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1
Topic name : Gastrointestinal absorption
and role of dosage forms in absorption of
drugs.
Student name :- Mr. Gaurav
Anil Patil
M pharm 1st Year
Pharmaceutics Department
Index
o Introduction
o Mechanism of absorption
o Role of different dosage forms in absorption of drugs
• Solution
• Suspension
• Capsules
• Tablets
o Reference
2
 Absorption
o The movement of unchanged drug from the site of
administration to the systemic circulation is called as
absorption.
Or
o The transportation of the unmetabolized drug from the site
of administration to the body circulation system.
3
Mechanism of absorption
There are three broad categories are :
 Transcellular/intracellular transport
Passive Transport Processes
A. Passive diffusion
B. Pore transport
C. Ion-pair transport
D. Facilitated diffusion
Active transport processes
A. Primary
B. Secondary
a. Symport (Co-transport)
b. Antiport (Counter transport) 4
 Para cellular / Intercellular Transport
 Endocytosis
A. Pinocytosis
B. Phagocytosis
5
 Steps involved in absorption of different dosage
forms
6
 Role of dosage form in drug
absorption
Conventional dosage forms may be broadly characterized
as:
• Solutions
• Suspension
• Capsules
• Tablets
7
 Solution
• Solutions such as syrups and elixirs show fast and often
complete absorption of drug because they do not have
dissolution problem.
• The factors that affect drug absorption from solution
include:
• Viscosity(Absorption rate decreases with increasing viscosity because the
slower rate of movement of drug molecules to the absorbing
membranes.)
• Solubilizes
• Stabilizers
• Stability
• The vehicle used in syrups, elixirs and emulsions may be
aqueous or non-aqueous(e.g., PEG, PG, alcohol) or non-
water miscible(e.g.. vegetable oils). 8
• The rate of drug absorption from non-aqueous or non-
water miscible vehicle based solution is less than the rate
of drug absorption from water based solution.
• The selection of vehicle for solution dosage form depends
on the physiochemical properties of the drug such as
• Solubility
• Partition Coefficient
• Ionization
• Hydrogen Bonding
• Surface activity
9
• For example
solution of paracetamol is prepared with PEG 400 as it is sparingly
soluble in water. Certain materials such as sorbitol or hydrophilic
polymers are added to a solution dosage form, to improve pourability
and palatability by increasing the viscosity of the preparation
• Due to good systemic availability, solutions are frequently
used as bioavailability standards.
10
 Suspension
Suspension
Fine particle
Dissolution
Solution
Absorption
.
o The factors that affect drug absorption from suspension
includes:
• Particle size
• Polymorphism 11
• Wetting agents
• Viscosity of the medium
• Suspending agents
• Drug in a suspension is in the solid form, but is finely
divided and has a large surface area.
• Weating agents present in the suspension helps in easy
penetration of drug into the absorption surface.
• Finally divided solid particles in suspension are stabilized
with suspending agents. Suspending agents retard
sedimentation of dispersed particles in suspension.
12
13
o Suspending agent may increase the viscosity of drug
vehicle and may decrease the rate of drug dissolution
which affect the absorption of the drug.
o For Example:
The blood levels of trimethoprim and
sulfamethoxazole were compared in 24 healthy subjects
following oral administration of 3 forms. The
absorption rate of each drug was significantly greater
with the suspension this with the tablet or capsule.
 Capsule
o Factors affecting the absorption :
• Drug particle size
• Dissolution rate
• Polymorphism
• Excipients
• Interactions
14
o In capsule ,on disruption of the shell the encapsulated
powder/granules mass should disperse rapidly to expose a
large surface area in the gastrointestinal fluids.
o Diluents added to capsules dosage form may affect the
dissolution of filled drug in capsule shell.
o Hydrophilic diluents are added in the capsule for poorly
water soluble drugs ,they enhance the dispersion rate of the
shell.
o drug absorption from capsule may also be affected by
particle size and chemical and physical incompatibility of
the drug with its excipients.
15
 Tablet
o There are various types of tablet formulations are
present
Compressed tablets>film coated tablets>enteric coated
tablets>sustained release tablet
16
o Factors that affect the absorption of tablet
• Effective surface area
• Dissolution
• Permeability
• API and excipients
o Most formulations require the incorporation of
hydrophobic lubricants, such as magnesium stearate, to
produce an acceptable tablet.
o Larger the quantity of lubricant in a formulation the
slower is the dissolution rate.
o Compression force may also be an important factor in
drug bioavailability from compressed tablets.
