Oral Controlled Drug Delivery

ORAL CONTROLLED DRUG DELIVERY SYSTEMS
Presented by: SOUMYA MISSULA M.Pharm Asst. Professor NRI College of Pharmacy Pothavarappadu (V), Agiripalli(M), Krishna District, A.P, India
11/11/2012
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CONTENTS
Introduction Advantages Disadvantages Development of various Novel drug delivery systems 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 fluid Sd = 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

Drug reservoir Semi-permeable coating Movable partition Osmotically active compartment Drug release from orifice follows ZERO ORDER KINETICS
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Hydrodynamic Pressure Controlled GI DDS:
Drug delivery orifice Shape retaining house Liquid drug formulation
SwellSable hydrophilic laminate
Annular openings
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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
GI FLUID TABLET TABLET
MICRO POROUS MEMBRANE
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b. Gastric fluid resistant intestine-targeted delivery systems
Stomach pH < 3
Gastric emptying
Intestinal fluid Gastric fluid Liable drug
pH >7.5
Gastric fluid Liable drug
Insoluble polymer
DRUG
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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
Film forming polymer Drug + buffer + excipient
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4.ION EXCHANGE RESIN SYSTEMS:

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
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GEL DISFUSSION CONTROLLED GI DDS

GEL FORMING SYSTEMS ARE
MULTILAMINATED DEVICES
COATING LAYER
DRUG LOADED CMC LAYER
SEALING LAYER CROSS-LINKED CMC LAYER
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HYDRODYNAMICALLY BALANCED SYSTEMS (FLOATING TABLET)
Gastric fluid Hydro colloids d>1 d<1

Colloidal Gel barrier
It must have sufficient structure to form a cohesive gel barrier It must maintain overall specific gravity lower than that of the gastric contents (1.004 to 1.010) It should dissolve slowly enough to serve as a drug reservoir It is prepared by incorporating one or more hydrocolloids into formulation and compressing into granules.
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7.Modulation of GI transit time: a) Swelling systems: they contain either tablets or capsules containing gelatin or reaction products 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
Floatation chamber
Drug reservoir
aperture
d)Inflatable systems: Fabricated by loading inflatable chamber with a drug reservoir, which is impregnated-drug polymeric matrix and then encapsulated into a capsule.
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INFLATABLE SYSTEMS:
capsule
Drug reservoir Inflatable chamber
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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 as
well 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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ORAL CONTROLLED DRUG DELIVERY SYSTEMS

2. Membrane permeation controlled delivery systems

3. pH controlled delivery systems 4. Ion-exchange delivery systems

1.Osmotically Controlled Release Systems:

Osmotic delivery orifice

Osmotic core containing drug Semi-permeable membrane

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

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

Drug delivery through orifice

Hydrodynamic Pressure Controlled GI DDS:

Drug delivery orifice Shape retaining house Liquid drug formulation

SwellSable hydrophilic laminate

2.Membrane permeation Controlled GI DDS:

GI FLUID TABLET TABLET

MICRO POROUS MEMBRANE

b. Gastric fluid resistant intestine-targeted delivery systems

Intestinal fluid Gastric fluid Liable drug

Gastric fluid Liable drug

Film forming polymer Drug + buffer + excipient

4.ION EXCHANGE RESIN SYSTEMS:

GEL DISFUSSION CONTROLLED GI DDS

DRUG LOADED CMC LAYER

SEALING LAYER CROSS-LINKED CMC LAYER

HYDRODYNAMICALLY BALANCED SYSTEMS (FLOATING TABLET)

Gastric fluid Hydro colloids d>1 d<1

they attain larger size than pylorus.

Drug reservoir Inflatable chamber

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