FORMULATION FACTOR EFFECTING
DRUG ABSORBTION
Presented by
PRIYANKA GRESESS ANAND
M.Pharm
Department of Pharmaceutics
INTEGRAL UNIVERSITY
LUCKNOW U.P
CONTENTS
1)-Introduction
2)-Manufacturing variables
3)- Type of dosage form
4)-Pharmaceutical ingredients/excipients
5)-products life and storage condition
6)-Conclusion
7)-Reference
5/30/2018 2
Introduction
• To gain entry in to the blood circulation,a drug
must be solubilize to pass from the absorbtion
site through biological membranes.
• Permeability of drug through biological
membranes is closely related to the molecular
structure of the drug,physicochemical
characteristics,formulation factor ,and the
physical and biochemical properties of the cell
membrane.
5/30/2018 3
DRUG ABSORBTION
Definition
Drug absorbtion is a pharmacokinetic parameter that
refers to the way a drug is absorbed from a
pharmaceutical formulation in to the bloodstream.
In general,lipid soluble drugs composed of smaller
molecules are more likely to absorbed .
the rate and extent of absorbtion mostly depends on
routes of administration and the way a drug product is
designed and manufactured.
.
5/30/2018 4
Dosage forms like tablet, capsule, powder, solution,
suspension, emulsion may vary the absorption.
Drug products that contain the same drug (active
ingredient) may have different inactive ingredients so
absorbtion of these drug from different products may
flactuate.
Absorbtion play a key role in determining how fast a
drug produces a clinical effect.
5/30/2018 5
Formulation Factor which can slower the rate of
absorbtion of drug are mentioned below –
Formulation Factors:-
Manufacturing variables: -
a). Method of granulation
Wet granulation yields a tablet that dissolves
faster than those made by other granulating
methods. But wet granulation has demerit like
formation of crystal bridge or chemical
degradation.
5/30/2018 6
b)-compression force-Higher compression force
yields a tablet with greater hardness hence have a
long D.T. but on other hand higher compression
force cause crushing of drug particles into
smaller ones with effective surface area which
decreasesD.T..
5/30/2018 7
5/30/2018 8
Drug formulations are designed to provide an
attractive, stable, and convenient use of
products.
Decreasing order dissolution rate of different
dosage forms as :-
solutions>solid solutions>suspensions,
capsules>coated capsules>tablets, and
controlled release formulations.
5/30/2018 9
5/30/2018 10
Solutions
Solutions shows faster absorption as compared to
solid dosage forms.
solutions are frequently used as bioavailability
standards.
Factor effecting absorbtion of solution:-
Viscosity
Solubulizer
Stability
surfactants
5/30/2018 11
Suspensions
• A drug in a suspension is in solid form, but is
finely divided and has a large surface area.
• Drug particles can diffuse readily between the
stomach and small intestine so that absorption
is relatively insensitive to stomach emptying
rate.
• Liquid dosage forms, therefore, have
advantages besides simple dissolution rate.
However, they also have some disadvantages,
including greater bulk, difficulty in handling, and
perhaps reduced stability.
5/30/2018 12
Capsules and tablets
• These formulations differ from each other in
that material in capsules is less impacted than
in compressed tablets.
• Once a capsule dissolves, its contents generally
disperse quickly.
• Tablets generally disintegrate in stages, first into
granules and then into primary particles. As
particle size decreases, dissolution rate
increases due to of increased surface area..
Pharmaceutical
Ingredients/Excipients
 Excipients are added to ensure
1. Stability
2. Uniformity
3. Functionability
4. Bioavailability
5. Acceptability
5/30/2018 13
Diluents
 Diluents are commonly added to tablet and
capsule formulations if the required dose is
inadequate to produce bulk.
 Eg:-Drug-diluent interaction resulting in poor
bioavailability of tetracycline & DCP
5/30/2018 14
Binders and granulating agent
Promote cohesive compacts before & after compression
 Eg polymeric materials like starch, cellulose derivatives, acacia,
PVP, etc.
COLOURANTS
 Very low concentration of water-soluble dye has inhibitory effect on
dissolution.
