Exenatide controlled-release microsphere composition

2014 
The invention aims to provide an exenatide controlled-release microsphere composition composed of exenatide or a salt thereof, a polymer blend and sucrose, wherein the weight content of the exenatide or the salt thereof is 10-20%, the weight content of the polymer blend is 76-89%, and the weight content of sucrose is 1-4%. The pharmaceutical composition exists in a microsphere form, has the property of long-term drug release, and can release exenatide in a time exceeding one month. The pharmaceutical composition has one characteristic that appropriate combination of two different PLGs is adopted in the pharmaceutical composition, the fluctuation of the exenatide concentration in plasma can be significantly reduced, and a release period is not delayed significantly. The pharmaceutical composition has another characteristic that the drug sudden release quantity is quite low under a high drug loading capacity situation. The exenatide microsphere composition has the drug loading quantity of not less than 10.0% and the sudden release quantity not exceeding 1.0%.
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