Presented By -: Amol A Pardeshi

Guided By -: Mrs. MRP Rao

AISSMS COLLEGE OF PHARMACY

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 Introduction
 Mechanism of drug release
 Formulation components of an osmotic

delivery system
 Classification of ODDS
 Factors affecting drug release rate

 References

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 Osmotically controlled drug delivery
systems utilize osmotic pressure for
controlled delivery of active agent.

Osmotic pressure :
It is colligative property of solution in which
a non-volatile solute is dissolved in a
volatile solvent.

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 Aqueous Solution
Pure
Of osmotic solutes
water

Semi permeable
membrane

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 It is defined as passage of solvent into a
solution through semi permeable
membrane .
 It can take place when a concentrated

solution is separated from a less

concentrated solution by a semi permeable
membrane.

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 It involves osmosis of gastrointestinal fluid across the semi
permeable membrane at a controlled rate.
 Dissolution of drug & osmotic agent to produce a
saturated drug solution within a tablet core.
 As the no. of molecules in solution increases, the osmotic
pressure within a tablet core increases.
 Outer coating (semi permeable membrane) is rigid.
 Therefore to reduce the osmotic pressure within the tablet,
saturated drug solution is emitted from a tablet core
through orifice.

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 The major formulation components of a
typical osmotic delivery system include :

1. Drug
2. Osmotic agents
3. Semi permeable membrane

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 Osmotic components usually are ionic
compounds consisting of either inorganic
salts or hydrophilic polymers.
 These materials maintain a concentration
gradient across the membrane.
 They also generate a driving force for the
uptake of water and assist in maintaining
drug uniformity in the hydrated formulation.

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Compound or Mixture Osmotic pressure (atm)

Sodium chloride 356

Fructose 355
Potassium chloride 245
Sucrose 150
Dextrose 82
Potassium sulphate 39
Mannitol 38
Sodium phosphate tribasic 36

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 Semi permeable membrane has important
role in controlling drug release.
 Membrane must meet several performance
criteria-:
1. Polymer must exhibit Sufficient wet strength
and water permeability so as to attain water
flux rate in the desired range.
2. Reflection coefficient (leakage of solute
through membrane) should approach the
limiting value of 1 .

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3. Membrane should be biocompatible.

e.g. Cellulose esters like cellulose acetate,

cellulose acetate butyrate, cellulose
triacetate and ethyl cellulose and
Eudragits.

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 Wicking agents -:
- It has ability to draw water in to the porous
network of a delivery device
- E.g. colloidal silicon dioxide, kaolin, titanium
dioxide, SLS, low molecular weight (PVP).
 Pore forming agents -:
- These agents are particularly used in the
pumps developed for poorly water soluble
drugs and in the development of controlled
porosity osmotic pumps.
- These pore forming agents cause the
formation of micro porous membrane.
- alkaline metal salts such as sodium chloride,
sodium bromide, potassium chloride,
potassium sulfate, potassium phosphate, etc.

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 Implantable osmotic pump.
 Oral osmotic pump.

 Implantable systems further classified as-:

1. For experimental use
2. For human use

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 For experimental use -:
ALZET-
 It is a miniature, implantable osmotic
pumps for laboratory animals.
 The pump are used to deliver homogenous
solutions or suspensions continuously at a
controlled rate for extended period.
 It consist of Drug reservoir, osmotic sleeve
& semipermeable membrane.

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Duros-:
 It is a miniature, implantable osmotic pumps for
long term , parenteral , delivery of drug in human.
 It consist of an impermeable, titanium alloy
cylinder capped on one end by semi permeable
membrane & another end by orifice for drug
delivery.
 Interior of implant contains a polymeric piston that
separates from drug reservoir.

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 These systems can be further classified as-:
 Single chamber osmotic system:
- Elementary osmotic pump
 Multi-chamber osmotic systems:
- push-pull osmotic pump
 Miscellaneous:
- Controlled porosity osmotic pumps
- Osmotic bursting osmotic pump
- Effervescent activity-based osmotic systems
- OROS- CT
- L-OROS

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Elementary osmotic pump -:
 It consist of an osmotic core containing drug
& if required osmotic agent , which is
coated with semi permeable membrane .
 When core imbibes water osmotically at a
controlled rate through semi permeable
membrane , forming a saturated drug
solution.
 The system delivers, via orifice, saturated
drug solution.

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Push-pull osmotic pump:
 It is modified elementary osmotic pump.
 It is used to deliver both poorly water soluble &
highly water soluble drug at a constant rate.
 It is resembles a standard bilayer coated tablet.
 One (upper) layer contains drug (60-80% of tablet
wt.) in formulation of polymeric osmotic agent &
other tablet excipients.
 This polymeric osmotic agent has ability to form a
suspension of drug in situ when this tablet layer
imbibes water.
 Other layer contains osmotic & colouring agent.

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 To increase the permeability of membrane , two layers of
the membrane are applied on pumps.
 The inner membrane is micro porous membrane, which is
made up of cellulosic materials containing some water
soluble pore forming agents.
 Semi permeable membrane covers this layer.
 When system is placed in an aqueous environment the
soluble components dissolve, resulting in microporous
membrane which provides greater flux of water into the
system.

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 This system is similar to elementary osmotic
pump except the delivery orifice is absent.
 When it is placed in an aqueous environment,
water is imbibed and hydraulic pressure is built
up inside until the wall ruptures and the
contents are released to the environment.
 Varying the thickness as well as area of the
semipermeable membrane can control release
of drug.
 The system is useful to provide pulsated release
of drug.

