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Published on: August 28, 2015
Investigation and Optimization of the Effect of Polymers on Drug Release of Norfloxacin from Floating Tablets
Dipak D Gadade1, Kalpana Sarda1, Sadhana R Shahi2
1Shri Bhagwan College of Pharmacy, Aurangabad, India.
Background:
Norfloxacin is fluoroquinolone anti-infective used in the treatment of urinary tract infections, prostatitis, gonorrhea and genital tract infections. It has plasma half life of 3 to 4 h requiring multiple dosing in the treatment. Releaseretarding polymers can be used to modulate the drug release of norfloxacin.
Objectives:
The objective of this study was to investigate the effect of release-retarding polymers on the drug release of norfloxacin from floating tablets.
Material And Methods:
Norfloxacin was procured as a gift sample from Concept Pharma Ltd. Aurangabad (India) and HPMC K100M was procured as a gift sample from Colorcon Asia Pvt. Ltd., Goa (India). The tablets were prepared by direct compression method and various pharmaceutical parameters were evaluated.
Results:
It was observed that all tablet formulations F1-F9 retained the drug release up to 12 h with good floating property but only Batch-F4 complies with the USP dissolution limits with a minimum floating lag time. The drug release kinetics were evaluated by the model-dependent (curve fitting) method using PCP Disso v3 software shows Batch-F4 shows to best fit with Peppas model for which R2 value was 0.9921 and the release exponent value was 0.6892.
Conclusions:
The drug release kinetics study indicates that the floating tablets release the drug by diffusion followed by erosion mechanism. Obtained in-vitro drug release data was analyzed by design expert software for drug release at first hour and at 12th h values and found that release the selected independent variables like HPMC K100M and sodium alginate concentration has a significant effect on drug release.
Insights
This study optimized norfloxacin floating tablets using release-retarding polymers, achieving 12-hour drug release. Batch-F4 demonstrated optimal performance, complying with USP limits and showing good floating properties.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Polymer Science
Background:
- Norfloxacin, a fluoroquinolone antibiotic, is used for various infections but requires frequent dosing due to its short half-life.
- Release-retarding polymers offer a strategy to control norfloxacin release and improve therapeutic efficacy.
- Floating tablet technology can enhance drug retention time in the gastrointestinal tract.
Purpose of the Study:
- To investigate the impact of release-retarding polymers on norfloxacin release from floating tablets.
- To optimize the formulation of norfloxacin-loaded floating tablets for sustained drug delivery.
- To evaluate the pharmaceutical properties and drug release kinetics of the developed floating tablets.
Main Methods:
- Norfloxacin and hydroxypropyl methylcellulose (HPMC K100M) were used in tablet formulations.
- Tablets were prepared using the direct compression method.
- In-vitro drug release, floating properties, and drug release kinetics were evaluated using specialized software.
Main Results:
- All tested formulations (F1-F9) exhibited drug release for up to 12 hours with satisfactory floating characteristics.
- Batch-F4 formulation met USP dissolution limits and displayed minimal floating lag time.
- Drug release kinetics analysis indicated that Batch-F4 best fits the Peppas model (R²=0.9921, release exponent=0.6892).
Conclusions:
- The floating tablets release norfloxacin via a combined diffusion and erosion mechanism.
- Formulation variables, specifically HPMC K100M and sodium alginate concentrations, significantly influence drug release.
- Batch-F4 represents a promising formulation for sustained norfloxacin delivery.
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