健康受试者中1.8%利多卡因局部给药系统与5%利多卡因贴剂的随机、开放标签生物等效性研究。
A Randomized, Open-Label, Bioequivalence Study of Lidocaine Topical System 1.8% and Lidocaine Patch 5% in Healthy Subjects.
作者信息
Gudin Jeffrey, Argoff Charles, Fudin Jeffrey, Greuber Emileigh, Vought Kip, Patel Kalpana, Nalamachu Sri
机构信息
Department of Anesthesiology, Englewood Hospital and Medical Center, Englewood, NJ, USA.
Department of Neurology, Albany Medical Center, Albany, NY, USA.
出版信息
J Pain Res. 2020 Jun 22;13:1485-1496. doi: 10.2147/JPR.S237934. eCollection 2020.
PURPOSE
This study was designed to characterize drug delivery with lidocaine topical system 1.8% vs lidocaine patch 5% through 2 PK studies.
PATIENTS AND METHODS
Two Phase 1, single-center, open-label, randomized PK studies were performed in healthy adults. In Study 1, 56 subjects received a single intravenous bolus of 0.7 mg/kg of lidocaine as a lead-in to allow for the accurate determination of apparent dose of both products. After a 7-day washout period, subjects were randomized to receive either lidocaine topical system 1.8% or lidocaine patch 5% for 12 hours followed by another 7-day washout period, after which subjects crossed over to receive the other treatment for 12 hours. In Study 2, 54 subjects were randomized to receive either lidocaine topical system 1.8% or lidocaine patch 5% for 12 hours. After a 7-day washout period, subjects crossed over to receive the other treatment. Adhesion and skin irritation assessments were performed after application of the products in Study 2. In both studies, serial blood samples were collected to measure the plasma concentration of lidocaine after product application. Safety assessments and adverse events were monitored in both studies.
RESULTS
The comparative PK analysis demonstrated that the two products, despite their difference in drug load and strength, are bioequivalent. Both products were well tolerated. In Study 2, dermal response scores (skin tolerability after removal) were similar between lidocaine topical system 1.8% and lidocaine patch 5%, with a mean irritation score per patch <1 (barely perceptible erythema), which is not considered to be clinically significant.
CONCLUSION
Bioequivalence was demonstrated between lidocaine topical system 1.8% and lidocaine patch 5%. A comparison of the single-time adhesion scores at 12 hours in Study 2 favored lidocaine topical system 1.8% over lidocaine patch 5%. Both products were well tolerated as a single application in healthy adult human subjects.
CLINICALTRIALSGOV
NCT04144192, NCT04149938.
目的
本研究旨在通过两项药代动力学（PK）研究，对1.8%利多卡因 topical 系统与5%利多卡因贴剂的药物递送特征进行表征。
患者与方法
在健康成年人中进行了两项1期、单中心、开放标签、随机PK研究。在研究1中，56名受试者接受了0.7mg/kg利多卡因的单次静脉推注作为导入，以便准确测定两种产品的表观剂量。经过7天的洗脱期后，受试者被随机分为两组，分别接受1.8%利多卡因 topical 系统或5%利多卡因贴剂12小时，随后再经过7天的洗脱期，之后受试者交叉接受另一种治疗12小时。在研究2中，54名受试者被随机分为两组，分别接受1.8%利多卡因 topical 系统或5%利多卡因贴剂12小时。经过7天的洗脱期后，受试者交叉接受另一种治疗。在研究2中，在应用产品后进行了粘附性和皮肤刺激性评估。在两项研究中，在产品应用后采集系列血样以测量利多卡因的血浆浓度。在两项研究中均监测了安全性评估和不良事件。
结果
比较PK分析表明，尽管两种产品在药物载量和强度上存在差异，但它们具有生物等效性。两种产品耐受性均良好。在研究2中，1.8%利多卡因 topical 系统和5%利多卡因贴剂的皮肤反应评分（去除后皮肤耐受性）相似，每贴的平均刺激评分为<1（仅可察觉的红斑），这在临床上不被认为具有显著意义。
结论
1.8%利多卡因 topical 系统和5%利多卡因贴剂之间具有生物等效性。研究2中12小时时单次粘附评分的比较显示，1.8%利多卡因 topical 系统优于5%利多卡因贴剂。两种产品在健康成年受试者中单次应用时耐受性均良好。
临床试验注册
NCT04144192，NCT04149938。
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