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.

Highlights

  • Oral route is the most convenient route for the drug delivery due to low cost of the therapy, ease of administration leads to high level of patient compliance and flexibility in the designing of dosage form

  • To improve the performance of oral controlled release dosage forms (OCRDFs), a new concept was discovered by scientists in drug delivery that is gastroretentive drug delivery systems (GRDDSs)

  • Xanthan gum could control the release of metronidazole up to 12 h due to its high molecular weight. These results indicate that xanthan gum has higher drug retarding ability than HPMCK4

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Summary

Introduction

Oral route is the most convenient route for the drug delivery due to low cost of the therapy, ease of administration leads to high level of patient compliance and flexibility in the designing of dosage form. Novel oral drug delivery systems classified into oral controlled release dosage forms (OCRDFs) and targeting dosage forms [1]. Variable and short gastric residence time results in decreased efficacy of the administered dose when administered in the form of OCRDF. To improve the performance of OCRDF, a new concept was discovered by scientists in drug delivery that is gastroretentive drug delivery systems (GRDDSs). A floating drug delivery system floats in the gastric juice without affecting the gastric emptying rate. This technique can provide therapeutically effective plasma drug concentration for longer durations, thereby reducing the dosing frequency and minimizing fluctuations and helps to increase a drug’s gastric residence time and reduces the variability in bioavailability [3]

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