Controlled release oral drug delivery system
Download
1 / 37

Controlled Release Oral Drug Delivery System - PowerPoint PPT Presentation


  • 1269 Views
  • Updated On :

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: [email protected] Cell No: 00919742431000. Contents.

Related searches for Controlled Release Oral Drug Delivery System

loader
I am the owner, or an agent authorized to act on behalf of the owner, of the copyrighted work described.
capcha
Download Presentation

PowerPoint Slideshow about 'Controlled Release Oral Drug Delivery System' - Sophia


An Image/Link below is provided (as is) to download presentation

Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author.While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server.


- - - - - - - - - - - - - - - - - - - - - - - - - - E N D - - - - - - - - - - - - - - - - - - - - - - - - - -
Presentation Transcript
Controlled release oral drug delivery system l.jpg

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: [email protected]

Cell No: 00919742431000


Contents l.jpg
Contents

  • Overview of Digestive system

  • Introduction

  • Advantages

  • Disadvantages

  • Mechanisms

    1.Dissolution

    2.Diffusion

    3.Combination of Dissolution & Diffusion

    4.Osmotic pressure controlled system

  • References

Nepal Pharmaceutical Ltd., Nepal


Digestive system l.jpg
Digestive System

Nepal Pharmaceutical Ltd., Nepal


Concept l.jpg
Concept

  • 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.

Nepal Pharmaceutical Ltd., Nepal


Plasma concentration time profile l.jpg
Plasma concentration time profile

Nepal Pharmaceutical Ltd., Nepal


Challenges in oral drug delivery l.jpg
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

Nepal Pharmaceutical Ltd., Nepal


Advantages l.jpg
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.

Nepal Pharmaceutical Ltd., Nepal


Disadvantages l.jpg
Disadvantages

  • Dose dumping.

  • Reduced potential for accurate dose adjustment.

  • Need of additional patient education.

  • Stability problem.

Nepal Pharmaceutical Ltd., Nepal


Mechanism aspects of oral drug delivery formulation l.jpg
Mechanism aspects of Oral drug delivery formulation

1.Dissolution :1.Matrix

2.Encapsulation

2.Diffusion :1.Matrix

2.Reservoir

3.Combination of both dissolution & diffusion.

4.Osmotic pressure controlled system

Nepal Pharmaceutical Ltd., Nepal


Dissolution definition l.jpg
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.

Nepal Pharmaceutical Ltd., Nepal


Noyes whitney equation l.jpg
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.

Nepal Pharmaceutical Ltd., Nepal


Matrix type l.jpg
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

Nepal Pharmaceutical Ltd., Nepal


Encapsulation l.jpg
Encapsulation

  • 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

Nepal Pharmaceutical Ltd., Nepal


Diffusion l.jpg
Diffusion

  • 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.

Nepal Pharmaceutical Ltd., Nepal


Matrix diffusion types l.jpg
Matrix Diffusion Types

  • Rigid Matrix Diffusion

    Materials used are insoluble plastics such as PVP & fatty

    acids.

  • 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

Nepal Pharmaceutical Ltd., Nepal


Matrix system l.jpg
Matrix system

Rate controlling step:

Diffusion of dissolved drug in matrix.

Nepal Pharmaceutical Ltd., Nepal


Higuchi equation l.jpg
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

volume.

Nepal Pharmaceutical Ltd., Nepal


Reservoir system l.jpg
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

Nepal Pharmaceutical Ltd., Nepal


Reservoir system19 l.jpg
Reservoir System

Rate controlling steps :

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

Nepal Pharmaceutical Ltd., Nepal


Dissolution diffusion controlled release system l.jpg
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

Nepal Pharmaceutical Ltd., Nepal


Osmotic pressure controlled drug delivery system l.jpg
Osmotic Pressure Controlled Drug Delivery System

  • Definition

  • Procedure

  • Diagram

  • Modifications

Nepal Pharmaceutical Ltd., Nepal


Slide22 l.jpg

Osmosis

- 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.

Nepal Pharmaceutical Ltd., Nepal


Osmotic pressure controlled system l.jpg
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,

Nepal Pharmaceutical Ltd., Nepal


Equation l.jpg
Equation

(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.

Nepal Pharmaceutical Ltd., Nepal


Osmotic pressure controlled system25 l.jpg
Osmotic Pressure Controlled System

Nepal Pharmaceutical Ltd., Nepal


Osmotic pressure controlled system26 l.jpg
Osmotic Pressure Controlled System

Nepal Pharmaceutical Ltd., Nepal


Modifications l.jpg

Modifications

- Immediate release system.

- Osmotically active compartment system


Immediate release system l.jpg
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.

Nepal Pharmaceutical Ltd., Nepal


Osmotically active system l.jpg
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

Nepal Pharmaceutical Ltd., Nepal


Some popular brand names used for ocdds l.jpg
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 )

Nepal Pharmaceutical Ltd., Nepal


Some examples of ocdds l.jpg
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)

Nepal Pharmaceutical Ltd., Nepal


Recent trends extended release formulation of bupropion l.jpg
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.

Nepal Pharmaceutical Ltd., Nepal



Recent trends oros technology alza corporation l.jpg
Recent Trends: OROS Technology (ALZA corporation)

ELEMENTARY OSMOTIC PUMP

  • 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

    orifice

  • Not suitable for water insoluble drugs.

  • Examples: Sudafed 24

    hours (Pseudoephedrine); Volmax (Salbutamol)

Nepal Pharmaceutical Ltd., Nepal


Recent trends geomatrix sky parma l.jpg
Recent trends: Geomatrix® (SKY Parma)

Products in market:

Cordicant -uno®

Madopar DR

SULAR ER

  • 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

Nepal Pharmaceutical Ltd., Nepal


References l.jpg
References

  • Novel drug delivery system , volume 50,

    Y.W.Chien

  • 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.

    www.google.com

Nepal Pharmaceutical Ltd., Nepal


Slide37 l.jpg

Thank you for listening me………

Nepal Pharmaceutical Ltd., Nepal


ad