Biopharmaceutical Study of Inclusion Complexes. I. Pharmaceutical Advantages of Cyclodextrin Complexes of Bencyclane Fumarate

概要

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Complexes of bencyclane fumarate (Ben) with cyclodextrins (CDs) were newly prepared and their characteristics were studied from a pharmaceutical viewpoint. The results of differential scanning calorimetry (DSC), X-ray diffractometry and thin-layer chromatography (TLC) were consistent with the formation of inclusion complexes. Water solubility of Ben-CDs were 2- to 8-fold lager than that of Ben. The stability of Ben in acidic media (pH 1.2) was considerably improved by complex formation with β-CD or γ-CD. Apparent first-order rate constants [h^<-1>] of hydrolysis of Ben were 6.5×10^<-2>, 5.5×10^<-2>, 1.0×10^<-2> and 1.7×10^<-2> for Ben, Ben-α-CD, Ben-β-CD and Ben-γ-CD, respectively. The intrinsic bitter taste of Ben was significantly reduced by inclusion complexation with CDs. Thus, there are clear pharmaceutical advantages of Ben-CD compared with Ben. In addition, a novel animal test method, which is helpful for studying astringent bitter-tasting drugs, is proposed.
社団法人日本薬学会の論文
1983-07-25