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30 Cards in this Set
- Front
- Back
Dissolution Tests
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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) |
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Rotating basket method
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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. |
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Paddle method
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Allow the dosage to sink to the bottom of the vessel.
Agitate the dissolution medium |
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Why are basic drugs dissolved in 0.1 N HCl?
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Protonation/dissolution in the stomach
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Why are acidic drugs dissolved in pH 7 buffer?
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Deprotinated/ionized in small intestine
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What is the dissolution /edium for neutral drugs
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Water
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What do you want to avoid when swallowing an oral tablet/capsule?
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Esophageal Adhesion
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What can you do to help avoid esophageal adhesion?
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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 |
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How do you maintain dissolution stability with storage conditions?
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Maintain ability to dissolve by keeping medication tightly sealed and away from high heat and humidity.
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Why can esophageal adhesions be dangerous?
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following adhesion, drug will dissolve there. Decrease in water causes an increase in concentration, irritation, inflammation, and ulceration.
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What drugs are dangerous if involved in esophageal adhesion?
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Aspirin
NSAIDS Tetracyclines ferrous sulfate KCl |
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Factors predisposing to adhesions
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shape
size surface properties patient position - supine then inc risk vol of water - if none, inc risk disease |
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Best way to take medications
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Take while standing. Take with a glassful of water and at least one hour before bedtime.
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Other types of tablets
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1. Buccal/Sublingual
2. Lozenges and Troches 3. Chewable 4. Vaginal inserts 5. Effervescent 6. Fast-dissolving |
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How are lozenges and troches intended to dissolve?
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Intended to dissolve slowly (e.g., 30 minutes) in the mouth, usually for a local effect
Ex - for thrush |
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How are lozenges prepared?
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Prepared and formulated like hard candy
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How are troches made?
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Compressed into a hard disc
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Chewable tablet disintegration
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Pleasant tasting and designed to disintegrate smoothly in the mouth
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How are chewable tablets prepared?
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By wet granulation and without a disintegrant
Chewing takes the place of a disintegrant |
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What do chewable tablets usually have a lot of?
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High mannitol or xylitol content and flavorants.
Gives cooling sensation in mouth |
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What are examples of chewable tablets?
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Vitamins
Antacids Antibiotics |
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How are Effervescent Tablets prepared?
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Prepared by compressing the drug with effervescent salt mixtures (e.g., sodium bicarbonate and citric
acid) CO2 released |
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How are effervescent tablets designed to be dissolved?
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In liquids prior to ingestion
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An example of effervescent tablets
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Effervescent KCl
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How are fast-dissolving tablets designed to disintegrate?
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Disintegrate rapidly and smoothly in the mouth before swallowing
Less than one minute |
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Claims for fast-dissolving tablets
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Easier to take and swallow - typically no H2O needed but see label
Possible faster onset of action , but often not true |
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Why is the faster onset of action not always true for fast-dissolve tabs?
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Drug dissolution can be rate limiting.
Drug particles may be coated |
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Methods of formulation and and manufacture of fast-dissolving tabs in the US
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Different methods are used to produce tablets that imbibe in water very quickly.
1. Lyophilization 2. Direct compression w/ special disintegrants |
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Lyophilization
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Freeze Drying
Leaves a very porous product Sponge-like, tablets usually brittle, special packaging/handeling b/c they are hygroscopic |
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Direct compression with disintegrants
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"Superdisintegrants"
Very hydrophilic and effervescent disintegrating The CO2 released helps disintegration Tablets must be well protected |