Pharmaceutics I - Exam 3

Powders can be defined as

intimate mixtures of dry, finely divided drugs or chemicals

What is the size of particles?

0.1 mcg to 10,000 mcg

Chartulae can be defined as

divided powder sachets

Insufflated powders can be defined as

finely divided powders that are intended for application in a body cavity

What are the 5 advantages of powders?

1. Stable
2. Dose flexibility
3. Can be incorporated into other dosage forms
4. Easy to store and transport
5. No disintegration step

What are the 4 desired powder properties for topical use?

1. finely divided
2. uniform size
3. non-irritating
4. free flowing

What are the 2 desired powder properties for internal use?

1. uniform particle size
2. uniform rate of dissolution

What equation is the dissolution rate dependent on?

Noyes-Whitney equation

How does the sieve number and particle size relate?

smaller sieve number = coarser particles

Hw does d50 sieve opening and particle size relate?

larger d50 sieve opening = coarser particles

Comminution can be defined as

the process of particle size reduction

What are 3 methods used for comminution?

1. trituration
2. pulverization
3. levigation

What are the 3 tools used for comminution?

1. ball mills
2. grinders
3. coffee mills

Trituration can be defined as

grinding together of 2 or more substances in a mortar to intimately mix them and reduce particle size

Pulverization can be defined as

Dissolving a compound in a volatile solvent and then letting the solvent evaporate leaving finely dividing particles

Levigation can be defined as

process of reducing the particle size of a solid by triturating it in a mortar or spatulating it with a small amount of a liquid in which the solid is not soluble

What 5 techniques are used to blend powders?

1. spatulation
2. trituration
3. sifting
4. tumbling
5. geometric dilution

What are diluents in topical bulk powder?

1. starch
2. talc

Are diluents used for topical bulk powder?

Yes

Are diluents used for internal bulk powder?

Not usually

What diluents are used for internal use bulk powder?

1. magnesium carbonate
2. magnesium oxide
3. calcium carbonate
4. starch
5. lactose

What is different about labeling topical or internal use bulk powder?

In topical, the concentration is used to express the amount of active ingredient.
In internal use, the weight of active ingredient per volume to be ingested is used.

What are the 3 ways to incorporate liquids into powder?

1. Absorb into an inert carrier material and then add with geometric dilution
2. Pasty materials can be added by mixing it with increased quantities until it dries out
3. High potency or flavoring can be mixed with alcohol and then sprayed in a fine mist over powder

How should bulk oral powders be packaged?

in glass, metal, or other containers with a wide mouth

How should topical powders be packaged?

in sifter-top containers or powder shakers

How should insufflations be packaged?

into plastic puffer units

What is the BUD of powders?

6 months or 25% with manufactured product

What are the 5 important characteristics of powders?

1. size
2. shape
3. density
4. electrostatic charge
5. adhering or repelling properties

Eutectics can be defined as

powders that become sticky or pasty or liquefy when mixed together

What are 4 common eutectics?

1. aspirin
2. lidocaine
3. menthol
4. salicylic acid

How should eutectics be blended?

triturated very lightly on a pill tile

Hygroscopic powders can be defined as

solid drugs or chemicals that absorb moisture from the air

Deliquescent powders can be defined as

hygroscopic drugs that absorb enough moisture to dissolve and form a solution

How do you dispense/store hygroscopic or deliquescent powders?

1. tight containers
2. desiccant packet
3. store in dry place
4. dilute with drying powder

Efflorescent powders can be defined as

drugs or chemicals containing water of hydration that may be released when the powders are manipulated or are stored under conditions of low relative humidity

Effervescent salts can be defined as

Granules or powders; when dissolved in water; they effervesce and release carbon dioxide

Explosive mixtures can be defined as

Powder combinations that may react
violently when mixed together

Granules can be defined as

a small compact particle of a substance.

Powder agglomerates can be defined as

irregular shape, larger size, powder particles

What are 5 advantages of granules?

1. flow better than powders
2. improve content uniformity
3. increase ease of wetting
4. increase compressibility
5. decrease caking

Tablet can be defined as

a mixture of active substances and excipients in powder, granule or crystalline form, pressed or compacted into a solid

What are 5 advantages of tablets?

1. Accurate dose
2. Stable
3. Convenient
4. Taste masking
5. Drug release flexibility

What the 3 disadvantages of tablets?

1. Degradation is necessary
2. Systemic distribution
3. Swallowing difficulty

What are the 2 main types of tablets?

