Stabilization of eptifibatide by cosolvents

Eptifibatide is a potent and highly specific inhibitor of platelet receptor glycoprotein IIb/IIIa and is indicated in the treatment of acute coronary syndrome. The commercial product Integrilin (R) (eptifibatide) Injection re quires a cold/refrigerator storage condition. In an effort to improve the d rug stability for room temperature storage and transportation, this study p roposed a semi-aqueous formulation that contains: 2 mg/ml eptifibatide, 10% , ethanol, 40% propylene glycol and 50% 0.025 M citrate buffer. The stabili ty study was conducted in the pH range 4.25-6.25 under accelerated temperat ures: 48, 60, 72.5 degreesC. The results indicate that the proposed semi-aq ueous vehicles substantially increased the drug stability in comparison wit h aqueous vehicles. The predicted drug shelf-lire T-90 at 25 degreesC shows that an almost twofold increase can be achieved by formulating eptifibatid e in the semi-aqueous vehicle, which is 60 months at its maximum stability of pH 5.75. as opposed to the 33 months in the aqueous vehicle at its maxim um stability of pH 5.25. (C) 2001 Elsevier Science B.V. All rights reserved .