COMPLEXATION AND PROTEIN BINDING. B.pharm

B pharm 2-1 sem physical pharmaceutics -1

1. COMPLEXATION AND
PROTEIN BINDING
COMPLEXATION . THIS IS A PROCESS OR TECHINQUE OF ASSOCIATION OR
COMBINATION OGF TWO OR MORE IONS MOLECULES ATOMS TO FROM COMPLEX.
COMPEX: ARE THE COMPOUND HAVING TWO COMPOUND 1 DONOR 2 ACCEPTOR
LIGNAND IS A COMPOUND CONTAIN THE LONE PAIR OF ELECTRONS ACCEPT THE
METAL ION TO FORM A COMPLEX

2. MECHANISM
•1DONOR –ACCEPTOR MECHANISM EG O2 , N2
•2 WEAK BOND AND HYDROGEN BOND ATTACHMENT
•3 PHYSICAL INTERACTION
•COMPLEXTION IN PHARMACEUTICS USED TO PHYSIOCHEMICAL
PROPERTIES ( CHEMICAL , PH) FORMULATIONS ( STABILITY , SOLUBILITY)N
•ADME PROCESS
•COMPENTS OF COMPLEXATION
•substrate ( acceptor) metal ion
•Ligand ; monodenatate1 Bidanate2 polydenote3
•Protein binding: protein + drug = complex
•By drug co-sehiveby zero order.

3. CLASSIFICATION OF COMPLEXATION
•1 . METAL ION COMPLEX 2 ORAGNIC COMPLEX 3 INCLUSSION \
•1.METAL IONCOMPEX ;
•1 INO RGANIC TYPE .they mostly provided one attachment side eg
ammonia metal+ inorganic lignand
•2 chelates. The chelates are compound more than one attachment of
metal ion egedta
•3 olefin type . These are the alkenes compexthesare oliycompunds.
Aqsolnmetal ion + lignand= complex mostly used as catalylst.
•4 AROMATIC TYPE ; metal ion combine with aromatic type like benzene
toluene egfenocence

4. Organic complex
Organic complex : Also called as addition complex because of molecules of
hydrogen are oxygen interaction of hydrogen bond covalent bond dipole moment.
Picric acid complex: the picric acid is a organic compound to use for the complex
with many drugs and any drugs it is the strongest acid also called as charge
transfer complex S1 to s2 higher electronic negativity to lower electronegativity
example. Butisin
applications :stability purpose ,new compound estimation of ceratinstudy
caffeine complex : organic compound used for the organic complex with acid
compound caffeine +acid compound
example Procaine
Applications: increase the stability of drugs, increases solubility of drug

5. polymer complex& Quinine hydrone
•poloymercomplex : This are the organic compounds polymers are
pharmaceutical additives
•Example. PEG utilisationof CMC polymer additives +drugs
•examples tanicacid
•applications: drugs slow release by 0 order
•Quininhydronecomplex :it is organic compound used for the
formation of complex with organic molecules and other HQ +
•benzoquinunalcohol solution
•applications increase the stability ofdrugs

6. inclusion type complex
inclusion type complex: Also called as entrapment complex This has two molecules systems 1 host
molecule 2 ghost molecule
Base of attachment by physical attraction
1.Channel type complex: those molecules form a channels the gas molecules enter trapedin the channel.
example urea molecules
2. Clathrates type complex: host molecule form a cage in the gas entrapped . The cage like structure and
guest trapedwith the host molecule interaction example k +
3 layer type complex :host molecules form a layer guest molecules are entrapped example hydrocarbon
4.Monomolecular type complex: single guest molecule is trapped Asprinas guest molecule
5.Micromolecular type complex multiple type of guest molecules entrapped

7. Applications of complexation &methods of
analysis
Physical state of compound liquid to solid change ,
reduction of volatility egiodine
increase the stability of drugs, increase the solubility of ,drugs increase
the chemical stability of drug
Methods of analysis: measurement of complex formation is expersedin
mathematically represents by k ,k = DC \D/c .k =equal to stability
constant. DC complex drug, D = uncomplexdrug, c= uncomplexagent ,
Methods 1. continues variation method 2. phtitration method
3 . Solubility method 4 .distribution method 5. spectroscopic method

8. continuous variation method
principle : The method is based on measurement of additive
properties like refractive index, dielectric constant .They are in different
direct constant and refractive index of molecules change in variation
occurs by different physio chemical properties
The graph changes the formation of complex formed. the graph no
changes no formation of complex.

9. PH TITRATION METHOD
•Based on pH change it is very useful to analysis complex .
•Complex between glycine and copper formation of complex ion cubric
Ion complex .when glycine is added to form a complex to release
glycine is a complexing agent decrease the PH by titration with BASE
NaOH. curve obtained to make a chemical combination

10. Solubility method&Distribution method &
Spectroscopy method
•Solubility method: presence of complexing agent PABA+ caffeine
Complexing agent is added to with combine drugs to form a complex.
Decreases solubility (pABA+ caffeine)/ PABA+ caffeine.
•Distribution method : Based on distribution of solute with between
two immiscible liquids in constant eg.i2 + ki= ki3
•Spectroscopy method : visible by uvspectroscopy. Light passes
through the solution sample and the base of the light is observed at
the peak of the drug.

11. Protein binding.
•IT is a process of complexation . Drug + protein = drug protein
complex. Protein bound drugs : bind with protein neither
metabolism nor excertedpharmalogicalinactive.
•Proteins : 1. albumin. 2. alpha acid glycoprotein 3 lipoprotein 4
globulin.
•Protein binding : 1 reversible = weak bond
•2 irreversible = strong bond = toxicity produced .
•1 ALBUMIN : FOR BIND SITE . MOST OF DRUGS I phase major
component of plasma protein. synthesis in liver .

12. PROTEINS
•2 .ALPHA -ACID GLYCOPROTEIN .
•BASIC DRUG CHLOZMAZINE , ACIDIC ; DICLOFANC NEUTRAL;
CYCLOPAM
•3 . Globulin : alpha steroids alpha 2 vitmADK
•4 BLOOD CELLS ; RBC BLOOD 40% BLOOD CELLS 95% RBC &
HEOMOGLOBIN .
•SIGINFANCE : ADME , DIAGONSIS

13. FACTORS EFFECT OF PB & COMPLEXATION
AND action
•1 drug related ; properties physio chemical con”cof drug .
•2 . Protein related : physiochemical binding . Protein low .
•3 drug interactions : displacement reaction b\w drug
4 patient related factor
•CM .ACTION ; Thermodynamically that constant enhances ,inhibit
solubility low action, absorption high, pvd,stability related , polar
distribution.

14. THANK YOU ALL BEST
•THANK YOU
• S . KALYAN B PHARM