Drug Absorption and Transport

Development Team
Principal Investigator Prof. Farhan J Ahmad
Jamia Hamdard, New Delhi

Dr. Javed Ali

Paper Coordinator
Jamia Hamdard, New Delhi

Dr. Manju Sharma

Content Writer Jamia Hamdard, New Delhi

Dr. Shibli Jameel Ahmad

Content Reviewer Jamia Hamdard, New Delhi

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List of Contents

1. Introduction - Drug absorption and Drug transport

2. Cell-membrane - Structure and Physiology

3. Mechanism of Drug transport

4. Active and Passive transport

5. Summary of Transport mechanisms and drugs absorbed through them

6. Absorption of Drug

7. Factors affecting absorption of drug

8. Methods for delaying absorption

9. Methods to facilitate absorption

10. Summary of mechanism of drug absorption from various non invasive route

11. Conclusions

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Drug Absorption
Drug absorption is defined as the process of movement of unchanged drug from the site
of administration to the systemic circulation. It is the primary aspect of pharmacokinetics and is
necessary for the following:
1. To determine the required dose of drugs.
2. To determine the frequency of administration of drug.
3. To ascertain the duration of the effective action of drug.
4. To predict the onset of the desired or undesired effect of drugs.

Dissolution –rate and absorption of drug

Drugs may be administered into the body in various dosage forms (tablets, capsules,
powders, suspensions, emulsion, solutions etc.). The first requirement for absorption is the
soluble state of the drug. Thus, if the drug is given in the solid form (tablet, capsule, powder
etc.), it has to be disintegrated and dissolved before its absorption. The dissolution rate depends
on many factors. High, intense agitation, low viscosity of the solvent, saturation of the solution,
smaller particle size and high solubility of the drug are the factors that increase the dissolution
rate. Esterification can also increase the dissolution rate.

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In addition to the above mentioned factors, tablet formulation factors like filters, binders,
lubricants and compression pressure etc. also affect absorption of the drug. A large tablet
disintegrates more quickly as compared to highly compressed small tablet. Dissolution rate can
also be influenced by gastric motility. Lower pH increases dissolution rate of weak bases but
decreases that of weak acids.

Drug Transportation
When a drug is in soluble state, it must pass through one or more biological membranes,
to be absorbed and distributed into organs and tissues. Drug molecules can cross cell membrane
by various transport mechanisms. Such movement of the drug across the membrane is called as
drug transport.

Cell-membrane- Structure and Physiology

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Fig 1. Structure of cell membrane

The cell membrane consists of two layers of phospholipids with proteins and sugars
embedded in them. In addition to phospholipids, the lipid cholesterol is also present. The
phospholipid molecules have a head, which is electrically charged and hydrophilic (water
loving), and a tail which has no charge and is hydrophobic (water hating). The phospholipid
bilayer is arranged like a sandwich with the hydrophilic heads aligned on the outer surfaces of
the membrane and the hydrophobic tails forming a central water –repelling layer. These
differences influence the transfer of substances across the membrane.

Membrane proteins

 These proteins that extend all the way through the membrane provide channels that allow
the passage of electrolytes and non-lipid soluble substances.

 Transmembrane proteins form channels that are filled with water and allow very small,
water-soluble ions to cross the membrane.

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 Some are involved in pumps that transport substances across the membrane.

In general, the bio-membrane acts like a semipermeable barrier permitting rapid and
limited passage of some compounds while restricting that of others.

Mechanism of Drug Transport

Fig. 2: Drug transport mechanisms

The three broad categories of drug transport mechanisms involved in absorption are:

1. Transcellular/ Intracellular transport

2. Paracellular/ intercellular transport

3. Vesicular transport

 Transcellular / Intracellular transport is defined as the passage of drugs across the GI

epithelium. It is the most common pathway for drug transport.

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 Paracellular / intercellular transport is defined as the transport of drugs through the
junctions between the GI epithelial cells.

 Vesicular transport is an energy dependent process but involves transport substances

within vesicles into a cell.

