COMPARATIVE-STUDY ON INCLUSION COMPLEXATION OF MALTOSYL-BETA-CYCLODEXTRIN, HEPTAKIS(2,6-DI-O-METHYL)-BETA-CYCLODEXTRIN AND BETA-CYCLODEXTRIN WITH FUCOSTEROL IN AQUEOUS AND SOLID-STATE


ACARTURK F., IMAI T., SAITO H., ISHIKAWA M., OTAGIRI M.

JOURNAL OF PHARMACY AND PHARMACOLOGY, cilt.45, sa.12, ss.1028-1032, 1993 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 45 Konu: 12
  • Basım Tarihi: 1993
  • Doi Numarası: 10.1111/j.2042-7158.1993.tb07174.x
  • Dergi Adı: JOURNAL OF PHARMACY AND PHARMACOLOGY
  • Sayfa Sayıları: ss.1028-1032

Özet

The complexation of fucosterol with three kinds of beta-cycrodextrin (beta-CyD) was investigated in aqueous solution and in the solid state. The solubility of fucosterol increased significantly on its complexation with maltosyl-beta-CyD and heptakis(2,6-di-O-methyl)-beta-CyD (DM-beta-CyD), while no appreciable increase was observed when complexed with beta-CyD. The stability constant of complexation with beta-CyD estimated from solubility determinations was greater for a 1:2 complex than for a 1:1 complex. On the other hand, 1:1 complexation of fucosterol with maltosyl-beta-CyD or DM-beta-CyD was greater than 1:2 complexation. The solid complexes were obtained in molar ratios of 1:2 and 1:3 for beta-CyD and maltosyl-beta-CyD complexes, respectively. The inclusion behaviour of fucosterol with maltosyl-beta-CyD was compared with beta-CyD in the solid state using DSC, powder X-ray diffractometry and CP/MAS C-13 NMR. Maltosyl-beta-CyD showed different inclusion behaviour compared with beta-CyD, and produced an amorphous structure of fucosterol on complex formation. The dissolution rate of fucosterol-maltosyl-beta-CyD complex was significantly faster than other complexes due to its high aqueous solubility and amorphous structure.