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cont... Complexation MMCP.MMDU -.ppt
1. UNIT - IV
Complexation & Protein
Binding
(CO 4)
By: Ms. Renu Saharan
Assistant Professor
M.M College of Pharmacy
Programme: Pharmacy Course: B. Pharm. (Complexation)
2. Programme: Pharmacy Course: B. Pharm. (Complexation)
MMCP VISION
• “Providing technical and practice oriented pharmacy
education to prepare students with attributes to meet the
need of industry and society”
MMCP MISSION
• To develop best technically competent pharmacy
professionals by inculcating desired attributes in them for
meeting industry demands.
• To make best pharmacists who can practice pharmacy to
become effective team member of healthcare system and
provide optimum pharmaceutical care solutions.
• Promotion of useful and innovative research to contribute in
development of nation and global society.
3. CO & PO (Physical Pharmaceutics I)
Programme: Pharmacy Course: B. Pharm. (Complexation)
4. Content
• Introduction
• Applications of complexes
• Classification of complexes
• Methods of analysis
• Protein binding
• Methods of determining drug-protein binding
Programme: Pharmacy Course: B. Pharm. (Complexation)
5. Chelates
The chelates are a group of metal ion complexes in which a
substance (Ligands) provides two or more donor groups to
combine with a metal ion.
Some of the bonds in a chelate may be ionic or of the primary
covalent type, whereas others are coordinate covalent links.
When the ligand provides one group for attachment to the
central ion, the chelate is called monodentate.
Pilocarpine behaves as a monodentate ligand toward Co(II),
Ni(II), and Zn(II) to form chelates of pseudotetrahedral
geometry.
Programme: Pharmacy Course: B. Pharm. (Complexation)
6. Olefin type –
The aqueous solution of certain metal ions like Pt, Fe, Pd, Hg and
Ag can absorb olefins such as ethylene to yield water soluble
complexes.
These are uses as catalyst in the manufacture of bulk drugs and
analysis of drugs.
Aromatic type –
Pi (π) complexes – Aromatic bases (Benzene, toluene and Xylene)
form pi-bond complexes with metal ions like Ag by Lewis acid-
base reactions.
Programme: Pharmacy Course: B. Pharm. (Complexation)
7. Sigma (σ) complexes – sigma bond complexes
involve in the formation of a sigma-bond
between ion and a carbon of aromatic ring.
“Sandwich” compounds – The are relatively
stable complexes involving in the delocalized
covalent bond between the d-orbital of
transition metal and a molecular orbit of the
aromatic ring.
Programme: Pharmacy Course: B. Pharm. (Complexation)
8. Organic molecular complexes:
An organic coordination compound or molecular complex
consists of constituents held together by weak forces of the
donor–acceptor type or by hydrogen bonds.
Donor Acceptor type – In this the bond is between uncharged
species but lacks charge transfer. The dipole-dipole interaction
and London dispersion forces (Dotted lines) make the complex
stable.
Programme: Pharmacy Course: B. Pharm. (Complexation)
12. Inclusion Compounds
• The class of addition compounds known as inclusion or
occlusion compounds results more from the architecture of
molecules than from their chemical affinity. One of the
constituents of the complex is trapped in the open lattice or
cage like crystal structure of the other to yield a stable
arrangement.
• Interaction is due to suitable molecular structure.
Programme: Pharmacy Course: B. Pharm. (Complexation)
15. Clathrates
• The clathrates crystallize in the form of a cagelike lattice in which the
coordinating compound is entrapped. Chemical bonds are not involved in
these complexes, and only the molecular size of the encaged component
is of importance. The stability of a clathrate is due to the strength of the
structure, that is, to the high energy that must be expended to decompose
the compound, just as a prisoner is confined by the bars that prevent
escape. Detailed study of clathrate compounds and showed that the highly
toxic agent hydroquinone (quinol) crystallizes in a cagelike hydrogen-
bonded structure. The holes have a diameter of 4.2 Å and permit the
entrapment of one small molecule to about every two quinol molecules.
Small molecules such as methyl alcohol, CO2, and HCl may be trapped in
these cages, but smaller molecules such as H2and larger molecules such
as ethanol cannot be accommodated. It is possible that clathrates may be
used to resolve optical isomers processes of molecular separation
Programme: Pharmacy Course: B. Pharm. (Complexation)
17. Cyclodextrins
• “Cyclodextrins are cyclic oligomers of glucose that can form
water-soluble inclusion complexes with small molecules and
portions of large compounds. These biocompatible, cyclic
oligosaccharides do not elicit immune responses and have low
toxicities in animals and humans. Cyclodextrins are used in
pharmaceutical applications for numerous purposes, including
improving the bioavailability of drugs. Of specific interest is
the use of cyclodextrin-containing polymers to provide unique
capabilities for the delivery of nucleic acids.”
Programme: Pharmacy Course: B. Pharm. (Complexation)
