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DISSOLUTION

MADE BY : UDAY JOSH

DISSOLUTION
Disintegration

Deaggregation

Drug in blood or other


fluids & tissues

DISSOLUTION

Dissolution refers to a process by which a solid phase


(e.g. a tablet or capsule) goes into solution phase such
as water. It is a process in which a solid substance
solubilizes in a given solvent i.e. mass transfer from the
solid surface to the liquid phase.

DISSOLUTION

Rate of dissolution is the amount of drug substance that


goes in solution per unit time under standardized
conditions of liquid/solid interface, temperature and
solvent composition.

Usually drugs in solution could only undergo ADME and


hence exert therapeutic action
Dissolution is often the rate limiting step in the absorption
of the drugs with low solubility

OFFICIAL METHODS OF
DISSOLUTION

DISSOLUTION APPARATUSES
Type I: Basket type
Type II: Paddle type
Type III: Reciprocating cylinder type
Type IV: Flow through cell type
Type V : Paddle over disk for transdermal system
Type VI: Cylinder type apparatus
Type VII: Reciprocating holder used for variety of solid dosage
forms.
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Apparatus 1 - Basket
Applications
IR dosage forms of soluble
drugs
Capsules
Beads
Delayed release / enteric
coated dosage forms
Floating dosage forms
Surfactants in media
pH change by media addition
or replacement
Standard parameters
900/1000 ml
1, 2, 4 liter vessels
50-100 rpm
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Apparatus 1 - Basket
Advantages

Broad experience
(more than 200
monographs)
Easy to operate
Robust
Can be easily automated
which is important for
routine investigations

Disadvantages
Hydrodynamic
dead
zone
under the basket, degassing is
particularly important
Formulation
screen

may

clog

the

Small disintegrated particles fall


out

Apparatus 1 - Basket

Apparatus 2 - Paddle
Method of first
choice !!!
Useful for
IR dosage forms of soluble
drugs
Tablets
Capsules
Beads
Delayed release / enteric
coated dosage forms

Standard parameters
900/1000 ml volume
50-75 rpm
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Sinker types
A small loose piece of nonreactive material such as not more than a
few turns of wire helix may be attached to dosage units that would
otherwise float . other validated sinker devices may be used

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Apparatus 2 - Paddle
Advantages
Easy to use
Robust
Can be easily adapted
to apparatus 5
Can be easily automated
which is important for
routine investigations

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Apparatus 2 - Paddle
Disadvantages
pH/media change is often difficult
Positioning

of

the

dosage

form

is

important.

Hydrodynamics vary with site of the dosage form in the


vessel (sticking, floating) and therefore may significantly
affect drug dissolution
Cone formation
Sinkers for floating dosage forms

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Coning

Apparatus 2 - Paddle

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Apparatus 3 Reciprocating
cylinder
Vessels: Cylindrical flat-bottomed
glass
Glass reciprocating cylinders: Inert
fittings and screens at the top and
bottom of the cylinders
Useful for
Tablets
Beads
Modified release formulations
Standard volume
200-250 ml per station

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Apparatus 3 Reciprocating
cylinder
Advantages
Media change fully automated
Ease of sampling
Suitable for QC testing of
products
Small media volumes suitable for
generating pH profiles
Hydrodynamics more similar to
those in the gastrointestinal tract
Disadvantages
Small volume (max. 250 ml)
Little experience
Surfactants cause foaming
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Apparatus 3 Reciprocating
cylinder

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Apparatus 4 FlowThrough Cell


Useful for

Low solubility drugs


Microparticles
Implants
Suppositories
Controlled release
formulations

Variations
Open system
Closed system
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Apparatus 4 Flow-Through
Cell

Advantages

Unlimited fluid supply makes


it ideal for testing poorly
soluble drugs
Gentle hydrodynamic
conditions and possibility of
varying hydrodynamics
during the test
Allows for rapid media change
Continuous sampling

Disadvantages
Deaeration necessary
High volumes of media
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Apparatus 4 Flow-Through Cell

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Cell types

Apparatus 5 Paddle over disk


Useful for

Transdermal patches
Standard volume
900 ml

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Apparatus 5 Paddle over


disk
Advantages

Standard
equipment
(paddle) can be
used, only add a
stainless steel disk
assembly
Disadvantages
Disk assembly

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Apparatus 6 Rotating cylinder


USP apparatus 7 Reciprocating
holder
Uses

vessel

assembly

from

Apparatus 1 but replaces basket


and shaft with a stainless steel
cylinder stirring element
Temperature: 32C
Dosage unit is placed on the
cylinder with release side out
Drug

products:

Reservoir

transdermal patches
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USP apparatus 7
Reciprocating holder
Similar to Apparatus 3 but with
different dimensions
Temperature:

32C

(for

transdermal dosage forms)


Various

devices

to

hold

transdermal patches, tablets,


capsules, implants
Speed: 20-50 dpm
Reciprocation through 2cm
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Summary
Immediate release dosage forms:

Apparatus 1 or 2 (preferably 2)
Controlled release dosage forms:

Apparatus 1 or 2 using different media


for QC
Apparatus 3 or 4 for R&D purposes
Beside the selection of an adequate
dissolution apparatus, adequate test
conditions are crucial for all purposes !
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THANK
YOU