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WorksheetsBiopharmaceutics and Pharmacokinetics
Total questions: 150
Worksheet time: 37hrs 16mins
The science that examines the inter-relationship of the physicochemical properties of the drug, the dosage form in which the drug is given, and the route of administration on drug’s bioavailability
Pharmacology
Biopharmaceutics
Toxicology
Pharmacokinetics
The branch of pharmacology that deals with disposition and fate of drug is
both
pharmacokinetics
pharmacodynamics
none
The application of pharmacokinetic principles in the safe and effective treatment of individual patients, and in the optimization of drug therapy
clinical pharmacy
clinical pharmacology
clinical pharmacokinetics
clinical biopharmaceutics
Is the application of pharmacokinetic principles to design, conduct, and interpretation of drug safety evaluation studies and in validating dose-related exposure in animals
Clinical pharmacokinetics
Clinical pharmacology
Clinical toxicokinetics
Clinical biochemistry
Which of the following statement is (are) correct?
pharmacodynamic parameters characterize the effects of a drug on the body
pharmacokinetic parameters describe the effects of the body on a drug
a receptor is that component of the body with which a drug interacts to produce its effects
none of the above
all of the above
The LADME system is employed in
the development of new active compounds
the development of new active compounds
the adjustment of dosage regimen
Is the delivery of the active ingredient from a dosage form into solution
Drug release
Absorption
Distribution
Metabolism
Excretion
Liberation as the first step, determines the following aspects;
onset of action
type of preparation
rate of absorption
bioavailability
Liberation is a process controlled by
age of the patient
characteristics of the drug
both
none of the above
Each statement below describes a characteristic of a particular route of drug administration. True statements include;
IV administration provides a rapid response
IM administration requires sterile technique
oral administration requires that the patient be alert
SC administration may cause local irritation
The IV route of administration may be preferred over the peroral route for some systemic-acting drugs because
the drug does not have to be absorbed
absorption is predictable and complete
a portion of the absorbed drug pass through the liver before entering the systemic circulation
first-pass effect is not avoided
Select the most appropriate route of drug administration for a 55-year old man who is brought to the emergency room with recurrent tonic-clonic seizures following a head injury
SC
rectal
oral
IV
inhalational
Select the most appropriate route of drug administration a 14 year-old boy who has type I diabetes mellitus and will be self-administering his insulin injections
rectal
SC
oral
sublingual
IV
What is the advantage of sublingual/buccal administration over peroral route of administration?
no occurrence of GI degradation
does not pass to the liver
drug is given directly in the circulation
The following is/are advantages of rectal route of administration except ;
alternate for patients having difficulty of swallowing drugs
a portion of the absorbed drug does not pass through the liver before entering the systemic circulation
absorption is predictable and complete
Drugs administered by inhalation are absorbed in the
small intestine
nasal mucosa
lungs
stomach
Micromeritics is;
he science of small particles
microscopic blood count method
a method of chemical analysis
an optical instrument
colorimetry
The smallest particle size approved by the FDA is ;
1-10 micro-meter
0-0.1 micro-meter
10-15 micro-meter
all
Which of the following methods is employed in promoting particle size reduction?
grinding
solid dispersion
levigation
milling
The process with the slowest rate constant in a system of simultaneous kinetic processes.
lag time
rate limiting step
bioequivalence
accumulation
A rate limiting factor in the dissolution of tablet is
disintegration of the tablet
thickness
content uniformity
local effect
Which of the following series in kinetic processes may be the rate-limiting step?