The major transport mechanisms are as follow:

1. Passive diffusion and filtration

2. Specialized transport
A) Carrier- mediated transport
i) Facilitated diffusion
ii) Active transport
3. Vesicular transport
a) Phagocytosis
b) Pinocytosis
4. Pore transport
5. Ion pair formation

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Fig 3: Major transport mechanisms

1. Passive Transport (downhill movement)

Passive transport processes do not require energy other than that of molecular motion
(Brownian motion) to pass through the lipid bilayer. It is the most important mechanism
for majority of the drugs. Majority of drugs (90%) diffuse across the membrane in the
direction of concentration gradient. There is no active role of the membrane. Lipid soluble
drugs diffuse by dissolving in the lipoid matrix of the membrane.
Characteristics
 Not requiring energy

 Having no saturation

 Having no carriers

 Not resisting competitive inhibition

Passive transport processes can be further classified into following types:

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a) Passive diffusion

b) Pore transport

c) Ion-pair transport

d) Facilitated or mediated –diffusion

a) Passive diffusion

It is a transfer process in which the drug molecules pass through a biological barrier
from the phase of higher concentration to the phase of lower concentration (i.e. along the
concentration gradient) without requiring any expenditure of energy by the biological
system.
Non-ionised drugs (nonelectrolytes can diffuse passively across the biological
barriers at a rate proportional to their lipid: water partition coefficient. Thus, drugs that are
highly lipid soluble can diffuse rapidly, whereas those that are less lipid soluble will
diffuse slowly. For weak electrolytes (i.e. partly ionized drugs), the diffusion would
depend upon the degree of ionization of the drug, the pH of the surrounding environment
and the lipid:water partition coefficient of their undissociated form. The weak electrolytes
are either weakly acidic drugs (i.e. which form salts with bases, e.g., phenytoin sodium,
phenobarbitone sodium, sodium salicylate, sodium sulphadiazine and potassium penicillin-
V) or weakly basic drugs (i.e., which form salts with acids and are available as
hydrochlorides or sulphates etc., e.g., morphine hydrochloride, amphetamine sulphate,
atropine sulphate, ephedrine hydrochloride and chloroquine phosphate).

Since the rate of passive diffusion of any weak acid or a weak base depends on its
degree of ionization which in turn depends upon the pH of the surrounding medium, a
relationship exists between its dissociation constant (pKa of the drug), the pH of the

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environment and the extent of its ionization. This relationship is expressed by Henderson-
Hasselbalch equation given below:

Henderson–Hasselbalch Equation

Where:
pKa = negative logarithm of acid dissociation constant

[A-] = ionized drug

[HA] = unionized drug

Implications of Henderson- Hasselbalch equation

 Acidic drugs( aspirin, phenytoin, barbiturates) are absorbed are largely unionized in
stomach and absorbed faster while basic drugs (morphine, diazepam, amphetamine) are
absorbed faster in intestine.
 Acidic drugs are excreted faster in alkaline urine – urinary alkalizers.
 Basic drugs are excreted faster in acidic urine – urinary acidifiers.
 Strongly acidic or strongly basic drugs and quaternary ammonium compounds remain
predominantly ionized at all pH and are, therefore poorly absorbed.

Filtration

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Fig 4: Passage of drugs across capillaries

 The free or unbound drugs of smaller molecular size can pass through the pores or spaces
between the cells by the process of filtration.
 It is purely a physical process where the rate of filtration is proportional to a pressure
gradient.
 This is an important mechanisms for the drugs of small molecular size.
(e.g., urea, alcohol, glucose) which are filtered through glomerulus.
 Passage of drugs through aqueous pores in membrane or through para cellular space.
 Lipid insoluble drugs can cross – if the molecular size is small.
 Majority of intestinal mucosa and RBCs have small pores and drugs cannot cross.
 But, capillaries have large paracellular space and most drugs can filter through these.

b) Pore Transport

 It is also called as convective transport, Bulk flow or filtration.

 The driving force for this process is the ‘hydrostatic pressure or the osmotic differences
across the membrane’.

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 The process is important in the absorption of low molecular weight, low molecular size
drugs.
 Example: Urea, Water, Sugar

c) Ion –pair transport

Yet another mechanism that explains the absorption of drugs like quaternary ammonium
compounds and sulphonic acids, which ionize under all pH conditions, is ion-pair
transport. Despite their low o/w partition coefficient values, such agents penetrate the
membrane by forming reversible neutral complexes with endogenous ions of the GIT like
mucin. Such neutral complexes have both the required lipophilicity as well as aqueous
solubility for passive diffusion. Such a phenomenon is called as ion-pair transport.
Propanolol, a basic drug, that form an ion-pair with oleic acid, is absorbed by this
mechanism.

d) Carrier-mediated Transport/ facilitated diffusion

 The mechanism is thought to involve a component of the membrane called as the carrier
that binds reversibly or non-covalently with the solute molecules to be transported.
 The carrier may be an enzyme or some other component of the membrane.
 The transport process is structure-specific i.e. the carriers have special affinity for and
transfer a drug of specific chemical structure only.
 The number of carriers is limited.

