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BIOPHARMACEUTICS &
PHARMACOKINETICS
Biopharmaceutical Consideration in
Dosage form Design
FACTORS AFFECTING GI ABSORPTION OF
DRUG FROM ITS DOSAGE FORM
Dept. of Pharamceutics, KCP, CBE - 32
DRUG SOLUBILITY & DISSOLUTION RATE
Dept. of Pharamceutics, KCP, CBE - 32 Physicochemical Properties of Drug Substances
DRUG SOLUBILITY & DISSOLUTION RATE
Dept. of Pharamceutics, KCP, CBE - 32 Physicochemical Properties of Drug Substances
THEORIES OF DRUG DISSOLUTION
1. Solution of the solid to form a thin film or layer at the solid / liquid
interface called Stagnant film or diffusion layer which is saturated with
the drug; this step is usually rapid
2. Diffusion of the soluble solute from the stagnant layer to the bulk of the
solution; this step is slower and is therefore the rate determining step in
drug dissolution
Diffusion layer model / Film Theory
THEORIES OF DRUG DISSOLUTION
This is the simplest and most common theory of dissolution.
Here the process of dissolution of solid particles in a liquid, in t
he absence of reactive or chemical forces, consecutive two steps
Diffusion layer model / Film Theory
THEORIES OF DRUG DISSOLUTION
Non sink conditions :-
Modified noyes-whitney’s equation represents the first order dissolution process,
the driving force which the concentration gradient (Cs- Cb), and this condition is
said as non sink condition , done only for in-vitro
Sink conditions :-
The in-vivo dissolution is always rapid than in-vitro dissolution because the
moment the drugs dissolves , it is absorbed in the systemic circulation , as a
jresult Cb= 0 and the dissolution is at maximum.
HIXON-CROWELL CUBE ROOT RELATIONSHIP
Dept. of Pharamceutics, KCP, CBE - 32
DANCKWERT’S MODEL/PENETRATION OR
SURFACE RENEWAL THEORY
Dept. of Pharamceutics, KCP, CBE - 32
DANCKWERT’S MODEL/PENETRATION OR
SURFACE RENEWAL THEORY
Dept. of Pharamceutics, KCP, CBE - 32
INTERFACIAL BARRIER MODEL
Dept. of Pharamceutics, KCP, CBE - 32
PARTICLE SIZE & SURFACE AREA
Dept. of Pharamceutics, KCP, CBE - 32
PARTICLE SIZE & SURFACE AREA
Dept. of Pharamceutics, KCP, CBE - 32
Three Reasons has been suggested for such an outcome
The hydrophobic surface of the drugs adsorbs air on to th
eir
surface which inhibits their wettability
PARTICLE SIZE & SURFACE AREA
The particles reaggregates to form large particles
due to their high
surface free energy, which either float on the sur
face or settle on the
bottom of the dissolution medium.
Electrically induced agglomeration owing to surf
ace charges prevents intimate contact of the dru
g with the dissolution medium
Dept. of Pharamceutics, KCP, CBE - 32
01 02
Use of surfactant as a wetting age
nt which
- decrease the interfacial tentio
n.
- displace the absorbed air with
the solvent.
Ex… Tween 80 on Phenacetin
PARTICLE SIZE & SURFACE AREA
 The absolute surface area of the hydrophobic drugs can be converted to their effectiv
e surface area by
Add hydrophilic diluents like P
EG, PVP,
dextrose etc. which coat the sur
face of
hydrophobic drug particles.
01 02
Molecular dispersion /Solid sol
ution where
the sparingly soluble drug is m
olecularly
trapped in the lattice of a hydro
philic agent such as Cyclodextri
ns
 In addition to increasing the dissolution rate, the second mechanism by which a redu
ction in particle
size improves drug dissolution is through an increase in its solubility
Solid dispersion where such a d
rug is
dispersed in a soluble carrier s
uch as PVP,
PEG, Urea etc.,
Dept. of Pharamceutics, KCP, CBE - 32
POLYMORPHISM & AMORPHISM
Dept. of Pharamceutics, KCP, CBE - 32
POLYMORPHISM & AMORPHISM
Dept. of Pharamceutics, KCP, CBE - 32
POLYMORPHISM & AMORPHISM
Dept. of Pharamceutics, KCP, CBE - 32
PSEUDOPLOYMORPHISM
Dept. of Pharamceutics, KCP, CBE - 32
SALT FORM OF DRUG
Dept. of Pharamceutics, KCP, CBE - 32
SALT FORM OF DRUG
Dept. of Pharamceutics, KCP, CBE - 32
Dissolution and absorption of an acidic drug administered in a salt form
SALT FORM OF DRUG
Dept. of Pharamceutics, KCP, CBE - 32
pH-PARTION HYPOTHESIS
Dept. of Pharamceutics, KCP, CBE - 32
pH-PARTION HYPOTHESIS - Drug pKa and GI pH
Dept. of Pharamceutics, KCP, CBE - 32
pH-PARTION HYPOTHESIS - Drug pKa and GI pH
Dept. of Pharamceutics, KCP, CBE - 32
LIMITATIONS OF pH-PARTION HYPOTHESIS
Dept. of Pharamceutics, KCP, CBE - 32
DRUG STABILITY
Dept. of Pharamceutics, KCP, CBE - 32
Thank you

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Factors influencing drug absorption bioavailability

  • 3. FACTORS AFFECTING GI ABSORPTION OF DRUG FROM ITS DOSAGE FORM Dept. of Pharamceutics, KCP, CBE - 32
  • 4. DRUG SOLUBILITY & DISSOLUTION RATE Dept. of Pharamceutics, KCP, CBE - 32 Physicochemical Properties of Drug Substances
  • 5. DRUG SOLUBILITY & DISSOLUTION RATE Dept. of Pharamceutics, KCP, CBE - 32 Physicochemical Properties of Drug Substances
  • 6. THEORIES OF DRUG DISSOLUTION
  • 7. 1. Solution of the solid to form a thin film or layer at the solid / liquid interface called Stagnant film or diffusion layer which is saturated with the drug; this step is usually rapid 2. Diffusion of the soluble solute from the stagnant layer to the bulk of the solution; this step is slower and is therefore the rate determining step in drug dissolution Diffusion layer model / Film Theory THEORIES OF DRUG DISSOLUTION This is the simplest and most common theory of dissolution. Here the process of dissolution of solid particles in a liquid, in t he absence of reactive or chemical forces, consecutive two steps
  • 8. Diffusion layer model / Film Theory THEORIES OF DRUG DISSOLUTION
  • 9.
