Stabilization of eptifibatide by cosolvents

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Abstract

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® (eptifibatide) Injection requires a cold/refrigerator storage condition. In an effort to improve the drug stability for room temperature storage and transportation, this study proposed a semi-aqueous formulation that contains 2 mg/ml eptifibatide, 10% ethanol, 40% propylene glycol and 50% 0.025 M citrate buffer. The stability study was conducted in the pH range 4.25-6.25 under accelerated temperatures: 48, 60, 72.5°C. The results indicate that the proposed semi-aqueous vehicles substantially increased the drug stability in comparison with aqueous vehicles. The predicted drug shelf-life T90 at 25°C shows that an almost twofold increase can be achieved by formulating eptifibatide 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 maximum stability of pH 5.25.

Original languageEnglish (US)
Pages (from-to)43-56
Number of pages14
JournalInternational Journal of Pharmaceutics
Volume218
Issue number1-2
DOIs
StatePublished - May 7 2001

Keywords

  • Cosolvents
  • Eptifibatide
  • Integrilin
  • Stability

ASJC Scopus subject areas

  • Pharmaceutical Science

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