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Fig 5: Facilitated diffusion

 This transport system operates down the concentration gradient (downhill transport) but at
a much faster rate than by simple diffusion.
 The driving force is concentration gradient (hence passive diffusion), no expenditure of
energy is involved.
 E.g. the entry of glucose into muscle and fat cell by glucose transporter GLUT 4.
 GI absorption of vitamin B12

Active transport (up-hill transport)

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Fig 6: Active transport

 It is process where the materials are transported across membranes against a concentration
gradient.
 The drug is transported from a region of lower to one of higher concentration i.e., against
the concentration gradient or ‘uphill transport’.
 Requires energy in the form of ATP.
 Examples: Sodium, potassium, iron, glucose and vitamins like niacin, pyridoxine and
ascorbic acid.

Active (concentrative) transporters

 Primary active transporters - generate energy themselves (e.g. ATP hydrolysis, the process
transfer only one ion/molecule and in only one direction, hence called as uniporter e.g.
absorption of glucose.

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 Secondary transporters - utilize energy stored in voltage and ion gradients generated by a
primary active transporter (e.g. Na+/K+-ATPase).
 Symporters (co-transporters) e.g. Na+ -glucose symporter
 Antiporters (exchangers) e.g. Na+/H+ antiporters

Fig 7: Secondary active transport

In secondary active transport processes, there is no direct requirement of ATP i.e.

it takes advantage of previously existing concentration gradient. The energy required in
transporting an ion aids transport of another ion or molecule (co-transport) either in same
direction or in the opposite direction. Accordingly, this process is further subdivided into:

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1) Symport involves in movement of both the molecules in the same direction
e.g. Na+ -glucose symporter uses the potential energy of the Na+ concentration gradient to
move glucose against its concentration gradient.
2) Antiport involves movement of molecules in the opposite direction e.g.
expulsion of H+ ions using the Na+ gradient in the kidneys.

Transport in Vesicles- ENDOCYTOSIS

 Also called Corpuscular or Vesicular transport

 It involves engulfing extracellular materials within a segment of the cell membrane to form
a saccule or a vesicle which is then pinched-off intracellularly.
 Only transport mechanism whereby a drug or compound does not have to be in an aqueous
solution in order to be absorbed.
 Includes two type of process:

Phagocytosis (cell eating) and Pinocytosis (cell drinking)

Phagocytic uptake of macromolecules

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Fig 8: Phagocytic uptake of macromolecules

Pinocytosis

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Fig 9: Pinocytosis

 It involves the invagination of a part of the cell membrane & trapping within the cell of a
small vesicle containing extra cellular constituents. The vesicle contents can then be
released within the cell, or extruded from the other side of the cell.
 This process is important in the absorption of oil soluble vitamins (A, D, E, K), vitamin B12
& in the uptake of nutrients like fats and starch.

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Summary of important transport mechanism and drugs absorbed through them

Absorption mechanism
Drugs absorbed
Passive diffusion
Most drugs having high lipophilicity and MW in the range

100-400.

Water-soluble drugs of MW less than 100.

Pore transport

Drugs that ionize at all pH conditions absorbed after

Pair transport
complexing with oppositely charged ions.

Structures- specific drugs with affinity for carriers

Carrier-mediated transport
transported from specific sites.

Macromolecular nutrients and drugs as solid particles or oily

Endocytosis
droplets.

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Absorption of Drugs

 Absorption is the transfer of a drug from its site of administration to the blood stream.
 Most of the drugs are absorbed by way of passive transport.
 Intravenous administration has no absorption phase.
 Not only the fraction of the administered dose that gets absorbed, but also the rate of
absorption is important.

Absorption of drug and dissolution rate

 The first requirement for absorption is soluble state of the drug.

 If the drug is given in the solid form, it has to be disintegrated and dissolved before its
absorption.
 The dissolution rate depends upon many factors.
 High temperature, intense agitation, low viscosity of the solvent, saturation of the solution,
smaller particle size and high solubility of the drug are the factors that increase the
dissolution rate. Esterification can also increase the dissolution rate.
 Tablet formulation factors like filters, binders, lubricants and compression pressure also
affect absorption of drug.

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 A large tablet disintegrates more quickly as compared to highly compressed small tablet.
 Dissolution rate can also be influenced by gastric motility.
 Lower pH increases dissolution rate of weak bases but decreases that of weak acids.

