Polycaprolactone And Polycaprolactone Triol Blends To Obtain A Stable Liquid Nanotechnological Formulation: Synthesis, Characterization And In Vitro - In Vivo Taste Masking Evaluation

Juliana Emanuelli ◽  
Viviane Pagnussat ◽  
Katherine Krieser ◽  
Julia Willig ◽  
Andréia Buffon ◽  
2018 ◽  
Vol 15 (11) ◽  
pp. 1105-1116
Basheer Al-Kasmi ◽  
Okba Al Rahal ◽  
Hind El-Zein ◽  
Abdul-Hakim Nattouf


Objective: The aim of the present research work was to prepare and evaluate taste-masked oral disintegrating tablets (ODT) of Fexofenadine hydrochloride. Methods: In the present work, Eudragit EPO, a taste masking agent and Karaya gum (GK) (natural), Sodium starch glycolate, and Croscarmellose sodium (CCS) (semi-synthetic) super disintegrants in three ratios (3, 6,9%) were used. Taste masked granules were prepared by different ratios of the drug: Eudragit EPO (1:1, 1:1.5, 1:2) by wet granulation method. The optimized taste-masked granules (1:2) were selected by sensory evaluation test to prepare 9 Fexofenadine ODT (FH1-FH9) formulations. These were evaluated for different parameters. Then desirability function (DF) was calculated for all formulations using disintegration time (DT), time taken for the tablet to release 90% of the drug (t 90%), and % drug dissolved in 10 min (Q10) as significant parameters. Results: The best formulation (FH6) showed the highest DF value due to less DT and 100% in vitro drug release within 15 min. Thus, FH6 formulation containing 9% CCS was selected as the best among the prepared formulations to which in vivo studies were performed on rabbits to find maximum plasma concentration (Cmax), time taken to reach maximum concentration (tmax), area under the curve (AUC), rate of elimination (Kel), absorption rate (Ka) and half-life(t1/2) and compared with Fexofenadine (Allegra) marketed tablets. Total bioavailability was increased for the test formulation compared to the reference formulation. Conclusion: Fexofenadine was successfully prepared as ODT with increased AUC and decreased tmax to which stability studies were conducted which were found to be stable.

2013 ◽  
Vol 50 (10) ◽  
pp. 39-46
V Prakash ◽  
L. Keshri ◽  
V. Sharma ◽  
K. Pathak

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

Polymers ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 522 ◽  
Katarzyna Wasilewska ◽  
Marta Szekalska ◽  
Patrycja Ciosek-Skibinska ◽  
Joanna Lenik ◽  
Anna Basa ◽  

The taste of drugs is an important factor affecting pharmacotherapy effectiveness, and obtaining formulations with acceptable organoleptic properties is still an ongoing issue in pharmaceutical technology. One of the innovative methods of taste masking is preparation of microparticles by the spray drying technique, utilizing polymers with different physicochemical properties. Rupatadine fumarate (RUP) is one of the newest antihistamines, with an innovative and multidirectional mechanism of action, and an extremely bitter taste. The aim of this work was to investigate the feasibility of utilizing organic or aqueous forms of ethylcellulose (EC) for the preparation of microparticles with RUP by the spray drying technique. Spray dried samples at different drug:polymer ratios were prepared using organic solution (Ethocel®) or aqueous dispersions of EC (Surelease®, Aquacoat® ECD). Evaluation of the taste masking efficacy was performed in vivo in human taste panel, in vitro based on dissolution test, and by self-constructed electronic tongue. It was shown that microparticles obtained from aqueous dispersions of EC have superior pharmaceutical properties in terms of both morphology and taste masking efficacy in comparison to those obtained from organic solution.

2019 ◽  
Vol 49 ◽  
pp. 547-555 ◽  
Xiaopeng Han ◽  
Shan Zhang ◽  
Zhuodong Chai ◽  
Yangyun Dong ◽  
Wei He ◽  

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 369 ◽  
Alison V. Keating ◽  
Jessica Soto ◽  
Claire Forbes ◽  
Min Zhao ◽  
Duncan Q. M. Craig ◽  

The unpalatability of antituberculosis drugs is often cited as a major cause of non-adherence in children, yet limited quantitative taste assessment data are available. The aim of this research was to quantify the bitterness of isoniazid, rifampicin, pyrazinamide, and ethambutol dihydrochloride using two in vivo (a human taste panel and a rat brief-access taste aversion (BATA) model) and one in vitro (sensor) method. The response of the Insent TS-5000Z electronic tongue was compared to the in vivo drug concentration found to elicit and suppress half the maximum taste response (EC50 in human and IC50 in rats). Using dose-relevant concentrations, an overarching rank order of bitterness was derived (rifampicin > ethambutol > pyrazinamid~isoniazid). In vitro, only ethambutol exhibited a linear response for all sensors/concentrations. Based on the EC50/IC50 generated, a ‘taste index’ was proposed to allow for anticipation of the likelihood of taste issues in practice, taking in account the saturability in the saliva and therapeutic doses; ethambutol and isoniazid were found to be the worst tasting using this measure. The study presents the first quantitative taste analysis of these life-saving drugs and has allowed for a comparison of three methods of obtaining such data. Such information allows the operator to identify and prioritise the drugs requiring taste masking to produce palatable formulations.

2014 ◽  
Vol 466 (1-2) ◽  
pp. 286-295 ◽  
Eun-Jin Yi ◽  
Ju-Young Kim ◽  
Yun-Seok Rhee ◽  
Su-Hyeon Kim ◽  
Hyo-Joong Lee ◽  

2017 ◽  
Vol 67 (1) ◽  
pp. 113-124 ◽  
Aleksandra Amelian ◽  
Marta Szekalska ◽  
Patrycja Ciosek ◽  
Anna Basa ◽  
Katarzyna Winnicka

Abstract Taste of a pharmaceutical formulation is an important parameter for the effectiveness of pharmacotherapy. Cetirizine dihydrochloride (CET) is a second-generation antihistamine that is commonly administered in allergy treatment. CET is characterized by extremely bitter taste and it is a great challenge to successfully mask its taste; therefore the goal of this work was to formulate and characterize the microparticles obtained by the spray drying method with CET and poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate 1:2:1 copolymer (Eudragit E PO) as a barrier coating. Assessment of taste masking by the electronic tongue has revealed that designed formulations created an effective taste masking barrier. Taste masking effect was also confirmed by the in vivo model and the in vitro release profile of CET. Obtained data have shown that microparticles with a drug/polymer ratio (0.5:1) are promising CET carriers with efficient taste masking potential and might be further used in designing orodispersible dosage forms with CET.

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