  • 10. Non sink conditions :- Modified noyes-whitney’s equation represents the first order dissolution process, the driving force which the concentration gradient (Cs- Cb), and this condition is said as non sink condition , done only for in-vitro Sink conditions :- The in-vivo dissolution is always rapid than in-vitro dissolution because the moment the drugs dissolves , it is absorbed in the systemic circulation , as a jresult Cb= 0 and the dissolution is at maximum.
  • 11. HIXON-CROWELL CUBE ROOT RELATIONSHIP Dept. of Pharamceutics, KCP, CBE - 32
  • 12. DANCKWERT’S MODEL/PENETRATION OR SURFACE RENEWAL THEORY Dept. of Pharamceutics, KCP, CBE - 32
  • 13. DANCKWERT’S MODEL/PENETRATION OR SURFACE RENEWAL THEORY Dept. of Pharamceutics, KCP, CBE - 32
  • 14. INTERFACIAL BARRIER MODEL Dept. of Pharamceutics, KCP, CBE - 32
  • 15. PARTICLE SIZE & SURFACE AREA Dept. of Pharamceutics, KCP, CBE - 32
  • 16. PARTICLE SIZE & SURFACE AREA Dept. of Pharamceutics, KCP, CBE - 32
  • 17. Three Reasons has been suggested for such an outcome The hydrophobic surface of the drugs adsorbs air on to th eir surface which inhibits their wettability PARTICLE SIZE & SURFACE AREA The particles reaggregates to form large particles due to their high surface free energy, which either float on the sur face or settle on the bottom of the dissolution medium. Electrically induced agglomeration owing to surf ace charges prevents intimate contact of the dru g with the dissolution medium Dept. of Pharamceutics, KCP, CBE - 32
  • 18. 01 02 Use of surfactant as a wetting age nt which - decrease the interfacial tentio n. - displace the absorbed air with the solvent. Ex… Tween 80 on Phenacetin PARTICLE SIZE & SURFACE AREA  The absolute surface area of the hydrophobic drugs can be converted to their effectiv e surface area by Add hydrophilic diluents like P EG, PVP, dextrose etc. which coat the sur face of hydrophobic drug particles. 01 02 Molecular dispersion /Solid sol ution where the sparingly soluble drug is m olecularly trapped in the lattice of a hydro philic agent such as Cyclodextri ns  In addition to increasing the dissolution rate, the second mechanism by which a redu ction in particle size improves drug dissolution is through an increase in its solubility Solid dispersion where such a d rug is dispersed in a soluble carrier s uch as PVP, PEG, Urea etc., Dept. of Pharamceutics, KCP, CBE - 32
  • 19. POLYMORPHISM & AMORPHISM Dept. of Pharamceutics, KCP, CBE - 32
  • 20. POLYMORPHISM & AMORPHISM Dept. of Pharamceutics, KCP, CBE - 32
  • 21. POLYMORPHISM & AMORPHISM Dept. of Pharamceutics, KCP, CBE - 32
  • 23. SALT FORM OF DRUG Dept. of Pharamceutics, KCP, CBE - 32
  • 24. SALT FORM OF DRUG Dept. of Pharamceutics, KCP, CBE - 32 Dissolution and absorption of an acidic drug administered in a salt form
  • 25. SALT FORM OF DRUG Dept. of Pharamceutics, KCP, CBE - 32
  • 26. pH-PARTION HYPOTHESIS Dept. of Pharamceutics, KCP, CBE - 32
  • 27. pH-PARTION HYPOTHESIS - Drug pKa and GI pH Dept. of Pharamceutics, KCP, CBE - 32
  • 28. pH-PARTION HYPOTHESIS - Drug pKa and GI pH Dept. of Pharamceutics, KCP, CBE - 32
  • 29. LIMITATIONS OF pH-PARTION HYPOTHESIS Dept. of Pharamceutics, KCP, CBE - 32
  • 30. DRUG STABILITY Dept. of Pharamceutics, KCP, CBE - 32