Enhancement of Antibacterial Activity of Clarithromycin using Piperine and its Formulation Development
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Abstract
The current study focuses on increasing antibacterial action of clarithromycin and its formulation. Although various clarithromycin tablets are available in the market, but its bioavailability is around 45% and dose given is 250-500mg twice daily. We propose to make use of Piperine for the first time in the prepared formulations to enhance its bio-efficacy and reduce dose. The literature has described Piperine as a potent bio-efficacy booster. Preformulation studies of pure drug Clarithromycin was done by determining its melting point, FTIR, DSC and λmax determination, Standard Calibration curve, etc. which confirmed drug. The compatibility of the drug with the excipients was then assessed using DCS, XRD, and SEM, which revealed that the drug is compatible with every excipient. Zones of inhibition against Staphylococcus aureus and Escherichia coli were measured after mixing CL and piperine in various ratios (1:0.5, 1:1, 1:1.5, 1:2, 1:3, and 1:4). Initially MIC of standard drug was evaluated against Staphylococcus aureus and Escherichia coli. Out of all the ratios, the 1:2 ratio displayed the greatest activity, following which a persistent zone of inhibition was seen. The optimized ratio, 1:2, was employed to develop the formulation. Gastro retentive effervescent floating tablets of Clarithromycin using different concentrations of HPMC K15, Polyethylene Oxide and Sodium Bicarbonate were taken. Formulation was optimized by using Design Expert 11 software, total 9 batches F1- F9 were formulated using two independent variables PEO (X1) and HPMC K15 (X2) whereas Floating Lag Time (Y1) and % Drug Release after 24 hr (Y2) were selected as dependent variable. Out of all these formulations F7 was found to be the optimized formulation. All the formulations were evaluated by various parameters and the results obtained were within the limits. Optimized formulation was also studied for release kinetics.
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References
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