Preparation and Characterization of Carboxymethylated and Cross-Linked Enset Starch as a Disintegrant in Tablets

Abstract

Starch and modified starches have been commonly employed as excipient in pharmaceutical industry. The use of non-modified or “native” starch,  However, is mostly confined due to limitation in several physicochemical properties. Cross-linked sodium carboxymethyl starch which is also known as sodium starch glycolate is extensively used in fast dissolving tablets to disperse the drugs within short span of time. In this study, enset starch was carboxymethylated and subsequently cross-linked. Carboxymethyl enset starch (CMES) was obtained by reacting enset starch and monochloroacetic acid (MCA) in the presence of sodium hydroxide. CMESs having different degree of substitution (DS) were cross-linked at various
concentrations (2.5, 5 and 10% w/w) of sodium hexametaphosphate (SHMP) to provide sodium starch glycolate of enset starch (SSG-E). The fourier transform infrared (FTIR) spectra confirmed the presence of carboxymethylated group in the modified starch granules with new band at 1608.52 cm-1. This dually modified enset starch (SSG-E) was evaluated as a potential disintegrant in paracetamol tablets in comparison with commercially available sodium starch glycolate, Disegel. Carboxymethylation was significantly influenced by reaction medium, reaction temperature and reaction time (p < 0.05). CMES with higher DS (0.437 ± 0.03) exhibited higher peak viscosity than CMES with lower DS (0.224 ± 0.01). Despite exhibiting greater swelling power, CMES showed significantly lower pasting viscosity compared to the native starch (p < 0.05). At 2.5% SHMP, the dually modified starch (SSG-E) exhibited significant increase in swelling but its rate of water-uptake was lower than that of Disegel. As the SHMP concentration was
increased from 2.5 to 5%, the swelling power decreased significantly (p < 0.05). When the concentration was increased to 10% the swelling power increased significantly (p < 0.05). At 2.5% SHMP concentration SSG-E showed a viscosity comparable to that of CMES. As the concentration of SHMP increased to 5 and to 10% w/w, significant decrease in viscosity (p < 0.05) was observed. Compared to the native enset starch (NES), the solubility of SSG-E was more than 4-fold, but its viscosity was much lower than that of CMESs. The SSG-E exhibited lower moisture sorption than CMES but higher sorption than NES. SSG-E showed good flowability, superior swelling power and solubility than NES. The disintegration time (DT) of paracetamol tablets containing SSG-E as a disintegrant was comparable to those tablets with similar concentration of Disegel. At 4% SSG-E, paracetamol tablets exhibited DT less than 1 min.

Keywords: carboxymethylation, degree of cross-linking, enset starch, paracetamol tablets, sodium starch glycolate