Functional Assessment of Four Types of Disintegrants and their Effect on the Spironolactone Release Properties

Abstract

Abstract. Spironolactone is a drug derived from sterols that exhibits an incomplete oral absorption due to its low water solubility and slow dissolution rate. In this study, formulations of spironolactone with four disintegrants named as croscarmellose sodium, crospovidone, sodium starch glycolate and microcrystalline cellulose II (MCCII) were conducted. The effect of those disintegrants on the tensile strength, disintegration time and dissolution rate of spironolactone-based compacts was evaluated using a factorial design with three categorical factors (filler, lubricant, and disintegrant). The swelling values, water uptake and water sorption studies of these disintegrants all suggested that MCCII compacts disintegrate by a wicking mechanism similar to that of crospovidone, whereas a swelling mechanism was dominant for sodium starch glycolate and croscarmellose sodium. The disintegration time of MCCII and sodium starch glycolate remained unchanged with magnesium stearate. However, this lubricant delayed the disintegration time of crospovidone and croscarmellose sodium. MCCII presented the fastest disintegration time independent of the medium and lubricant employed. The water sorption ratio and swelling values determined sodium starch glycolate followed by croscarmellose sodium as the largest swelling materials, whereas crospovidone and MCCII where the least swelling disintegrants. The swelling property of sodium starch glycolate and croscarmellose sodium was strongly affected by the medium pH. The disintegration time of spironolactone compacts was faster when starch was used as a filler due to the formation of soft compacts. In this case, the type of filler employed rather than the disintegrant had a major effect on the disintegration and dissolution times of spironolactone.

The effect of superdisintegrants on the properties and dissolution profiles of liquisolid tablets containing rosuvastatin

“…The fastest dissolution was observed in samples with Kollidon Õ , which showed also the best disintegration properties. The similar results were given in the study performed by Rojas et al 45 dealing with spironolactone tablets. Also Preetha et al 46 observed that tablet with crospovidone released the drug faster than tablets with sodium starch glycolate or croscarmellose sodium.…”

Coated pellets with delayed-release glucose for prevention of hypoglycemic episodes

“…As water is absorbed into the interior of particle pores, polymer chains expand into a three-dimensional network in which water is retained. Large three-dimensional swelling of carboxymethyl starch par- ticles was reported, whereas another superdisintegrant, croscarmellose sodium, is able to swell in three dimensions only partially and its swelling ability is therefore lower (20). Slow release in the PEG sample may be attributed to the osmotic effect of polyethylene glycol, which is probably less effective in higher coating concentrations than the swelling ability of disintegrants.…”

A Comparative Study of Different Proportions of Superdisintegrants: Formulation and Evaluation of Orally Disintegrating Tablets of Salbutamol Sulphate

“…22 Quick water uptake and good swelling ability of CCS and SSG is ascribed to the carboxylic moieties in their structure which upon hydration results in gelation. 23 Particle size and amorphous content in the disintegrant may also affect easy water accessibility.…”