Department of Molecular and Clinical Pharmacology, Materials Innovation Factory, University of Liverpool, Liverpool L7 3NY, UK.
Tandem Nano Ltd., Liverpool L22 3GL, UK.
Molecules. 2019 Jul 24;24(15):2685. doi: 10.3390/molecules24152685.
In recent years, advances in pharmaceutical processing technologies have resulted in development of medicines that provide therapeutic pharmacokinetic exposure for a period ranging from weeks to months following a single parenteral administration. Benefits for adherence, dose and patient satisfaction have been witnessed across a range of indications from contraception to schizophrenia, with a range of long-acting medicines also in development for infectious diseases such as HIV. Existing drugs that have successfully been formulated as long-acting injectable formulations have long pharmacokinetic half-lives, low target plasma exposures, and low aqueous solubility. Of the statins that are clinically used currently, atorvastatin, rosuvastatin, and pitavastatin may have compatibility with this approach. The case for development of long-acting injectable statins is set out within this manuscript for this important class of life-saving drugs. An overview of some of the potential development and implementation challenges is also presented.
近年来,药物制剂技术的进步使得一些药物得以面世,这些药物在单次注射给药后能够提供长达数周到数月的治疗性药代动力学暴露。从避孕到精神分裂症等一系列适应症中,都观察到了在依从性、剂量和患者满意度方面的获益,同时也有许多长效药物正在开发中,用于治疗艾滋病等传染病。已经成功制成长效注射制剂的现有药物具有较长的药代动力学半衰期、较低的靶血浆暴露和较低的水溶解度。目前在临床上使用的他汀类药物中,阿托伐他汀、瑞舒伐他汀和匹伐他汀可能与这种方法兼容。本文阐述了长效注射用他汀类药物开发的理由,这类药物是重要的救命药物。本文还介绍了一些潜在的开发和实施挑战。