Introduction
Mechanisms of protein drug binding
Kinetics of protein drug binding
Classes of protein drug binding.
1. Binding of drug to blood components.
(a) Plasma proteins
(b) Blood cells
2. Binding of drug to extravascular tissue protein
Determination of Protein-drug Binding
Factors affecting protein drug binding
Significance of protein/tissue binding of drug
The phenomenon of complex formation of drug with protein is called as Protein drug binding. The proteins are particularly responsible for such an interaction. A drug can interact with several tissue components.
Introduction
Mechanisms of protein drug binding
Kinetics of protein drug binding
Classes of protein drug binding.
1. Binding of drug to blood components.
(a) Plasma proteins
(b) Blood cells
2. Binding of drug to extravascular tissue protein
Determination of Protein-drug Binding
Factors affecting protein drug binding
Significance of protein/tissue binding of drug
The phenomenon of complex formation of drug with protein is called as Protein drug binding. The proteins are particularly responsible for such an interaction. A drug can interact with several tissue components.
Sanjo College of Pharmaceutical Studies, Physical Pharmaceutics I , 3rd semester B.Pharm, Complexation & protein binding, Classification in detail, determination methods, application of complexes in pharmacy.
R. VIJAYAKUMAR., M Pharm,
Research Scholar
department of Pharmaceutical Technology.
Anna university- BIT
Tiruchirappalli
III Semester.
UNIT-IV / Micromeritics
Solubility of drugs: Solubility expressions, mechanisms of solute solvent interactions, ideal solubility parameters, solvation & association, quantitative approach to the factors
influencing solubility of drugs, diffusion principles in biological systems. Solubility
of gas in liquids, solubility of liquids in liquids, (Binary solutions, ideal solutions)
Raoult’s law, real solutions. Partially miscible liquids, Critical solution temperature . Distribution law, its limitations and applications
The details about the elimination of the drug from the body by various methods. drug metabolism, drug transformation, drug elimination process. factors affecting.
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Suspension , types of suspension, difference between flocculated and deflocculated suspension and interfacial properties of suspended particles
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typers and sub-types, advantages,disadvantages,working of different rotational viscometers.
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4th semester B.Pharm.
Physical Pharmacuetics,
B.pharm, As per the PCI semester syllabus,
!THIS SLIDE IS SIMPLIFIED BULLETINS, USE THIS SLIDE AND REFER MORE RESPECTIVE TEXTBOOKS!.
THANK YOU:
introduction
mechanisms of protein drug binding
binding of drugs
binding of drugs to blood components
determination of protein drug binding
factors affecting
significance
Sanjo College of Pharmaceutical Studies, Physical Pharmaceutics I , 3rd semester B.Pharm, Complexation & protein binding, Classification in detail, determination methods, application of complexes in pharmacy.
R. VIJAYAKUMAR., M Pharm,
Research Scholar
department of Pharmaceutical Technology.
Anna university- BIT
Tiruchirappalli
III Semester.
UNIT-IV / Micromeritics
Solubility of drugs: Solubility expressions, mechanisms of solute solvent interactions, ideal solubility parameters, solvation & association, quantitative approach to the factors
influencing solubility of drugs, diffusion principles in biological systems. Solubility
of gas in liquids, solubility of liquids in liquids, (Binary solutions, ideal solutions)
Raoult’s law, real solutions. Partially miscible liquids, Critical solution temperature . Distribution law, its limitations and applications
The details about the elimination of the drug from the body by various methods. drug metabolism, drug transformation, drug elimination process. factors affecting.
Suspension, type of suspension, interracial property of suspended particles Dheeraj Saini
Here you find
Suspension , types of suspension, difference between flocculated and deflocculated suspension and interfacial properties of suspended particles
Rotational Viscometers,
The viscometers that used to measure the viscosity using retarding force due to the viscous drag.
typers and sub-types, advantages,disadvantages,working of different rotational viscometers.
1.cup and bob viscometer,
2.cone and plate viscometer,
plug flow development, etc.
Chapter: Rheology
4th semester B.Pharm.
Physical Pharmacuetics,
B.pharm, As per the PCI semester syllabus,
!THIS SLIDE IS SIMPLIFIED BULLETINS, USE THIS SLIDE AND REFER MORE RESPECTIVE TEXTBOOKS!.
