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专利性Rel-Ease药物递送技术:实现肽、蛋白质和小分子持续递送的机遇。

Proprietary Rel-Ease drug delivery technology: opportunity for sustained delivery of peptides, proteins and small molecules.

作者信息

Ye Ming, Bhat Gajanan, Johnston Kevin A, Tan Heow, Garnick Marc

机构信息

Praecis Pharmaceuticals Inc., 830 Winter Street, Waltham, MA 02451, USA.

出版信息

Expert Opin Drug Deliv. 2006 Sep;3(5):663-75. doi: 10.1517/17425247.3.5.663.

Abstract

Proprietary Rel-Ease (Praecis Pharmaceuticals) drug delivery technology uses biocompatible polymers as carriers to incorporate a drug into a polymer matrix through opposite charge interaction or complexation. The resulting low solubility complexes can be used to prepare sustained release depot injections or potentially sustained release formulations for oral administration. As a regulatory approved and commercialised drug delivery technology, Rel-Ease is used in abarelix for injectable suspension, a monthly depot injection for the treatment of patients with advanced prostate cancer. The technology offers high drug loading and minimal-to-no initial burst effect in vivo. It uses aqueous processes and is compatible for complexation with many peptide and protein therapeutics; its mechanism can also be applied to many small-molecule therapeutics and offers conventional and alternative methods for sustained release delivery via an oral route.

摘要

专利性的Rel-Ease(Precis制药公司)药物递送技术使用生物相容性聚合物作为载体,通过电荷相互作用或络合作用将药物掺入聚合物基质中。所得的低溶解度络合物可用于制备缓释长效注射剂或潜在的口服缓释制剂。作为一种获得监管批准并已商业化的药物递送技术,Rel-Ease被用于注射用阿巴瑞克混悬液,这是一种用于治疗晚期前列腺癌患者的每月一次长效注射剂。该技术具有高载药量,且在体内具有最小至无初始突释效应。它采用水性工艺,与许多肽和蛋白质治疗药物具有络合相容性;其作用机制也可应用于许多小分子治疗药物,并提供了通过口服途径进行缓释递送的传统方法和替代方法。

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