STUDIES ON ANALYSIS AND STABILITY OF SULTAMICILLIN AND ITS TABLET FORMULATION
Shivani J. Patel, Prof. Dr. Jayant B. Dave, Prof. Dr. Dhrubo Jyoti Sen* and Prof. Dr. C.N. Patel
Ampicillin is a β-lactam antibiotic that is advantageously combined with sulbactam, β-lactmase inhibitor to extend antimicrobial spectrum of Ampicillin. The combination is official in USP as injectable preparation. The combination cannot be administered as orally as sulbactam is not stable at an acidic pH. Sultamicillin is a novel compound that helps to ensure administration by oral route. Sultamicillin is mutual prodrug formed by reacting Ampicillin and Sulbactam with methylene diol to form diester with carboxylic acid group of both the drugs. Sultamicillin hydrolyses into Ampicillin and Sulbactam into body, the desired drugs. Sultamicillin is difficult to handle and not very stable in solid form. Sultamicillin Hydrochloride salt greatly enhances solubility but does not solve the problem of handling difficulty and stability in solid state. Salt with toluene sulfonic acid called sultamicillin tosilate solves the problem and this is official in European Pharmacopeia and British Pharmacopeia. Sultamicillin is marketed as 375 mg capsules world over and in India for oral use. The capsules are indicated for various systemic infections including anerobes and are also used empirically where causative organisms are not known. The combination is currently used in special indications of antimicrobial therapy. Sultamicillin is an oral form of mutual prodrug antibiotic containing ampicillin, a β-lactam antibiotic and sulbactam, a β-lactamase inhibitor. Sultamicillin is used orally as tablets and is as effective as ampicillin and sulbactam injection in the empirical therapy of variety of infections. The objective was to develop suitable UV spectrophotometric and HPLC method that can separate Sultamicillin from its hydrolysis products- ampicillin and sulbactam so that they can be used for thermal & hydrolytic stability study of the drug and its tablet dosage form.
Keywords: Ampicillin, Sulbactam, Sultamicillin, Sultamicillin tosilate, Toluene sulphonic acid, Mutual prodrug, Solubility, logP, ?max-UV, IR, Reversed phase HPLC, Student’s t-test.
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