Principles of masking organoleptic properties of bitter tasting medicines

Abstract

Patient compliance of drug therapy is the key factor in achieving the pharmaceutical effect. Taste masking is particularly important in pediatrics and geriatrics because the unpleasant taste negatively affects drug uptake. Patient compliance can be improved through balanced organoleptic properties of medicines. It is particularly important to choose optimal correction method for medicines with high concentration of the active substance. Hopantenic acid has been chosen as a model drug due to its bitter taste. Taste masking technologies for creating a new dosage form with optimal organoleptic properties are proposed in the article. The objective is to achieve an experimentally justified choice of technological approach to masking bitter taste of a substance and to create a new dosage form on its basis. Materials and methods. Alternative technologies were considered to solve this problem: granulation, creation of complexes with ion-exchange resins, introduction of a gel composition and taste-masking using sweeteners. Organoleptic properties in dry compositions (pure substance of hopantenic acid, granulate and resinate based on it), and also after preparation of liquid dosage forms and incorporation them into gel, were evaluated by A. I. Tentsova method. Choice of sweetener and its concentration to achieve an optimally balanced taste took place at the final stage. Hopantenic acid was chosen as a model substance. Hopantenic acid is a nootropic drug stimulating cognitive functions, nervous system, enhancing intellectual functioning, decreasing nervous system activity, with anticonvulsant action. The main therapeutic indications are mental retardation, dementia, epilepsy. Results and discussion. The study has shown that optimal technology for masking unpleasant taste of hopantenic acid is its introduction into a gel composition, and a promising dosage form is an oral gel. Compri-Zucker G sweetener (Südzucker АG, Germany) in concentration of 5 % has been chosen to create pleasant taste due to its highest taste rating. Conclusion. It has been determined as a result of the study that oral gel with active drug concentration of 5 % and sweetener concentration of 5 % has optimal organoleptic properties. Thus, this combination of active and additional substances can be considered the most perspective for developing a new dosage form of a medicine.