disintegration and dissolution of the unit
diffusion of active drug through the intestinal wall
dissolution of the active drug
disintegration only
The rate limiting step in bioavailability of a conventional compressed tablet or drugs that are poorly soluble in aqueous media is the rate of ;
disintegration of the drug
transport of the drug molecules across the
intestinal mucosal cells
dissolution of the drug
biotransformation of the drug by the liver prior to systemic absorption
If the particle size decreases;
dissolution rate increases
surface area increases
rate of diffusion decreases
all
The effect of reduced particle size of a drug is;
increased absorption
increased disintegration
increased hardness
all
Factors affecting dissolution rate to correlate with bioavailability;
particle size of the drug
presence of surfactant
patient acceptance
Which of the following physicochemical constants may be useful when predicting the solubility of a chemical;
pH of solution
pKa of the chemical
solubility parameters
valence of chemicals
dissolution rate
The equation that best describe the overall rate of drug dissolution
Henderson-Hasselbaclh equation
Michelis-Menten equation
Noyes-Whitney equation
Fick’s First Law of Difussion
Dissolution rate tests can be used to predict bioavailability if;
dissolved drug remains free in GIT
dissolved drug is decomposed in the GIT
drug is hydrolyzed in the GIT
all of them
Which of the following factors affect the dissolution in the lipid membrane of the lipoid soluble unionized fluid compartment ;
pH
pKa
lipid/water partition coefficient
Which of the following factor/s is inversely proportional to the rate of dissolution in the lipid membrane of lipoid soluble unionize substances?
particle size
lipid/water partition coefficient
surface area
diffusion coefficient
difference in drug concentration in two phases separated by a semipermeable membrane
Dissolution rate is increased by;
decreased in surface area
decrease in particle size
the formation of molecular aggregates
all
The ratio of drug concentration in the lipoid phase over the concentration of the drug in the aqueous phase is equal to
APC
pKa
pH
Concentration gradient
The partition coefficient can be considered as;
an index of the relative affinity of a drug for two immiscible solvents
an index of comparative solubilities in solvents
a parameter of the relative rate of partitioning from one phase into another
The lipid phase which is usually employed in the determination of apparent partition coefficient
water
corn oil
cottonseed oil
octanol
buffer solution at pH 7.4
With decreasing oil/water partition coefficient, the polarity of drug;
increases
decreases
no change
polarity is not related to solubility
The mathematical equation used in determining the ratio between ionized and unionized drug include;
Noyes whitney equation
Fick’s First Law of diffusion
Henderson Hasselbalck equation
none
The extent of ionization of a weak electrolyte drug is dependent on the
pH of the media and pKa of the drug
particle size and surface area of the drug
oil:water partition coefficient of the drug
Noyes Whitney equation of the drug
polymorphic form of the drug
pH is equal to pKa when the ionized form is
greater than unionized
less than unionized
neither greater or less than unionized
equal to unionized
A change of pH in the aqueous phase alters the of electrolytes.
degree of ionization
degree of dissociation
degree of acidification
degree of purification
The ionization constant of a drug is important in bioavailability since it determines the following ;
its aqueous solubility
dissolution rate
pH of the medium
extent of protein binding
Free acid and free bases are practically insoluble in water. Which of the following alkaloids exhibits good water solubility?
morphine SO4
cocaine
atropine
lidocaine
Most drugs are
strong electrolytes
non-electrolytes
weak electrolytes
highly ionic
None of the above, because many drugs are either weak acids or weak bases
Which of the following is a characteristic of weak electrolytes?
