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    ORAL CONTROLLED DRUG DELIVERYSYSTEMS

    Presented by:

    SOUMYA MISSULAM.Pharm

    Asst. ProfessorNRI College of PharmacyPothavarappadu (V), Agiripalli(M),

    Krishna District, A.P,India

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    CONTENTS

    Introduction

    Advantages

    Disadvantages

    Development of various Novel drug deliverysystems

    Conclusion

    References

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    Oral Controlled Drug Delivery Systems (OCDDS

    ) is a drug delivery system that

    provides continuous oral delivery of drug in a PREDICTABLE &

    REPRODUCIBLE KINETICS for a preterm delivery.

    ADVANTAGES: Reduction in dosing frequency

    Reduced fluctuations in circulating drug levels

    Increased patient compliance or acceptance

    Avoidance of night time dosing

    More uniform effect Reduction in GI irritation and dose-related side effects

    DISADVANTAGES:

    Highly expensive

    Unpredictable and often poor invivo-invitro correlation Dose dumping

    Reduced potential for dosage adjustment

    Increased potential for first-pass clearance

    Poor systematic availability

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    Compounds that are unsuitable for design:

    Drugs with elimination half-life less than 2 hours

    Those drugs that are administered in large doses

    Drugs whose therapeutic index is narrow Poorly water-soluble drugs (dissolution-rate limited)

    Drugs with long elimination half-life

    Drugs which undergo extensive first-pass clearence

    Compounds available in controlled release form:

    Vitamins

    Hormones

    Tetracycline

    Caffeine

    Reserpine

    Isosorbide di nitrate Phenobarbital

    Aspirin

    Aminophylline etc.,

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    DEVELOPMENT OF VARIOUS NOVEL DRUG DELIVERY SYSTEMS FOR

    ORAL CONTROLLED-RELEASE DRUG ADMINISTRATION:

    1. Osmotically controlled-release delivery systems

    a.Osmotically controlled DDS with single compartment

    b.Osmotically controlled DDS with two compartment

    c.Osmotic bursting

    d.Hydro dynamic pressure controlled by DDS

    2. Membrane permeation controlled delivery systems

    a. Microporous membrane permeation

    b. Gastric fluid resistant intestine-targeted delivery systems

    3. pH controlled delivery systems

    4. Ion-exchange delivery systems

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    5.Gel Diffusion controlled delivery systems

    6. Hydrodynamically Balanced systems

    7. Modulation of GI transit time

    Swelling systems

    Expanding systems

    Floating systems

    Inflatable systems

    Bio(muco)adhesive systems

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    1.Osmotically Controlled Release Systems:

    Osmotically Controlled Release DDS with single compartment:

    Osmotic delivery orifice

    Osmotic core containing drug

    Semi-permeable membrane

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    Rate of drug delivery from orifice is given by..,

    (Q/t)z = Pw AM(s-e) SD

    hM

    Where,

    PW = water permeability

    AM =Effective surface area

    hM = Thickness of membrane

    s=Osmotic pressure of Saturated solution of the drug or the salt

    c = Osmotic pressure of GI fluidSd = Solubility of the drug

    Osmotic Pressure Controlled DDS with 2 compartments

    Osmotically active compartment absorbs water from the GI fluid to create

    an osmotic pressure.

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    Drug delivery through orifice

    Semi-permeable coating

    Drug reservoir

    Movable partition

    Osmotically active compartment

    Drug release from orifice follows ZERO ORDER KINETICS

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    Hydrodynamic Pressure Controlled GI DDS:

    Liquiddrug

    formulation

    Drug delivery orifice

    Annular openings

    Shape retaining house

    SwellSable hydrophilic laminate

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    Absorption causes laminate to SWELL & EXPAND which generates

    HYDRODYNAMIC PRESSURE in the system.

    PUSH-PULL osmotic systems.

    2.Membrane permeation Controlled GI DDS:

    a.Microporous membrane permeation

    TABLET

    GI FLUID MICROPOROUS

    MEMBRANETABLET

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    b. Gastric fluid resistant intestine-targeted delivery systems

    Gastric fluid

    Liable drug

    Gastric fluid

    Liable drug

    DRUG

    GastricemptyingStomach

    pH < 3

    Intestinal fluid

    pH >7.5Insoluble

    polymer

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    Drug + buffer + excipient

    Film forming polymer

    3.pH CONTROLLED GI DDS:

    Designed for controlled release of ACIDIC or BASIC drugs in GI tract at

    rate independent of the variation in GI pH

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    DRUG ION exchange resin granules

    Polymer coating

    Ex: Drug resin complex of phenylpropanolamine administered once every 12 hrs

    for 2 weeks.

    The rate of drug release is not dependent upon the pH conditions, enzyme

    activates and temperature or volume of GIT

    The system is administered in the form of large number of particles which may

    eliminate the effect of gastric emptying

    Can be formulated as a stable liquid suspension type of pharmaceutical dosage

    form

    4.ION EXCHANGE RESIN SYSTEMS:

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    GEL DISFUSSION CONTROLLED GI DDS

    COATING LAYER

    SEALING LAYER

    CROSS-LINKED CMC LAYER

    DRUG LOADED CMC LAYER

    GEL FORMING SYSTEMS ARE

    MULTILAMINATED DEVICES

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    HYDRODYNAMICALLY BALANCED SYSTEMS (FLOATING TABLET)

    Hydro colloids d 1ColloidalGelbarrier

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    7.Modulation of GI transit time:

    a) Swelling systems:

    they contain either tablets or capsules containing gelatin or reactionproducts of gelatin.

    they attain larger size than pylorus.

    b) Expanding systems:

    It is prepared by compressing medicated polymer layer between two

    layers of water insoluble polymer

    It is rolled into configuration by gelatin band.

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    c) Floating systems:

    They contain floating chamber filled with vacuum or harmless air.

    The drug reservoir is enclosed inside micro porous compartments

    d)Inflatable systems:

    Fabricated by loading inflatable chamber with a drug

    reservoir, which is impregnated-drug polymeric matrix and then

    encapsulated into a capsule.

    Floatation chamber

    Drug reservoir

    aperture

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    capsule

    Drug reservoir

    Inflatable chamber

    INFLATABLE SYSTEMS:

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    e)Bio (muco) adhesive systems:

    The system is coated with muco adhesive polymer which binds with Mucin.

    Characters required for the biomucous adhesive polymer:

    1.Have molecular flexibility.

    2.Should contain hydrophilic functional polymers.

    3.Should posses a specific mol.wt, chain length and conformation

    Examples:CMC, Carbopol, Tragacanth , HPMC, Acacia, Gelatin, Pectin etc.

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    CONCLUSION:

    CONTROLLED ORAL DELIVERY provide effective local aswell as systemic drug levels at desirable sites with improved

    safety profiles.

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    REFERENCES:

    NOVEL DRUG DELIVERY SYSTEMS BY Chein

    CONTROLLED DRUG DELIVERY By Robinson

    www.pubmed.com

    www.google.com

    .

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    http://www.pubmed.com/http://www.google.com/http://www.google.com/http://www.pubmed.com/
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