Lactone stable formulation of camptothecin or 7-ethyl...

A - Human Necessities – 61 – K

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A61K 31/47 (2006.01) A61K 9/48 (2006.01) A61K 47/18 (2006.01) A61K 47/26 (2006.01) A61K 9/107 (2006.01)

Patent

CA 2188297

Camptothecin (CPT) and 7-ethyl camp- tothecin (ECPT), are poorly soluble in water. Because of their poor water-solubility, they have not been directly administered by par- enteral or oral routes in human patients for the purpose of inhibiting the growth of tumors. The invention provides a pharmaceutically ac- ceptable formulation in the form of an acidic solution or suspension comprising (1) CPT or ECPT, preponderantly in the desired lactone form (1a') (wherein R is hydrogen or ethyl) and (2) dimethylisosorbide or dimethylacetamide.

La camptothécine (CPT) et la 7-éthyle camptothécine (ECPT) sont faiblement solubles dans l'eau et, pour cette raison, on ne les a pas administrées directement par voie orale ou parentérale à l'homme dans le but d'inhiber la croissance de tumeurs. L'invention concerne une formulation acceptable sur le plan pharmacologique, sous la forme d'une solution ou suspension acide comprenant (1) CPT ou ECPT, de manière prépondérante dans la forme lactone souhaitée (1a') (dans laquelle R représente hydrogène ou éthyle) et (2) diméthylisosorbide ou diméthylacétamide.

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