Design and in Vitro Characterization of Floating Tablets of Metronidazole

Abstract

Objective: The objective of the present study was to formulate the effervescent floating matrix tablet of metronidazole and to evaluate the effect of varying concentrations of hydrophilic polymers on drug release.
 Methods: Drug excipients interaction was studied by Fourier transform infrared spectrophotometer. The effervescent floating matrix tablets were prepared by direct compression technique using hydroxypropyl methylcellulose (HPMCK4) and xanthan gum alone and in combination as release retardants. Microcrystalline cellulose was used as diluent. Sodium bicarbonate was used as effervescent agent. The prepared matrix tablets were evaluated for their physicochemical parameters such as weight variation, hardness, friability, content uniformity, buoyancy time, and in vitro dissolution.
 Results: Micromeritic properties and post-compression parameters were evaluated and all the parameters were found within the acceptable limit. The drug release data were subjected to different models to evaluate release kinetics and mechanism of drug release. The matrix tablets prepared with xanthan gum and a mixture of xanthan gum and HPMCK4 were retarded the drug release up to 12 h. The release mechanism of metronidazole was evaluated on the basis of release exponent n value in Peppas model. The n value of the formulations ranged from 0.46 to 0.89 which indicated Case II transport and zero-order release.
 Conclusion: Floating matrix tablet is the simple, efficient, and economic method to sustain the release of metronidazole to eradicate Helicobacter pylori in peptic ulcer disease.

Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of H. pylori: Preparation and In Vitro Characterization

“…The same trend exhibited by F4 and F6 prepared with HPMC alone or in combination with sodium alginate had better compressibility followed by retarded floating behavior. These results are in agreement with the findings of other authors who manipulated flow behavior and compaction of different grades of HPMC [ 29 ].…”

“…It was observed that HPMC K4M, due to less viscosity and low molecular weight, could not maintain matrix integrity sufficiently when used alone and did require sodium alginate combination to control the drug release. It is important to study matrix integrity of the floating tablets, because lack of tablet physical integrity could result into smaller fragments after being broken down and an escape from GIT [ 29 ]. Drug release from floating tablets up to larger extent does not depend on agitational intensity or rotational speed of the release media.…”

“…Randomly selected five floating tablets from each batch were subjected to hardness testing. The hardness value was expressed in kg/cm 2 unit [ 29 ]. Roche friabilator was used to determine friability of prepared tablets.…”

Formulation and evaluation of floating tablet of nimesulide by direct compression method

“…In our study, the use of HPMC resulted in an immediate release of drugs without any control of drug release. However, it showed quiet control in drug release when used in combination with another polymer, which was also observed in research by Eswaraiah et al that HPMC due to its lower viscosity and low molecular weight, could not maintain matrix integrity sufficiently when used alone and did require combination of other polymer to control drug release [28]. The data of dissolution revealed that the combination use of the polymer showed an increase in total floating time than used in individual form.…”

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“…Chinna eswaraiah et al, (2019) 17 clarifies the effervescent floating matrix tablet of metronidazole and assesses the impact of fluctuating groupings of hydrophilic polymers on sedate discharge. Drug excipients association was concentrated by Fourier change infrared spectrophotometer.…”