World Journal of
Pharmaceutical and Life Sciences

CHEMISTRY OF β-LACTAM SULTAMICILLIN AS A MUTUAL PRODRUG OF AMPICILLIN AND SULBACTAM WORKS AS AN AZABICYCLO [3.2.0] HEPTANE CARBOPENAM BIOPRECURSOR

Shivani J. Patel, Prof. Dr. Jayant B. Dave and Prof. Dr. Dhrubo Jyoti Sen*

ABSTRACT

A large number of therapeutic medications have undesirable properties that may generate pharmacological, pharmaceutical, or pharmacokinetic barriers in clinical drug applications. Metabolism of drugs by Phase-I & Phase-II metabolic pathways for possibility of active metabolites, which could in turn useful for rational designing of bioprecursor prodrugs of the active principle of interest. Prodrug is a substance which after administration is metabolized into a pharmacologically active drug. Actually Prodrug has least medicinal value in in-vitro/in-vivo but after biotransformation by metabolism in in-vivo it releases the active medicament. A drug is a substance which is a chemical entity, has definite structural skeleton, obtained by natural or synthetic or semisynthetic source, which can fit on bioreceptor platform having controlling capacity to control over the biochemical malfunction. Every drug is xenobiotic because it is coming from outer source (xeno) and active in biological unit (biotic). Prodrug is the precursor of drug which is made by derivatization of the same to enhance the bioavailability by pharmacokinetics, lipid solubility by partition coefficient and increase the physicochemical & biochemical parameters by pharmacodynamics. Prodrug is a precursor (forerunner) of a drug. A prodrug must undergo chemical conversion by metabolic processes before becoming an active pharmacological agent. For example, sultamicillin is a prodrug. It is not active in its ingested form. It has to be broken down before becoming active as a drug. It is a compound that on administration undergoes chemical conversion by metabolic processes to yield active moieties of ampicillin and sulbactam. This is also is called as biotransformation which produces active drug for pharmacological response from prodrug which is inactive by itself.

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