A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/47 (2006.01) A61K 9/48 (2006.01) A61K 31/4745 (2006.01) A61K 47/12 (2006.01) A61K 47/16 (2006.01) A61K 47/18 (2006.01) A61K 47/26 (2006.01) A61K 47/28 (2006.01)
Patent
CA 2176604
10-hydroxy 7-ethyl camptothecin (HECPT), an active metabolite of the camptothecin analog CPT-11, is poorly soluble in water. Because of its poor solubility, HECPT has not been directly administered by parenteral or oral routes in human patients for the purpose of inhibiting the growth of tumors. The invention provides a pharmaceutically acceptable formulation in the form of an acidic solution or suspension comprising (1) HECPT, preponderantly in the desired lactone form (1a) and (2) dimethylisosorbide or dimethylacetamide.
Cette 10-hydroxy 7-éthyle camptothécine (HECPT) qui est un métabolite actif de l'analogue CPT-11 de la camptothécine, est faiblement soluble dans l'eau. Etant donné cette faible solubilité, on ne peut l'administrer directement par voie parentérale ou orale chez l'homme, dans le but d'inhiber la croissance des tumeurs. Cette invention procure une formulation pharmaceutiquement acceptable sous la forme d'une solution ou d'une suspension acide comprenant (1) la HCEPT, principalement sous la forme lactone recherchée, et (2) du diméthylisosorbide ou du diméthylacétamide.
Haridas Kochat
Hausheer Frederick Herman
Bionumerik Pharmaceuticals Inc.
Mcfadden Fincham
LandOfFree
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