| Background and objectives : levofloxacin − an antibiotic that is one of the most widely used by physicians − is becoming available in several formulations on the market, it is essential to assess whether these different formulations are therapeutically equivalent. Therefore, the physicochemical characteristics of six brands of 500 mg levofloxacin tablets were evaluated in this investigation. These characteristics included weight uniformity, friability, hardness, disintegration time, dissolution profiles in various pH buffers, and similarity factor analysis. Methods: All six brands of levofloxacin tablets (designated S1-S6) were assessed for compliance with pharmacopeial standards, including weight variation, hardness, disintegration time, and friability. Using equipment compliant with the United States Pharmacopeia (USP) standards, dissolution profiles for each brand were determined over a period of 30 minutes using phosphate buffer solutions with pH values of 4.5 and 6.8.. Results: Mean weights of tablets were obtained during the weight uniformity test, with ranges of S6 (498.61 mg) to S2 (528.45 mg). Variation of tablet weights was measured as a standard deviation, with S1 showing the least variation (SD = 1.75 mg) and S4 showing the most variation (SD = 3.99 mg). All formulations tested for friability complied with the Pharmacopeia's limit of 1% or less, with values between 0.08%-0.09%. Hardness of tablets (6.46 kg/cm² - 8.10 kg/cm²) was acceptable for each formulation, but S1 (SD = 0.56) and S2 (SD = 0.83) exhibited greater variability from the mean than the other formulations. Disintegration times ranged from 5.5 to 10 minutes, and conformed to regulatory guidelines for disintegration time of 15 minutes or less, with S1 disintegrating the most quickly. Dissolution testing at pH 4.5 for all formulations except S6 released 95% or more of the drug within 30 minutes; the fastest release was S1 (98.8%). Testing at pH 6.8 improved dissolution rates with near complete release from S1 and S2 (>99%) at 30 minutes. S6 had the slowest dissolution from pH 6.8 (94.9%). The pH dependent solubility of levofloxacin was demonstrated by quicker & more complete dissolution at pH 6.8. In vitro dissolution data demonstrated only S2 met > 50 for similarity to the reference product (S1) at both pH 4.5 and 6.8. Only S5 had a similar profile to S1 at pH 4.5. S3, S4 and S6 all exhibited dissimilar profiles at both pH demonstrating less predictable release profiles. Conclusion: These findings indicate brands can vary greatly when it comes to manufacture quality, some of which are much more consistent with regard to their weight, hardness, and dissolution properties. All formulations conformed to the requirements of the pharmacopeia, but variability in manufacturing, particularly regarding dissolution, can certainly influence the bioavailability of the drug. In addition, this study demonstrates how important strict quality-control measures are to ensuring there is a therapeutic equivalence among the brands of a drug, especially for critical dose antibiotic medications, e.g. levofloxacin. |
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