pharm 125 - tablets

_____ are solid dosage forms where the drug substance is blended with excipients and compressed into final dosage

tablets

T/F some tablets may have poor bioavailability and cause local irritation

T (class IV)

What does BCS stand for?

Biopharmaceutics Classification System

A drug from BCS Class 1 has

high solubility, high permeability

A drug from BCS Class 2 has

low solubility, high permeability

T/F the low solubility of Class II drugs is the rate limiting step

T

What can you add to Class II drugs to improve solubility?

reduce particle size

salt formation

solid dispersion

complexation

lipid formulation

What is the criteria for low solubility for BCS?

highest dose given cannot be dissolved in 250mL H2O

What is the criteria for low permeability for BCS?

< 85% bioavailability

A drug from BCS Class 3 has

high solubility, low permeability

What could you add to Class III drugs to improve permeability?

permeation enhancers, prodrugs, bioadhesives

A drug from BCS Class 4 has

low solubility, low permeability

Compressed tablets are formed by the application of high pressure to _____ or _______

powders, granules

Name the tablet type:

simplest form, no coating

uncoated

Name the tablet type:

compressed tablet surrounded by sugar coating

sugar-coated tablets (SCT)

Name the tablet type:

compressed tablet covered with a thin layer or film of polymeric substance

film-coated tablets (FCT)

T/F sugar coated tablets are the first choice for formulators

F, FCTs are first choice

Name the tablet type:

Compressed tablet coated with substance that resist dissolution in gastric fluid, but disintegrates in the intestine

delayed-release (DRT) or enteric-coated tablets (ECT)

When would you use an enteric-coated tablet?

Want tablet to resist gastric acids but disintegrate in the intestine

Name the tablet type:

compressed tablet made by more than one compression cycle

multiple compressed tablets (MCTs)

When are multiple compressed tablets (MCT) used?

1. need to separate API for stability purposes

2. mixing is inadequate for guaranteeing uniform distribution

Name the tablet type:

prepared by compressing additional tablet granulation on a previously compressed granulation

layered tablet (type of MCT)

Name the tablet type:

prepared by feeding previously compressed tablets into a special tableting machine and compressing another granulation layer around the performed tablets

press-coated tablets (type of MCT)

Name the tablet type:

tablets with API and a mix of sodium bicarbonate and an organic acid (tartaric or citric acid)

effervescent tablets

Effervescent tablets are a mix of ______ and _______

citric acid/tartaric acid, sodium bicarbonate

When effervescent tablets dissolve, they liberate CO2 which acts as a ________

disintegrator

Do chewable tablets require a disintegrant?

No, they disintegrate when chewed

To be classified as a rapid dissolving tablet (RDT) or orally disintegrating tablet (ODT), the tablet must disintegrate in _____

30s (FDA)

T/F RDTs or ODTs require little or no H2O for administration and can be prepared through freeze drying

T

Buccal tablets are placed in the side of the _____ and dissolve/erode ______

cheek, slowly

Sublingual tablets are placed under the ______ and dissolve _____

tongue, fast

T/F buccal and sublingual tablets undergo first pass metabolism

F

Group ___ excipients help to impart satisfactory processing and compressing characteristics to the formulation

1

Group ___ excipients help to give additional desirable physical characteristics to the finished tablet

2

Diluents fall into group __ excipients

1

What is the purpose of a diluent or filler?

increase bulk and tablet size

What type of excipient is lactose?

diluent

What type of excipient is starch?

diluent

What type of excipient is dicalcium phosphate?

diluent

Starch can be used as a diluent, _______, and ________

binder, disintegrant

What type of excipients are dextrose, sucrose, mannitol, and sorbitol?

diluent, sweetener

Binders fall into group __ excipients

1

What are binders for?

ensure tablet remained intact after compression

Too much binder can lead to ____

disintegration

Too little binder can lead to _____

tablet falling apart

What type of excipient is starch paste?

binder

What type of excipient is polyvinylpyrrolidone (PVP)?

binder

What type of excipient is gelatin?

binder

What type of excipient are cellulose derivatives?

binder

__________ are excipients that prevent adhesion of the tablet to the surface of dies/punches

lubricants

Lubricants fall into group ___ excipients

2

The most common lubricants are _____ such as ________ _______

hydrophobic, Mg stearate

In the mixing process, lubricants are added _____

last

What type of excipient is calcium stearate?

lubricant

What type of excipient is stearic acid?

lubricant

What type of excipient is colloidal silica?

lubricant

What type of excipient is Talc?

lubricant, glidant

What type of excipient is sodium benzoate?

