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Colon Specific Drug Delivery System
 

Colon Specific Drug Delivery System

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This presentation is about colon targrte drug delivery with morden technologies and new approaches

This presentation is about colon targrte drug delivery with morden technologies and new approaches

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    Colon Specific Drug Delivery System Colon Specific Drug Delivery System Presentation Transcript

    • Seminar on
      Colonspecific
      Drug Delivery
      Prepared By:-
      Ashish Savaliya,
      M.Pharm-II P’Ceutics,
      NIMS University,Jaipur
      • milestones
      Introduction
      Anatomy of colon
      Disorders of colon
      P’Ceutical Approaches
      Platform Technologies
      Innovative Devices
      Advantages
      25-Nov-10
      NIMS University,Jaipur
      2
    • Disadvantages
      Applications
      Conclusion
      References
      25-Nov-10
      NIMS University,Jaipur
      3
      • Introduction
      25-Nov-10
      NIMS University,Jaipur
      4
      Targeted delivery of drugs to the colon is usually to achieve one or more of four objectives.
      • To reduce dosing frequency
      • To delay delivery to the colon to achieve high local concentrations in the treatment of diseases of the distal gut,
      • To delay delivery to a time appropriate to treat acute phases of disease (chronotherapy),
      • To deliver to a region that is less hostile metabolically, e.g., to facilitate absorption of acid and enzymatically labile materials, especially peptides.
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      5
      • Anatomy of Colon
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      • Disorders of Colon
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      7
      Inflammatory bowels disease
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      Ulcerative colitis
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      9
      Crohn’s disease
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      Colon Cancer
      • Colon and rectum cancer - 10% in menand 11% women
      • >55,000 Total Colorectal Cancer Deaths
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      NIMS University,Jaipur
      11
      • P’ceutical Approaches
      Covalent linkage of drug with carriers
      pH sensitive systems
      Microbial triggered systems
      Timed release systems
      Osmotic controlled systems
      Bioadhesivesystems
      Pressure dependent release systems
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      • Covalent linkage of drug with carriers
      Azo Conjugates (N = N)
      Cyclodextrin Conjugates
      Glycoside Conjugates
      DextranConjugates
      Polypeptide Conjugates
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      13
      • pH sensitive systems
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      • Mechanism of pH dependent system
      pH sensitive polymer
      Drug core
      Drug in
      Upper
      GIT
      On Reaching to COLON
      Drug core
      Drug release
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      15
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      • Microbial triggered systems
      Bacterial count in the colon is much higher around 𝟏𝟎𝟏𝟏-𝟏𝟎𝟏𝟐CFU/ml.
      400species
      Fundamentally anaerobicin nature.
      Predominant species: Bacteroides, BifidobacteriumandEubacterium.
      Major metabolic processes occurring in the colon are hydrolysis and reduction.
       
