Effect of Chloroquine and Halofantrin on the Dissolution Profile of Ciprofloxacin.
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Nigerian Journal of Health and Biomedical Sciences
Objective: To investigate the potential interaction between ciprofloxacin and some representative antimalarial agents using in-vitro dissolution tests. Methods: The in-vitro dissolution of ciprofloxacin (CP) (250mg and 500mg tablets respectively) was studied using U.S Pharmacopoeia (USP) Apparatus 2 in the presence of varying concentrations of chloroquine (CQ) and halofantrlne (HF). The dissolution media used were 0.1 N HCl and distilled water. The CQ concentration range used was of 0.69 - 3.47M while halofantrine was 0.56 -1.11M. Both concentrations of CQ and HF chosen were within their dosage regimen. A validated HPLC method capable of concomitant elution of CP/CQ/HF was used for the determination of CP in the dissolution mixture. Results: The mean reduction in the maximal quantity of dissolved drug, Qmax in the presence of varying concentrations of CQ was 47.8% and 45.4% (322.0 ± 17.48mg and 279.53 ± 14.62mg) with 500mg CP tablets in distilled water and 0.1N HCl respectively, and 43.4% and 37.6% (169.9 ± 4.1mg and 144.53± 4.0mg) with 250mg CP tablets in distllled water and 0.1 N HCl respectively. The reduction in the presence of HF was 75.0% (132.8 ± 11.62mg) with 500mg CP tablets and 48.3% (118.9 ± 0.36mg) with 250mg CP tablets in 0.1N HCl. The reduction in a max appears to be- directly related to the quantity of CQ/HF present, the difference was significant with CQ (p=0.027) and with HF (p = 0.02). There also appears to be a direct correlation between the amount of CQ in the medium and the pH of the medium, the trend being reduction in pH with increasing concentration of CQ. Conclusion: We conclude that the release of CP is inhibited by the presence of CQ and HF. This suggests there is a potential interaction between CP and the test substrates at the absorption site, which may lead to reduced availability of CP. "This has an implication in therapeutic outcomes particularly in a malaria endemic environment, such as ours, where these antimalarial drugs are frequently co-administered with ciprofloxacin. KEY WORDS: Fluoroquinolones, Chloroquine, Halofantrine, Chemotherapy, Dissolution tests, Drug interaction.
Chloroquine , Drug interaction , Dissolution tests , Chemotherapy , Research Subject Categories::PHARMACY::Pharmaceutical chemistry
Akinleye MO, Chukwuani CM, Coker HAB and Adepoju-Bello AA (2011). Akinleye MO, Chukwuani CM, Coker HAB and Adepoju-Bello AA (2011). Effect of Chloroquine and Halofantrin on the Dissolution Profile of Ciprofloxacin. Nigerian Journal of Health and Biomedical Sciences, 10 (1):18-24.. Nigerian Journal of Health and Biomedical Sciences, 10 (1):18-24.