Abstract

SYNTHESIS AND CHARACTERIZATION OF PRODRUG

Nisha Kumbhar*

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Abstract

The prodrug term involves chemically modified inert compound which upon administration releases the active parent drug to elicit its pharmacological response within the body. For many years, prodrug strategy has been developed enormously to solve many unwanted drug properties. This approach has several advantages over conventional drug administration and it has the potential to be quite effective method for the treatment of diseases in the future. In most cases, prodrugs contain a promoiety (linker) that is removed by enzymatic or chemical reactions, while other prodrugs release their active drugs after molecular modification, such as an oxidation or reduction reactions. In some cases, two biologically active drugs can be linked together in a single molecule called a codrug. In a codrug, each drug acts as a linker for the other. It is important to ensure that the prodrug should be pharmacologically inactive, rapidly converted to its active drug and a non-toxic moiety by metabolic reactions. In this chapter we describe the general terms related to prodrugs, and the ways by which prodrug strategy is used to overcome many pharmaceutical and pharmacokinetic problems such as, low bioavailability by increasing or decreasing lipophilicity of the parent drug, site selectivity for higher absorption and less toxicity, short duration of action to increase patient compliance, rapid metabolism to increase oral bioavailability and masking bitter sensation of commonly used drugs, which is crucial for geriatric and pediatric patient compliance.

Keywords: Prodrugs, Prodrugs history, Physicochemical properties, Chemical reactions, Prodrug metabolism, Permeability, Lipophilicity.