Ekenlebie Edmond, Einfalt Tomaž, Karytinos Arianna Irò, Ingham Andrew
School of Pharmacy, Aston University, Birmingham, UK.
Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia.
Pharm Pat Anal. 2016 Sep;5(6):407-416. doi: 10.4155/ppa-2016-0024. Epub 2016 Nov 2.
Injectable products are often the formulation of choice for new therapeutics; however, formulation in liquids often enhances degradation through hydrolysis. Thus, freeze-drying (lyophilization) is regularly used in pharmaceutical manufacture to reduce water activity. Here we examine its contribution to 'state of the art' and look at its future potential uses. A comprehensive search of patent databases was conducted to characterize the international patent landscape and trends in the use of freeze-drying. A total of 914 disclosures related to freeze-drying, lyophilization or drying of solid systems in pressures and temperatures equivalent to those of freeze-drying were considered over the period of 1992-2014. Current applications of sublimation technology were contrasted across two periods those with patents due to expire (1992-1993) and those currently filed. The number of freeze-drying technology patents has stabilized after initial activity across the biotechnology sector in 2011 and 2012. Alongside an increasing trend for patent submissions, freeze-drying submissions have slowed since 2002 and is indicative of a level of maturity.
注射用产品通常是新型治疗药物的首选剂型；然而，液体制剂往往会因水解作用而加速降解。因此，冷冻干燥（冻干）在制药生产中经常被用于降低水分活性。在此，我们探讨其对“现有技术水平”的贡献，并展望其未来的潜在用途。我们对专利数据库进行了全面检索，以描述冷冻干燥技术的国际专利格局及应用趋势。在1992年至2014年期间，共筛选出914项与冷冻干燥、冻干或在与冷冻干燥相当的压力和温度下对固体系统进行干燥相关的专利披露。通过对比两个时间段（即将到期的专利，1992 - 1993年；当前提交的专利）升华技术的当前应用情况。在2011年和2012年生物技术领域出现初步活跃之后，冷冻干燥技术专利数量已趋于稳定。除了专利申请呈上升趋势外，自2002年以来，冷冻干燥技术的申请数量有所放缓，这表明该技术已达到一定的成熟度。
