synAgile Corporation, Jackson, WY, 83001, USA.
Sci Rep. 2024 Nov 5;14(1):26826. doi: 10.1038/s41598-024-78145-4.
When short plasma half-life drugs act only briefly, they require frequent or continuous administration. We report the engineering of a non-invasive oral drug delivery system for long-term, continuous administration of these drugs. Their non-invasive, long-term, continuous administration at daily doses exceeding 100 mg has, for many years, been considered an insurmountable challenge. We show that over 1200 mg/day of 4:1 levodopa-carbidopa (LD-CD) can be non-invasively and continuously extruded when formulated as a semisolid paste, loaded with 63%w/w of the solid drugs. The drug delivery system comprises a reusable orthodontic retainer with a co-molded pocket into which the patient inserts after each meal a new 1 mL propellant-driven, prefilled, disposable, drug delivery extruder. The paste is delivered to the lingual side of the teeth where it is mixed with saliva and swallowed. As reported elsewhere, a 15-day, 16 patient open label clinical trial of the drug delivery system continuously extruding LD-CD paste significantly reduces the variability of the plasma LD concentration and alleviates symptoms of advanced Parkinson's disease (PD) as compared to LD-CD tablets.
当短半衰期的药物作用时间短暂时,它们需要频繁或连续给药。我们报告了一种非侵入性口服药物输送系统的工程设计,用于这些药物的长期、连续给药。多年来,这些药物的非侵入性、长期、连续每日剂量超过 100 毫克一直被认为是一个无法克服的挑战。我们表明,当以半固体糊剂的形式配制并负载 63%w/w 的固体药物时,每天可以非侵入性地连续挤出超过 1200 毫克的 4:1 左旋多巴-卡比多巴(LD-CD)。药物输送系统包括一个可重复使用的正畸保持器,带有一个共模制的口袋,患者每餐饭后将一个新的 1 毫升推进剂驱动、预填充、一次性药物输送挤出器插入其中。糊剂被输送到牙齿的舌侧,在那里与唾液混合并吞咽。正如在其他地方报道的那样,与 LD-CD 片剂相比,连续挤出 LD-CD 糊剂的药物输送系统的 15 天、16 名患者开放标签临床试验显著降低了血浆 LD 浓度的变异性,并缓解了晚期帕金森病(PD)的症状。