exist entirely as ions
exist both as ionic and a molecular form
exist entirely in molecular form
may be undissociated
Characteristics of salts of electrolytes include ;
higher solubility
more rapid dissolution rate
lower solubility
slow dissolution rate
Acids are _____ when deprotonated
charged
unionized
nonpolar
none
Significant site of absorption of many acidic and neutral compounds but not for basic compounds
kidney
stomach
liver
all
According to pH partition theory, a weakly acidic drug will most likely be absorbed from the stomach because
the drug will exist primarily in the unionized, more lipid soluble form
he drug will exist primarily in the ionized, more water-soluble form
weak acids are more soluble in acid medium
the ionic form of the drug facilitates dissolution
Weak acids are greatly unionized at
high pH
low pH
neutral pH
all
The excretion of weak acid will be more rapid in alkaline urine than in acidic urine because
all drugs are excreted in alkaline urine
he drug will exist primarily in the unionized form
he drug will exist primarily in the ionized form
weak acids cannot be reabsorbed from the kidney tubules
Weak acids are reabsorbed into the bloodstream when
the urinary pH is high
the urine is made alkaline
the urinary pH is low
all situations apply
Penicillin Na+ are greatly unionized at
high pH
low pH
neutral pH
all
Based on the relation between the degree of ionization and the gastric solubility of a weak acid, the drug aspirin (pKa 3.49) will be most soluble at
pH 1.0
pH 2.0
pH 3.0
pH 4.0
pH 6.0
The concentration of the ionic moiety of weak acids increases with
decreasing pH of aqueous solution
increasing pH of aqueous solution
increasing pOH of aqueous solution
all
Weak bases are greatly ionized at
high pH
low pH
neutral pH
all
Morphine sulfate will most likely be absorbed from the small intestine because
the molecular form will be more lipid soluble form
the drug will exist primarily in the ionized and more water soluble form
the drug will exist primarily in the ionized and more water soluble form
basic drugs are more lipid soluble in alkaline media
Alteration of urine pH can alter renal elimination of certain toxins. Which of the following toxicants may be safely eliminated by alkalinization of the urine?
phencyclidine
salicylates
amphetamines
all
Reasons for chemical variations
change the structure of the active compound in order to increase pharmacologic response
maintain the basic structure but change solubility by addition of either salts, ester, ethers, or complexes
both
none
Introduction of salts increases
lipophilic property
hydrophilic property
solubility in nonpolar solvents
none
Which condition usually increases the rate of drug dissolution from a tablet?
increase in the particle size of the drug
use of ionized, or salt, form of the drug
decrease in the surface area of the drug
use of free acid or free base form of the drug
use of sugar coating around the tablet
To generally increase the solubility of a poorly soluble drug in an aqueous medium, the process is
complexation
adsorption
prepare into a derivative
The ions of added electrolyte require water for hydration reducing the amount of water available for the solution of the non-electrolyte is the phenomenon of
salting in
salting out
clathrate formation
chelation
It is the phenomenon when organic substituted ammonium salts or salts of various inorganic acids are added to mixtures of organic non-electrolytes causing the dissolution of the undissolved solutes
chelation
clathrate formation
salvation
salting in
The resulting solid when a drug and polymer like PVP or PEG are dissolved in a solvent with the drug, then the solvent is evaporated
hydrates
co-precipitates
solid-in-solid solution
solvation
These are formed when a substance is capable of forming channels or cages which can take up another substance into the intraspace of the structure
co-precipitates
solvates
drug-clathrate complexes
hydrates
An agent that take up another substance into its intraspace structure is called
macromolecular carriers
hydrates
polymorphs
clathrate forming agents
Which of the following is a clathrate forming substance?
urea
mucin
melt of mannitol
theobroma oil
Polymorphism is generally defined as
substance that may exist in more than one crystalline form or amorphous form
substance that may exists only in metastable form
substance that has different viscosity time to time
substance that reduces interfacial tension
Polymorps exist only in
solid state
semisolid
liquid
gas
Different polymorphs of the same drug exhibit differences in all aspects;
chemical structure
melting points
solubilitie
molecular sizes
The following statements are true except
amorphous form is more soluble than that of the crystalline form
amorphous form has a higher dissolution rate than the crystalline form
crystalline form requires a higher amount of energy to free a molecule of the drug from it than does the amorphous form
amorphous form requires a higher amount of energy to free a drug molecule from it than does the crystalline form
Which of the following statements is correct?
polymorphism exist only in liquid state
penetration occurs if each molecule is bounded to the surface molecules
the most stable form of polymorphs are those with highest stability but with lowest dissolution rate
clathrate forming agents retard transition of polymorphs
Theobroma oil is an example of
amorphous form
metastable polymorph
stable polymorph
all
Which of the following crystal form gives the best dissolution rate?
