Tablets

Question 1

Definition of pills and tablets?

Answer 1

-Pills: Small, round, solid dosage forms for oral administration, a generic term for tablets and capsules, but pharmaceutically incorrect

-Tablets: solid drug delivery system containing a medicinal substance made by compression or molding

-Compressed tablets are manufactured, molded can be manufactured or compounded

Question 2

How long does it take to release the drug in compressed tablets?

Answer 2

designed to release the drug immediately (rapidly) after ingestion, within 15-30 minutes

Question 3

Why are tablets sometimes multiple compressed?

Answer 3

-multiple drugs that are physically not compatible (compress Granulate 1 than Granulate 2)
-1 layer with IR drug and 1 layer with delayed release

Question 4

What are compressed-coated tablets?

Answer 4

-Tablet within a tablet -> core tablet coated with another tablet

-the coat may be another drug or the coat can delay the release of the drug
-> so the patient does not need to take multiple tablets

Question 5

What are CAPLETs?

Answer 5

Capsule-shaped tablets, film or gelatin-coated for easy swallowing

Question 6

Difference between Brand name and Generics?

Answer 6

-No difference in active drug, strength, and dosage
-Insurance: Generics are usually covered, for Brand, covered when there is no generic form

-Price: The brand is more expensive
-Inactive ingredients: may differ but both are approved by FDA

WHENEVER it’s GENERIC it may show: Compare to..

Question 7

What are the different localization of administration for compressed tablets?

Answer 7

-Buccal: often flat and oval to stick in the cheek or buccal pouch
erode slowly, used for local effect (some may go into the system), fungi, or delivering anesthetics

-Lozenges: effect on the oral cavity, they do not erode but slowly dissolve like candy, also include systemic absorption through the cheek or bc of added liquids

-Sublingual: under the tongue, e.g. nitroglycerin

-chewable tablets: rapidly dissolved after chewing, larger doses for children and adults with difficulties with swallowing

-fast dissolving: have superdistntergrant
-Effervescent: contain granular effervescent salts (citric acid and base) that produce gas (carbon dioxide takes care of acidity)

Question 8

Why does sublingual dissolve quickly?

Answer 8

-under the tongue, dissolve rapidly (bc of super disintegrant)and avoids first-pass effect because absorption
e.g. nitroglycerin dissolves rapidly to prevent heart attack in the emergency

Question 9

What is the benefit of Aspirin in an Effervescent form?

Answer 9

The emerging carbon dioxide pushes the aspirin faster (an thereby gets absorbed earlier) into the intestine bc ASPIRIN is gastro irritating and should not stay long in the stomach

Question 10

What is the difference between IR and modified release tablets?

Answer 10

-IR: Release the drug in 15-30 minutes with peaks in concentration and quick drop

-modified release: Release the drug slower and steadier into
the bloodstream reaches pick and goes down slowly

Question 11

What are molded tablets (tablet triturated)

Answer 11

-Soft and designed for rapid dissolution, cylindrical in shape
-Mostly diluent (lactose and sucrose) and a moistening
agent (alcohol and water

-Triturated with API -> make a paste -> Spread paste in mold, allow to dry and punch out with pegboard

Question 12

Why are tables coated?

Answer 12

-Drug protection from oxygen, light, and moisture
-Taste masking (glycerin)
-easier to swallow
-easier to identify

Question 13

What are the types of coating?

Answer 13

-Film coating (thin)
-Gelatin coating: makes it smooth to swallow easy
-Sugar coating
-Enteric coating/ delayed release

Question 14

Properties of Film-coated tablets:

Answer 14

-Thin layer of a polymer (celluloses) and quickly rupture

-provide protection from the external environment or create a modified-release drug delivery system

Question 15

Purpose and problem of sugar coating:

Answer 15

-Mostly for taste masking and it dissolves quickly, but the weight of the tablet increase by 50%

Question 16

What are the benefits of enteric coated/delayed-release tablets?

Answer 16

-Bypass the stomach bc of pH that will degrade the drug + GI irritation -> the coating is resistant to the low pH

-delayed-release: dissolve in the small intestine where it gets absorbed

Question 17

What are the process steps in manufacturing tablets?

Answer 17

API + excipient -> mix and form granules -> DRY -> Compress (apply pressure) -> Coating -> Packaging

Question 18

What is direct compression?

Answer 18

Drugs with good flow and compression properties are mixed with direct compressible excipients - NO GRANULES

-it is fast bc direct, but it is costly bc compressible excipients are expensive

Question 19

What is wet granulation?

