Reduction of bitterness of antihistaminic drugs by complexation with β-cyclodextrins was written by Ono, Nao;Miyamoto, Yuji;Ishiguro, Takako;Motoyama, Keiichi;Hirayama, Fumitoshi;Iohara, Daisuke;Seo, Hakaru;Tsuruta, Satoshi;Arima, Hidetoshi;Uekama, Kaneto. And the article was included in Journal of Pharmaceutical Sciences in 2011.Synthetic Route of C21H29Cl3N2O2 This article mentions the following:
Reduction of bitterness of antihistaminic drugs by cyclodextrin (CyD) complexation was examined The stability constant (Kc) of the 1:1 CyD inclusion complexes with antihistaminic drugs increased in the order of 2-hydroxypropyl-β-CyD (HP-β-CyD) ≈ β-CyD > γ-CyD > α-CyD for diphenhydramine and epinastine, and HP-β-CyD ≈ β-CyD > α-CyD > γ-CyD for hydroxyzine, cetirizine, and dl-chlorpheniramine. The inclusion complexes inhibited the adsorption of antihistaminic drugs to lipid membrane using liposomes, as the magnitude of Kc increased. From human gustatory sensation tests, β-CyD and HP-β-CyD potently suppressed the bitterness of antihistaminic drugs in a dose-dependent manner. Further, an artificial taste sensor anal. revealed that β-CyD and HP-β-CyD inhibited the bitterness of antihistaminic drugs in solution The results suggest that CyDs suppress the bitterness of antihistaminic drugs in solutions through the formation of inclusion complexes. These results may provide useful information for masking or elimination of bitterness of drugs using CyDs. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:1935-1943, 2011. In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3Synthetic Route of C21H29Cl3N2O2).
2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol dihydrochloride (cas: 2192-20-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Synthetic Route of C21H29Cl3N2O2
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics