The Influence of the Intergranular Superdisintegrant Performance on New Drotaverine Orodispersible Tablet Formulations

Abstract

The main objective of this study consists in establishing the influence of the intergranular superdisintegrant on the specific properties of drotaverine hydrochloride fast-dissolving granules (DROT-FDGs) and orodispersible tablets (DROT-ODTs). The orodispersible tablets were obtained by the compression of the FDGs and excipient mixture with an eccentric tableting machine. To develop DROT-ODTs, two types of superdisintegrant excipients in different concentrations (water-soluble soy polysaccharides (SSP) (1%, 5%) and water-insoluble soy polysaccharides—Emcosoy® STS IP (EMCS) (1%, 3%, 5%)) were used, resulting in five formulations (D1–D5). The DROT-FDGs and the DROT-ODTs were subjected to pharmacotechnical and analytical evaluation. All the orodispersible tablets obtained respect the quality requirements in terms of friability (less than 1%), crushing strength (ranging between 52 N for D2 and 125.5 N for D3), and disintegration time (<180 s). The in vitro release of drotaverine from ODTs showed that all formulations presented amounts of active substance released greater than 85% at 10 min. The main objective, developing 30 mg DROT-ODTs for children aged between 6 and 12 years by incorporating the API in FDGs, was successfully achieved.

Ion exchanger‐based electrodes for determination of highly lipophilic physiologically active amines: Peculiarities of functioning and ways for improving analytical characteristics

“…It is characteristic that the strongest difference between the experimentally obtained E -pH dependence and the calculated one is observed for the most hydrophobic of the studied amines, amiodarone. At the same time, the coincidence of the experimental and calculated dependences for drotaverine, which is one of the most hydrophobic amines (LogP = 5.35, pKa = 7.11 [45]; seems, at first glance, unexpected. Perhaps that the high affinity of drotaverine for octanol is caused by the presence in its molecule of four electron-donating groups capable of interacting with octanol through the formation of hydrogen bonds, whereas in the case of NPOE this possibility is absent.…”