Factors Affecting Absorption of a Drug

A) PHARMACEUTICAL FACTORS

I. Physiochemical properties of Drug:

1. Drug solubility and dissolution rate

2. Particle size and effective surface area

3. Polymorphism and morphism

4. Salt form of the drug

5. Lipophilicity of the drug pH-partition hypothesis

6. pKa of the drug and gastrointestinal pH

7. Drug stability

8. Stereo chemical nature of the drug

II. Dosage form characteristics and Pharmaceutical Ingredients

1. Disintegration time ( tablets/capsules)

2. Dissolution time
3. Manufacturing variables
4. Pharmaceutical ingredients ( excipients/adjuvants)

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5. Nature and type of dosage form
6. Product age and storage conditions

B. PATIENTS –RELATED FACTORS

1. Age
2. Gastric emptying time
3. Intestinal transit time
4. Gastrointestinal pH
5. Disease states
6. Blood flow through GIT
7. Gastrointestinal contents ( other drugs, food, fluids, GI contents)
8. Contact time with gastrointestinal mucosa
9. Presystemic metabolism (gut wall enzymes, hepatic enzymes)
10. Route of administration

Route of administration:

Topical:

 Depends on lipid solubility – only lipid soluble drugs penetrate intact skin – only
few drugs are used therapeutically
 Examples – GTN, Hyoscine, Fentanyl, Nicotine, testosterone and estradiol
 Organophosphorous compounds – systemic toxicity
 Abraded skin: tannic acid – hepatic necrosis
 Cornea permeable to lipid soluble drugs

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 Mucus membranes of mouth, rectum, vagina etc., are permeable to lipophillic
drugs

Subcutaneous and Intramuscular:

 Drugs directly reach the vicinity of capillaries – passes capillary endothelium and
reach circulation
 Passes through the large paracellular pores
 Faster and more predictable than oral absorption
 Exercise and heat – increase absorption
 Adrenaline – decrease absorption

Absorption via Gastrointestinal Tract

 Oral Route ( from mouth, stomach, intestine, colon)
 Physical properties – Physical state, lipid or water solubility
 Dosage forms:
 Particle size
 Disintegration time and Dissolution rate
 Formulation – Biopharmaceutics
 Physiological factors:
 Ionization, pH effect
 Presence of Food
 Presence of other agents
 The rate of absorption from faster to lowest is:
Sublingual→ rectal → oral
Buccal/ sublingual and Rectal – bypasses liver

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Fig 10 : Buccal/ sublingual – bypasses liver

The two sites for oral mucosal delivery of drugs are:

 Sublingual route: The drug is placed below the tongue allowed to dissolve.
 Buccal route: The medicament is placed between the cheek and the gum.

Influence of food on Drug absorption

Delayed Decreased Increased Unaffected

Aspirin Penicillins Griseofulvin Methyldopa

Paracetamol Erythromycin Diazepam Propylthiouracil
Diclofenac Ethanol Water soluble vitamins Sulphasomidine
Nitrofurantoin Tetracyclines
Digoxin Levodopa
Iron

 As a general rule, drugs are better absorbed under fasting conditions and presence of
food retards or prevent it.

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Oral Administration – 1st pass metabolism

Before the drug reaches the systemic circulation, the drug can be metabolized in the liver
or intestine. As a result, the concentration of drug in the systemic circulation will be reduced.
Absorption via Parenteral sites

 Except when given intravenously, the drug has to cross biological membranes.
 Drugs when injected intravenously are completely absorbed and rapidly distributed.
 Drugs when injected intramuscularly and subcutaneously are absorbed by passive
diffusion from the injection site to the plasma /lymph.
 Absorption of drugs from i.m. injection is usually more rapid than from S.C. sites
because of the higher vascularity of the muscle.
 The extent of absorption from the highest to lowest is:
Intravenous →intramuscular →subcutaneous.
However, the absorption from these sites is reduced in patients with circulatory failure (shock) in
whom the tissue perfusion gets decreased.
 Drugs when injected intravenously are completely absorbed and rapidly distributed.
 According to the rate of absorption:

Inhalation→Sublingual→Rectal→Intramuscular→Subcutaneous→Oral→Transdermal
Example – Nitroglycerine:
 i.v. effect – immediate,
 S L effect – 1 to 3 min and
 per rectal – 40 to 60 minutes
Absorption via Lungs

 Lipid –soluble drugs when given in:

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 a vaporized form (general anesthetics), or as aqueous solution spray (salbutamol) or as
spray of suspended particles (disodium cromoglycate) are absorbed by simple diffusion
from the pulmonary epithelium and mucous membrane of trachea and lungs.
 Absorption is rapid because of the large surface area and high vascularity.
 First pass metabolism is avoided.
Absorption via Topical sites (skin, cornea, mucous membranes)
 Majority of drugs applied topically are meant to exert their effects locally.
 Absorption of most drugs through intact skin is of course poor as the keratinised
epithelium behaves like a barrier to permeability.
 However, the underlying dermis is quite permeable to many lipid-soluble drugs and
therefore significant absorption can occur if the skin is abraded.
 A transdermal application of some drugs (nitroglycerin, scopolamine and clonidine) and
application of some drugs on mucus membranes (oxytocin and vasopressin as nasal
spray) enhances the systemic absorption mainly because of the thin and highly vascular
absorbing surface.
 Ophthalmic drugs in form of drops or ointment are absorbed through the cornea.

