Department of Pharmaceutical Sciences, College of Pharmacy, Texas A&M University, College Station, Texas.
Department of Pharmaceutical Sciences, College of Pharmacy, Texas A&M University, College Station, Texas
J Pharmacol Exp Ther. 2019 Sep;370(3):529-543. doi: 10.1124/jpet.118.255828. Epub 2019 Apr 22.
Advanced drug delivery technologies, in general, enable drug reformulation and administration routes, together contributing to life-cycle management and allowing the innovator to maintain the product monopoly. Over the years, there has been a steady shift from mere life-cycle management to drug repurposing-applying delivery technologies to tackle solubility and permeability issues in early stages or safety and efficacy issues in the late stages of drug discovery processes. While the drug and the disease in question primarily drive the choice of route of administration, the oral route, for its compliance and safety attributes, is the most preferred route, particularly when it comes to chronic conditions, including pain, which is not considered a disease but a symptom of a primary cause. Therefore, the attempt of this review is to take a stock of the advances in oral delivery technologies that are applicable for injectable to oral transformation, improve risk-benefit profiles of existing orals, and apply them in the early discovery program to minimize the drug attrition rates.
先进的药物输送技术通常能够实现药物的重新配方和给药途径的改变,共同促进药物的生命周期管理,并使创新者能够维持产品的垄断地位。多年来,人们一直在从单纯的生命周期管理向药物重新定位转变——将输送技术应用于早期的溶解度和渗透性问题,或药物发现过程后期的安全性和疗效问题。虽然药物和疾病是选择给药途径的主要驱动因素,但口服途径因其顺应性和安全性而成为最受欢迎的途径,尤其是在涉及慢性疾病(如疼痛)时,疼痛本身并不被认为是一种疾病,而是一种主要病因的症状。因此,本次综述旨在评估适用于将注射剂转化为口服制剂的口服给药技术的进展,改善现有口服制剂的风险效益比,并将其应用于早期发现计划中,以最大限度地降低药物淘汰率。