H2O soluble lubricant

What type of excipient is SLS?

lubricant, surfactant

Can hydrophobic lubricants (ex: stearates) interfere with disintegration and dissolution?

yes

_____ are excipients that improve flow characteristics of powder mixtures by reducing interparticulate friction

glidants

Glidants fall into group ___ excipients

2

The most common glidant is

colloidal silicon dioxide (SiO)

_______ are excipients that are added to facilitate tablet breaking or disintegration after administration

disintegrants

The following are examples of?

starch, microcrystalline cellulose, crospovidone

facilitated H2O uptake

How do facilitated H2O uptake disintegrants work?

transport liquid into tablet pores to help break it into fragments

The following are examples of?

sodium starch glycolate, croscarmellose sodium crospovidone, pregelatinized starch

disintegrants that work by swelling, AKA super-disintegrants

Disintegrants are added before ______ and during ________

granulation, lubrication

The most common method for adding colour to tablet formulation involves dissolving the die in _______ _______ prior to ________

binding solution, granulation

For shinier and brighter colour, you should add colouring agents during the ______ step

coating

______ are excipients that absorb moisture or fluids in formulations

sorbents

What is the most common tablet preparation method?

wet granulation

The main process for wet granulation is

forming solid bridges (binding) between granules

Name the tablet manufacturing process described below:

1. premix drugs and excipients

2. add granulating liquid

3. screen the wet mass through a sieve

4. dry the wet granules using a fluid bed dryer

5. mill/sieve dried granules

6. add lubricant

7. compress into tablets

wet granulation

What are two methods to achieve dry granulation?

1. slugging - prep large tablet then mill

2. roller compaction - powder pressed between rollers then ground

Describe the steps for direct compression for tablet manufacturing.

blend/mix ingredients then compress

What is wet massing?

step in wet granulation, process of using liquid binder to lightly agglomerate the powder mixture

T/F wet massing should only be carried out by low shear mixers/granulators

F, can be carried in other machines such as high shear mixers

Can fluid-bed granulators carry out wet massing?

Yes, can be coupled with drying

Can spray dryers carry out wet massing?

yes

Can extruders and spheronizers carry out wet massing?

yes

When using a fluid-bed granulator, at what rate will small/friable granules be dried? What about larger/controlled granules?

small, friable = rapid

larger = slow

Can you use spray dryers for heat-sensitive granule production?

yes

Extruders and spheronizers produce _____ and _____ pellets with a smooth surface and narrow size distribution

dense, spherical

T/F extruders and spheronizers are used for dry granulation

F

T/F extruders and spheronizers make granules for immediate drug release

F, controlled drug release

T/F extruders and spheronizers create large particles

F

The following steps describe which machine:

1. dry mixing

2. wet massing

3. extrusion

4. spheronization

5. drying

6. screening

extruder and spheronizer

Extrusion produces _____ shaped particles and spheronization produces _____ shaped particles

cylindrical, spherical

In the wet granulation process, when can extrusion and spheronization be performed?

after wet massing, before drying

What kind of granulation is used for moisture or thermal sensitive drugs?

dry granulation

In dry granulation, is slugging or roller compaction more commonly used?

roller compaction

______ is when fine powder is compressed into sheets then granulated to form uniform sized granules. it is a part of _________

roller compaction, dry granulation

Compared to wet granulation, dry granulation has _____ steps

fewer

T/F direct compression is more expensive as it requires special excipients

T

Between wet and dry granulation, which one produces the softer tablets?

dry, no solid bridges form

Who invented the tablet machine?

William Brockendon

Tablet machine components:

_______ stores the material for compressing

hopper

Tablet machine components:

_______ distributes materials into the dies

feed frame

Tablet machine components:

_______ controls the size and shape of the tablet

dies