Stable highly concentrated formulations of fluorescein...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01) A61K 9/06 (2006.01) A61K 31/365 (2006.01) A61K 41/00 (2006.01) A61K 47/40 (2006.01) A61N 5/06 (2006.01)

Patent

CA 2143115

The present invention relates to stable highly concentrated formulations of specific fluorescein derivatives, to the preparation of said formulations and the use thereof, especially for the photodynamic therapy of secondary cataract. The invention principally relates to an aqueous solution comprising a fluorescein diester, preferably a fluorescein di-lower alkyl ester, most preferably fluorescein diacetate, and a partially etherified .beta.-cyclodextrin the ether substituents of which are hydroxyethyl, hydroxypropyl or dihydroxypropyl groups, some of which ether substituents may bemethyl or ethyl groups, said .beta.-cyclodextrin ether having a water-solubility of more than 1.8 g in 100 ml of water, preferably hydroxy-.beta.-cyclodextrin.

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