Preparation and evaluation of taste masked oral suspension of arbidol hydrochloride

The purpose of this study was to cover the bitter taste of arbidol hydrochloride(ARB)and develop dry suspension with combination of solid dispersion and flavors.Taste masking was successfully done by solid dispersion using octadecanol as the carrier by fusion method.Suspending agents,carriers and other excipients were selected.Differential scanning calorimetry(DSC)and Fourier transform infrared spectroscopy(FTIR)were performed to identify the physicochemical interaction between drug and carrier,DSC analysis indicated that ARB was amorphous in the solid dispersion,FTIR spectroscopy showed no interaction between drug and carrier.Taste masking was evaluated on six volunteers with a score of 4.9.The results demonstrated successful taste masking.Water was used to study the in vitro dissolution performance of the three formulations of commercial tablet,capsule and self-made suspension.The self-made suspension showed a lower and slower release,the insoluble carrier octadecanol blocked the drug dissolving from the solid dispersion.It was indicated from the primary stability study,the self-made suspensions were sensitive to high temperature,high humidity and strong light conditions,they should be stored in sealed containers away from heat,light and humidity.

Development and evaluation of taste-masked dry suspension of cefuroxime axetil for enhancement of oral bioavailability

Cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally.This work was to mask the bitter taste of CA and enhance its oral bioavailability.Dry suspensions were prepared by means of wet granulation method and solid dispersion method.Binders,suspending agents and other compositions involved in the formulation were optimized.The differential scanning calorimetry(DSC)analysis indicated that CA was amorphous in the solid dispersion with stearic acid as the carrier,which contributed to an improvement of the dissolution rate.Taste evaluation was performed by three volunteers and taste masking was successfully achieved by the methods mentioned above.A pH 7.0 phosphate buffer was adopted to study the in vitro dissolution performance of the three formulations,i.e.,two self-made dry suspensions and the commercial one.With a better release characteristic and a satisfying taste masking ability,the solid dispersion suspension was selected as the optimal formulation for the further pharmacokinetic study in beagle dogs.The values of Cmax and AUC0e12 for the solid dispersion suspension were about 1.78-fold and 2.17-fold higher than these of reference suspension,respectively.The obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability.

Taste masking of ciprofloxacin by ion-exchange resin and sustain release at gastric-intestinal through interpenetrating polymer network

The aim of the study was to taste mask ciprofloxacin(CP)by using ion-exchange resins(IERs)followed by sustain release of CP by forming interpenetrating polymer network(IPN).IERs based on the copolymerization of acrylic acid with different cross linking agents were synthesised.Drug-resin complexes(DRCs)with three different ratios of drug to IERs(1:1,1:2,1:4)were prepared&evaluated for taste masking by following in vivo and in vitro methods.Human volunteers graded ADC 1:4,acrylic acid-divinyl benzene(ADC-3)resin as tasteless.Characterization studies such as FTIR,SEM,DSC,P-XRD differentiated ADC 1:4,from physical mixture(PM 1:4)and confirmed the formation of complex.In vitro drug release of ADC 1:4 showed complete release of CP within 60 min at simulated gastric fluid(SGF)i.e.pH 1.2.IPN beads were prepared with ADC 1:4 by using sodium alginate(AL)and sodium alginate-chitosan(AL-CS)for sustain release of CP at SGF pH and followed by simulated intestinal fluid(SIF i.e.pH 7.4).FTIR spectra confirmed the formation of IPN beads.The release of CP was sustain at SGF pH(<20%)whereas in SIF media it was more(>75%).The kinetic model of IPN beads showed the release of CP was non-Fickian diffusion type.

taBOX: A water-soluble tetraanionic rectangular molecular container for conjugated molecules and taste masking for berberine and palmatine

A water-soluble macrocycle that bears four carboxylate anions has been designed and prepared,which forms a rectangular cavity that can efficiently encapsulate discrete electron-deficient aromatic compounds,including berberine and palmatine.This macrocycle is revealed to be highly biocompatible and able to inhibit the bitter taste of the two drugs.

Optimization of Jiawei Qing'e Oral Fast Disintegrating Tablets Based on Response Surface-Central Composite Design

Abstract: Objective To apply the response surface-central composite design to developing and optimizing the oral fastdisintegrating tablets (ODT) formulation for Jiawei Qing’e, a kind of prescription of Chinese herbal medicine.Methods The bitterness of Jiawei Qing’e was masked using Eudragit E-100 by solvent evaporation technique.Response surface approach was applied to investigating the interaction of formulation parameters in optimizing theformulation. The independent variables were Eudragit E-100/drug ratio (X1), amount of disintegrants (X2), and theamount of diluents (X3). The disintegration time (Y1), hardness (Y2), and weight variations of the tablets werecharacterized. Results The models predicted levels of X1= 4.63%, X2= 5.25%, and X3= 34.33%, for the optimalformulation having a hardness of 3.0 kg with the disintegration time of 30 s within experimental region. The observedresponse of Y1= 26.5 s and Y2= 3.14 kg reasonably agreed with the predicted response. Conclusion Responsesurface methodology shows the good predictability and reliability in optimizing the formulation. The optimized ODTof Jiawei Qing’e has acceptable taste, rapid disintegrating ability, and good mechanical strength.