meta-stable polymorph
amorphous
stable polymorph
Ability of chemical compound to exist as optically active stereoisomers or enantiomers is ;
polymorphism
chirality
chemical variation
chelation
The property of absorbing moisture from the atmosphere include
micronization
hygroscopicity
viscosity
ionization
Refers to a more comprehensive concept that includes the drug formulation and the dynamic interactions among the drug, its formulation matrix, its container, and the patient
Drug delivery system
Dosage form
Capsules
Tablets
The ultimate evaluation of dosage forms or delivery system is in
disintegration time
thickness
clinical effectiveness
taste
Are additives which are necessary in formulating a dosage form from the drug
Vehicle substances
Inert substances
Excipients
All
Those multiple source drug products that contain identical amount of the identical active ingredients in identical dose forms are called
chemical equivalents or pharmaceutical equivalents
biologic equivalents
therapeutic equivalents
pharmaceutical alternates
therapeutic alternates
The instability which could lead to the rejection of a drug product
problem of bioavailability
substantial changes in the appearance of the dosage forms
extensive chemical degradation of the active drug
all
Which of the following types of dosage form does not require dissolution prior to absorption
tablet
suspension
parenteral solutions
modified dosage form
capsules
The advantage of solid dosage form for administration is A. most stable B. faster dissolution C. faster disintegration D. faster absorption than other forms
most stable
faster dissolution
faster disintegration
faster absorption than other forms
A suspension is not a suitable dosage form for what type of injection?
ID
IM
IV
SC
Oral
The purpose of enteric coating of the tablets may be ;
protect the gastric mucosa from irritant drugs
protect the drug from action of gastric fluids
protect the patient from drug sensitization
A dosage form for which the drug release characteristics of time course and/or drug release location are chosen to accomplish therapeutic or convenience objectives
modified release dosage forms
sustained release dosage forms
conventional dosage forms
all
Dose dumping is defined as ;
an intended sudden release of large amounts of drugs into systemic circulation
unintended sudden release of large amounts of drugs into systemic circulation
slow release of the drug into systemic circulation
slow absorption of the drug into the systemic circulation
The controlled release dosage form is sometimes necessary for action of some drugs for the purpose of;
prolonging absorption of the drug itself
delay the absorption of the drug
for immediate action
That portion of a prolonged release dosage form which liberates the drug from the form at a slower rate that is unrestricted absorption rate
depot phase
release phase
dissolve phase
all
In general, various oral dosage forms can be ranked in which of the following expected order of availability (fastest to slowest)
aqueous solution, capsule, tablet, powder, coated tablet, suspension
capsule, tablet, coated tablet, powder, suspension, aqueous solution
aqueous solution, suspension, powder, capsule, tablet, coated tablet
suspension, aqueous solution, powder, capsule, coated tablet, tablet
Which of the following properties of surfactants tend to increase the rate of dissolution?
