Stable solutions of rebeccamycin analog
AssigneeBristol-Myers Squibb Company
InventorsUbrani V. Venkataram, Miriam K. Franchini, Joseph B. Bogardus
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Abstract
Stable solutions of rebeccamycin analog consist essentially of (a) water, (b) 8-N-(diethylaminoethyl)rebeccamycin in an effective dosage amount, and (c) pharmaceutically acceptable acid such that the presence of a molar equivalence thereof would solubilize (b), said acid being present in excess of said molar equivalence to provide a stabilizing pH ranging from 3 to 4, preferably from 3.0 to 3.6. A preferred solution contains 10 mg/ml of the free base and tartaric acid in equimolar amount with the free base to provide a pH of 3.5. Preferably, the solution is prepared by forming a suspension of 8-N-(diethylaminoethyl)rebeccamycin in water and adding acid to provide a pH ranging from 3 to 4.
Claims13
A stable solution consisting essentially of
- (a) water,
- (b) 8-N-(diethylaminoethyl)rebeccamycin in an effective dosage amount at a concentration up to 50 mg/ml of water, and
- (c) a pharmaceutically acceptable acid, a molar equivalence of which will solubilize compound (b), said acid being present in said solution in an amount in excess of said molar equivalence to provide a stabilizing pH for said solution ranging from 3.0 to 3.6.
Method of preparing a stable aqueous solution of 8-N-(diethylaminoethyl)rebeccamycin, said method comprising the steps of:
- (a) forming a suspension of 8-N(diethylaminoethyl)rebeccamycin in water at a concentration of at least 1 mg/ml of water,
- (b) adding a pharmaceutically acceptable acid to said suspension, a molar equivalence of which will solubilize the 8-N(diethylaminoethyl)rebeccamycin present in the suspension formed in step (a), said acid being added in an amount in excess of said molar equivalence to provide a stabilizing pH for said solution ranging from 3.0 to 3.6.
Dependencies are inferred from the claim text.