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30 Cards in this Set

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Dissolution Tests
Dissolution tests measure the rate and extent of the drug in the tablet to go into solution

Particularly important test for drugs with limited water solubility (where dissolution is RLS for absorption)
Rotating basket method
The tablet is placed inside a stainless steel wire basket, which
is rotated at a fixed speed while immersed in a dissolution
medium (at body temperature) contained in a cylindrical
vessel.
Paddle method
Allow the dosage to sink to the bottom of the vessel.
Agitate the dissolution medium
Why are basic drugs dissolved in 0.1 N HCl?
Protonation/dissolution in the stomach
Why are acidic drugs dissolved in pH 7 buffer?
Deprotinated/ionized in small intestine
What is the dissolution /edium for neutral drugs
Water
What do you want to avoid when swallowing an oral tablet/capsule?
Esophageal Adhesion
What can you do to help avoid esophageal adhesion?
Wetting capsules with water or saliva can help swallowing. (sofens shell)

Do not crush or chew enteric coated tablets

Maintain dissolution stability by storing tablets under proper conditions
How do you maintain dissolution stability with storage conditions?
Maintain ability to dissolve by keeping medication tightly sealed and away from high heat and humidity.
Why can esophageal adhesions be dangerous?
following adhesion, drug will dissolve there. Decrease in water causes an increase in concentration, irritation, inflammation, and ulceration.
What drugs are dangerous if involved in esophageal adhesion?
Aspirin
NSAIDS
Tetracyclines
ferrous sulfate
KCl
Factors predisposing to adhesions
shape
size
surface properties
patient position - supine then inc risk
vol of water - if none, inc risk
disease
Best way to take medications
Take while standing. Take with a glassful of water and at least one hour before bedtime.
Other types of tablets
1. Buccal/Sublingual
2. Lozenges and Troches
3. Chewable
4. Vaginal inserts
5. Effervescent
6. Fast-dissolving
How are lozenges and troches intended to dissolve?
Intended to dissolve slowly (e.g., 30 minutes) in the mouth, usually for a local effect

Ex - for thrush
How are lozenges prepared?
Prepared and formulated like hard candy
How are troches made?
Compressed into a hard disc
Chewable tablet disintegration
Pleasant tasting and designed to disintegrate smoothly in the mouth
How are chewable tablets prepared?
By wet granulation and without a disintegrant

Chewing takes the place of a disintegrant
What do chewable tablets usually have a lot of?
High mannitol or xylitol content and flavorants.

Gives cooling sensation in mouth
What are examples of chewable tablets?
Vitamins
Antacids
Antibiotics
How are Effervescent Tablets prepared?
Prepared by compressing the drug with effervescent salt mixtures (e.g., sodium bicarbonate and citric
acid)

CO2 released
How are effervescent tablets designed to be dissolved?
In liquids prior to ingestion
An example of effervescent tablets
Effervescent KCl
How are fast-dissolving tablets designed to disintegrate?
Disintegrate rapidly and smoothly in the mouth before swallowing

Less than one minute
Claims for fast-dissolving tablets
Easier to take and swallow - typically no H2O needed but see label

Possible faster onset of action , but often not true
Why is the faster onset of action not always true for fast-dissolve tabs?
Drug dissolution can be rate limiting.

Drug particles may be coated
Methods of formulation and and manufacture of fast-dissolving tabs in the US
Different methods are used to produce tablets that imbibe in water very quickly.

1. Lyophilization
2. Direct compression w/ special disintegrants
Lyophilization
Freeze Drying
Leaves a very porous product

Sponge-like, tablets usually brittle, special packaging/handeling b/c they are hygroscopic
Direct compression with disintegrants
"Superdisintegrants"
Very hydrophilic and effervescent disintegrating

The CO2 released helps disintegration

Tablets must be well protected