Research progress of taste masking and evaluation technology of medicine / 中国药科大学学报

@#Most drugs taste bitter and irritating, resulting in poor compliance of patients, and the bad odor affects the therapeutic effect. The successful research and development of a drug should not only conform to the five quality characteristics of effectiveness, stability, safety, uniformity and economy, but also the compliance of patients to drugs with bad odor. The development of taste masking techniques is critical for bitter drugs.This review describes the principles, advantages and drawbacks of traditional taste masking techniques, and introduces the mechanism and application of novel taste masking techniques, such as melt granulation, hot melt extrusion, 3D printing, drug complex preparation, and bitter taste inhibitors. The in vitro evaluation methods of drug taste masking effect, such as functional magnetic resonance imaging, in vitro dissolution, and electronic tongue technology, are described. And introduce in vivo evaluation methods, such as animal and human taste, in the field of taste masking effect. A new strategy of BP neural network prediction model for drug taste evaluation is proposed, with a view to providing theoretical reference for the future research on drug taste masking.

Flavored Self Microemulsifying Lipid Formulations for Masking the Organoleptic Taste of Pharmaceutical Actives.

The field of SMEDDS is designed to enhance bioavailability of poorly-water soluble compounds. Yet, these systems have the capacity to solubilize aqueous-based materials within its lipid matrix as L2 phase (W/O microemulsion). This characteristic is utilized in this investigation to incorporate aqueous flavors within oil vehicle as an approach to mask bitter taste of drugs. Miscibility profiles and self-micro-emulsifying regions for various lipid composites were screened by constructing ternary phase diagrams using different types of oil, cosurfactant and surfactant. Solubility of bitter taste model drug was measured in various optimized vehicles. Dynamic equilibrium phase studies were performed and phase boundaries were determined for the lipid-aqueous flavors-water systems. Self-micro-emulsifying system comprising Crodamol GTCC/ Glycerox 767HC /Croduret 40 ss at ratios of {0/80/20}, {6/54/40} or {10/40/50} have shown capacity to solubilize, aqueous-based materials including; strawberry flavor, sucrose and citric acid as L2 phase. Phase behavior study has revealed that clear dispersions can be obtained at all dilutions with water. Potential flavored self-microemulsifying lipid formulations representing type III lipid class system were developed. Aqueous flavors loaded into these vehicles can be used to mask bitter tastes in oral pharmaceuticals.