Eptifibatide powder injection

Abstract

The invention belongs to the field of medicinal preparations and relates to an eptifibatide powder injection, which mainly comprises eptifibatide, carbohydrates and an acidity regulator. The eptifibatide powder injection has the characteristics of high concentration and good stability, can be used for treating acute coronary syndrome including unstable angina pectoris and non-Q wave infarction andcan also be used in percutaneous coronary intervention including angioplasty and atherectomy.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to eptifibatide powder injection. Background technique [0002] Eptifibatide (Efibate) is a glycoprotein II b / IIIa receptor antagonist, which binds to the GPIIb / IIIa receptor on the platelet membrane and occupies the binding site on it, allowing the platelet GPIIb / IIIa receptor The body cannot bind to fibrinogen, thereby inhibiting platelet aggregation. Clinically indicated for the treatment of acute coronary syndromes, including unstable angina or non-Q-wave myocardial infarction (ie, persistent episodes of chest pain within 24 hours, ECG changes, and / or elevated cardiovascular system enzymes); also for percutaneous coronary use Interventional therapy, including angioplasty or atherectomy. In July 1998, it was first listed in the United States under the trade name Intrifiban by Schering-Plough Company, and in 1999 it was launched in Europe under the trade name Intrifiban. ...

AI Technical Summary

Problems solved by technology

The solubility of Efibuta in water is low. When the pH value reaches 7, it is easy to precipitate out of the solution. The general co-solvent has little effect on its solubility, and has certain viscosity and aggregation. Therefore, the maximum concentration of the infusion solution is generally 20mg / ml, so that the volume of the same dose of efibat injection for each patient will be very large, so that even if a large dose bottle of 100ml: 200mg is given, more than 2 bottles will be needed. Need to occupy a larger space, and the cost will increase accordingly

In addition, efibat has poor stability in aqueous solution, and when the pH value is lower than 4, the related substances increase significantly

At the same time, in the process of preparation, high temperature will reduce the activity of eptifibatide, and the high viscosity makes it difficult to freeze-dry the drug preparation.

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