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Controlled Release Oral Drug Delivery System. Dr. Basavaraj K. Nanjwade M.Pharm., Ph.D Professor of Pharmaceutics Department of Pharmaceutics JN Medical College KEL University, Belgaum- 590010, Karnataka, India E-mail: Cell No: 00919742431000. Contents.

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controlled release oral drug delivery system

Controlled Release Oral Drug Delivery System

Dr. Basavaraj K. Nanjwade M.Pharm., Ph.D

Professor of Pharmaceutics

Department of Pharmaceutics

JN Medical College

KEL University, Belgaum- 590010, Karnataka, India


Cell No: 00919742431000

  • Overview of Digestive system
  • Introduction
  • Advantages
  • Disadvantages
  • Mechanisms



3.Combination of Dissolution & Diffusion

4.Osmotic pressure controlled system

  • References

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digestive system
Digestive System

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  • Controlled drug delivery is one which delivers the drug at a predetermined rate, for locally or systemically, for a specified period of time.
  • Continuous oral delivery of drugs at predictable & reproducible kinetics for predetermined period throughout the course of GIT.

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plasma concentration time profile
Plasma concentration time profile

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challenges in oral drug delivery
Challenges in Oral Drug Delivery
  • Development of drug delivery systemDelivering a drug at therapeutically effective rate to desirable site.
  • Modulation of GI transit timeTransportation of drug to target site.
  • Minimization of first pass elimination

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  • 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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  • Dose dumping.
  • Reduced potential for accurate dose adjustment.
  • Need of additional patient education.
  • Stability problem.

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mechanism aspects of oral drug delivery formulation
Mechanism aspects of Oral drug delivery formulation

1.Dissolution :1.Matrix


2.Diffusion :1.Matrix


3.Combination of both dissolution & diffusion.

4.Osmotic pressure controlled system

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dissolution definition
Dissolution Definition:
  • Solid substances solubilizes in a given solvent.
  • Mass transfer from solid to liquid.
  • Rate determining step: Diffusion from solid to liquid.
  • Several theories to explain dissolution –

Diffusion layer theory (imp)

Surface renewal theory

Limited solvation theory.

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noyes whitney equation
Noyes Whitney Equation

dc/dt = kD.A (Cs – C )

dc/dt = D/h A. (Cs – C)

dc/dt = Dissolution rate.

k= Dissolution rate constant (1st order).

D = Diffusion coefficient/diffusivity

Cs = Saturation/ maximum drug solubility.

C =Con. Of drug in bulk solution.

Cs-C=concentration gradient.

h =Thickness of diffusion layer.

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matrix type
Matrix Type
  • Also called as Monolith dissolution controlled system.
  • Controlled dissolution by:

1.Altering porosity of tablet.

2.Decreasing its wettebility.

3.Dissolving at slower rate.

  • First order drug release.
  • Drug release determined by dissolution rate of polymer.
  • Examples: Dimetane extencaps, Dimetapp extentabs.

Soluble drug

Slowly dissolving matrix

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  • Called as Coating dissolution controlled system.
  • Dissolution rate of coat depends upon stability & thickness of coating.
  • Masks colour,odour,taste,minimising GI irritation.
  • One of the microencapsulation method is used.
  • Examples: Ornade spansules, Chlortrimeton Repetabs

Soluble drug

Slowly dissolving or erodible coat

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  • Major process for absorption.
  • No energy required.
  • Drug molecules diffuse from a region of higher concentration to lower concentration until equilibrium is attainded.
  • Directly proportional to the concentration gradient across the membrane.

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matrix diffusion types
Matrix Diffusion Types
  • Rigid Matrix Diffusion

Materials used are insoluble plastics such as PVP & fatty


  • Swellable Matrix Diffusion

1. Also called as Glassy hydrogels.Popular for sustaining

the release of highly water soluble drugs.

2. Materials used are hydrophilic gums.

Examples : Natural- Guar gum,Tragacanth.

Semisynthetic -HPMC,CMC,Xanthum gum.

Synthetic -Polyacrilamides.

Examples: Glucotrol XL, Procardia XL

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matrix system
Matrix system

Rate controlling step:

Diffusion of dissolved drug in matrix.

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higuchi equation
Higuchi Equation

Q = DE/T (2A.E Cs)Cs.t)1/2

Where ,

Q=amt of drug release per unit surface area at time t.

D=diffusion coefficient of drug in the release medium.

E=porosity of matrix.

Cs=solubility of drug in release medium.

T=tortuosity of matrix.

A=concentration of drug present in matrix per unit


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reservoir system
Reservoir System
  • Also called as Laminated matrix device.
  • Hollow system containing an inner core surrounded in water insoluble membrane.
  • Polymer can be applied by coating or micro encapsulation.
  • Rate controlling mechanism - partitioning into membrane with subsequent release into surrounding fluid by diffusion.
  • Commonly used polymers - HPC, ethyl cellulose & polyvinyl acetate.
  • Examples: Nico-400, Nitro-Bid

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reservoir system19
Reservoir System

Rate controlling steps :

Polymeric content in coating, thickness of coating, hardness of microcapsule.

