Authors
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Garba, M. A.
Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Author
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Bashir, A.
Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Author
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Danmusa, U. M.
Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Author
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Abdullahi, Z.
Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Author
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Bashir, A. I. J.
Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Author
Keywords:
Metformin, Cephalexin, Pharmacokinetics, Drug interaction, HPLC
Abstract
Background: Several drugs were often used to obtain a therapeutic objective or to treat a
coexisting disease. The use of multiple drugs concomitantly can give rise to drug-drug interactions
could diminish therapeutic efficacy or increase the toxicity of one or more of the administered
drugs.
Aim: To determine the effects of co-administration of cephalexin on the pharmacokinetics of
metformin in freshly diagnosed type 2 diabetic patients.
Methods: Twelve patients with age 25-55 years, weight range 50-70 kg, and height 1.5 -1.75 m
took part in the study. A 2 x 2 double-blind randomized cross over study was conducted for the
study. Each of the patients received orally either 1 g of metformin with placebo or a combination
of 1 g of metformin and 500 mg of cephalexin. Blood samples were collected at an interval of 0,
0.5, 1.5, 3.0, 4.0, 6.0, and 8.0 hours and stored at -4 0C before analysis. Plasma was obtained from
the blood and the drug was extracted from the plasma using three times its volume of acetonitrile.
The samples were analyzed for metformin using an adopted and validated HPLC method on a
reversed phase column C-8, 4.6 x 150 nm, mobile phase acetonitrile/potassium dihydrogen
orthophosphate (21:79), and a UV detector at 236 nm.
Results: The systemic disposition of metformin was altered by the co-administration of
cephalexin, Cephalexin increased Cmax and AUC by an average of 54% and 19%, respectively, and
reduced renal clearance by 17%. The renal clearance of metformin was reduced in a time
dependent manner in the presence of cephalexin.
Conclusion: It was concluded that co-administration of cephalexin and metformin showed
interaction that may lead to adverse effect.
Author Biographies
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Garba, M. A., Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Lecturer in the Department of Pharmaceutical and Medicinal Chemistry at Kaduna State University. He specializes in pharmacokinetic modeling and drug-drug interaction studies, particularly focusing on metabolic disorders and the optimization of HPLC analytical methods.
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Bashir, A., Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Researcher at Kaduna State University who contributed to the clinical study design and the collection of blood samples from Type 2 diabetic patients.
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Danmusa, U. M., Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Academic staff at Kaduna State University involved in the development and validation of the HPLC method used for the simultaneous determination of metformin in human plasma.
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Abdullahi, Z., Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
A researcher specialising in pharmacology who assisted in the statistical analysis of pharmacokinetic parameters.
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Bashir, A. I. J., Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria.
Lecturer at Kaduna State University with expertise in toxicology and pharmacology. Contributed to the interpretation of the competitive inhibition mechanisms between cephalexin and metformin.
