Complex of anti-fungal agent and cyclodextrin and method

Details Complex of anti-fungal agent and cyclodextrin and method Complex of anti-fungal agent and cyclodextrin and method

1984-07-27

1989-11-28

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 58, 536 65, 536 46, 536112, A61K 3170, C07H 1708

Patent

active

048837857

ABSTRACT:
An anti-fungal complex formed of a polyene anti-fungal agent, such as amphotericin B, and cyclodextrin, preferably .gamma.-cyclodextrin, is provided. The complex which includes amphoterin B has improved water solutility and stability over prior art amphotericin B anti-fungal agents. A method for forming the complex is also provided wherein anti-fungal agent, such as amphoterin B, is dissolved in an aqueous solution of cyclodextrin of pH ranging from about 9 to about 12 and the resulting solution is maintained at a pH ranging from about 6 to about 8 to form the subject complex. The solution can be lyophilized as desired to achieve higher solubility.

REFERENCES:
patent: 4383992 (1983-05-01), Lipari
patent: 4423040 (1983-12-01), Rajadhyaksha
patent: 4438106 (1984-03-01), Wagu et al.
patent: 4482709 (1984-11-01), Iwao et al.
patent: 4497803 (1985-02-01), Harada et al.
Saenger, W., "Cyclodextrin Inclusion Compounds in Research and Industry," Angew. Chem. Int. Ed. Engl., 19, 344-362, (1980).
Uekama et al., "Enhanced Bioavailability of Acetohexamide by .alpha.-Cyclodextrin Complexation," Yakugaku Zasshi, vol. 100, 1980, pp. 903-909.
Cserhali et al., "Effect of Water-Soluble .beta.-Cyclodextrin Polymer on the Lipophilicity of Polymyxin Examined by Reversed Phase Thin-Layer Chromatography", Journal of Chromatography, 259, (1983), 107-110, Elsevier.

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