Drug Absorptio N: Iqra Khan 08 3 Year MBBS

Drug
Absorptio
n
Iqra Khan
08
3rd Year MBBS
Drug: a chemical substance used in the treatment, cure,
prevention, or diagnosis of disease or used to otherwise enhance
physical or mental well-being.
Absorption: the process of absorbing something or of being

absorbed
Drug Absorption: It is the process of drug transport from the site

of administration to the system circulation by crossing biological
membrane/s.
Why is absorption of drug important?
To reach its receptor and produce biological effects

Pharmacokinetics
Oral
Stomach, intestine to circulation
Rectal
Rectum to circulation
Intramuscular
Muscles to circulation
Intravenous
No need for absorption, directly goes into circulation
In order to absorb what must the drug do?
Cross the membrane

Drug factors
 Solubility
 Ionization
 pH of media
 pKa
 Molecular weight
 Disintegration
Solubility of Drug
 Drugs which are lipophilic easily cross the membrane

readily
 Drugs which are lipophobic or hydrophilic have

difficulty crossing the membrane
Ionization
 Only non ionized (non polar) drugs diffuse across
the membrane
 Non polar drugs are lipid soluble
 Polar are drugs are water soluble and are not

readily absorbed by the biological membrane
 Lipid soluble = non ionized molecules (NaCl)
 Hydrophilic = ionized molecules (Na+, Cl-)
 The more lipid soluble a drug is, more the absorption
 The more water soluble a drug is, less the absorption

pH
 Acidic drugs are better absorbed in acidic media

(Stomach)
 Basic drugs are better absorbed in basic media

(Intestine)
Importance of pH of media and drug pKa
 Degree of ionization depends on the pKa of drug and pH of body fluids
 pKa: value of drug when the concentration of ionized and non ionized
form of drug is equal
 If pka of a drug is equal to the pH of the medium, then 50% of the drug is
ionized and 50% is non ionized
pKa = 2 pKa = 6 pKa = 8 pKa = 9
Molecular
Weight
 Smaller the size or
lesser the molecular
weight, more the
absorption
 Inversely proportional
Disintegration
Dissolution
Drug Disintegration
into
given GIT to smaller Absorption
molecules aqueous
orally
media
Patient factors
 Surface area
 GIT Motility
 Contents of GIT
 Blood supply at absorptive site
 Destruction of drug in GIT

Surface
Area
 Large surface area = greater absorption
 Surface area of intestine is far greater than that of stomach,

more drug absorption takes place in intestine
GIT Motility
 Drugs are better absorbed in normal GIT movement.
 A drug must have sufficient time at the absorption site for

optimum absorption
Blood supply
 More circulation = maintained concentration gradient
 Thus, more absorption will take place

Contents of GIT
 Interaction with food substances
 Other drugs
Destruction of Drug
 In GIT there is HCL and various other enzymes that can cause
destruction of the drug before absorption occurs.
BIOAVAILABI
LITY
Fraction of the
administered
drug that reaches
systemic
circulation
 If 100mg of a drug is administered orally and 60mg reaches the
systemic circulation then the bioavailability of the drug will be 60%
Bioavailability lets us determine:
 The amount or proportion of drug absorbed from a formulation or
dosage form
 The rate at which the drug was absorbed
 The duration of the drug’s presence in the biologic fluid
 The relationship between drug blood level and clinical efficacy

and toxicity
 Absorption is very important aspect of pharmacokinetic study of
drug
 Knowledge of absorption helps us decide route of administration
 Knowledge of absorption gives us an idea about the

bioavailability of drug that in turn helps us decide the dose
 We require knowledge of absorption of a drug to prepare

different formulations
MC
Qs
The route of drug administration that gives the most rapid
onset of the pharmacological effect is
(a)Intramuscular injection
(b) Intravenous injection
(c) Intradermal injection
(d) Peroral administration

