Selective inhibition of bitter taste of various drugs by lipoprotein.
Previously, we demonstrated that lipoprotein composed of phosphatidic acid (PA) and beta-lactoglobulin (LG) selectively and reversibly suppress the frog taste nerve response to bitter substances. In the present study, we examined the effects of various lipoproteins on the taste sensation to various stimuli in humans by a psychophysical method. Among various lipoproteins composed of different of lipids and proteins, the lipoproteins composed of PA and proteins were most effective in suppressing bitter taste. The lipoproteins composed of PA and LG, bovine serum albumin, ovalbumin, alpha-lactoalbumin or casein similarly suppressed effects on sensation of bitter taste. Using PA-LG, the effects on taste sensation to various stimuli were examined. The bitter taste of all twelve substances examined was inhibited, while saltiness of NaCl and sweetness of sucrose were not inhibited. The inhibition of bitter taste was completely reversible. Masking of the target sites for bitter substances on the taste receptor membranes with PA-LG seems to contribute to the inhibition of bitter taste. Direct binding of the bitter substances to PA-LG in the medium also contributes to the inhibition of bitter taste of certain substances. Among various drugs, basic and hydrophobic substances such as quinine, denatortium and propranolol have low taste thresholds and are said to be the most bitter. PA-LG most effectively suppressed the bitter taste of such substances. PA originates from soybeans and the proteins used except for bovine serum albumin originate from milk or eggs, and hence the lipoproteins can be safely used to mask the bitter taste of drugs.
D002110:Caffeine / Q000009:adverse effects; D002626:Chemistry, Pharmaceutical; D004347:Drug Interactions; D064420:Drug-Related Side Effects and Adverse Reactions; D005079:Excipients; D006801:Humans; D007782:Lactoglobulins / Q000494:pharmacology; D008074:Lipoproteins / Q000138:chemical synthesis / Q000494:pharmacology*; D010712:Phosphatidic Acids / Q000494:pharmacology; D010713:Phosphatidylcholines / Q000494:pharmacology; D011803:Quinine / Q000009:adverse effects; D012710:Serum Albumin, Bovine / Q000494:pharmacology; D012965:Sodium Chloride / Q000494:pharmacology; D013395:Sucrose / Q000494:pharmacology; D013649:Taste / Q000187:drug effects*; D013652:Taste Threshold; D014280:Triglycerides / Q000494:pharmacology
D005079:Excipients; D007782:Lactoglobulins; D008074:Lipoproteins; D010712:Phosphatidic Acids; D010713:Phosphatidylcholines; D014280:Triglycerides; D012710:Serum Albumin, Bovine; D002110:Caffeine; D012965:Sodium Chloride; D013395:Sucrose; D011803:Quinine