Abstract
APSAC (anisoylated plasminogen streptokinase activator complex) is a prodrug of the fibrinolytic lys-plasminogen streptokinase complex. Is is prepared by acylation of the serine hydroxyl group in the active centre of plasminogen, and is formulated as a freeze-dried powder for reconstitution and intravenous administration. The acyl group is labile in solution, and to a lesser extent also in the lyophilised state. Here we report a method for stabilising the prodrug by formulation with a water-soluble acylating agent. On reconstitution, any free hydroxyl groups formed during storage are rapidly reacylated while essentially full acylation is maintained for the required period in solution.
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