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Drug
release
form
matrix
Matrix erosion
Biodegradable Hydrolytic
cleavage of
polymer polymer chains
Diffusion
dC = D dc
dt dx
Implantable
depot Suspension
Examples
Oral osmotic
Transdermal Zero pressure
order
Matrix
dissolution
Solution
controlled First
release order
release
system
F = (Mt /M ) = Km tn
n= 1
Swelling controlled
Release rate independent of time.
Zero order/case II .
n= between 0.5-1
Diffusion and swelling
Release is time depended.
First order/anamolus /non-
fickian.
fig:- graph of drug release kinetics
Diffusion and
dissolution controlled Swellable & erodible
dosage form polymer.
Used
for???
when release of drug depends
upon its diffusion as well as on
fickian relaxation of polymer.
4/19/2016 sagar kishor savale 22
Table :- Describes the limits of this analysis.
0.50 < m< 1.00 0.45 < m< 0.43 < m< 0.85 Anomalous
0.89 transport
m - accumulated fraction,
b = 1 indicates exponential curve,
a - time scale process, b= 2 indicates sigmoid curve,
Ti -lag time ( generally zero), b= 3 indicates parabolic curve.
b - shape factor.
Hopfenberg Model
Mt /M = 1 [1 (kot)/ (C0a0)] n
Mt is the amt of drug dissolved in time t.
Ko is erosion rate constant.
drug release from slabs, spheres and infinite cylinder displaying
heterogeneous erosion
Graphical representation
4/19/2016
Mt/M Vs Time.
sagar kishor savale 25
HOW DO WE COME TO
KNOW WHICH MODEL IS
HOW DO WE
FIT.
USE THESE CAN ONE FORMULATION
MODELS FOLLOW DIFFERENT
EQUATIONS AT A TIME
MODEL F1 F2 F3 F4
HIGUCHI
Polymer disentanglement
Swelling/rubbery gel layer
Disentanglement + dissolution
Non fickian release
equilibrium
Rubbery- solvent
Front (S)
Water penetration
Fig: one dimensional swelling processlee fig.
Non fickian
water Case ii Zero order
transport
Diffusion +
Anomalous First order
Dissolution
Empirical Mechanistic
No
physiochemical physiochemical
phenomenon. phenomenon.
Mt =0 (, )d
M
- dispersion parameter .
- porosity of the device.
- pore size parameter, exact geometry and the encapsulated
drug .
wetting
Salt
formation
Factor
affecting
drug release
Form / state mechanism
of drug Temp
Viscosity HPMCK4M
Binders HPMC K100M
GELATIN
EC particle
size
griseofulvin
4/19/2016 sagar kishor savale 42
Release profile comparison
Statistical methods-ANOVA, MANOVA
Model independent method- AUC, etc.
Model dependent methods- all stated models.
Similarity factor(f2)
Fickian diffusion
THEORETICAL For slab ,
STANDPOINT
may be defined by spheres,cylinder
an initial t time
6. Martins physical pharmacy &pharmaceutical sciences, fifth edition, Patrick J. sinko ,lippincott
Williams & Wilkins publication ,p.337-349.
7. Compaction properties, drug release kinetics and fronts movement studies from matrices
combining mixtures of swellable and inert polymers, International Journal of Pharmaceutics,
September 2007, 6173.
8. Desai S.J, Sing P, Simonelli A.P, Higuchi W.I, Investigation of Factors Influencing Releaese of
Solid Drug Dispersed In Inert Matrices, III, Quantitative Studies involving the Polyethylene
Plastics Matrix, Journal of Pharmaceutical Sciences, 1966a, 55, 1230-1234.
9. Higuchi W.I, Analysis of Data on the Medicament Release from Ointments, J. Pharm. Sci,
1962, 51, 802 804.
10. Judit Dredin*, Istvin Antal, Istvin R/lcz .Evaluation of mathematical models describing drug
release from lipophilic matrices ,International,Journal of Pharmaceutics.