17
THANK
YOU
18

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Role of dosage form in absorption of drugs.pptx

  • 1. 1 Topic name : Gastrointestinal absorption and role of dosage forms in absorption of drugs. Student name :- Mr. Gaurav Anil Patil M pharm 1st Year Pharmaceutics Department
  • 2. Index o Introduction o Mechanism of absorption o Role of different dosage forms in absorption of drugs • Solution • Suspension • Capsules • Tablets o Reference 2
  • 3.  Absorption o The movement of unchanged drug from the site of administration to the systemic circulation is called as absorption. Or o The transportation of the unmetabolized drug from the site of administration to the body circulation system. 3
  • 4. Mechanism of absorption There are three broad categories are :  Transcellular/intracellular transport Passive Transport Processes A. Passive diffusion B. Pore transport C. Ion-pair transport D. Facilitated diffusion Active transport processes A. Primary B. Secondary a. Symport (Co-transport) b. Antiport (Counter transport) 4
  • 5.  Para cellular / Intercellular Transport  Endocytosis A. Pinocytosis B. Phagocytosis 5
  • 6.  Steps involved in absorption of different dosage forms 6
  • 7.  Role of dosage form in drug absorption Conventional dosage forms may be broadly characterized as: • Solutions • Suspension • Capsules • Tablets 7
  • 8.  Solution • Solutions such as syrups and elixirs show fast and often complete absorption of drug because they do not have dissolution problem. • The factors that affect drug absorption from solution include: • Viscosity(Absorption rate decreases with increasing viscosity because the slower rate of movement of drug molecules to the absorbing membranes.) • Solubilizes • Stabilizers • Stability • The vehicle used in syrups, elixirs and emulsions may be aqueous or non-aqueous(e.g., PEG, PG, alcohol) or non- water miscible(e.g.. vegetable oils). 8
  • 9. • The rate of drug absorption from non-aqueous or non- water miscible vehicle based solution is less than the rate of drug absorption from water based solution. • The selection of vehicle for solution dosage form depends on the physiochemical properties of the drug such as • Solubility • Partition Coefficient • Ionization • Hydrogen Bonding • Surface activity 9
  • 10. • For example solution of paracetamol is prepared with PEG 400 as it is sparingly soluble in water. Certain materials such as sorbitol or hydrophilic polymers are added to a solution dosage form, to improve pourability and palatability by increasing the viscosity of the preparation • Due to good systemic availability, solutions are frequently used as bioavailability standards. 10
  • 11.  Suspension Suspension Fine particle Dissolution Solution Absorption . o The factors that affect drug absorption from suspension includes: • Particle size • Polymorphism 11
  • 12. • Wetting agents • Viscosity of the medium • Suspending agents • Drug in a suspension is in the solid form, but is finely divided and has a large surface area. • Weating agents present in the suspension helps in easy penetration of drug into the absorption surface. • Finally divided solid particles in suspension are stabilized with suspending agents. Suspending agents retard sedimentation of dispersed particles in suspension. 12
  • 13. 13 o Suspending agent may increase the viscosity of drug vehicle and may decrease the rate of drug dissolution which affect the absorption of the drug. o For Example: The blood levels of trimethoprim and sulfamethoxazole were compared in 24 healthy subjects following oral administration of 3 forms. The absorption rate of each drug was significantly greater with the suspension this with the tablet or capsule.
  • 14.  Capsule o Factors affecting the absorption : • Drug particle size • Dissolution rate • Polymorphism • Excipients • Interactions 14
  • 15. o In capsule ,on disruption of the shell the encapsulated powder/granules mass should disperse rapidly to expose a large surface area in the gastrointestinal fluids. o Diluents added to capsules dosage form may affect the dissolution of filled drug in capsule shell. o Hydrophilic diluents are added in the capsule for poorly water soluble drugs ,they enhance the dispersion rate of the shell. o drug absorption from capsule may also be affected by particle size and chemical and physical incompatibility of the drug with its excipients. 15
  • 16.  Tablet o There are various types of tablet formulations are present Compressed tablets>film coated tablets>enteric coated tablets>sustained release tablet 16
  • 17. o Factors that affect the absorption of tablet • Effective surface area • Dissolution • Permeability • API and excipients o Most formulations require the incorporation of hydrophobic lubricants, such as magnesium stearate, to produce an acceptable tablet. o Larger the quantity of lubricant in a formulation the slower is the dissolution rate. o Compression force may also be an important factor in drug bioavailability from compressed tablets. 17