surface tension lowering effect
increased surface tension
absence of peptizing action
all
When non-polar substances are dissolved in polar solvent using surfactants, the process is called
HLB
Solubilization
Emulsification
Gelatinization
A disadvantage of some inert diluents for powders as a dosage form is
adsorbs onto the active drug substance
high cost
drugs may not be released immediately
Process of transferring chemical substances from the GIT through its wall into the blood and lymphatic stream
diffusion
adsorption
absorption
convective transport
Sorption is the collective term used to describe
Penetration
Adsorption
Permeation
disposition
Are substances that have no pharmacological properties of their own but can improve the penetration of drugs into the skin or mucosa
sorption promoters
solubilizing agents
binders
all
The following are the mechanisms by which drugs containing sorption promoters penetrate the skin
decrease viscosity of the medium
chelation of intercellular groups
chelation of intercellular groups
all
A second substance tends to accumulate to the surface of a first substance due to intermolecular forces of attraction is a phenomenon of
chemisorption
absorption
adsorption
all
Obtained when the drug product is administered at the site where the pharmacological response is desired and when the drug released from the product acts by absorption to the skin or mucosa or penetrates into the skin or mucosa, but does not enter the systemic circulation or lymphatic system
systemic effect
local effect
mean transit time
micro constants
The physical barrier to transport in the body
Carrier molecule
Inactive complex
Unit membrane
kahit alin na jan
The theory which states that cell membrane is made up of bi-lipid layers and fluid protein molecules interpersed between 2 layers of lipid layer
Fick’s law
Fluid Mosaic
Ariens and Stephenson
Stokes law
Membranes are responsible for which of the following processes;
Uptake of liquid material
Uptake of solid material
Extrusion of waste materials
for permeation and transport
ALL
Membrane potential is due to the;
Adsorption of protein to the outside of the lipid layer
Different distribution of ions in the extracellular and intracellular fluid
pH of the medium
Absorption is not involved when a drug is administered by which of the following routes
IV
intra- arterial
intraspinal
ALL
Drugs administered by buccal route are absorbed in the
small intestine
nasal mucosa
lungs
mouth cavity
stomach
Which of the following is the first process that must occur before a drug can become available for GI absorption from a tablet dosage form?
dissolution of the drug in the GI fluids
ionization of the drug
disintegration of the tablet
dissolution of the drug in the blood
adsorption of the drug on the mucosal surface of the skin
In general, the form of a drug that can be absorbed faster is ;
Ionized form
Unionized form
Bound form
Factors influencing absorption include/s;
total surface area available for absorption
contact time at the absorption surface
blood flow to the absorption site
ALL
The following are factors affecting GIT absorption, except
pKa value of the drug and pH of drug product
Perfusion rate
Osmotic pressure
None of the choices
Which of the following events modify drug absorption?
physiologic constituent of digestion
drug interaction
certain disease state
Due to their anatomical structure, the organ that is considered as the most important site of drug absorption is
large intestine
stomach
small intestine
mucous membrane of the mouth
rectum
Specific organ of the animal used for In vivo test of active transport mechanism
Duodenum
Ascending colon
Ileum
transverse colon
As soon as drug has passed the epithelium of the GI mucosa, it can reach the systemic circulation by;
Entering through the villi
Entering through the lacteals
Both
None
Factor affecting gastric emptying time of a drug
age of a person
time of the day
body posture
ALL
Rate of gastric emptying is slowed down by the following ;
Vigorous exercise
Fatty foods
Hot meals
Hunger
Emotional stress
A condition that may increase the time of gastric emptying is /are;
Depression
stressful
Lying on the right side
In the oral administration of drugs for aged people, the possible consequence/s when the gastric emptying time is increased is/are;
Reduce mixing of intestinal content
Delayed transfer to small intestine
Change in epithelial transfer
ALL
The lesser the gastric emptying time, the faster the gastric emptying rate
TRUE
FALSE
ERRONEOUS
NOT VALID
Factors delay transit time
increasing viscosity
liquid diet
water
lying on the right side
Atropine causes which of the following effects;
Delayed GI absorption
Accelerated renal excretion
Accelerated metabolism
Reduced biliary excretion
Conditions may not decrease drug absorption;
vigorous exercise
laxatives
surgery
initially large volume of meal during unfed state
Absorption of vitamin A from the GI tract depends on;
the presence of bile in the intestine
which salt is used
cid-base balance
needs of the patient
pH of the intestine
Increase drug absorption except ;
Increased blood flow to the site of administration
Decreased particle size
Increased surface area dedicated to absorption
Increased lipid solubility
