Effect of mode of superdisintegrant incorporation on tableting properties of metronidazole granules

Abstract

Superdisintegrants are a special class of excipients used in a tablet formulation to aid disintegration and possibly enhance the release kinetics of a drug. The intragranular and extragranular effect of sodium starch glycolate (SSG) or croscarmellose sodium (CCM) as superdisintegrants on tableting properties of metronidazole granules were investigated. The granules were characterized for particle size analysis, angle of repose, bulk and tapped densities as well as Carr's index (CI) and Hausner's ratio (HR). Tablets were prepared from each batch of granules weighing 500 mg on a single punch tablet press using 12 mm flat-faced punches and compressed at 57.5 MPa. The tablets were kept at 25 ± 2 °C/75 % RH for 24 h to allow for elastic recovery and the properties of weight variation, content uniformity, thickness, crushing strength (CS), disintegration time (DT), and drug-release were evaluated. The results showed that all the batches of granules exhibited good flow based on angle of repose < 30° , CI < 20 %, and HR ≤ 1.2. The evaluated tablet properties demonstrated that intragranular addition of either SSG or CCM lowered the CS and DT when compared to the extragranular effect. This indicates that the incorporation mode of superdisintegrant in a tablet formulation exerts an influence on tablet properties.

Impact of Compressional Force, Croscarmellose Sodium, and Microcrystalline Cellulose on Black Pepper Extract Tablet Properties Based on Design of Experiments Approach

“…In some cases, the use of CCS exceeding approximately 7.5% has been reported to prolong the DT of rapidly disintegrating tablets containing aspirin, ibuprofen, and ascorbic acid [22]. Although sodium starch glycolate (SSG) is commonly used as a disintegrant due to its good swelling and water uptake properties compared to CCS [26], CCS was found to be superior to SSG in terms of shortening the DT [27]. In this work, CCS had the main impact on DT compared to other properties (Figure 1b), while the other properties were not significantly affected by CCS.…”