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大幅降低治疗性单克隆抗体浓缩溶液粘度的大分子极性添加剂。

Bulky Polar Additives That Greatly Reduce the Viscosity of Concentrated Solutions of Therapeutic Monoclonal Antibodies.

作者信息

Larson Alyssa M, Weight Alisha K, Love Kevin, Bonificio Amanda, Wescott Charles R, Klibanov Alexander M

机构信息

Arsia Therapeutics, Cambridge, Massachusetts 02139.

Arsia Therapeutics, Cambridge, Massachusetts 02139.

出版信息

J Pharm Sci. 2017 May;106(5):1211-1217. doi: 10.1016/j.xphs.2017.01.018. Epub 2017 Jan 28.

Abstract

The viscosity of concentrated aqueous solutions of 3 clinical monoclonal antibodies (mAbs), Erbitux®, Herceptin®, and Rituxan®, has been reduced up to over 10-fold by adding certain bulky polar additives instead of saline at isotonic levels. Because these additives are also found not to compromise mAbs' stability against aggregation induced by stresses, a drug-delivery modality switch from intravenous infusions to more convenient and inexpensive parenteral options like subcutaneous injections may become possible.

摘要

通过添加某些体积较大的极性添加剂而非等渗水平的生理盐水,3种临床单克隆抗体(mAb)——爱必妥®、赫赛汀®和利妥昔单抗®——的浓缩水溶液粘度降低了10倍以上。由于还发现这些添加剂不会损害mAb抵抗应激诱导聚集的稳定性,药物递送方式可能会从静脉输注转变为更方便且便宜的非肠道给药方式,如皮下注射。

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