THANK YOU:
introduction
mechanisms of protein drug binding
binding of drugs
binding of drugs to blood components
determination of protein drug binding
factors affecting
significance
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2. PROTEIN BINDING
● The phenomenon of complex formation of drug
with protein is called protein binding.
● A protein bound drug is neither metabolised
nor excreted hence it is pharmacologically
inactive.
● Protein + drug = Protein drug complex
3. Protein binding may be divided into
two groups-
● Reversible binding- The drug binds the
Protein with weak bonds such as-
hydrogen bonds or van der waals forces.
● These type of drugs can unbound and
shows its therapeutic action.
4. ● Irreversible binding- The drug binds
with protein by strong covalent
bonding and often a reason for the
carcinogenicity and toxicity.
● Order of binding of drug with
protein:
Albumin > glycoprotein >lipoprotein>
globulin
5.
6. ● Binding of drugs to albumin
2.Digoxine
1. Warfarin & site
Azapropazone
4.Diazepam
sit
3. Tamoxifen
site
7.
8. ● Significance of protein binding with drug:-
● Absorption- When there is more protein binding
by the drug then it will distrub the absorption
equilibrium.
● The rate of absorption is decreased when
protein is bind with drug.
● Distribution- The protein bound drug doesn’t
cross the BBB, placental barrier and glomerulus.
Thus it decrease the distribution of drug.
9. Metabolism- Protein binding decreases the
metabolism of drug and enhance the biological half
life. Only unbound fraction get metabolised.
Elimination- Only the unbound druf is capable of
being eliminated. Protein binding prevent the entry
of drug to the metabolizing organ (liver) and
glomerulus filtration.
Systemic solubility of drug – Lipoprotein act as
vehicle for hydrophobic drugs like steriods,heparin,
oil soluble vitamins.
10. Drug action- Protein binding inactivates the
drug because sufficient concentration of drug
cannot be build up in the receptor site for
action.
Diagnisis – The chlorine atom of chloroquine
replaced with radiolabeled l-131cab be used to
visualise melanomas of eyes and disorders of
thyroid gland.
11. Factors affecting protein binding
Drug related factors:
1. Physiochemical factors of drug- Binding affinity depend on physical and
chemical properties of drug.
Increase in lipophilicity Increase the drug binding with the protein.
2. Concentration of drug- Alteration in concentration of drug substance
as well as the protein molecules cause alteration in protein binding.
At low concentration, most drug may bound to protein.
At high concentration, more free drug may present owing to saturation
of binding site on protein.
12. 3. Affinity of drug for binding component-
● This depend on affinity of protein molecule to bind to drug.
● Eg. Digoxine hascmore affinity for protein of cardiac muscle
than those of skeletal muscles.
● Factors related to protein:
1.Physiochemical property- Lipoprotein bind with lipophilic drug.
2. Concentration of protein- Disease state affect the
concentration of protein in blood. It Increase the concentration of
protein and protein binding in the body.
13. 3.No. Of binding sites- Presence of more binding sites in protein
increase protein binding of drug.
Eg Albumin has more no. Of binding site.
● Factors related to age:
1.Age- Neonata have low albumin content thus less drug binding.
2. Disease state- Disease states increase the Albumin thus
increse protein binding.
14. Method of measuring the unbound drug concentration
● Equilibrium dialysis method
● In this method the Albumin is placed in visking cellulose bag and drug in
different concentration is placed in the outside vessel.
● As the dialysis continue, the drug molecules permeate through the
membrane and enter into the bag.
● As a result the dryg protein binding is observed. Albumin being
macromolecules can’t pass through the membrane to outside vessel.
● As time ellapsis more amount of drug permeate and available in the bag.
● If binding occurs the drug concentration in the body containing protein
should be greater than its concentration in the outside vessel.
16. 2. Dynamic dialysis method:
● The apparatus consist of a 400ml jacketed (with a temperature control)
beaker into which 200ml of buffer solution is placed.
● Around 70ml of drug (blank) and drug protein solution is placed in a dialysis
bag and suspended in the buffer solution. The solution is is stir
continuously.
● During dialysis the free drug present in the bag permeate through the
membrane and reaches the buffer solution.
● Such a transport shift the equilibrium in favour of full drug molecules in the
bag.
● Every 5 or 10 mins. Sample of solution are withdrawn from the beaker and
an equivalent quantity of buffer solution is return to the beaker
● The amount of drug present in the solution is estimated by a suitable
method (UV rays)