A novel and discriminative method of in vitro disintegration time for preparation and optimization of taste-masked orally disintegrating tablets of carbinoxamine maleate

Abstract

The primary objective of this study was to mask bitter taste and decrease the disintegration time of carbinoxamine maleate (CAM) orally disintegrating tablets (ODTs). In order to screen the prescription of ODTs, a novel modified in vitro disintegration method (MIVDM) was developed to measure the in vitro disintegration time. In this method, different concentrations of ethanol served as disintegration medium in order to delay the in vitro water absorption and disintegration process of tablets. The MIVDM demonstrated good in vitro and in vivo correlation and proved more precise and discriminative than other reported methods. In this research, ion exchange resins (IERs) were used to mask bitter taste for improving mouthfeel. The drug-resin ratio and reaction temperature were investigated to obtain the optimum carbinoxamine resin complexes (CRCs). The characterization of CRCs revealed an amorphous state. ODTs were prepared by direct compression. Superdisintegrants and diluents of ODTs were screened first. Further optimization was carried out by using Box-Behnken design. The effect of (X) mannitol/microcrystalline cellulose ratio, (X) the amount of low-substituted hydroxypropylcellulose and (X) the hardness was investigated for achieving the lowest (Y) in vitro disintegration time. Technological characterization, wetting time, water absorption ratio, and roughness degree were evaluated. The CRCs and ODTs proved successful taste-masking efficiency. The end product improved patients' compliance. The developed MIVDM was practical for commercial use.

Ion Exchange Resins as Carriers for Sustained Drug Release

“…It has a very short half-life necessitating frequent dose administration (3 -4 times a day). It can also cause gastrointestinal irritation and have a bitter taste [65]. Generally, children are affected by allergic rhinitis; hence the drug is preferred in the form of an oral liquid suspension for better compliance.…”

Strategies for Taste Masking of Orodispersible Dosage Forms: Time, Concentration, and Perception

“…Many ion resins, such as Indon 234, Kyron T-314, and a selection of the Amberlite series, − can be utilized as disintegrants, which disintegrate more quickly with the lower dosage and do not lump, compared with traditional disintegrating agents. , Its working principle is related to the resins’ core absorption and swelling properties, improving drug taste without additional disintegrating agents, suitable for taste masking in oral disintegrating dosage forms . However, to yield the optimal masking effect without affecting other properties of the dosage forms like the drug release, types, and dosage of resins should be considered when using DRC taste masking in the orodispersible dosage forms. , If it performs well, then the above consideration will be unnecessary.…”

Overview on the Orally Disintegrating Tablet Formulations

“…Püskürterek kurutulmuş laktoz kullanılarak hazırlanan tabletlerin diğer tabletlere göre daha kısa zamanda dağıldığı belirlenmiştir. 22 Yaygın olarak kullanılan süper dağıtıcı maddeler ve etki mekanizmaları Tablo 2'de görülmektedir. 23 Hacim arttırıcılar: Formülasyonda hacim arttırıcılar, seyreltici ve dolgu maddelerinin etkinliklerine katkıda bulunmaktadırlar.…”