Process for preparing crystal forms and solvates of dirithromyci

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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536 72, 536 74, C07H 100

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056356137

ABSTRACT:
The invention provides Form II dirithromycin, a novel polymorph of dirithromycin. Also disclosed are the acetone, 1-butanol, 1-propanol, and 2-propanol solvates of dirithromycin, which provide an efficient means for preparing and isolating Form II. Processes for preparing and isolating Form II dirithromycin from these solvates or from Form I dirithromycin are provided. A process for obtaining Form II dirithromycin from non-solvated dirithromycin is also provided. Another aspect of the invention is an improved tablet containing Form II dirithromycin as the active ingredient.

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Allen, P. V. et al., 67 Journal of Pharmaceutical Sciences, 1087-1092 (1978).
Chemical Abstracts 85:25320x, p. 251 (1976).
Pelizza, G. et al., 31 Farmaco Ed. Sc. 254-263 Article referred to by Chemical Abstracts 85:25320x.
Egutkin, H. L., et al., Khim.-Farm. Zh., 18(7), 858-61, 1984.
J. Firl, et al., Journal of Antibiotics, vol. XLIII, No. 10, pp. 1271-1277, Oct. 1990, Tokyo, Japan.
European Search Report.

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