A Proposed Methodology for In Vitro Evaluation of Bitterness in Drug Solutions and In Vitro Drug Release Samples

作者：Dev Kapil; Kharb Vandana; Singh Anupama; Saharan Vikas Anand^*; Jadhav Hemant; Purohit Suresh

来源：Journal of Pharmaceutical Innovation, 2014, 9(3): 183-191.

DOI：10.1007/s12247-014-9185-2

• Taste assessment
• Bitterness threshold
• Taste panel
• Drug release
• Ondansetron
• In vitro

Ethical and safety concerns, paediatric taste panels and predictivity in early drug development for strategic decisions are some of the reasons for seeking in vitro methods of bitterness evaluation for drugs and drug products. In this study, taste panel studies and in vitro drug release studies have been performed, correlated to each other and proposed as an analytical tool for evaluation of bitterness. %26lt;br%26gt;Bitterness threshold and bitterness scores for different solutions of ondansetron hydrochloride (ONS) were estimated by taste panel studies. In vitro drug release studies on taste-masked drug product in pharmacopoeial apparatus and an in-house-developed apparatus were performed and correlated to drug release studies in oral cavity. %26lt;br%26gt;Concentration of 22 mu g/ml and below was perceived bitterless by all the volunteers of taste panel. A second-order polynomial equation (y = 0.6206x (2) -aEuro parts per thousand 0.2011x -aEuro parts per thousand 0.7796; correlation coefficient R (2) = 0.991) was derived as a relationship between bitterness score and log ONS concentration. Drug release in in-house-assembled apparatus and oral cavity were not statistically different (alpha = 0.05) at both 60 and 120 s. %26lt;br%26gt;Bitterness threshold and bitterness scores are helpful in evaluation of bitterness in drug solutions and samples obtained from drug release studies.

• 出版日期2014-9
• 单位河北医科大学