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7/30/2019 Oral Controlled Drug Delivery
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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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