Lecture 6+7: Tablets

Question 1

immediate-release tablets

Answer 1

-release meds with no rate-control

Question 2

extended release tablets

Answer 2

-release meds over extended period

Question 3

rapidly disintegrating or dissolving tablets

Answer 3

-disintegrate in mouth within 1 min, some within 10 secs

Question 4

Tablet manufacturing processes

Answer 4

-wet granulation
-dry granulation
-direct compression

Question 5

direct compression

Answer 5

-tablet manufacturing process
-less steps
-no granulation
-GOOD flowability, content uniformity, and compressiblity

Question 6

Tablet manufacturing processes:

Answer 6

1. die filling
2. tablet compression
3. tablet ejection

Question 7

Excipients for tablets

Answer 7

-diluents/fillers
-binders
-disintegrants
-glidants
-lubricants
-Mg stearate, talc, sodium stearyl fumarate

Question 8

Diluents/fillers

Answer 8

-add bulk to formulation for size
-lactose, mannitol, starch

Question 9

binders

Answer 9

-promote adhesion of particles
-allow granulation to be prepared and maintain integrity of the final tablet
-water, alcohol, starch paste, sucrose syrup, PVP, MCC

Question 10

more binder in tablets leads to

Answer 10

-harder tablets
-slower disintegration time
-slower dissolution rate

Question 11

disintegrants

Answer 11

-promote breakup of tablets after administration to smaller particles for ready drug availability
-starch, cellulose derivatives

Question 12

Glidants

Answer 12

-enhance flow of material into the tablet dies
-collodial silicone dioxide, talc

Question 13

Lubricants

Answer 13

-prevent fill material from sticking to punches and dies
-decrease adhesion, friction, and punch/die wear
-Mg stearate, talc, sodium stearyl fumarate

Question 14

Negativve effects of over-lubrication with Mg stearate

Answer 14

-reduce tablet hardness or tensile strength
-slow dissolution due to hydrophobic nature of Mg stearate
-some drugs incompatible with Mg stearate

Question 15

Tablet coating functions

Answer 15

-provide special traits of drug release (enteric coating)
-protect drug from environment
-mask taste
-improve swallowing
-identification

Question 16

Types of tablet coatings

Answer 16

-sugar
-film
-compression

Question 17

Sugar coating

Answer 17

-tablets with sugar layer
-water soluble
-dissolves quickly
-usually round and smooth
-like M&Ms (advil)
-enteric

Question 18

Cons of sugar coating

Answer 18

-multi steps: sealing, coating, smoothing, polishing
-time consuming
-need expertise
-increases tables size and weight up to 50%

Question 19

Film coating

Answer 19

-thin film of polymeric materials
-single stage
-better for controlled release
-breakable
-via spraying
-polymer in liquid eith pigments and plasticizers
-drying of liquid leaves film coating around tablet

Question 20

immdiate-release Film coating

Answer 20

-nonfunctional
-soluble in water

Question 21

modified release Film coating

Answer 21

-functional
-delayed release (enteric)(SOLUBLE only pH>5)
-extended release (NOT soluble in water)

Question 22

Film coating formation

Answer 22

-rapid solvent evaporation
-deposit and spreading of coating liquid droplets on tablets
=sticky residue
-coating polymers get more viscous as evaporation
-complete drying occurs slowly

Question 23

Film coating requirement

Answer 23

-liquid needs to be atomized into droplets
-tablets need good mixing and agitating (each tablet needs to pass thru spraying zone)
-hot air to evaporate solvent
-exhaust to remove dust and evaporated solvent

Question 24

Film coating formulations

Answer 24

-polymer
-plasticizer
-colorant
-solvent

Question 25

Polymer film coating formulation

Answer 25

-solubility determines selection for immediate/modified release -low viscosity desired -permeability masks taste, limits exposure to air, modifys release

Question 26

Polymer film coating mechanical properties

Answer 26

-film strength: resist mechanical stress -film flexibility: minimize cracking -film adhesion: ensure product integrity

Question 27

Polymer coatings for immediate release

Answer 27

-cellulose derivatives (HPMC) -vinyl derivatives (PVP and PVA)

Question 28

Polymer film coatings for modified release

Answer 28

-cellulose derivatives: EC, CA

Question 29

Plasticizer film coating formulation

Answer 29

-reduce brittleness -enhance flexibility of polymers -PEG, esters

Question 30

Colorant film coating formulation

Answer 30

-water soluble (dyes) and INsoluble (pigments) -insoluble better bc better stability, opacity, and covering power -iron oxide (red) -titanium dioxide (white)

Question 31

Solvent film coating formulation

Answer 31

-organic solvents better bc fast drying -meant for modified release that needs to be protected from environment

Question 32

Film coated products

Answer 32

-uniformity -NO visual or functional defects -compliant with specifications

Question 33

Coating defects

Answer 33

-bad uniformity -poor penetration -not enough passes thru spray zone -low mech strength -bad adhesion -surface too wet -color inhomogeneity -delamination/peeling

Question 34

Tablet Quality Control

Answer 34

-general appearance (size/shape/markings) -drug content and release (weight, disintegration, dissolution, stability, hardness, friability)

Question 35

Crushing strength

Answer 35

-tablet hardness -4-6kg

Question 36

friability

Answer 36

-tablet mass loss during drum rotating at 20 bpm for 100 roations -max weight loss < 1%

Question 37

Extended-release tablets

Answer 37

-allows reduction in dosing frequency from that necessitated by conventional dosage form

Question 38

Pros of extended release

Answer 38

-less fluctuation in blood levels -frequency reduction in dosing -enhanced convenience and compliance -reduction in adverse side effects

Question 39

Types of extended release dosage forms

Answer 39

-coated beads, granules, and microspheres -matrix tablets -osmotic pump tablets

Question 40

matrix tablets

Answer 40

-embed drug slowly in dissolving matrix with polymer HPMC as metrix material -tablet core and gel layer

Question 41

osmotic pump tablet

Answer 41

-semipermeable membrane -osmotic core with drug -water -delivery orifice

Question 42

Considerations of using modified-release

Answer 42

-do NOT crush or chew -NOT interchangable with immediate release version -some materials may not be dissolved = shows up in stool