Optimization of HPMC K100M and Sodium Alginate Ratio in Metronidazole Floating Tablets for the Effective Eradication of Helicobacter pylori
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Aim and Objective
The objective of the present study is the Formulation and evaluation of metronidazole floating tablets (MZFT) that are designed to retain in the stomach for a long time for better eradication of Helicobacter pylori (H. pylori), a main cause of peptic ulcer.
Optimization of ratio of synthetic and natural polymers; HPMC K100M and sodium alginate respectively was studied. Drug-excipent compatibility by physical observation and FT-IR studies. Pre-compression studies on directly compressible blends, postcompression studies: Wt. variation, hardness, thickness, floating characteristics, release profiles and kinetics; in vivo X-ray radiographic studies in rabbit and accelerated stability studies as per ICH guidelines of optimized formulation were studied.
Physical observations and FT-IR studies revealed that there was no interaction between the drug and any of the proposed polymers. All the directly compressible blends have good flow characteristics. Post-compression parameters: Wt. variation, hardness, thickness are in acceptable limits. Drug release kinetics of batch F8 (HPMC K100M: Sodium alginate ratio; 14: 1 respectively) suggests it extends the drug release up to 8 h, with a zero order release profile (r2 = 0.999). Drug release process is predominantly by diffusion (as Higuchi r2 = 0.885); and the mechanism of diffusion is by super case-II transport (as Korsemeyer-Peppas, n = 1.033). It is exhibiting floating lag time of 10.3 sec; total floating time and matrix integrity were maintained up to 8 h. Hence F8 is an optimized batch. It passes the test for stability as per ICH guidelines. X-ray radiographic studies of BaSO4 loaded placebo of optimized F8 batch in rabbit, concludes the in vivo floating of MZFT up to 8 h.
These stomach targeted effervescent floating tablets could maintain the minimum inhibitory concentration for sufficient time to allow for local eradication and thereby achieve better efficiency of therapy with improved patient compliance, reduced costs and minimized side effects caused by immediate release dosage forms. Optimization of ratio of synthetic and natural polymers (HPMC K100M and sodium alginate) plays a major role in the success of formulation of MZFT.
Metronidazole floating tablets, HPMC K100M, sodium alginate, in vitro buoyancy studies, in vivo X-ray radiographic studies.