Answer 19

Drugs and excipient mix are converted into granules with a liquid binder (starch) and passed through a sieve -> Lubricants (reduce friction) are added -> Compression

Question 20

What is the purpose of dry granulation?

Answer 20

Drugs sensitive to water would degrade when adding a binder
-> make it in a dry form -NO BINDER,
-but compress it to form a big slug tablets -> break it and pass it through a sieve and compress it again

Question 21

What are the manufacturing defects of Capping and Lamination?

Answer 21

-Capping: breaks into two layers
-Lamination: into multiple layers

Reason: not enough binder, not enough lubricant, too dry, puncher and die are worn out, too much pressure

Question 22

What are the manufacturing defects of Picking and Sticking?

Answer 22

Picking: Stuck on punches (maybe bc of engraving of punch)

Sticking: adheres (stuck) on die (maybe cs of ejection issue)

Reason: too much binder, not dry enough, not enough lubricant

Question 23

How does tablet coating work?

Answer 23

tablets are in a rotator, and the coating solution is spray on the tablet

Question 24

What defects can occur in tablet coating?

Answer 24

-Blistering
-Chipping: a piece of the coated surface is chipped off, mostly on the edge

-Picking: sticking to punches or pan
-Orange peel effect: a rough surface that can be easily peeled off like an orange
-Mottling: uneven distribution of color

-Bridging: coating comes off where the monogram is imprinted

Question 25

What is the purpose of excipients?

Answer 25

-Safety and efficacy
-Stability and bioavailability
-Assist in manufacture
-Color

Question 26

What is the largest part in a compressed tablet?

Answer 26

Active drug and diluent (filler)
-> active drug may be lower when the drug more potent

Question 27

What are Diluents (Fillers)?

Answer 27

Function: add bulk, more cohesion, uniformity, more flow
Types: Organic and Inorganic; Water soluble and Insoluble
Examples: Lactose, Mannitol, Sorbitol, Cellulose products, calcium carbonate

Question 28

What are Binders?

Answer 28

Function: convert powder to granules, and promote cohesiveness, some may have direct compression properties

Types: Natural or synthetic/semisynthetic

Examples: Cellulose, Gelatin, Gums, Liquids, Starch, combinations (sugar-starch)

Question 29

What are disintegrants?

Answer 29

-Induce break-up in aqueous solution, it has an affinity for water -> absorb water -> swell and burst = DISINTEGRATION

Example: corn and potato starch (starch can be a binder and disintegrant)
Superdesintegrants: sodium starch glycolate, povidone

Question 30

Explain wetting agents/surfactants:
needed for OILY and lipophilic drugs

Answer 30

-consists of a polar head (towards the water) and a non-polar tail (towards the drug) -> forms micelles with the drug so the nonpolar part of the drug is trapped -> able to dissolve in micelles

wetting agent: improves the spread of water around particles
surfactant: decrease surface tension at the interface

Examples:
-nonionic surfactants: Spans and Tweens, SLS, SDS

Question 31

What are Lubricants?

Answer 31

-reduce friction by forming a layer between the tablet and the die wall -> to prevent sticking to punches
-hydrophobic -> they retard the solubility of the drug -> low concentration
-added last

Examples: Magnesium stearate, stearic acid, zinc stearate

Question 32

What are Glidants?

Answer 32

-Forms a layer around granules, preventing they stick together -> improves the flow of granules and prevents sticking to punches

Examples: Cornstarch (can also be Binder and Lubricant, Talc, often a silicate

Question 33

What types of sweeteners are added to tablets?

Answer 33

Natural: dextrose, stevia (not for diabetic patients)
Artificial: saccharin, aspartame, anhydrous citric acid (mask bitter taste)

Question 34

What are the requirements for tablets?

Answer 34

-Tablet weight and weight variation: must be in a range +/- 10 %
-Content uniformity: 9 of 10 should be in +/-15%
-Thickness: +/- 5%
-Hardness: measuring breaking force (4 to 10 kg)
-Friability: Stress-test -> 0.8% or less
-Tablet disintegration: has to disintegrate in a specific time (30min) at 37°C
-Tablet dissolution: sample and see how much of the drug has dissolved after some time

Question 35

What are the best practices for splitting according to the FDA?

Answer 35

-if sit is approved to be splittable it is found in the HOW SUPPLIED section
-don’t split and store tablets
-not all tablets are suitable to be split with the splitter
-when the brand is changed ensure that it is still splittable

Question 36

What are the reasons for recalls?

Answer 36

-Contamination with carcinogens
-Packaging error
-Labeling error

Question 37

Role of pharmacist in case of recall?

Answer 37

-continue taking meds until health care provide replaces it
-quarantine the affected lots
-if possible replace with a different manufacturer