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Biopharmaceutical study of inclusion complexes. I. Pharmaceutical advantages of cyclodextrin complexes of bencyclane fumarate.

1983; Pharmaceutical Society of Japan; Volume: 31; Issue: 7 Linguagem: Inglês

10.1248/cpb.31.2416

1347-5223

Keiji Fujioka, Yuji Kurosaki, Shigeji Sato, Tetsuo Noguchi, Takeshi Noguchi, Yoshiya Yamahira,

Chromatography in Natural Products

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.