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 y-CD. Apparent first-order rate constants [h-1] of hydrolysis of Ben were 6.5xl0-2 5.5xl0-2 l.OxlO-2 and 1.7x l0-2 for Ben, Ben-a-CD, Ben-β-CD and Ben-y-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.
|Number of pages||8|
|Journal||Chemical and Pharmaceutical Bulletin|
|Publication status||Published - Aug 1983|
- bencyclane fumarate
- inclusion complex
ASJC Scopus subject areas
- Drug Discovery