms can affect

solubility

dissolution

absorption

DSC machine: differential scanning colorimeter

- studies how much degredation is taking place

- interaction = signifcant degredation, much change excipient (one melting point in the middle)

- no interaction = no degredation, we can use excipient (2 different melting points)

molded

compressed

no longer molded actually "extrude"

- make dough and then extrude through press

(like making pasta noodles)

Steps in tablet manufacturing

(each step in process is unit operation)

1. weighing:  wet/dry/dc

2. particle size reduction:  wet/dry/dc 

3. blending: wet/dry/dc

4. wetting and dough formation: wet

5. extruding: wet

6. drying: wet

7. screen: wet/dry

8. lubricant: wet/dry/dc

9. compression: wet/dry/dc

1. grind drug:  reduce particle size

2. blend:  w/diluents, distinegrants, binders

3. agglomerate: add liquid to make dough

4. pellet: press it though a mesh and get pellets

5. dry: dry pellets in oven

6. screen: filter out uniform size

7. blend: add lubricant to help w/flow properties of granules

8. compress: into a tablet

dry granulation

(slugging)

1. grind: reduce particle size

2. blend: w/diluents, disintegrants, binders

3. slugging & compacting: get a pellet

4. crush: get granules

5. screen: weed out uniform granules

6. blend: add lubricant to help w/flow properties of granules

7. compress: into a tablet

direct compression

1. grind

2. blend: w/diluents, disintegrants, binders

- adjuvants: di-tab + others

- avicel: microcrystalline cellulose

3. compress

di-tab

+

others

punchs and dies

process

1. lower punch drops down

2. allows powder to fill cavity

3. feed shoe moves powder

4. upper feeds compress powder into tablet

5. upper punch withdrawals

6. lower punch compresses

single punch

(makes #)

rotary punch

(makes #)

spherical

shallow

standard

deep

flat face

caplete

flat face bevel edge

oval

modified ball

tablets are prepared by forcing wet titurate in to a mold to form the tablets

- usually use volatile solvent that will evaporate

- don't use on a commercial scale

1. compression coating

2. sugar coating

3. film to protect or delay release

4. enteric coating

5. gelatin coating

6. chocolate or colored coating

1. load tablet into tablet coater

2. pan rotate

3. spray solution w/warm air to coat tablet

4. allow solvent suck out via exhaust

5. polish to shine

mutliple compressed tablet

tablets made by more than one compression cycle

- layered tablets

- compression coated tablets

1. weight variation

2. thickness

3. content uniformity (85-115% strength)

4. dissolution: specific time, found in monographs (USP guidlines)

5. disintegration: solid dosage forms will break into smaller particles

- uncoated: 30 minutes

- coated: up to 2 hours

6. stability: up to 2 years or more

7. hardness:  retain during manufacturing and S&H

- proportional to compaction pressure

(increase pressure = increase harndess)

8. friability: tablets roll and fall, spin fall apparatus test

- determine weight loss-indication of integrity during handling

1. disintegration

2. disintegration of granules

3. dissolution of primary drug particles

4. solvated molecules

5. move into systems

Noyes-Whitney Equation

for dissolution rate

dC/dt = kS(Cs - Ct)

k is dissolution constant

S is surface area of dissolved drug

Cs is saturaton conc. of the drug

Ct is conc. of drug in dissolution medium at time t.

- increasing force of pack = increases hardess

- increasing amount of lubricant = longer to dissolve

1. cellulose

2. lactose

3. mannitol

4. starch

1. starch

2. acacia

3. sodium alginate

4. cellose

5. pvp

(polyvinylpyrrolidine)

1. starch

2. alginates

3. pvp

(polyvinylpyrrolidine)

4. cellulose

diluent

binder

disintegrant

diluent

binder

disintegrant

binder

(sodium alginate)

disintegrant

pvp

(polyvinylpyrrolidone)

binder

disintegrant

1. talc

2. stearic acid salts (Na, Mg)

3. surfactants (lipophilic, brig)

4. waxes

1. magnesium oxide

2. bentonite

3. silicon dioxide

1. lactose

2. sucrose

3. dextrose

4. mannitol

5. kaolin

6. precipitate chalk