Development and evaluation of bilayer tablets of combination of antibiotics for the treatment of sexually transmitted disease

ABSTRACT The present research work was envisaged to develop bilayer tablets to improve therapeutic efficacy of antibiotic combination for the treatment of sexually transmitted diseases. The combination of two antibiotics i.e. cefixime trihydrate and ofloxacin were used for the preparation of bilayer tablets which act against genito-urinary infections. The formulations comprise of cefixime trihydrate as immediate release layer formulated using different superdisintegrants and ofloxacin as extended release layer containing HPMC K100M. Evaluation of bilayer tablets were performed for the immediate release cefixime layer and sustain release ofloxacin layer with optimization of excipients. The immediate release layer of cefixime showed complete release within 30 min and ofloxacin release was extended up to 24 hours. The similarity factor value of ofloxacin sustained release layer was found to be 87.01 for initial and 80.35 after 3 months stability when compared with marketed reference product. The present study revealed that cefixime trihydrate and ofloxacin bilayer tablets were successfully developed for the use against sexually transmitted infections.

Influence of Sodium CMC and HPMC on the Physical Characteristics of Ofloxacin Floating Matrix Tablets.

Aims: Sustained release floating drug delivery systems or gastro retentive drug delivery systems enables prolonged and continuous input of drug to the upper part of gastrointestinal tract and improves the bioavailability of medication. A new strategy is proposed for the development of floating drug delivery systems of Fluoroquinolone antibiotic, Ofloxacin, a potent moiety for treating UTI’s. Methodology: Various rate retarding polymers like HPMC K4M, HPMC 5 cps and swelling agent as Sodium carboxymethyl cellulose in different proportions were tried and optimized to achieve the drug release for 8 hr. All the formulations were evaluated for floating properties, swelling characteristics and in vitro drug release studies. The in vitro drug release was found to be matrix diffusion controlled. Optimized formulation was subjected to intermediate stability studies at various combinations of temperature and humidity according to ICH guidelines. Results: Lower hardness and higher thickness decreased the floating lag time and increased floating duration. Based on drug release studies, formulation F5 was optimized as the best formulation because it released about 89.27 ±2.6% of the drug at the end of 8 hr while other formulations released not more than 80 ±2.2%. This may be due to high NaCMC content which might have caused excessive channeling, thereby giving a burst release. Optimized formulation F5 was found to follow zero order kinetics with r2 value of 0.993. Conclusion: In conclusion we have been proved that HPMC K4M has retarded the drug release, while HPMC 5cps has facilitated high buoyancy time for the tablets. NaCMC has influenced as channeling agent. Formulation F5 was optimized for its long buoyancy time, prolonged duration of drug release, zero order and diffusion controlled drug release kinetics which can assure 100% bioavailability.