Chemical, biopharmaceutical and microbiological profiles of ciprofloxacin tablets in the Nigerian market

Abstract

Background: The number of ciprofloxacin hydrochloride brands in the Nigerian market is continuously increasing; hence, there is need to establish their bioequivalence in the interest of public health. This study assessed the chemical, biopharmaceutical, and microbiological profile of thirty brands of ciprofloxacin (500 mg) tablets in Nigerian market.

Method: Quality parameters evaluated include weight uniformity, thickness and diameter, hardness, friability, disintegration, dissolution, identity, and antibacterial profile. Content of active ingredients was determined by a slightly modified and validated HPLC method.

Results: Results of thickness, diameter, and hardness tests of all the brands fell within acceptable limits. The percentage of brands within acceptable range for weight uniformity, friability, disintegration, dissolution, and active ingredient are 86.67, 96.67, 93.33, 26.67, and 93.33% respectively. About 87% of the tested generic version of ciprofloxacin demonstrated in-vitro antibacterial bioequivalence to the reference drug. The abysmal low dissolution rate of 26.67 % is a source of concern as it suggests a potential poor bioavailability of the active ingredient of these drugs.

Conclusion: The failure of a large portion of the tested brands may be due to deliberate counterfeiting, failure of current good manufacturing practices (cGMP) by manufacturers or poor handling by wholesalers/retailers. The study therefore recommends effective post marketing surveillance and enforcement of cGMP by the concerned regulatory agency in Nigeria.

Keywords: Bioequivalence, ciprofloxacin, quality, GMP, drug faking, and infectious diseases

Résumé
Contexte: Le nombre de marques de chlorhydrate de ciprofloxacine sur le marché nigérian ne cesse d’augmenter; par conséquent, il est nécessaire d’établir leur bioéquivalence dans l’intérêt de la santé publique. Cette étude a évalué le profil chimique, biopharmaceutique et microbiologique de trente marques de comprimés de ciprofloxacine (500 mg) sur le marché nigérian.

Méthode: Les paramètres de qualité évalués comprennent l’uniformité du poids, l’épaisseur et le diamètre, la dureté, la friabilité, la désintégration, la dissolution, l’identité et le profil antibactérien. La teneur en ingrédients actifs a été déterminée par une méthode HPLC légèrement modifiée et validée.

Résultats: Les résultats des tests d’épaisseur, de diamètre et de dureté de toutes les marques se situaient dans des limites acceptables. Le pourcentage de marques dans la plage acceptable pour l’uniformité du poids, la friabilité, la désintégration, la dissolution et l’ingrédient actif est de 86,67, 96,67, 93,33, 26,67 et 93,33% respectivement. Environ 87% de la version générique testée de la ciprofloxacine a démontré une bioéquivalence antibactérienne in vitro avec le médicament de référence. Le faible taux de dissolution abyssal de 26,67% est une source de préoccupation car il suggère une mauvaise biodisponibilité potentielle de l’ingrédient actif de ces médicaments.

Conclusion: L’échec d’une grande partie des marques testées peut être dû à une contrefaçon délibérée, à un échec des bonnes pratiques de fabrication actuelles (cGMP) par les fabricants ou à une mauvaise manipulation par les grossistes / détaillants. L’étude recommande donc une surveillance post-commercialisation efficace et l’application des BPF par l’organisme de réglementation concerné au Nigéria.

Mots clés: Bioéquivalence, ciprofloxacine, qualité, BPF, contrefaçon de médicaments et maladies infectieuses

Correspondence: Dr. Olufunmilayo E. Adejumo, Department of Pharmaceutical and Medicinal Chemistry, Olabisi Onabanjo University, Sagamu, Nigeria. E-mail: funmilayo@yahoo.co.uk

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