Method for preparing polymorphism of irinotecan hydrochloride

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C546S042000

Reexamination Certificate

active

07488825

ABSTRACT:
A method for preparing a novel crystalline polymorphic irinotecan hydrochloride which is excellent in the solubility in water and reduced in the content of impurities is provided. A method for preparing c-type crystals of irinotecan hydrochloride having diffraction peaks (2θ) at 9.15°, 10.00°, 11.80°, 12.20°, 13.00° and 13.40° in the powder X-ray diffractometry characterized by mixing irinotecan with one or more solvents selected from the group consisting of acetone, acetonitrile and tetrahydrofuran, adding hydrochloric acid, and collecting the formed crystals.

REFERENCES:
patent: 62-47193 (1987-10-01), None
patent: 3-4077 (1991-01-01), None
patent: 7-277981 (1995-10-01), None
patent: 10-017472 (1998-01-01), None
patent: 2005-525367 (2005-08-01), None
patent: 03/074527 (2003-09-01), None
Pages 12, 14, 18 and 19 of 60/360,684.
Seigo Sawada: Synthesis and Antitumor Activity of 20(S)-Camptothecin Derivatives: Carbamate-Linked, Water-Soluble Derivatives of 7-Ethyl-10-hydroxycamptothecin1), Chemical & Pharmaceutical Bulletin, vol. 39, No. 6, pp. 1446-1454, 1991.

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