Jordan Journal of Pharmaceutical Sciences, Volume 7, No. 2, 2014
- 144 -
© 2014 DAR Publishers/The University of Jordan. All Rights Reserved.
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shahalamkhan@yahoo.com
Received on 8/9/2013 and Accepted for Publication on
16/3/2014.
Comparative in-vitro Pharmaceutical Evaluation of Four Brands of
Metronidazole Tablets Marketed in Gulf Region
Reem Khamis Al Naimi and Shah Alam Khan
1
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1
Department of Pharmacy, Oman Medical College, Muscat, Sultanate of Oman
ABSTRACT
Metronidazole is an antiprotozoal drug which is also effective against anaerobic bacteria. It exhibits pronounced
in-vitro and in-vivo activity against Trichomonas vaginalis and E. histolytica. Many different brands and dosage
forms of Metronidazole are available in the gulf countries that place physicians and pharmacists in a dilemma of
drug substitution in case of non availability of a particular brand. The present study was aimed to evaluate the
pharmaceutical equivalence of four brands of 250 mg Metronidazole tablets marketed in Middle East countries.
Four brands of Metronidazole tablets were purchased locally from the retail pharmacy outlets in Muscat, Oman
and their solubility, partition coefficient (log P) and pharmaceutical quality were assessed by using in-vitro tests
as per the United States Pharmacopoeia (USP) and unofficial standards as recommended by the manufacturers.
Selected brands of Metronidazole were found to be highly soluble, highly permeable and also passed all the
official and unofficial in- vitro quality control tests prescribed for the tablets except hardness test. All brands of
Metronidazole tablets released more than 70% of their drug content within 45 minutes. Thus, based on the above
results, it can be concluded that tested brands of Metronidazole tablets being eligible for biowaiver, are
pharmaceutically equivalent and therefore can be considered for drug substitution for each other.
Keywords: Metronidazole Tablets, Antiprotozoal, Pharmaceutical Equivalence, Dissolution.
INTRODUCTION
Metronidazole is an antiprotozoal and antiparasitic
agent commonly used to treat amoebiasis, giardiasis,
trichomoniasis and other microbial diseases caused by
anaerobic bacteria.
1
It is also listed in the important WHO
essential medicine list.
2
Metronidazole in combination
with other drugs is quite effective and beneficial therapy
in the management of H. pylori infection.
3
Chemically it
is 2-(2-methyl-5-nitro-1H-imidazol-1-yl) ethanol (Fig. 1)
and occurs as white to pale yellow microcrystalline
powder, slightly soluble in water and alcohol.
4
However,
it dissolves readily in dilute hydrochloric acid solution. It
is a prodrug that requires reductive activation of the nitro
group by susceptible organisms. It is usually completely
and promptly absorbed after oral intake, reaching
concentrations in plasma of 8 - 13 mg within 0.25 - 4 h
after a single 500 mg dose.
5
Therefore, it can be inferred
that slight change in the physicochemical characteristics
and dissolution will affect its biopharmaceutics and thus
its quality and efficacy.
There are many multinational brands and dosage
forms of Metronidazole available in the market of gulf
countries. Some of these brands are manufactured in
Middle East countries such as Saudi Arabia, Jordan,
UAE, Oman and some are imported from other parts of
the world. Various brands available in the market are
considered pharmaceutically equivalent if they contain
the same amount of active ingredient in the identical
dosage form and meet the same compendial or other