IPS1 - H. -Complexation

Proverbs 16:3

Complexation

This characterizes the covalent and non-covalent interactions between two or more compounds that are capable of independent existence.

Complexation

Once ____ occurs, the physical and chemical properties of the complexing species are altered. These properties include solubility, stability, partitioning, energy absorption and emission, and conductance of the drug.

● Solubility

● Stability

● Partitioning

● Energy absorption and emission

● Conductance of the drug

Once complexation occurs, the physical and chemical properties of the complexing species are altered. These properties include _____

Coordination compounds

Complexes are also known as ____

Complexes / Coordination Compounds

Compounds formed through a donor-acceptor mechanism (a type of LEWIS acid-base reaction) between two or more different chemical constituents.

● Donor (Lewis base)

● Acceptor (Lewis acid)

Components of Complexes / Coordination Compounds

Donor

[Components of Complexes / Coordination Compounds]

Any NONMETALLIC atom or ion that can donate an electron pair

Acceptor

[Components of Complexes / Coordination Compounds]

A constituent that accepts a share in the pair of electrons, is frequently a METALLIC ion, although can also be a NEUTRAL atom

● Metal Ion Complexes

● Organic Molecular Complexes

● Inclusion/Occlusion Compounds

Types of Complexes

● Inorganic type

● Chelates

● Olefin type

● Aromatic type

[TYPES OF COMPLEXES]

Types of METAL ION COMPLEXES

● Quinhydrone type

● Picric acid type

● Caffeine and other drug complexes

● Polymer type

[TYPES OF COMPLEXES]

Types of ORGANIC MOLECULAR COMPLEXES

● Channel lattice type

● Layer type

● Clathrates

● Monomolecular type

● Macromolecular type

[TYPES OF COMPLEXES]

Types of INCLUSION/OCCLUSION compounds

Coordination Complexes

[METAL ION COMPLEXES]

Metal Ion complexes are also known as ___

Inorganic Type

[METAL ION COMPLEXES]

This type involves Lewis acid - base reaction, which forms the coordinate covalent bond.

Metal ion (Lewis acid) + Ligand (Lewis base)

Inorganic Type

[METAL ION COMPLEXES]

Diamminesilver (I) complex: Ag+ + 2(NH3) ⟶ [ Ag(NH3)2 ]+

Diamminesilver (I) complex: Ag+ + 2(NH3) ⟶ [ Ag(NH3)2 ]+

[METAL ION COMPLEXES]

Ag+ + 2(NH3) ⟶ [ Ag(NH3)2 ]+

Inorganic Type

[METAL ION COMPLEXES]

Hexamminecobalt (III) complex: Co+3 + 6NH3 ⟶ [Co(NH3)6]+

Hexamminecobalt (III) complex

[METAL ION COMPLEXES]

Co+3 + 6NH3 ⟶ [Co(NH3)6]+

Chelates

[METAL ION COMPLEXES]

A compound containing a ligand (typically ORGANIC) bonded to a central metal atom at two or more points (multidentate ligand).

Chelates

[METAL ION COMPLEXES]

● Hemoglobin

● Chlorophyll

● Cisplatin and carboplatin

Hemoglobin

[METAL ION COMPLEXES]

An an IRON complex that is essential for the transport of oxygen in the blood and tissues

Chlorophyll

[METAL ION COMPLEXES]

A molecule contains a MAGNESIUM atom held in a PORPHYRIN ring.

Cisplatin and carboplatin

[METAL ION COMPLEXES]

These are PLATINUM (II) complexes that have proved to be useful agents in the treatment of cancer.

platinum (II)

[METAL ION COMPLEXES]

Cisplatin and carboplatin are ___ complexes that have proved to be useful agents in the treatment of cancer.

Chelating agents

[METAL ION COMPLEXES]

These organic compounds that can assimilate and fix metallic ions and thus remove them from the body. They are useful in cases of poisoning and tissue damage from metals.

Chelating agents

[METAL ION COMPLEXES]

Examples are

● Ethylenediaminetetraacetic acid (EDTA)

● 2,3-Dimercaptopropanol (BAL, British Anti-Lewisite, Dimercaprol)

● Ethylenediaminetetraacetic acid (EDTA)

● 2,3-Dimercaptopropanol (BAL, British Anti-Lewisite, Dimercaprol)

[METAL ION COMPLEXES]

Both are chelating agents for LEAD and MERCURY poisoning.

