Abstract
Metronidazole has the potential to produce local stomach specific action in order to treat Helicobacter pylori induced peptic ulcer disease. The current project executes the development of osmotically controlled bioadhesive metronidazole loaded effervescent floating tablets with optimized floating and swelling behavior. Direct compression technique was used to prepare the tablets. The designed formulations exhibited physico-chemical properties within acceptable optimum limits as per pharmacopeial requirements. The results of tablet floating studies revealed that all formulations, except F1 and F5, had good buoyancy characteristics (TFT > 12 h except F2 and F8 with TFT of 6 h). Formulation F2 containing guar gum in higher concentration with carbopol and formulation F8 containing guar gum in 50% decreased concentration in combination with HPMC and carbopol had enhanced FLT appreciably, with least TFT as compared to formulations F3, F4, and F6 (ANOVA; p ≤ 0.05). Formulation batches of F3, F4, and F6 exhibited appreciable FLT as well as TFT and were optimized formulations. Out of the above mentioned optimized batches, F4 and F6 formulations showed low FLT (4 and 5 s respectively). The results of the swelling study indicated a proportionate increase in the swelling index with increase in time. A significantly higher swelling ratio was found with formulation F6 and F4 compared with that of F7 and F8 (ANOVA; p ≤ 0.05). Additionally, the impact of pH change, agitational intensity, as well as increasing concentration of NaCl was investigated on drug release. It was observed that agitational intensity had no effect on drug release rate while increasing concentration of NaCl produced an increased drug release from the dosage form as compared to the drug release exhibited by the formulations in the absence of NaCl. Overall, this project could have valuable contribution in the fabrication of metronidazole loaded effervescent floating tablets. Gastro-retentive systems are expected to enhance local stomach specific action of anti H. pylori agents based on their buoyancy and swelling behavior.
Highlights
Drug administration through the oral route is considered as the most appropriate, feasible, and the most convenient mode as far as the delivery of drugs is concerned, with numerous benefits such as safety, self-administration, cost economical, non-invasive, and improved patient compliance [1]
The oral route is sometimes associated with different issues that are major obstacles, e.g., patterns of gastric emptying, minimum drug residence, failure of drug targeting in specific area, and negligible drug release [2]
Metronidazole was kindly gifted by Ferozsons Laboratories, Nowshehra, KPK, Pakistan; HPMC K4M, carbopol, guar gum (Dow Chemical Company, Midland, MI, USA), chitosan and sodium alginate were used as bio-adhesive polymers, microcrystalline cellulose employed as diluent, talc as glidant, magnesium stearate
Summary
Drug administration through the oral route is considered as the most appropriate, feasible, and the most convenient mode as far as the delivery of drugs is concerned, with numerous benefits such as safety, self-administration, cost economical, non-invasive, and improved patient compliance [1]. Metronidazole has bactericidal effect and is efficacious to kill microorganisms, either facultative anaerobes or obligate anaerobes. It sits right in the cusp among medications selected for the management of Helicobacter pylori, i.e., it constitutes an important member of triple regimen therapy as an active adjunct [3,4]. Metronidazole is a class 1 type of drug in the biopharmaceutical classification system. It undergoes absorption in the stomach and possesses pH-independent effects [5,6]. Metronidazole exhibits a rapid and almost complete absorption when given orally [7]
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