 E.g. brilliant blue retards dissolution of sulfathiazole
5/30/2018 15
Lubricants
To aid flow of granules
 To reduce interparticle friction
 Sticking of particles to dies & punches
 Eg:- sodium and magnesium stearates &
waxes.
5/30/2018 16
DISINTEGRANTS
 These Agents overcome cohesive strength of tablet & break them on
contact with water which is an important for tablet to dissolve.
eg MCC
BUFFERS
 They create right atmosphere for dissolution
e.g. buffered aspirin tablets
 Buffer containing potassium cations inhibit the drug absorption
e.g. vitamin B2 & sulphanilamide
5/30/2018 17
SURFACTANTS
 They may enhance or retard drug absorption
1. Promotion of wetting & dissolution of drugs
2. Better membrane contact of drug for absorption
3. Enhanced membrane permeability of the drug
5/30/2018 18
Product age and storage conditions
• Product aging and improper storage
conditions adversely affect B.A.
E.g. –precipitation of drug in solution
decrease rate of drug dissolution
& absorption .
5/30/2018 19
CONCLUSION
• Absorption plays an major role to attain the desired
therapeutic action with minimal side effects at the given
period of time.
• Formulation factors influencing drug absorption helps us to
focus on formulating drug with proper attainment of
permeability of drugs to systemic circulation at given time
5/30/2018 20
REFERENCE
• 1. Brahmankar D.M., Jaiswal S.B., First edition,
“Absorption of Drugs” Biopharmaceutics and
Pharmacokinetics – A treatise, Vallabh Prakashan, Delhi
1995, Page No. 5-75.
• 2. Shargel L., Andrew B.C., Fourth edition “Physiologic
factors related to drug absorption” Applied
Biopharmaceutics and Pharmacokinetics, Prentice Hall
International, INC., Stanford 1999. Page No. 99-128.
• 3. Pharmaceutics , the Science of Dosage form Design By
M.E. Aulton
• 4. Swarbrick J., Boylan J.C., “Absorption” Encyclopedia
of Pharmaceutical Technology, Marcel Dekker, INC., New
York 1988:1-32.
5/30/2018 21

Formulation factor effecting drug absorbtion

  • 1.
    FORMULATION FACTOR EFFECTING DRUGABSORBTION Presented by PRIYANKA GRESESS ANAND M.Pharm Department of Pharmaceutics INTEGRAL UNIVERSITY LUCKNOW U.P
  • 2.
    CONTENTS 1)-Introduction 2)-Manufacturing variables 3)- Typeof dosage form 4)-Pharmaceutical ingredients/excipients 5)-products life and storage condition 6)-Conclusion 7)-Reference 5/30/2018 2
  • 3.
    Introduction • To gainentry in to the blood circulation,a drug must be solubilize to pass from the absorbtion site through biological membranes. • Permeability of drug through biological membranes is closely related to the molecular structure of the drug,physicochemical characteristics,formulation factor ,and the physical and biochemical properties of the cell membrane. 5/30/2018 3
  • 4.
    DRUG ABSORBTION Definition Drug absorbtionis a pharmacokinetic parameter that refers to the way a drug is absorbed from a pharmaceutical formulation in to the bloodstream. In general,lipid soluble drugs composed of smaller molecules are more likely to absorbed . the rate and extent of absorbtion mostly depends on routes of administration and the way a drug product is designed and manufactured. . 5/30/2018 4
  • 5.
    Dosage forms liketablet, capsule, powder, solution, suspension, emulsion may vary the absorption. Drug products that contain the same drug (active ingredient) may have different inactive ingredients so absorbtion of these drug from different products may flactuate. Absorbtion play a key role in determining how fast a drug produces a clinical effect. 5/30/2018 5
  • 6.
    Formulation Factor whichcan slower the rate of absorbtion of drug are mentioned below – Formulation Factors:- Manufacturing variables: - a). Method of granulation Wet granulation yields a tablet that dissolves faster than those made by other granulating methods. But wet granulation has demerit like formation of crystal bridge or chemical degradation. 5/30/2018 6
  • 7.
    b)-compression force-Higher compressionforce yields a tablet with greater hardness hence have a long D.T. but on other hand higher compression force cause crushing of drug particles into smaller ones with effective surface area which decreasesD.T.. 5/30/2018 7
  • 8.