1. Molded
2. Compressed

What are the 11 types of compressed tablets?

1. Immediate release
2. Delayed release
3. Multiple compressed
4. Sugar coated
5. Film coated
6. Gelatin coated
7. Enteric coated
8. Buccal/sublingual
9. Chewable
10. Effervescent
11. Lozenge
12. Melt extrusion

What is a tablet composed of?

1. Drug substance
2. Excipient
3. Diluent/Filler
3. Binder
4. Lubricant
5. Glidant
6. Disintegrant
7. Compression Enhancer
8. Colorant
9. Flavorant/Sweetner

How much of a tablet is typically binder?

4-6%

How much of a tablet is typically lubricant?

0.5-1%

How much of a tablet is typically glidant?

How much of a tablet is typically disintegrant?

3-6%

How much of a tablet is typically compression enhancer?

15-25%

How much of a tablet is typically colorant, flavor, sweetener?

What is a common filler?

lactose monohydrate

Binder can be defined as

Polymer to form granules and improve tablet compaction

What are 3 common binders?

1. Providone (PVP)
2. HPC
3. PEG

Lubricant is used for

reduces adhesion to tooling

What are 2 common lubricants?

1. Magnesium stearate
2. Talc

Glidant can be used for

Improve flow properties

When is glidant added?

before compression

What are 2 common glidants?

1. colloidal silicon dioxide
2. talc

What are the 2 types of disintegrants?

1. Starch
2. Superdisintegrants

How much of a tablet is typically starch disintegrant?

1-5%

How much of a tablet is typically superdisintegrant?

2-4%

How does starch help with disintegration?

Swells in water

What are 4 common superdisintegrants?

1. sodium starch glycolate
2. croscarmellose sodium
3. crospovidone
4. CO2

What is a common common enhancer?

microcrystalline cellulose

What material is dry granulation used for?

good for materials prone to degradation by moisture or temperature

In wet or dry granulation does the active or diluent have to have cohesive properties?

dry

What are good candidates for direct compression?

1. Potassium salts
2. Ammonium chloride
3. Methenamine

S7 tool steel can be defined as

shock resistant, air hardening tool steel, designed for high impact. won't chip

What is the weight of a large tablet?

>800 mg

What 6 things are tablets evaluated on?

1. Appearance
2. Color
3. Odor
4. Thickness
5. Hardness
6. Friability

What variation is allowed for thickness of tablets?

~5%

How is hardness measured?

by applying force to the radial axis until it breaks

What is the required hardness of oral tablets?

4-8 kg

What is the required hardness of chewable tablets?

3 kg

What is the required hardness of a modified release tablet?

10-20 kg

What are the 6 common tablet defects?

1. Picking and Sticking
2. Capping and Lamination
3. Orange Peel
4. Erosion
5. Bridging
6. Roughness

Picking and Sticking is caused by

tablet punches during compression

Capping and Lamination is due to

excessive compression force

Orange peel is due to

Excessive drying during film coating

Erosion is due to

soft tablets

Roughness is due to

excessive drying during film coating

Bridging is due to

insufficient flow during film coating

Friability can be defined as

a tablet's ability to withstand abrasion during packaging, handling, and shipment

How much weight loss is permissible during friability test?

1% or less

Uniformity of Dosage units can be defined as

the degree of uniformity in the amount of drug substance among dosage units

What 2 methods are used to demonstrate uniformity of dosage units?

1. Weight variation
2. Content uniformity

When is Weight Variation used?

Applied when 25 mg or more that comprises 25% or more by weight of the dosage form

What are the steps of Weight Variation?

Select at least 30 dosage units, weigh 10 units, use assay results assuming homogenous distribution

What are the steps of content uniformity?

1. Select at least 30 dosage units
2. Assay 10 units individually
3. Calculate acceptance value
4. If 1 unit is outside of +/- 15% test 20 additional units.
5. If more than 1 unit is outside of +/- 15% or 1 unit is outside of +/- 25% then dose fails

Tablet -> granule/aggregate =

disintegration

Granule/aggregate -> Fine particle =

disaggregation

Tablet -> drug in solution =

dissolution

Granule/aggregate -> drug in solution =

dissolution

Fine particle -> drug in solution =

dissolution

Disintegration can be defined as

the breakdown of a tablet into smaller particles

Disintegration test can be defined as

test where dry dosage is placed in basket rack assembly and shaken within a set time and temperature

How many cycles per minute in a disintegration test?

29-32

What is the temperature of the disintegration test?

35-39 degrees C