Quantitative prediction of the bitterness of atomoxetine hydrochloride and taste-masked using hydroxypropyl-β-cyclodextrin:A biosensor evaluation and interaction study  

作　　者：Shuying Li Ying Zhang Abdur Rauf Khan Shuwang He Yingxin Wang Jiangkang Xu Guangxi Zhai 

机构地区：[1]Department of Pharmaceutics,College of Pharmacy,Shandong University,Jinan,250012,China [2]Department of Pharmaceutical Development,Shandong Dyne Marine Biopharmaceutical Limited Corporation,Rongcheng,264300,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2020年第4期492-505,共14页亚洲药物制剂科学（英文）

基　　金：Support received from the National Major Scientific and Technological Special Project for“Significant New Drugs Development”during the Thirteenth Five-year Plan Period,P.R.China(2018ZX09721003-002-004);the Major Research Project of Shandong Province,P.R.China(2018GSF118004);the Key Research and Development Program of Shandong Province,P.R.China(2018CXGC1411)for their support and encouragement in carrying out this work.

摘　　要：The bitterness of a drug is a major challenge for patient acceptability and compliance,especially for children.Due to the toxicity of medication,a human taste panel test has certain limitations.Atomoxetine hydrochloride(HCl),which is used for the treatment of attention deficit/hyperactivity disorder(ADHD),has an extremely bitter taste.The aim of this work is to quantitatively predict the bitterness of atomoxetine HCl by a biosensor system.Based on the mechanism of detection of the electronic tongue(Etongue),the bitterness of atomoxetine HCl was evaluated,and it was found that its bitterness was similar to that of quinine HCl.The bitterness threshold of atomoxetine HCl was 8.61μg/ml based on the Change of membrane Potential caused by Adsorption(CPA)value of the BT0 sensor.In this study,the taste-masking efficiency of 2-hydroxypropyl-β-cyclodextrin(HP-β-CyD)was assessed by Euclidean distances on a principle component analysis(PCA)map with the SA402B Taste Sensing System,and the host–guest interactions were investigated by differential scanning calorimetry(DSC),powder X-ray diffraction(XRD),nuclear magnetic resonance(NMR)spectroscopy and scanning electron microscopy(SEM).Biosensor evaluation and characterization of the inclusion complex indicated that atomoxetine HCl could actively react with 2-hydroxypropyl-β-cyclodextrin.

关 键 词：Atomoxetine HCl E-tongue Quantitative prediction Host–guest interaction 

分 类 号：R943[医药卫生—药剂学]