PRESENTED BY

DEORE PRASHANT ASHOK

Department of Pharmaceutics
M. Pharm. I Semester (2014-2015)

R. C. Patel Institute of Pharmaceutical Education

and Research, Shirpur .

Email-prashantdeore92@gmail.com Mo.09881261646

10/10/2014 1
 CONTENTS
 Dissolution

 Dissolution vs Solubility

 Expression of Solubility

 Drug Dissolution Process

 Theories of Dissolution

 References

10/10/2014 2
 DISSOLUTION
Dissolution is defined as a
process in which a solid
substance solubilises in a
given solvent.

(i.e. mass transfer from

the solid surface to the
liquid phase.)

10/10/2014 3
 DISSOLUTION SOLUBILITY

Dissolution rate is defined as Absolute solubility is defined

the amount of solid substance as the maximum amount
of
that goes into solution solute dissolved in a
per given
unit time under standard solvent under standard
conditions of temperature, conditions of temperature
,
pH, solvent composition pressure and pH.
and
constant solid surface area.

It is a
10/10/2014 dynamic process. It is a static process. 4
EXPRESSION OF
SOLUBILITY
DESCRIPTIVE TERM PARTS OF SOLVENT REQUIRED
FOR 1 PART OF SOLUTE

Very soluble Less than 1 part

Freely soluble 1 to 10 parts
Soluble 10 to 30 parts
Sparingly soluble 30 to 100 parts
Slightly soluble 100 to 1000 parts
Very slightly soluble 1000 to 10000 parts
Practically insoluble More than 10000 parts

10/10/2014 5
 DRUG DISSOLUTION PROCESS

10/10/2014 6
 Cont….

 The effectiveness of a tablet in the drug

releasing absorption depends on four steps - for

1. The initial step involves the breaking of a tablet

into granules (disintegration).

2. Some times, these granules further break to yield

fine
particles (deaggregation)

3. The next step involves the releasing of the drug into solution
(dissolution)

4. Absorption.
10/10/2014 7
THEORIES OF
DISSOLUTION
 Three Theories:

1. Diffusion layer model / Film theory

2. Danckwert’s model / Penetration or Surface renewal theory

3. Interfacial barrier model / Double barrier or

Limited
solvation theory

10/10/2014 8
1) Diffusion layer model

 It involves two steps :

1. Solution of the solid to form stagnant film or diffusive layer
which is saturated with the drug.
2. Diffusion of the soluble solute from the stagnant layer to the
bulk of the solution; this is rate determining step in drug
dissolution.
10/10/2014 9
 Cont….

 The rate of dissolution is given by Noyes and Whitney:

dC/dt = k (Cs- Cb)…………(1)

where,
dC/dt = dissolution rate of the
drug k = dissolution rate
constant
Cs= concentration of drug in
stagnant layer
Cb= concentration of drug in the
bulk of the
solution at time t
10/10/2014 10
 Cont….
Equation (1) was based on Fick’s second law of diffusion .
Nernst and Brunner incorporated Fick’s first law of diffusion and
modified the Noyes-Whitney’s equation to :

dC/dt = DAKw/o (Cs-Cb) …………. (2)

Vh
where,
D = diffusion coefficient of drug
A = surface area of dissolving solid
Kw/o = water/oil partition coefficient of drug
V = volume of dissolution medium
h = thickness of stagnant layer
(Cs – Cb) = conc. gradient for
diffusion of drug
10/10/2014 11
 Cont….

Limitation :
The Noyes-Whitney’s equation assumes that the surface area of the
dissolving solid remains constant during dissolution, which is practically not
possible for dissolving particles.
Hence, dissolution methods that involves use of constant surface area discs
are employed to determine the rate of dissolution.
To account for the particle size decreases and change in the surface area
accompanying dissolution, Hixson and Crowell’s cubic root law of
dissolution is used:

Wo1/3– W1/3= K.t …………(3)

where,
W = mass of drug remaining to be dissolved at time
t K = dissolution rate constant
Wo = original mass of the drug

10/10/2014 12
2) Danckwert’s model
1. Danckwert takes into account the eddies or packets that are present in the
agitated fluid which reach the solid-liquid interface, absorb the solute by
diffusion and carry it into the bulk of solution.
2. These packets get continuously replaced by new ones and expose to new
solid surface each time, thus the theory is called as surface renewal
theory.

10/10/2014 13
 Cont….

 The Danckwert’s model is expressed by equation:

V. dC/dt= dm/dt = A ( Cs-Cb). √(γ.D)……….(4)

where,
m =mass of solid dissolved
γ = rate of surface
renewal

10/10/2014 14
3) Interfacial barrier model

 The diffusion layer model and Danckwert’s model were

based on two assumptions:
1. The rate determining step that controls dissolution is the
mass transport.
2. Solid-solution equilibrium is achieved at the solid/liquid
interface. According to the interfacial barrier model, an
intermediate concentration can exist at the interface as a result
of solvation mechanism and is a function of solubility rather
than diffusion.
When considering the dissolution of a crystal, each face of
crystal will have a different interfacial barrier.

10/10/2014 15
 Cont….

 Such a concept is given by the following

equation :

G = Ki (Cs-Cb)………(5)
where,
G = dissolution rate per unit area
Ki = effective interfacial transport constant

10/10/2014 16
REFERENCES
1. Brahmankar D.M., Jaiswal S.B. (2009), “Biopharmaceutics and
Pharmacokinetics-A Treatise” Vallabh Prakashan, 2nd Edition, Page
No. 15-48

2. Government of Indian ministry of health and family welfare (2014),

“Indian Pharmacopoeia” Indian Pharmacopoeia commission,
Ghaziabad, Volume-1, Page No. 174

3. Subrahmanyam C.V.S. (2000), “Text book of Physical Pharmaceutics”

Vallabh Prakashan, 2nd Edition, Page No. 85-105

4. Banakar U.V. (1992), “Pharmaceutical Dissolution Testing” Informa

helthcare, 1st Edition, Page No. 1-30

10/10/2014 17
 Thank
You
10/10/2014 18