    • 25-Nov-10
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      18
      • Colonic Microflora
      Human intestinal microflora distribution in number (Log 10- scale) per gram faeces.
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      NIMS University,Jaipur
      19
      • Enzymes in Colon
      Reducing enzymes
      • Nitroreductase
      • Azoreductase
      • N-oxide reductase
      • Sulphoxidereductase
      • Hydrogenase
      Hydrolytic enzymes
      • Esterases
      • Amidases
      • Glycosidases
      • Glucuronidase
      • Sulfatase
      • Azoreductases, which reduces azo-bonds selectively and
      • Polysaccharidaseswhich degrades the polysaccharides.
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      • Timed Release Systems
      • Releases the drug after a predetermined lag time.
      • The lag time usually starts after gastric emptying because most of the time-controlled formulations are enteric coated.
      • The enteric polymer coat prevents drug release in the stomach.
      • Drug release from these systems is not pH dependent.
      • Various polymers used are: polyacrylates, methylcellulose, HPMC, CMC etc.
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      21
      Lag phase of
      ~ 5 h is
      observed.
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      22
      • Platform Technologies
      PULSINCAP
      OROS-CT
      CODES™
      PORT® SYSTEM
      TIME CLOCK® SYSTEM
      COLAL-PRED™
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      • PULSINCAP
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      24
      • OROS-CT
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      • CODES™
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      26
      • PORT® SYSTEM
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      • TIME CLOCK® SYSTEM
      • Solid dosage form coated
      with lipid barriers containing
      carnauba wax and bees wax
      along with surfactants.
      • Further coated with enteric
      coating polymer to prevent
      premature drug release, but
      the release is independent of
      pHor digestive state of the
      gut
      Wax coating with
      surfactant
      Enteric coating
      Drug core
    • 25-Nov-10
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      • COLAL-PRED™
      • Pellets containing the drug (prednisolone metasulphobenzoate) with a coating of ethylcelluloseand a specific form of amylose (derived from starch).
      • After completion of succsesfulphase I and II trials ‘Alizyme’obtained approval for Phase III clinical trial of COLAL-PREDTM in maintenance of remission of ulcerative colitis.
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      29
      • Innovative Devices
      Philips’ Intelligent pill
      Enterion Capsule
      InteliSite®capsule
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      • Philips’ Intelligent pill
      • Is device of ‘Philips research’ available in market from 2008
      • The ‘iPill’ is a capsule and it has been designed to be swallowed and to pass through the digestive track naturally. It can be electronically programmed to control the delivery of medicine according to a pre-defined drug release profile.
      • The iPilldetermines its location in the intestinal tract by measuring the local acidity (pH difference)of its environment.
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      • The iPillreleases medicine from its drug reservoir via a microprocessor controlled pump, allowing accurate programmable drug delivery.
      • The capsule is designed to measure local temperature, and report measurements wirelessly to an external receiver unit.
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      • It can be used in treatment of Crohn’s disease, Ulcerative colitis and Colon cancer.
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      • Enterion Capsule
      • The Enterioncapsule has recently been developed by Phaeton Research, Nottingham, UK, for targeted delivery of a wide range of different drug formulations into any region of the colon.
      • The capsule can be loaded with either a liquid formulation (eg. solution, suspension) or a particulate formulation (eg. powder, pellets, minitablets, etc.)
      • The floor of the drug reservoir is the piston face, which is held back against a compressed spring by a high-tensile strength polymer filament. A radioactive marker is placed inside a separate sealed tracer port to allow real-time visualization of the capsule location using the imaging technique of gamma scintigraphy.
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      • When the capsule reaches the target location in the gastrointestinal tract, the contents are actively ejected by the external application of an oscillating magnetic field.
      • This magnetic field induce power in a tuned coil antenna, embedded in capsule wall. This power is fed to a tiny heater resistor located in capsule.
      • This heater resistor increases temperature & releases the spring & drives the piston.
      • The resulting increase in pressure within the drug reservoir forces off the O-ring sealed cap and ejects the drug or drug formulation into the surrounding GI fluids.
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      • InteliSite®capsule
      • The InteliSite® capsule is an ingestible, radio-controlled device capable of delivering either liquid or powder drug formulations, on demand, to a specific region of the gastrointestinal tract.
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      • The InteliSite® capsule is loaded with a drug solution or powder formulation in a specially designed reservoir. When the capsule reaches the desired location in the gastrointestinal tract it is externally activated by remote control.
      • Activation is accomplished by exposing the capsule to a radio frequency magnetic field that induces a small amount of heat in the capsule's activation assembly. This causes two shape-memory alloy wires to straighten, rotating an inner sleeve of the capsule in relation to an outer sleeve.
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      • The rotation process aligns a series of slots in the sleeve surfaces permitting the contents to be released into the specific area of the GI tract. After activation, the InteliSite® capsule passes harmlessly through the body.
    • 25-Nov-10
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      • Advantages
      • Patient compliance and treatment efficacy
      • Useful in treatment of ulcerative colitis, crohn's disease, irritable bowel syndrome and carcinomas
      • Low dose is required ,so less side effect
      • Used for local and systemic action
      • Gastric irritation can be avoided
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      • Disadvantages
      • There is less fluid in colon than in small intestine and hence, dissolution is a problem for water soluble drugs.
      • Binding of drug to dietary residues, intestinal secretions etc., reduce concentration of free drugs.
      • Some micro flora may degrade the drug.
      • Small luminal surface area and relative tightness of tight Junctions in colon, delay the systemic absorption.
      • Onset of action is slow.
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      • Applications
      LOCAL ACTIONS
      1.    Ulcerative colitis.
      2.    CHRON'S disease.
      3.    Irritable bowel syndrome.
      4.    Metastatic human colon cancer.
      SYSTEMIC ACTIONS
      Molecules degraded/poorly absorbed from upper G.I.T such as peptides and proteins are better absorbed from colon.
      For achieving chemotherapy for diseases that are sensitive to circadian  rhythm such as Asthma, angina, arthritis.
    • 25-Nov-10
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      • Conclusion
      • Colonic drug delivery are one of the major challenges.
      • Management of Local pathologies requires efforts in decreasing or eliminating side effects .
      • Conventional dosage forms need to be drastically improved in their design.
      • Drug delivery to specific site i.e. colon is a potential alternativefor improvement in therapy.
      • Colon provides favorable factors and conditions for designing of delivery systems.
      • High commercial viability. Increasing number of international patents and research work in this particular mode of drug delivery itself shows its potential for pharmaceutical market.
    • 25-Nov-10
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      • References
      • Modified-Release Drug Delivery Technology by Michael J. Rathbone, Jonathan Hadgraft.
      • Colonic Drug Delivery by Clive G. Wilson
      • Time Dependent System For Colonic Drug Delivery by GourMukherji
      • Pulsincap System For Colonic Drug Delivery by HowardN.E.Stevens
      • The Enterion Capsule by David V. Prior, Alyson L. Connor, and Ian R. Wilding*
      • InteliSite Capsule - Data courtesy of Scintipharma, Inc. - Lexxington, Kentucky U.S.A.
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