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 This is commercially important variation of EOP.
 Poorly soluble drug may precipitate at the pH of gastric fluid, when
such drug is delivered through osmotic pump it may precipitate on
the orifice.
 An effervescent compound ( potassium bicarbonate) can be
incorporated to overcome this problem.
 When delivered from the pump with the drug solution, the
bicarbonate reacts with acid in the exterior environment generating
carbon dioxide.
 The expansion of gas dispenses the precipitated drug, and
preventing the blockage of the orifice.

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 It is developed by Alza co-operation.
 It is used as a once or twice a day formulation
for targeted delivery of drugs to the colon
 It consist of an enteric coat, SPM & core.
 Core consist of two compartments

- one compartment consist of drug near to

orifice.
- Second compartment consist of osmopolymer

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 Liquid OROS controlled release systems are
designed to deliver drugs as liquid
formulations.
 It combine the benefits of extended-release
with high bioavailability.
 These are of two types -:

- L-OROS Soft cap

- L-OROS Hard cap

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 The liquid drug formulation is present in a
soft gelatin capsule, which is surrounded
with the barrier layer, the osmotic layer,
and semi permeable membrane.
 A delivery orifice is formed through these
three layers.
 When the system is in contact with the
aqueous environment, water is imbibed &
results in the development of osmotic
pressure inside the system forcing the liquid
formulation to break through the hydrated
gelatin capsule shell at the delivery orifice.

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 It is similar to L-OROS Soft cap.
 It is consists of a liquid drug layer, a barrier
layer, and an osmotic engine but present in
a hard gelatin capsule.
 Then it is coated with SPM.

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 Orifice size
 Solubility
 Osmotic Pressure

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 The size of the orifice must be larger than a
minimum size (600µ), to minimize
hydrostatic pressure.
 This is necessary step in achieving zero

order drug release.

 The size of the orifice must be smaller than

a maximum size (1 mm) , to minimize

diffusional contribution to delivery rate.

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 Mechanical drill
 Laser drill
 Indentation
 Use of leachable substances in the

semipermeable coating e.g. controlled

porosity osmotic pump

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 The tablets in which holes are to be formed are
charged in the hopper.
 The tablets drop by gravity into the slots of the
rotating feed wheel and are carried at a
predetermined velocity to the passageway
forming station
 The passageway forming station, each tablet is
tracked by an optical tracking system.
 During tracking, the beam is transmitted by
the optical tracking mechanism onto the
surface of the moving tablets

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 It moves with the moving tablets as the
mirror oscillates clockwise.
 The walls of the tablet absorb the energy of

the beam and gets heated ultimately

causing piercing of the wall thus forming
orifice.

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 The release rate depends on the solubility of the solute
inside the drug delivery system.
 Therefore, drugs should have sufficient solubility to be
delivered by osmotic delivery.
 Various solubility modifying approaches include:

- Use of swellable polymers

- Use of wicking agents
- Use of effervescent mixtures
- Use of cyclodextrin derivatives
- Use of alternative salt form

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 There is no requirement for the system to
disintegrate for the release of drug to occur.
 Delivery of drugs takes place in solution form, which
is ready for absorption.
 Delivery rate is independent of pH and outside
agitation.
 The in vivo delivery rate of drug is expected to be
same as that in vitro.
 Due to its zero order release profile it is used in
early stages of drug research, such as drug
screening, animal toxicology .

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 Special equipment is required for making an orifice
in the system.
 If the coating process is not well controlled there is a
risk of film defects, which results in dose dumping.
 Residence time of the system in the body varies with
the gastric motility and food intake.
 It may cause irritation or ulcer due to release of
saturated solution of drug.

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 Elementary osmotic pump
Brand Name API
Efidac 24 Chlorpheniramine
Acutrim Phenylpropanolamine
Sudafed 24 Pseudoephedrine

 Push-pull osmotic systems

Brand Name API
Ditropan XL ®
Oxybutynin chloride
Procardia XL® Nifedipine

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 Implantable osmotic systems

Brand Name API

Viadur® Leuprolide acetate

Chronogesic™ Sufentanil

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1. Parmar NS, Vyas SK ;Osmotic pump –A novel
drug delivery system. In: Jain NK, editor.
Advances in controlled & novel drug
delivery.1st ed, 2005. Delhi :CBS publishers.
p -18-35.
2. Wilson CG, Shah HK ;programmed drug
delivery systems & the colon. In: Rathbone
MJ, Handgraft J, Lane ME , editor. Modified
release drug delivery technology. 2nd edition,
Vol-1, USA :Informa Healthcare , p-329-330.

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3. Sinko PJ . Nonelectrolyte . In : Sinko PJ
editor. Martin’s Physical and
Pharmaceutical Science . 5th ed.
Philadelphia : Lippincott Williams and
Wilkins ;2006.p.124-137
4. Lordi NG. Sustained release dosage
forms . In : Lachman L, Lieberman HA
,Kaing JL . 3rd ed. Mumbai :Varghese
publishing house ; 1990.p.455

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5. R. K. Verma, D. M. Krishna, S. Garg.
Review article on Formulation aspects in
the development of Osmotically controlled
oral drug delivery systems , J. Control.
Release, 79, 7-27; 2002.

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Thank you

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