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201.controlled Release Oral Drug Delivery System
201.controlled Release Oral Drug Delivery System
201.controlled Release Oral Drug Delivery System
Contents
Introduction
Advantages
Disadvantages
Types
References
Terminology:
Sustained Release Drug Delivery Systems:
Sustained release constitutes any dosage form that provides
medication over an extended time to maintain therapeutic blood or tissue
levels of the drug.
improvement in
tolerability
Reduction in healthcare cost
Maximum utilization of drug enabling reduction in total
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Implant
10%
Oral CR
60%
Inhalation
27%
Protein Binding:
Distribution:
The distribution of drugs into tissues can be one important factor in the overall
drug elimination kinetics, since it not only lowers the concentration of circulating drug but
it also can be rate-limiting in its equilibration with blood and extracellular fluid.
Metabolism:
Hydralazine is metabolized by the intestinal wall and/or the liver during
absorption, although it is well absorbed.
In contrast, Bromocriptine is incompletely absorbed, the poor bioavailability of
which is further reduced by first pass metabolism in the liver resulting in an absolute
bioavailability of only 6%.
Advantages
Total dose is low.
Reduced GI side effects.
Reduced dosing frequency.
Better patient acceptance and compliance.
Less fluctuation at plasma drug levels.
More uniform drug effect
Improved efficacy/safety ratio.
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Disadvantages
Dose dumping.
Reduced potential for accurate dose adjustment.
Need of additional patient education.
Stability problem.
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Dissolution Definition:
Mass transfer from solid to liquid.
Rate determining step: Diffusion from solid to liquid.
Several theories to explain dissolution
Diffusion layer theory
Surface renewal theory
Limited solvation theory.
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Matrix Type
Also called as Monolith dissolution controlled
system.
Soluble drug
polymer.
extentabs.
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Slowly
dissolving
matrix
Encapsulation
Called as Coating dissolution controlled
system.
Soluble drug
irritation.
used.
Repetabs
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Slowly
dissolving
or erodible
coat
Diffusion
Major process for absorption.
No energy required.
Drug molecules diffuse from a region of higher concentration to lower
membrane.
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These
systems
are
hallow
containing an inner core of drug
surrounded in a water insoluble
polymer membrane.
The polymer can be applied by
coating
or
microencapsulation
techniques .
Mechanism ....partitioning the drug
in
to
the
membrane
with
subsequent
release
in
to
surrounding fluid by diffusion.
Disadvantage..
Polymers .HPC,
ethyl
cellulose
Dose
dumping
polyvinyl acetate.
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membrane.
of parts of membrane.
Insoluble
membrane
Entry of
dissolution
fluid
Drug
diffusion
system.
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Pore created by
dissolution of
soluble fraction of
membrane
2.
1.Effervescent/gas generating
system:
gas generation increases size of DS
&decreases density.
Types: 1.conventional matrix tablets.
2.Layered matrix tablets.
3.core-coated tablets.
Prepared by:chitosan,NaHco3,citric
acid.
a)Swelling/expanding system.
b)Inherently low density system
weight as retention
eg.Feo,Tio2,Baso4
Attached to mucin
REFERENCES
Novel drug delivery system , volume 50,
Y.W.Chien
The theory & practice of industrial pharmacy,
Thank you
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NKV