B
(e) Subcutaneous injection
Acidic drugs mainly bind to plasma
(a) Albumin
(b) á1 – acid glycoprotein
(c) Both (a) and (b)
(d) None of the above
B
After peroral administration, drugs generally are absorbed best
from the
(a) Buccal cavity
(b) Stomach
(c) Duodenum
(d) Ileum
(e) Rectum
C
The passage of drug molecules from a region of high drug
concentration to a region of low drug concentration is known as
(a) Active transport
(b) Bioavailability
(c) Biopharmaceutics
(d) Simple diffusion
(e) Pinocytosis
D
The initial distribution of a drug into tissue is determined
chiefly by the
(a) Rate of blood flow to tissue
(b) Glomerular filtration rate (GFR)
(c) Stomach emptying time
(d) Affinity of the drug for tissue

A
(e) Plasma protein binding of the drug
Bioavailability of drug refers to
(a) Percentage of administered dose that reaches systemic

circulation in the unchanged form
(b) Ratio of oral to parental dose
(c) Ratio of orally administered drug to that excreted in the faeces
(d) Ratio of drug excreted unchanged in urine to that excreted as

metabolites
A
The most important factor governing absorption of a drug from
intact skin is
(a) Molecular weight of the drug
(b) Site of application
(c) Lipid solubility of the drug
(d) Nature of the base used in the formulation

C
Pharmacokinetics is
(a) The study of absorption, distribution, metabolism and excretion of

drugs
(b) The study of biological and therapeutic effects of the drugs
(c) The method of development of new pharmacological agent
(d) The study of carcinogenic activity of a new drug
A
In which form the drug is absorbed more rapidly?
(a) In aqueous solution
(b) In suspension
(c) In oily solution
(d) In solid form
A
Following compartment constitutes the largest percentage
(a) Plasma
(b) Intestinal fluid
(c) Intracellular fluid
(d) Fat
C
Thank you!

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Drug

Absorption: the process of absorbing something or of being

Drug Absorption: It is the process of drug transport from the site

To reach its receptor and produce biological effects

Cross the membrane

 Drugs which are lipophilic easily cross the membrane

 Drugs which are lipophobic or hydrophilic have

 Non polar drugs are lipid soluble

 Polar are drugs are water soluble and are not

 Hydrophilic = ionized molecules (Na+, Cl-)

 The more lipid soluble a drug is, more the absorption

 The more water soluble a drug is, less the absorption

 Acidic drugs are better absorbed in acidic media

 Basic drugs are better absorbed in basic media

 Degree of ionization depends on the pKa of drug and pH of body fluids

 Blood supply at absorptive site

 Destruction of drug in GIT

 Surface area of intestine is far greater than that of stomach,

 Drugs are better absorbed in normal GIT movement.

 A drug must have sufficient time at the absorption site for

 More circulation = maintained concentration gradient

 Thus, more absorption will take place

 Interaction with food substances

 The rate at which the drug was absorbed

 The duration of the drug’s presence in the biologic fluid

 The relationship between drug blood level and clinical efficacy

 Knowledge of absorption helps us decide route of administration

 Knowledge of absorption gives us an idea about the

 We require knowledge of absorption of a drug to prepare

(b) Intravenous injection

(c) Intradermal injection

(d) Peroral administration

(b) á1 – acid glycoprotein

(c) Both (a) and (b)

(d) None of the above

(a) Buccal cavity

(a) Active transport

(d) Simple diffusion

(a) Rate of blood flow to tissue

(b) Glomerular filtration rate (GFR)

(c) Stomach emptying time

(d) Affinity of the drug for tissue

(a) Percentage of administered dose that reaches systemic

(b) Ratio of oral to parental dose

(c) Ratio of orally administered drug to that excreted in the faeces

(d) Ratio of drug excreted unchanged in urine to that excreted as

(a) Molecular weight of the drug

(b) Site of application

(c) Lipid solubility of the drug

(d) Nature of the base used in the formulation

(a) The study of absorption, distribution, metabolism and excretion of

(b) The study of biological and therapeutic effects of the drugs

(c) The method of development of new pharmacological agent

(d) The study of carcinogenic activity of a new drug

(a) In aqueous solution

(c) In oily solution

(d) In solid form

(b) Intestinal fluid

(c) Intracellular fluid