Complexation and protein binding .pdf

complexationa nnd protein binding ppt b pharmacy 3 rd semster physiccal pharmacuetics

1. Complexation & Protein Binding
By Aditi
B.Pharma - 2nd year

2. Topics …
1.Introduction and Classification
2.Application of complexation
3.Methods of Analysis
4.Protein Binding
5.Complexation and drug action
6.Crystalline structure of complexes

3. 1.Introduction &
Classification .

4. Complexation :
The association between 2 or
more molecules form a non
bonded entity with a well defined
stoichiometry .
●Complexes are formed by
combination of CENTRAL
ATOM & LIGANDS.
●The mostly formed coordinates
bond and also some compounds
have forces van der waals forces
and dipole bonding .
Example : cisplatin (anticancer)

5. Classification Of Complexation...
INCLUSION
COMPLEXES
03
●Based on entrapment of guest into
host .
●No bond formation
●Also called OCCLUSION
COMPLEXES
ORGANIC
MOLECULAR
COMPLEXES
02
●Based on addition mechanism
●Non covalent bonds formation
METAL ION
COMPLEXES
01
●Based on donor and acceptor
mechanism
●Covalent bond formation
●COORDINATING COMPOUNDS

6. Organic
molecular
complexes
●Quinhydrone
type
●Picric acid type
●Caffeine type .
●Polymeric
complexes
COORDINATING
COMPLEXES
●Inorganic
complexes
●Chelates type
●Olefin type
●Aromatic type





Inclusion complexes
●Clathrate complexes
●Channel lattice
complexes
●Layer type complexes
●Monomolecular and
macromolecular
complexes

7. Chelates type

A group of metal
complex ion in
which a ligand
provides 2 or more
sites for combine
with a central
metal atom
EXAMPLE : EDTA


Olefin type

Interaction of
aqueous solution
of metal ion with
olefin complexes
EXAMPLE
:SILVER OLEFIN
COMPLEX
Aromatic type
● ℼ bond complex
: EXAMPLE
iodine with
benzene
● ?????? bond
complexes :
EXAMPLE HCL &
ALCL3 WITH
TOLUENE
● SANDWICH
COMPLEXES :
EXAMPLE
FERROCENE
Inorganic
complexes

Ligand provides only
one site for binding
central metal atom

EXAMPLE :
HEXAMINE
COBALTⅢCHLORIDE
METAL ION COMPLEXES …

8. ORGANIC MOLECULAR COMPLEXES
1
Quinhydrone complex type a
They are formed when the alcohol
solution of benzoquinone and
hydroquinone is mixed in
equimolar concentration .
2
Picric acid type
Picric acid form complexes with
weak base .
EXAMPLE :BUTESIN PICRATE
COMPLEX
3
Caffeine complexes
When drug like benzocaine and
procaine form complexes with
caffeine
4
Polymeric complexes
Polymeric material such as
polyethylene glycols ,
carbowaxes , carboxymethyl
cellulose , salicylic acid forms
complexes with various drugs

9. INCLUSION COMPLEXES
Layer type
complexes

The guest molecules are
entrapped in the layer
EXAMPLE :BENTONITE
Monomolecular
complexes &
macromolecule
complexes
MONOMOLECULAR
COMPLEXES : It involve the
entrapment of a single guest
molecules in the cavity of one
host molecule .
EXAMPLE :CYCLODEXTRINS
MACROMOLECULAR
COMPLEXES :It involves
entrapment of more no. of
molecules (guest) in the cavity
of host molecules




Channel lattice
complex

The channels are formed
by crystallization of the
host molecules the guest
compounds are usually
limited to long ,
unbranched chain
compounds .
EXAMPLE : VIT.A
PALMITATE COMPLEXED
WITH UREA PREVENTS
OXIDATION
Clathrates

Compounds in which a
molecule of a GUEST
compound gets entrapped
within the cage like structure
formed by the association of
several molecules of a HOST
compound .
EXAMPLE : WATER
+ISOPROPYL ALCOHOL +
WARFARIN SODIUM =WHITE
CRYSTALLINE SOLID

10. APPLICATION OF COMPLEXATION…

11. METHOD OF ANALYSIS …
1.Stoichiometry
ratio of ligand =
metal /donor
:acceptor
2.Stability constant
of complex
Generally
estimate
2
paramete
rs .
Lorem ipsum
tempus

12. 1.Method of continuous variation
Methods
2.Distribution method
Of
Solubility method
Analysis
4.PH titration method

13. Explanation of methods of analysing …

14. PROTEIN BINDING

15. PROTEIN BINDING EXPLANATION

16. Complexation and Drug action …
1.Complexes can alter the pharmacological activity of the agents by inhibiting
interaction with receptor
2.Protein binding complexes also affect absorption, metabolism and drug action
interfacing with receptor site of action (inactive the drug )
3.The action of drug to remove toxic metals from human bodies is through
complexation reaction
4.In some cases complexation also leads to poor solubility or decreases absorption
of the drug in the body .
5.The irreversible protein binding also inhibit the drug action by not release the
drug from protein
6.EXAMPLE : completion of drug in the GIT fluids may alter and extent of drug
absorption .

17. Crystalline structure of complexes
1.Complex compounds cover the range from the quite simple inorganic salts to
elaborate metal organic hybrid material .
2.Their present uses and their potential application are diverse due
to their composition , their molecular and crystal structures and their
physical and chemical properties .
3.beside their use as chemical reactant complexes compounds are considered for
extraction process and as active agents in remedies and for drug delivery .

18. Thank you
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