Abstract

SYNTHESIS OF INCLUSION COMPLEXES OF SOME HETEROCYCLICS WITH Î’-CYCLODEXTRIN FOR PHARMACOLOGICAL ACTIVITY

Chandra Bhushan Kumar* and Dr. Prasanta Kumar Biswal

.

Abstract

Heterocyclic compounds may be classified into aliphatic and aromatic. The aliphatic heterocyclics are the cyclic analogues of amines, ethers, thioethers, amides, etc. There properties are particularly influenced by the presence of strain in the ring. The heterocyclic compounds may have three, four, five, six or seven membered rings. Thiazolidin-4-ones and its derivatives have played an important role in medicine, because of their diverse chemical reactivity and broad spectrum of biological activities such as anti-cancer, analgesic, anti-inflammatory, antidepressant, antidiabetic, anti-viral, anti-convulsant, anti-bacterial and anti-fungal activities. These above facts were acts as an inspiration to develop some new 4-thiazolidinone derivatives. But these therapeutic agents acquire low aqueous solubility, which in a major challenge for formulation chemists that can be solved by various technological approaches during the pharmaceutical product development stage. Several difficulties are faced in designing formulations for better absorption and with enhanced bioavailability. One of the important approaches is to encapsulate the drug in the hydrophobic cavity of cyclodextrin to produce inclusion complex and to increase the bioavailability. Cyclodextrins are one of the most commonly used host cavities, which provide a conical cavity for the water insoluble drugs to be encapsulated there by making them more water soluble, improve bioavailability, get better stability, decline volatility, conversion of liquid or gas into solid form, reduce side effects etc.

Keywords: Heterocyclic, Thiazolidin-4-one, Cyclodextrin, Complex, Solubility, Bioavailability