Part 5 Flashcards
What are 4 measures of the level of bioequivalence
-pharmaceutical equivalents
-pharmaceutical alternatives
-biological equivalents (bioequivalents)
-therapeutic equivalents
What are pharmaceutical equivalents
Drug products are considered to be equivalents if they contain the same active ingredient and are identical in strength or concentrations, dosage form, and route of administration
What are pharmaceutical alternatives
pharmaceutical alternatives are those drug products that contain the same therapeutic components, but are different salts, esters, or complexes of that moeity, OR are different dosages or strengths
What are biological equivalents (bioequivalents)
bioequivalents ARE PHARMACEUTICAL EQUIVALENTS that exhibit comparable bioavailability when studied under similar experimental conditions
what are therapeutic equivalents
therapeutic equivalents are pharmaceutical equivalents that can be expected to have the same clinical effect when administered to patients under the conditions specified in the label
Bioequivalence means equivalence of bioavailability of two or more ____ (or _____) of the same drug.
If the products have similar bioavailability when tested under similar conditions, they are considered ________
bioequivalence means equivalence of bioavailability of 2 or more PRODUCTS (or dosage forms) of the SAME DRUG
bioequivalent
What is evaluated to determine if 2 different products or dosage forms of the same drug are bioequivalent?
the parameters of bioavailability are evaluated for bioequivalence
(Cmax, Tmax, and AUC)
100mg Ibuprofen and 100mg salt ibuprofen – what is the term for these
these are pharmaceutical alternatives because they contain the same therapeutic moiety but are different salts of that moeity
Explain the starting steps of conducting a bioequivalence study
-a panel of 24 or more subjects is used
-usually HEALTHY subjects are selected
-subjects should be a similar age and weight
-all subjects are evaluated by a physician to assure they are suitable for participation in the study
Is a bioequivalence study blinded?
yes —- it is double blinded.
Neither the researcher nor the subject knows what product is being given to the subject
Explain how a double blinded bioequivalence study is conducted
-the subjects are divided into 2 groups. All subjects receive both products, but one product at a time.
-blood samples are collected at predetermined times and the concentration of drug in each blood sample is determined.
- a washout period is used (baseline) to assure that the 1st product is virtually eliminated from the body before the 2nd product is administered
(DOUBLE BLIND)
Explain how the results of a bioequivalence study are analyzed
-the data is analyzed by an IMPARTIAL researcher or agency to avoid bias
-Average plasma-drug concentration vs time for each product is plotted
-Cmax, Tmax, and AUC for both products is determined.
-these 3 parameters are compared to determine bioequivalence
What are 2 ways to control the plasma profile
-formulation
-administration (dosage form?)
Oral
mouth
Peroral
gastrointestinal tract via mouth
sublingual
under the tongue
parenteral
other than the gastrointestinal tract (by injection)
intravenous
vein
Intra-arterial
artery
intracardiac
heart
intraspinal/intrathecal
spine
intraosseous
bone
intra-articular
joint
intrasynovial
joint fluid area
intracutaneous/intradermal
skin
subcutaneous
beneath the skin
intramuscular
muscle
epicutaneous (topical)
skin surface
transdermal
skin surface
conjunctival
conjunctiva
intraocular
eye
intranasal
nose
aural
ear
intrarespiratory
lung
Name the dosage forms available for nitroglycerin
-sublingual
-buccal
-oral
-ointment
-transdermal infusion system
What dosage form has the fastest onset time
IV/SL (also buccal!)
between the dosage forms of nitroglycerin, which has the longest duration and the slowest onset of action?
transdermal infusion system
Name some advantages of the oral route of administration
-natural
-uncomplicated
-convenient
-safe
name some disadvantages of the oral route of administration
slow drug response (parenteral is much faster)
irregular absorption (food, stomach acid, enzymes)
What is the purpose of enteric coating on tablets
to prevent the drug from being released into the stomach. instead, it dissolves in the intestines. This allows the tablet to safely pass through the acidic environment of the stomach, where certain drugs may be destroyed
Tablets are formed by ___ or _____
compression or molding
What are diluents in oral tablets?
diluents are fillers that are used to prepare tablets of the proper size and consistency
What are disintegrants in oral tablets
used for the break up of compressed ingredients in the tablet. this ensures prompt exposure of drug particles to the dissolution process, ENHANCING DRUG ABSORPTION
Besides enteric coatings, what is the use of other coatings on oral tablets
to protect the tablet against moisture, light, and air destruction during storage, OR to conceal the bitter taste from the taste buds of a patient
Which absorbs faster — capsules or tablets?
capsules
The shell of a capsule is hard or soft, usually composed of ______
gelatin
capsules vary in size from ___ to ___.
Which is the largest size
000-5
000 being the largest size
What are caplets
capsule-shaped and coated tablets
capsules are a __ dosage form
solid
In suspensions, the the drug particles must be ___ in the vehicle
INSOLUBLE
What is a major advantage of suspensions over tablets and capsules
-a large dosage of the drug can be administered. easier to adjust the dose of a suspension rather than a tab or cap
-absorption is faster in suspensions because the particles are readily available for dissolution
(HIGH DISSOLUTION RATE)
therefore, higher bioavailability
Which has the largest surface area – tablet, capsule or suspension? what does this mean?
suspension
therefore, suspensions have the highest dissolution rate and thus the highest bioavailabilty
Why are solutions absorbed much more rapidly than those administered in solid form?
because disintegration and dissolution are not required
What are elixirs?
solutions sweetened by a hydroalcoholic vehicle
What are syrups?
type of solution which use a sucrose solution as the sweet vehicle, resulting in a viscous solution
what are magmas
very viscous
Powders are similar to suspensions in that….
its easy to adjust the dosage
what is the alimentary tract
another name for GI tract
