Nigerian Quarterly Journal of Hospital Medicine

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Comparative Dissolution Profiles of Representative Quinolones in Different Media

MO Akinleye, AA Jolaoso, HAB Coker


Background: Quinolones have a broad spectrum of activity against bacteria and are a class of synthetic antimicrobial modeled after nalidixic acid.
Objective: To determine the dissolution efficiencies of ciprofloxacin and sparfloxacin in 0.1NHCL, deionized water, 0.1M acetic acid and pH 7.4 phosphate buffer.
Methods: The in-vitro dissolution profiles of ciprofloxacin (250mg and 500mg) and sparfloxacin (200mg) tablets were studied in the respective media using US Pharmacopoeia (USP) Apparatus II. In order to monitor the comparative rate of dissolution, samples were withdrawn from the
medium for quantification over nine pre-determined time points during a total period of two hours. Samples were analyzed by an HPLC method capable of concurrent elution of ciprofloxacin/sparfloxacin.
Results: The medium with most stable release pattern for the representative quinolones was 0.1M acetic acid, followed by 0.1NHCl, distilled water and pH 7.4 buffer respectively. The %Q of Ciprofloxacin(CP) and 3 0 Sparfloxacin(SP) was found to conform entirely to both USP2004 and FDA specifications. Sparfloxacin was found to be unstable due to cloudiness observed in 0.1N HCl medium. The CP and SP showed highest %Q in 0.1M max acetic acid compared to other media. This result has
implication in the choice of medium for dissolution testing of quinolones, particularly for comparative purposes in the absence of specific monograph recommendations. Furthermore, it supports the change from 0.1N to 0.01NHCl for ciprofloxacin in the USP as a monographic modification.
Conclusion: We conclude that there is a need to have a general-purpose dissolution medium for comparing profiles of different quinolones, 0.1M acetic acid may be a suitable candidate. Furthermore, the study may serve as guidance to the drug regulatory authorities in formulation of monographs for the drugs.

Key words: Ciprofloxacin, Sparfloxacin, media and Dissolution tests

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