Abstract

Aims: This research was done to study the effects of types and concentrations of lubricants on the dissolution and disintegration profile of metronidazole tablets formulated using Sida acuta gum as a binder.
 Methodology: Sida acuta gum (SAG) was extracted from powdered dried leaves of Sida acuta. Metronidazole granules were produced by wet granulation technique using different concentrations (1 and 2%) of SAG as a binder and mixed with different concentrations (0.5, 1.0, and 1.5%) of magnesium stearate (MS) or sodium lauryl sulphate (SLS) as a lubricant. The granules/lubricant -mix was compressed into tablets and evaluated for hardness, weight uniformity, drug content, disintegration time, friability and in vitro drug release.
 Results: The hardness for the tablets was from 4.08 to 7.97 Kgf. The friability was from 0.02±0.45 to 3.40±0.43%. Tablets from formulations A1-A3, B2, and B3 failed the friability test. Formulations prepared with 1% SAG were more friable than those formulated with 2% SAG. Disintegration time for formulations A1-A3 (1% SAG + MS) ranged from 19.07 to 63.5 min, while that of A4-A6 (2% SAG + MS) was from 39.06 to 81.48 min. Formulations B1-B3 (1% SAG + SLS) had disintegration time that ranged from 4.22 to 6.8 min while that of B4-B6 (2% SAG + SLS) was from 9.35 to 15.90 min. The % drug release at 60 min for formulations that contained SAG and MS was 76.60-104.28% and SAG and SLS was 99.89-101.35%
 Conclusion: Metronidazole tablets formulated using SLS as lubricant disintegrated faster than those formulated using magnesium stearate as lubricant. Percentage drug release from tablets containing SLS was slightly higher than those that contained magnesium stearate. Higher concentrations of the lubricants produced softer tablets.

Highlights

  • Drugs administration through the oral route is the most convenient and frequently used route of drug delivery because it grants the availability of many options in dosage form design [1]

  • These results show that the granules had low interparticulate friction and good flow

  • The results show that an increase in binder concentration leads to an increase in the disintegration time of the metronidazole tablets [28]

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Summary

Introduction

Drugs administration through the oral route is the most convenient and frequently used route of drug delivery because it grants the availability of many options in dosage form design [1]. Tablet as a dosage form is the most common drug delivery system and several types of tablets have been formulated They include; oral tablets for ingestion such as conventional tablets, multiple compressed tablets, layered tablets, modifiedrelease tablets, delayed action tablets, and floating tablets; tablets used in the oral cavity such as lozenges, sublingual tablets, and buccal tablets; and tablets administered by other routes such as vaginal tablets and implants [3]. They are produced using different techniques such as wet granulation, direct compression, or dry granulation. Excipients used for manufacturing of tablets include; binders, disintegrants, fillers, sweeteners, flavours, colourants, sorbents, anti adherent, lubricants, and glidants [5]

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