In-vitro Comparative Evaluation Of Different Co-trimoxazole Tablet Products Obtained From Drug Retail Outlets In Addis Ababa

Evaluation studies provide a means of identifying quality differences between same productsrnobtained from various manufacturers and quality evaluations are crucial in the era of increasingrnresistance to antibacterial agentsrnThe introduction of trimethoprim in combination with sulphamethoxazole constitutes anrnimportant advance in the development of clinically effective antimicrobial agents. In much of thernworld the combination of sulphamethoxazole with trimethoprim in the proportion of 5 to 1 isrnknown as Co-trimoxazole. Co-trimoxazole has been used in a diverse range of infections due tornsensitive bacteria and is widely prescribed for various indications. By virtue of sequentialrnblockade of microbial folic acid synthesis the antimicrobial combination has excellent in vitrorninhibitory activity against many common respiratory and urinary tract pathogens, as well as manyrnnosocomial-infecting strains. In patients infected with the human immunodeficiency virus (HIV),rntrimethoprim-sulphamethoxazole provides prophylactic and therapeutic potency againstrnPneumocystis carinii but at the risk of side effects. Trimethoprim-sulphamethoxazole (TMPSMX)rnis also used for treatment of pulmonary and disseminated nocardiosis and some forms ofrnWagener’s granulomatosis, as well as for prophylaxis of spontaneous bacterial peritonitis.rnBacterial resistance to trimethoprim-sulphamethoxazole is a rapidly increasing problem and isrnexacerbated by use of substandard products. In this work, it is aimed to evaluate the physicalrnproperties and the dissolution profiles of trimethoprim-sulphamethoxazole tablets produced byrnten different manufacturers and are obtained from drug outlets in Addis Ababa.rnX I IrnAccordingly, the different tablets were evaluated for physical properties (Diameter, thickness,rnshape, hardness, friability and disintegration time) and their dissolution profiles were comparedrnby the USP XXVI paddle method.rnThe tablets investigated in this study could roughly be grouped as those, which exhibited, delayedrndrug release and those, which released the drug contained immediately. The tablets evaluated inrnthis study differed in many of their physical properties. The average weights ranged fromrn502.41mg (Bactrim) to 709.98mg (Cotrimol), 480mg being the expected strength of therncombination. The mean disintegration times ranged from 0.17 (±0) minutes (Cotrimoxazole) torn13.05 (±5.24) minutes (Lagatrim).rnNine of the tested products gave an assay value above the lowest limit (93%-107%) specified inrnthe pharmacopoeia. Assay values greater than the upper limit for sulphamethoxazole wasrnobtained with four of the evaluated products. One product gave an assay value greater than thernupper limit for both sulphamethoxazole and trimethoprim.rnMost of the tablets released the drug contained in an increasing fashion from the 5th minute to thern60th minute with varying proportion of increment. Products obtained from Europe released mostrnof the drug within the first 5 to 10 minutes. More than 90 % of trimethoprim is released within 5rnminutes from Bactrim and Septrin and with in 10 minutes from Lagatrim and Deprim. WhilernLagatrim and Septrin released more than 90 % of their Sulphamethoxazole within 10 minutes,rnBactrim and Deprim released their Sulphamethoxazole within 20 minutes. However the EuropeanrnX I I Irnand the non-European products differed significantly in their sulphamethoxazole release. Bothrnproducts showed a comparable trimethoprim release pattern. All of the tested products releasedrnmore than 90% of the trimethoprim after one hour, ranging from 92.81%-Cotreich to 111.77%-rnSeptrin.rnThe very long t90% values of Cotreich and Cotrimol (60 & 45minutes respectively) forrntrimethoprim, the very long t50% & t90% values of Cotreich (38 and >60minutes respectively) forrntrimethoprim and sulphamethoxazole, and the very long t90% values of Cotreich, Cotrimol andrnKanprim (>60 minutes) for sulphamethoxazole indicate that these products could result in lowerrnrate and extent of bioavailability in the body. Similar problems could be encountered with thernrelatively long t90% values of Cotrimoxazole (45minutes) and Oriprim (40minutes) forrnSulphamethoxazole. The smaller amount of sulphamethoxazole and trimethoprim released fromrnproducts with delayed release could compromise the in vivo efficacy of these tablets.

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