摘要

Leuprolide acetate is a highly active analogue of luteinizing hormone releasing hormone. It can be used clinically to treat hormone receptor-positive breast cancer and other sex hormone-dependent diseases. Leuprolide acetate is not easily absorbed after oral administration and has a short half-life. Currently, leuprolide acetate sustained-release microspheres are prepared to improve bioavail-ability and reduce administration times. However, sustained-release microspheres need to have multiple characteristics to be suitable for clinical applications, including appropriate microparticle size, high drug loading, high encapsulation efficiency, low initial burst effect and long drug release cycle. These characteristics need to be balanced. In this article, the main characteristics of the domestically marketed leuprolide acetate sustained-release microsphere preparations and clinical application are evaluated and reviewed, so as to provide reference for the further development and rational application of leuprolide acetate sustained-release microspheres.

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