Borkar Nrupa, Mu Huiling, Holm René
Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, Copenhagen, 2100, Denmark.
Drug Product Development, Janssen Research and Development, Johnson & Johnson, Turnhoutseweg 30, Beerse, 2340, Belgium.
Asian J Pharm Sci. 2018 Nov;13(6):507-517. doi: 10.1016/j.ajps.2017.11.004. Epub 2017 Dec 6.
Parkinson's disease (PD) is a chronic debilitating disease affecting approximately 1% of the population over the age of 60. The severity of PD is correlated to the degree of dopaminergic neuronal loss. Apomorphine has a similar chemical structure as the neurotransmitter dopamine and has been used for the treatment of advanced PD patients. In PD patients, apomorphine is normally administered subcutaneously with frequent injections because of the compound's extensive hepatic first-pass metabolism. There is, hence, a large unmet need for alternative administrative routes for apomorphine to improve patient compliance. The present review focuses on the research and development of alternative delivery of apomorphine, aiming to highlight the potential of non-invasive apomorphine therapy in PD, such as sublingual delivery and transdermal delivery.
帕金森病(PD)是一种慢性致残性疾病,影响着约1%的60岁以上人群。PD的严重程度与多巴胺能神经元损失的程度相关。阿扑吗啡具有与神经递质多巴胺相似的化学结构,已被用于治疗晚期PD患者。在PD患者中,由于该化合物广泛的肝脏首过代谢,阿扑吗啡通常需要频繁皮下注射给药。因此,对于阿扑吗啡的替代给药途径以提高患者依从性存在着巨大的未满足需求。本综述聚焦于阿扑吗啡替代给药方式的研究与开发,旨在突出非侵入性阿扑吗啡疗法在PD中的潜力,如舌下给药和透皮给药。