  • 9.
    Drug formulations aredesigned to provide an attractive, stable, and convenient use of products. Decreasing order dissolution rate of different dosage forms as :- solutions>solid solutions>suspensions, capsules>coated capsules>tablets, and controlled release formulations. 5/30/2018 9
  • 10.
    5/30/2018 10 Solutions Solutions showsfaster absorption as compared to solid dosage forms. solutions are frequently used as bioavailability standards. Factor effecting absorbtion of solution:- Viscosity Solubulizer Stability surfactants
  • 11.
    5/30/2018 11 Suspensions • Adrug in a suspension is in solid form, but is finely divided and has a large surface area. • Drug particles can diffuse readily between the stomach and small intestine so that absorption is relatively insensitive to stomach emptying rate. • Liquid dosage forms, therefore, have advantages besides simple dissolution rate. However, they also have some disadvantages, including greater bulk, difficulty in handling, and perhaps reduced stability.
  • 12.
    5/30/2018 12 Capsules andtablets • These formulations differ from each other in that material in capsules is less impacted than in compressed tablets. • Once a capsule dissolves, its contents generally disperse quickly. • Tablets generally disintegrate in stages, first into granules and then into primary particles. As particle size decreases, dissolution rate increases due to of increased surface area..
  • 13.
    Pharmaceutical Ingredients/Excipients  Excipients areadded to ensure 1. Stability 2. Uniformity 3. Functionability 4. Bioavailability 5. Acceptability 5/30/2018 13
  • 14.
    Diluents  Diluents arecommonly added to tablet and capsule formulations if the required dose is inadequate to produce bulk.  Eg:-Drug-diluent interaction resulting in poor bioavailability of tetracycline & DCP 5/30/2018 14
  • 15.
    Binders and granulatingagent Promote cohesive compacts before & after compression  Eg polymeric materials like starch, cellulose derivatives, acacia, PVP, etc. COLOURANTS  Very low concentration of water-soluble dye has inhibitory effect on dissolution.  E.g. brilliant blue retards dissolution of sulfathiazole 5/30/2018 15
  • 16.
    Lubricants To aid flowof granules  To reduce interparticle friction  Sticking of particles to dies & punches  Eg:- sodium and magnesium stearates & waxes. 5/30/2018 16
  • 17.
    DISINTEGRANTS  These Agentsovercome cohesive strength of tablet & break them on contact with water which is an important for tablet to dissolve. eg MCC BUFFERS  They create right atmosphere for dissolution e.g. buffered aspirin tablets  Buffer containing potassium cations inhibit the drug absorption e.g. vitamin B2 & sulphanilamide 5/30/2018 17
  • 18.
    SURFACTANTS  They mayenhance or retard drug absorption 1. Promotion of wetting & dissolution of drugs 2. Better membrane contact of drug for absorption 3. Enhanced membrane permeability of the drug 5/30/2018 18
  • 19.
    Product age andstorage conditions • Product aging and improper storage conditions adversely affect B.A. E.g. –precipitation of drug in solution decrease rate of drug dissolution & absorption . 5/30/2018 19
  • 20.
    CONCLUSION • Absorption playsan major role to attain the desired therapeutic action with minimal side effects at the given period of time. • Formulation factors influencing drug absorption helps us to focus on formulating drug with proper attainment of permeability of drugs to systemic circulation at given time 5/30/2018 20
  • 21.
    REFERENCE • 1. BrahmankarD.M., Jaiswal S.B., First edition, “Absorption of Drugs” Biopharmaceutics and Pharmacokinetics – A treatise, Vallabh Prakashan, Delhi 1995, Page No. 5-75. • 2. Shargel L., Andrew B.C., Fourth edition “Physiologic factors related to drug absorption” Applied Biopharmaceutics and Pharmacokinetics, Prentice Hall International, INC., Stanford 1999. Page No. 99-128. • 3. Pharmaceutics , the Science of Dosage form Design By M.E. Aulton • 4. Swarbrick J., Boylan J.C., “Absorption” Encyclopedia of Pharmaceutical Technology, Marcel Dekker, INC., New York 1988:1-32. 5/30/2018 21