Bioavailability and methods of enhancing bioavailabilityPresentation Transcript
BIOAVAILABILITY AND METHODS
OF ENHANCING BIOAVAILABILITY
UNDER THE GUIDANCE OF
Associate Professor. Syed Mohammed Kazim
Nizam Institute of Pharmacy & Research Centre
Deshmukhi (V), Nalgonda.
AFFILIATED TO JNTUH.
CAUSES OF LOW BIOAVAILABILITY
First pass metabolism
Poorly water soluble, slowly absorbing oral drugs
Insufficient time for absorption in GIT
Poor dissolution (highly ionized and polar)
Metabolism by luminal microflora
Methods of Enhancing Bioavailability
1.Enhancement of drug solibulity:
f. Use of surfactants
g. Molecular encapsulation with cyclodextrins
h. Eutectic mixtures
2. Enhancement of drug permeability
a. Lipid technologies
b. Ion Pairing
c. Penetration enhancers
3. Enhancement of drug stability
d. Enteric coating
f. Use of metabolism inhibitors
4. Enhancement of gastrointestinal retention
Optizorb® technology is a combination of ingredients, which work together to speed up the
rate at which the paracetamol tablet disintegrates and dissolves in the stomach.
contains paracetamol 500mg along with super-disintegrants.
The new combination disperses five times faster and is absorbed 37% faster than standard
HOT-MELT EXTRUSION TECHNOLOGY
The development of novel drugs with poor solubility and bioavailability brought
the application of HME into the realm of drug-delivery systems.
HME involves the application of heat, pressure and agitation through an
extrusion channel to mix materials together, and subsequently forcing them out
through a die.
HME extrusion has been shown to molecularly disperse poorly soluble drugs in a
polymer carrier, increasing dissolution rates and bioavailability.
ENHANCEMENT OF BIOAVAILABILITY BY
INCREASING PERMEABILITY THROUGH
NANOPARTICLE SYSTEMS WITH CHELATION AGENTS:
Increased BBB permeability and lower toxicity
Nanoparticles made of natural or artificial polymers ranging in size from about
10–1000 nm and present a possible tool to transport drugs across the BBB
The advantages of nanoparticles include reduced drug toxicity, improved
biodistribution and therapeutic efficacy
The mechanism by which the nanoparticles deliver drugs into the brain may be
involved in the preferential absorption of ApoE and/or B.
The particles also appear to mimic LDL and interact with the LDL receptor,
resulting in their uptake by brain endothelial cells
BIOAVAILABILITY ENHANCEMENT BY BBB
Fighting Alzheimer's disease with nanotechnology
FORMATION OF FIBRILS
BETA AMYLOID PEPTIDES
BREAKING THROUGH TO THE BRAIN, TO DELIVER A
CURE FOR PARKINSON’S
Nanotechnology uses a microscopic “bubble” transport system
it enables drugs to traverse the normally uncrossable blood brain barrier.
Vesicles are one of the few things in the body that can permeate the BBB,
however, pathogens are able to break down the BBB, enabling substances such
as bacteria or other toxins to attack parts of the brain
The nanovesicles are highly stable and provide a controlled release mechanism
Nano bubble releasing drug
D.M. BRAHMANKAR SUNIL B. JAISWAL Biopharmaceutics and pharmacokinetics a
Treatise,Second Edition..Page No:345-363
CVS SUBRAHMANYAM. Text book of Biopharmaceutics and pharmacokinetics .
Wilson CG, Clarke CP, Starkey YY, Clarke GD. Comparison of a novel fast-dissolving acetaminophen
Martin physical pharmacy and pharmaceutical sciences 5th edition
Leon shargel.applied biopharmaceutics and pharmacokinetics
Pharmacokinetic and Bioequivalence Study Evaluating a New Paracetamol/Caffeine Formulation in
Healthy Human Volunteers Dongzhou J. Liu1 *, Mitchell Kotler1 and Scott Sharples2 1Medical Affairs
and New Products Research and Development, GlaxoSmithKline, Parsippany, NJ 07054, USA 2Celerion,
2420 W Baseline Rd, Tempe, AZ 85283, USA
• Wilson CG, Clarke CP, Starkey YY, Clarke GD. Comparison of a novel fast-dissolving
• Martin physical pharmacy and pharmaceutical sciences 5th edition
• Leon shargel.applied biopharmaceutics and pharmacokinetics 4th Edition.
• Pharmacokinetic and Bioequivalence Study Evaluating a New Paracetamol/Caffeine
Formulation in Healthy Human Volunteers Dongzhou J. Liu1 *, Mitchell Kotler1 and
Scott Sharples2 1Medical Affairs and New Products Research and Development,
GlaxoSmithKline, Parsippany, NJ 07054, USA 2 Celerion, 2420 W Baseline Rd, Tempe,
AZ 85283, USA
• Milogibaldi, Biopharmaceutics and clinical pharmacokinetics 4th Edition Page no 146.
• Venkateshwarlu, Fundamentals of Biopharmaceutics and pharmacokinetics Page no 331.
• Remington’s Pharmaceuticals sciences volium 1 Page no 1037
• Remington’s Pharmaceuticals sciences volium 1 Page no 1041
• Robert E Notary, Biopharmaceutics and pharmacokinetics.
• Indian Journal of Pharmaceutical sciences.