Decreased pH when the drug is a weak base
Factors affecting membrane transport include /s;
pKa
Diffusivity
Partition coefficient
Presence or absence of a charge
Surfactants
The following mechanisms of absorption require the presence of drug in aqueous solution;
passive diffusion
convective transport
facilitated transport
pinocytosis
The transfer of most drugs across biologic membranes occurs by ;
Passive diffusion
Active transport
Facilitated transport
Pinocytosis
Ion-pair transport
In the diffusion controlled system, the initial rate of dissolution is directly proportional to the;
pKa
pH
quantity of free acid
solubility of the drug in the dissolution medium
Equation followed by passive diffusion;
Noyes-whitney
Van Slyke
Fick’s law
Henderson- Hasselbalch
According to Fick’s Diffusion Equation, the rate of transport of a drug by passive diffusion is;
independent of the concentration gradient
inversely proportional to the membrane surface
inversely proportional to the membrane thickness
inversely proportional to the partition coefficient
independent of the diffusion constant of drug
All of the following statements about Fick’s law as it pertains to simple diffusion are true except;
The greater the concentration gradient, the greater the rate of absorption
The smaller the surface area, the greater the drug flux
The greater the lipid-water partition coefficient, the greater the drug flux
Diffusion constant is directly proportional to the temperature
Diffusion constant is inversely related to the molecular size
The driving force for passive absorption of a drug is the;
specific carrier proteins and shows saturation kinetics
concentration gradient across a membrane separating body compartment
BOTH
NONE
The ratio of drug concentration in 2 phases separated by a semipermeable membrane
APC
pKa
concentration gradient
elimination half-life
The rate of diffusion of drugs across biological membranes is most commonly
independent on the concentration gradient
directly proportional to the concentration gradient
dependent on the availability of carrier substrate
dependent on the route of administration
When considering drug transport, passive diffusion involves drug movement from an area of ;
high concentration to an area of higher concentration
high concentration to an area of lower concentration
low concentration to an area of higher concentration
high concentration to an area of equally high concentration
Characterize transport of a drug in solution across a membrane by passive diffusion;
Membrane thickness
Volume outside compartment
Partition coefficient
Membrane length
Lipid/water partition coefficient permits;
Convective transport
Active transport
Passive transport
on-pair transport
The following compounds are absorbed via convective transport ;
sulfonic acids
ionized sulfonamides
weak organic acids
vitamin A
vitamin B12
Types of carrier mediated transport system;
Active transport
Facilitated transport
Passive diffusion
Ion-pair transport
Carrier-mediated transport systems
consume energy
structure specific
may be adversely affected by certain chemicals
all statements are true
A transport mechanism in which drug moves from an area of low concentration to an area of high concentration;
passive diffusion active transport
convective transport
ion-pair transport
active transport
The following are the characteristics of active transport;
against a concentration gradient
against a concentration gradient
carrier mediated
requires the expenditure
ALL
Sodium pump is a special type of ;
Active transport
Passive transport
Convective transport
Ion-pair transport
When active transport system becomes saturated, the rate process will be
Zero order
Pseudo- order
First order
Pseudo-first order
The following are the characteristics of facilitated diffusion transport;
against concentration gradient
Follows saturation kinetics
Carrier mediated
competitive inhibition if two compounds are transported by the same mechanism
the process is selective for certain ionic or structural configurations of the drug
Feature common to all carrier-mediated transport processes;
movement is along a concentration gradient
movement is along a concentration gradient
displays a Michaelis-Menten kinetics
can be characterized by allosteric inhibition
Formation of pairs (for highly ionized compounds) with endogenous substrate present at the GIT to form neutral complexes that are absorbed by passive diffusion ;
Pinocytosis
Convective transport
Ion- pair transport
Facilitated transport
The cell membrane is capable of forming vesicles which may engulf drug substances outside the cell membrane to transport drug (via the engulfed drug) into the compartment
Ion-pair
Passive diffusion
Convective transport
Pinocytosis
Mechanism of absorption of drugs in order of their importance;
Active-passive-convective transport
Passive diffusion-convective transport-active transport
Convective-active-passive
Active- pinocytosis-passive
The partitioning of drug molecules among numerous locations in the body
absorption
distribution
metabolism
excretion
The sum of all body regions in which the drug concentration is an instantaneous equilibrium with that in blood or plasma;
clearance
accumulation
depot phase
central compartment