Methods for delaying Absorption

1. Using an appropriate dosage form

 The “slow release” dosage forms like retard tablets (e.g. potassium chloride retard
tabs. diclofenac sodium sustained release tabs), spansules (e.g. iron formulations and
isosorbide dinitrate spansules), depot injections (e.g. testosterone depot and fluphenazine
depot inj.), subcutaneous implants (e.g. testosterone pellets) are some ways to obtain a
slow but sustained absorption of drugs.
2. Changing the physical characteristics of the drug

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1. Physical characteristics of some drugs may also be changed to retard their absorption,
e.g. insulin zinc suspension.
2. Depending upon the pH of the reaction, insulin can form a fine amorphous zinc
suspension (semilente) which is relatively rapidly absorbed or
3. a cloudy zinc suspension (ultralente) which is slowly absorbed.
4. Depending on the effect desired, each can be used separately or can also be mixed
together (lente) to produce an immediate but sustained effect.
5. Similarly, procaine penicillin-G is such a salt of penicillin which is only slightly
water soluble. When injected as an aqueous suspension it is slowly absorbed and
exerts a prolonged action.

3. Adding a vasoconstrictor drug or applying a tourniquet

1. The addition of a vasoconstrictor drug, like noradrenaline or adrenaline to a solution
of a local anesthetic, e.g. xylocaine, reduces the absorption of the local anesthetic
into the general circulation.
2. This prolongs the local anesthetic effect and reduces the chances of systemic
toxicity.
3. Application of a tourniquet to arrest the blood flow followed by the i.v. injection of
local anesthetic below the tourniquet (e.g. in whole limb) delays the systemic
absorption but prolongs the local anesthetic effect.
4. Decreased peripheral blood flow in conditions of “shock” significantly reduces the
rate of absorption of injected drugs.

Methods to Facilitate Absorption

The rate limiting factors in absorption from the injection sites are:
1. Diffusion through the tissue.
2. Removal by local blood flow.

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 By adding hyaluronidase (an enzyme which breaks down the intercellular matrix) to the
injection fluid increases the rate of diffusion through the interstitial spaces and greatly
speeds up the drug absorption.
 Similarly, the absorption from the site of injection may be increased by increasing the
local blood flow by applying hot fermentation or doing massage.

Summary of mechanisms and drugs absorbed from various non-invasive routes

Routes Absorption Drugs Delivered

Mechanism(s)

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1. Buccal/Sublingual Passive diffusion, carrier- Nitrites and nitrates antianginals,

mediated transport nifedipine, morphine, fenoterol etc.

2. Rectal Aspirin, paracetamol, theophylline, few

Passive diffusion barbiturates, etc.

3. Transdermal Passive diffusion Nitroglycerine, lidocaine, scopolamine,

testosterone, betamethasone, etc.
Passive diffusion, endocytosis,
4. Intramuscular Phenytoin, digoxin, several steroids and
pore transport
antibiotics and many other drugs

5. Subcutaneous Passive diffusion Insulin, heparin, C.R. implants.

Passive diffusion, pore Salbutamol, cromolyn sodium,

6. Inhalation beclomethasone
transport
Antihistamines , phenylpropanolamine.
7. Intranasal Passive diffusion, pore
transport

8. Intraocular Passive diffusion Atropine, pilocarpine, adrenaline, antibiotics

etc.

9. Vaginal Passive diffusion Steroidal drugs and contraceptives,

metronidazole etc.

Conclusions

1. Absorption is movement of the drug from its site of administration into the
systemic circulation.
2. There are various factors that influence the absorption of the drug.
3. Except when given i.v. the drug has to cross biological membranes.

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4. The movement of drug across the biological membrane is called as drug transport.
5. Drugs are transported across the membranes by: Passive diffusion and specialized
transport.
6. A drug might be absorbed by more than just one mechanism. e.g. Cardiac
glycosides are absorbed both passively as well as by active transport.
7. The transport mechanism also depends upon the site of drug administration.
8. There are various methods used to delay and to facilitate the rate of absorption of
drug.

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