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dissolution diffusion controlled release system
Dissolution & Diffusion Controlled Release system
  • Drug encased in a partially soluble membrane.
  • Pores are created due to dissolution of parts of membrane.
  • It permits entry of aqueous medium into core & drug dissolution.
  • Diffusion of dissolved drug out of system.
  • Ex- Ethyl cellulose & PVP mixture dissolves in water & create pores of insoluble ethyl cellulose membrane.

Insoluble membrane

Entry of dissolution fluid

Drug diffusion

Pore created by dissolution of soluble fraction of membrane

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osmotic pressure controlled drug delivery system
Osmotic Pressure Controlled Drug Delivery System
  • Definition
  • Procedure
  • Diagram
  • Modifications

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- Movement of solvent from lower to higher concentration.

- The passage of solvent into a solution through semipermeable membrane.

Semipermeable Membrane

Molecules are permitted only to one component (Water).

Osmotic pressure

It is the hydrostatic pressure produced by a solution in a space divided by asemipermeable membrane due to difference in concentration of solutes.

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osmotic pressure controlled system
Osmotic Pressure Controlled System
  • Provides zero order release
  • Drug may be osmotically active, or combined with an osmotically active salt (e.g., NaCl).
  • Semipermeable membrane usually made from cellulose acetate.
  • More suitable for hydrophilic drug.
  • Examples: Glucotrol XL, Procardia XL,

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(Q/t) z = Pw Am/ hm (πs-πe )

(Q/t)= Rate of zero order drug release.

Pw, Am & hm= water permeability, effective surface

area & thickness of semipermeable membrane.

πs= osmotic pressure of saturated solution of

osmotically active drug or salt in system.

πe = osmotic pressure of GI fluid.

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osmotic pressure controlled system25
Osmotic Pressure Controlled System

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osmotic pressure controlled system26
Osmotic Pressure Controlled System

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- Immediate release system.

- Osmotically active compartment system

immediate release system
Immediate Release System
  • Activation of system is done.
  • Dividing a dose into two parts.
  • One third immediate release.
  • Two third controlled release.
  • Encapsulated into semipermeable membrane.

e.g. : Phenyl propanolamine.

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osmotically active system
Osmotically active system
  • Two compartments separated by movable partition.
  • Osmotically active compartment absorbs water from GIT.
  • Creates osmotic pressure.
  • Partition moves upward & then drug releases.
  • Ex: Nifedipine.

Delivery orifice

Drug compartment

Movable partition

Osmotically active compartment

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some popular brand names used for ocdds
Some Popular Brand names used for OCDDS
  • Spansule capsule ( SK & F )
  • Sequal capsule (Lederle )
  • Extentab tablets ( Robins )
  • Timespan tablet ( Roche )
  • Dospan tablet ( Merrell Dow )
  • Chronotab tablet ( Schering )
  • Plateau capsule ( Marion )
  • Tempule capsule ( Armour )

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some examples of ocdds
Some Examples of OCDDS
  • Propranolol (Inderal LA)
  • Methyiphenidate HCl (RitalinSR)
  • Iron (Slow-Fe)
  • GITS-Prazosin (Minipress)
  • Morphine sulfate (Roxanol SR)
  • Decongestant & antihistamine (Resaid SR, Novafed SR Dristan)
  • Pseudoephedrine HCI (Sudafed SA)
  • Potassium (Micro-K, Slow-K, Klotrix)
  • Antitussive combinations (Rescap, Ornade Spansules)
  • Chlorpheniramine maleate (ChlorTrimeton)
  • Decongestant, antihistamine and anticholinergic (Dallergy, Supres)

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recent trends extended release formulation of bupropion
Recent Trends : Extended release formulation of Bupropion
  • Bupropion is used in the treatment of major depressive disorder.
  • Conventional formulation has to be administered 3 times daily
  • Initially 150 mg ER formulation was introduced for bid regimen

Later on 300 mg ER formulation was introduced for once daily regimen

  • For ER formulation provide similar Cmax and AUC values as compared to immediate release formulation at steady state.

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recent trends oros technology alza corporation
Recent Trends: OROS Technology (ALZA corporation)


  • Single layer tablet: Drug

core (water soluble drug

with or without excipients)

  • Semipermeable membrane

with a drilled orifice

  • Water imbibition by the core

because of osmotic action

results in drug dissolution,

which is released at a

controlled rate through the


  • Not suitable for water insoluble drugs.
  • Examples: Sudafed 24

hours (Pseudoephedrine); Volmax (Salbutamol)

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recent trends geomatrix sky parma
Recent trends: Geomatrix® (SKY Parma)

Products in market:

Cordicant -uno®

Madopar DR


  • This technology Controls amount, timing and location of release in body.
  • -Formulation with predictable and
  • reproducible drug release profile.
  • Controls rate of drug diffusion
  • throughout release process,
  • ensuring 100% release Products

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  • Novel drug delivery system , volume 50,


  • The theory & practice of industrial pharmacy,

Leon Lachman , Herbert A.Lieberman,

Joseph L.Kanig,3 rd edition.

  • The Eastern pharmacist, november 1993.

Sustained release drugs, V R.Gudsoorkar & D.Rambhau

page 27-32

  • Biopharmaceuitics & pharmacokinetics,

D M.Brahmankar & Sunil B. Jaiswal.

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Thank you for listening me………

Nepal Pharmaceutical Ltd., Nepal