Essay Example on Formation of ternary Complexes

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Formation of ternary complexes When a water soluble polymer and CD and a drug mixed together in a solution to obtain the so called ternary complexes it is possible increase to drug solubilization when compared to the polymer and CD separately which is a result of the synergistic effect between the components Formulations containing drug CD complexes with the addition of a water soluble polymer have proven to be capable of increasing the bioavailability of formulations while reducing the amount of CD by up to 80 73 In the presence of water the polymer aids in the wettability of particles resulting in the accelerated dissolution and increased amount of drug delivered in vitro 74 The interaction of water soluble polymers with drug may occur by means of ion ion ion dipole dipole dipole electrostatic bonds Vander Waals force or 3 center 2 electron bonds 75 Similarly the interaction between polymers and CDs and drug CD complexes begins to occur on the external surface of the CD molecule CDs polymers and drug CD complexes form aggregates capable of solubilizing drugs and other hydrophobic molecules 76 as shown in figure Figure 4

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Representation of ternary complex formation between drugs CD and water soluble polymer 1 22 3 Acetyl Coumarin 3AC Coumarins and their derivatives form an elite class of compounds occupying an important place in the realm of natural products and synthetic organic chemistry 77 3 acetyl coumarins are important initial compounds for the synthesis of coumarins and the synthesis of coumarins and their derivatives has attracted considerable attention from organic and medicinal chemists for many years as a large number of natural products contain this heterocyclic nucleus Coumarin benzopyrones or 2 oxo 2H chromene is a compound containing two structures of six membered heterocyclic rings with two oxygen atoms Classification of coumarins includes simple coumarin furanocoumarins pyranocoumarins and coumarins substituted in the pyrone ring 78 Simple coumarins are compound that undergoes hydroxylation alkoxylation and alkylation to form its derivatives Coumarin can be found in several plants notably with high concentration in the tonka bean Dipteryx odorata vanilla grass 

Anthoxanthum odoratum woodruff Galium odoratum mullein Verbascum spp and sweet grass Hierochloe odorata It has a sweet scent readily recognized as the scent of newly mown hay and has been used in perfumes since 1882 Natural coumarin compounds can be found in flowers seeds fruits trunk stem and foliage and suitable solvents can be used in extraction for its isolation Coumarins also can be produced through organic synthesis although it can be found naturally in several green plants The 3 Acetylcoumarin is also known as 2H 1 Benzopyran 2 one or 3 Acetyl 2H chromen 2 one 3 Acetylcoumarin exists in two polymorphic forms i e form


A Triclinic and form B Monoclinic 1 23 Structure of 3AC Molecular formula of 3AC is C11H8O3 Figure 5 Structure of 3 AcetylCoumarin 1 24 Synthesis of 3AC 3 Acetylcoumarin was prepared according to the procedure reported previously 5 A mixture of salicyaldehyde 0 5 mol and ethyl acetoacetate 0 5 mol was stirred and cooled To this mixture 10 g of piperidine was added with shaking The mixture was maintained at freezing temperature for 2 3 hours resulting in a yellow colored solid mass which was separated out It was recrystallized from ethanol to get the target compound 79 Figure 6 Synthesis of 3 

Acetyl coumarin by Knoevenagel reaction 1 25 Properties of 3AC Table 3 Properties of 3AC Molar mass 188 1794 Appearance Pale Yellow Melting point 120 1220 C Solubility in water Sparingly soluble 1 26 Uses of 3 Acetyl Coumarin 3 Acetyl Coumarin is important initial compoundfor the synthesis of coumarin and their derivatives has attracted considerable attention from organic and medicinal chemists 1 27 Applications of 3 Acetyl Coumarin 3 Acetyl Coumarin application ranges from additive in food perfumes cosmetics pharmaceuticals In the preparation of insecticides 80 As optical brightners 80 As dispersed fluorescent and tunable laser dyes 80 Coumarin have varied bioactive for example inhibition of platelet aggregation 80 As anticancer 81 Inhibition of steroid 5 α reductase 82 1 28 Polymer


A polymer is defined as a macromolecule formed by the repeated combination of several simple molecules Monomers through covalent bonds 1 29 Poly vinylpyrrolidone PVP Poly vinylpyrrolidone PVP also commonly called polyvidone or povidone is a polymer made from the monomer vinylpyrrolidone It is also called briefly PVP is one of the numerous products 83 84 of the acetylene chemistry founded by Reppe 1 30 Preparation of PVP By the reaction of acetylene with formaldehyde 1 4 butenediol is obtained which is hydrogenated to butanediol After oxidative cyclization to butyroacteone and its reaction with ammonia pyrrolidone is formed by the removal of water Finally the vinyl group is introduced to form N Vinyl pyyrrolidone 2 1 2 oxo pyrrolidinyl ethylene The polymerization of vinylpyrrolidone produces the polymeric material fig Vinylpyrrolidone can polymerized either in bulk in solution or in suspension Figure 7 Synthesis of N vinyl pyrrolidone from acetylene and formaldehyde Figure 8 Polymerization of vinyl pyrrolidone 1 31 Properties of PVP Structure Colour White powder PVP Polyvinylpyrrolidone is a nonionic water soluble polymer and can be applied in a variety of fields of use owing to following advantageous characteristics Good solubility in water as well as various organic solvents Good affinity to various polymers and resins High hygroscopicity Good film formation property Good adhesiveness to various substrates Good chelate complex formation property 1 32 Application of PVP A survey of most important application of VP polymers is reported below

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