Comparative bioavailability of sublingual vs. oral levothyroxine in patients with post-thyroidectomy hypothyroidism: A single-dose pilot study.

IF 3 3区医学 Q2 PHARMACOLOGY & PHARMACY

British journal of clinical pharmacology Pub Date : 2026-10-01 Epub Date: 2026-06-22 DOI:10.1002/bcp.70661

Osama Shoaip, Mahmoud Bassiony, Rana Elbayar, Mohanned Mohsen, Hagar Elhammady, Rawda Elsaadany, Nehal M Ramadan

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引用次数: 0

Abstract

Aim: To evaluate the relative bioavailability of sublingual vs. oral levothyroxine (L-T4) in post-thyroidectomy patients, aiming to overcome gastrointestinal absorption variability.

Methods: This open-label, randomized, parallel-group pilot study enrolled 15 de novo hypothyroid patients following total thyroidectomy (oral: n = 7, sublingual: n = 8). Participants received a single 700-μg L-T4 dose under fasting conditions. Pharmacokinetic parameters, including baseline-corrected AUC, Cmax and Tmax, were determined via noncompartmental analysis.

Results: Sublingual administration resulted in a Geometric Mean Ratio (GMR) of 1.283 (90% CI: 0.849-1.938) for total systemic exposure (AUC_0-∞) and 1.123 (90% CI: 0.815-1.547) for early exposure (AUC_0-48) compared to the oral route. Due to the small sample size and inter-subject variability, these differences did not reach statistical significance. Elimination kinetics (T_1/2, MRT) were route-independent, while sublingual delivery showed lower apparent clearance (CL/F), supporting improved bioavailability.

Conclusion: Sublingual L-T4 achieved numerically higher systemic exposure with comparable elimination kinetics to the oral route. These findings suggest sublingual delivery is a promising, practical alternative that mitigates fasting constraints. Large-scale crossover studies are needed to definitively establish bioequivalence and long-term efficacy.

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舌下与口服左甲状腺素在甲状腺切除术后甲状腺功能减退患者中的生物利用度比较：单剂量先导研究

目的：评价舌下和口服左旋甲状腺素（L-T4）在甲状腺切除术后患者中的相对生物利用度，以克服胃肠道吸收变异性。方法：这项开放标签、随机、平行组的试点研究纳入了15例甲状腺全切除术后的新发甲状腺功能减退患者（口服：n = 7，舌下：n = 8）。参与者在禁食条件下接受单次700 μg L-T4剂量。药代动力学参数，包括基线校正的AUC、Cmax和Tmax，通过非区隔分析确定。结果：与口服途径相比，舌下给药导致全系统暴露（AUC0-∞）的几何平均比（GMR）为1.283 (90% CI: 0.849-1.938)，早期暴露（AUC0-48）的几何平均比（GMR）为1.123 （90% CI: 0.815-1.547）。由于样本量小，且受试者间存在差异，这些差异未达到统计学意义。消除动力学（T1/2， MRT）与途径无关，而舌下给药显示较低的表观清除率（CL/F），支持提高生物利用度。结论：舌下L-T4达到数值上更高的全身暴露，消除动力学与口服途径相当。这些发现表明舌下分娩是一种有希望的、实用的替代方法，可以减轻禁食的限制。需要大规模的交叉研究来确定生物等效性和长期疗效。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

British journal of clinical pharmacology 医学-药学

CiteScore

6.30

自引率

8.80%

发文量

419

审稿时长

1 months

期刊介绍： Published on behalf of the British Pharmacological Society, the British Journal of Clinical Pharmacology features papers and reports on all aspects of drug action in humans: review articles, mini review articles, original papers, commentaries, editorials and letters. The Journal enjoys a wide readership, bridging the gap between the medical profession, clinical research and the pharmaceutical industry. It also publishes research on new methods, new drugs and new approaches to treatment. The Journal is recognised as one of the leading publications in its field. It is online only, publishes open access research through its OnlineOpen programme and is published monthly.