Organic Molecular Complexes

[TYPES OF COMPLEXES]

These are formed as a result of NONCOVALENT interactions between ligand and substrate.

Organic Molecular Complexes

[TYPES OF COMPLEXES]

The interaction occurs through electrostatic forces, van der Waals forces, charge transfer, H bonding, or hydrophobic effects.

● Caffeine + Gentisic acid

● Benzocaine + Sodium salicylate

[ORGANIC MOLECULAR COMPLEXES]

Drug Complexes

Caffeine + organic acid anions

[ORGANIC MOLECULAR COMPLEXES]

These form insoluble complexes making caffeine LESS SOLUBLE which provides caffeine in a form that masks its normal bitter taste. (Water in Oil Formulation)

Caffeine + gentisic acid (organic acid)

[ORGANIC MOLECULAR COMPLEXES]

This organic acid makes insoluble complex or less soluble caffeine, masking the bitter taste of caffeine and serve as a suitable state for CHEWING caffeine tablets.

Caffeine + organic acid anions

[ORGANIC MOLECULAR COMPLEXES]

These also provide an EXTENDED-release form.

Benzocaine + Sodium Salicylate

Binding of sodium salicylate with benzocaine significantly influences the release of benzocaine.

[ORGANIC MOLECULAR COMPLEXES]

These drug complex improves drug ABSORPTION and bioavailability.

Polymer Type Complexes

[ORGANIC MOLECULAR COMPLEXES]

Povidone (Polyvinylpyrrolidone, PVP) + Iodine = Povidone-Iodine

Povidone (Polyvinylpyrrolidone, PVP) + Iodine = Povidone-Iodine

[ORGANIC MOLECULAR COMPLEXES]

An example of polymer type complex

Povidone (polyvinylpyrrolidone, PVP)

[ORGANIC MOLECULAR COMPLEXES]

This is used in the pharmaceutical industry as a synthetic POLYMER vehicle for dispersing and suspending drugs.

● Aerodine

● Betadine

[ORGANIC MOLECULAR COMPLEXES]

Povidone's most common use is in the topical povidone-iodine solution (____), where iodine is released as an antiseptic.

antiseptic

[ORGANIC MOLECULAR COMPLEXES]

Povidone's most common use is in the topical povidone-iodine solution (Aerodine, Betadine), where iodine is released as an ___.

Inclusion/Occlusion Compounds

[TYPE OF COMPLEXES]

These complexes are formed between interacting molecules in which guest molecules are ENTRAPPED in a host molecule through the unique molecular architecture of the host.

Channel Lattice

[INCLUSION/OCCLUSION COMPOUNDS]

The host component crystallizes to form channel-channel like structure.

● Choleic acids

● Starch-iodine complex

● Urea and Thiourea

[INCLUSION/OCCLUSION COMPOUNDS]

Examples of CHANNEL LATTICE compounds.

Layer/ Intercalation

[INCLUSION/OCCLUSION COMPOUNDS]

Guest molecule is diffused between layer of CARBON atom, HEXAGONALLY, alternating later of guest and host molecules

● Clay montmorillonite complexes

● Graphite

[INCLUSION/OCCLUSION COMPOUNDS]

Examples of LAYER INTERCALATION

Clathrate

[INCLUSION/OCCLUSION COMPOUNDS]

Molecule of a guest compound gets entrapped within CAGE-like structure

● Hydroquinone

● Warfarin sodium

[INCLUSION/OCCLUSION COMPOUNDS]

Examples of CLATHRATES

Monomolecular

[INCLUSION/OCCLUSION COMPOUNDS]

Single host molecule

Cyclodextrin

[INCLUSION/OCCLUSION COMPOUNDS]

Example of MONOMOLECULAR compound

Molecular sieves

[INCLUSION/OCCLUSION COMPOUNDS]

Macromolecular compounds are also known as ___

● Zeolites

● Dextrins

● Silica gels

[INCLUSION/OCCLUSION COMPOUNDS]

Examples of MACROMOLECULAR/ MOLECULAR SEIVES