数据日期 2026-10-29 · 生成时间 2026-10-29 06:03
研究问题
Type 2 Diabetes (T2D) is a complex metabolic disorder characterized by peripheral insulin resistance and progressive pancreatic β-cell dysfunction, culminating in sustained hyperglycemia [1,2].
方法
Samples were collected at predetermined time points, filtered through 0.45 μm Nylon Titan® membrane filters, and analyzed without replacement of the dissolution medium.；The amounts of dissolved sitagliptin and metformin was quantified by high-performance liquid chromatography coupled with UV detection (HPLC–UV) using a Phenomenex® Luna SCX column (50 × 4.6 mm, 5 μm).；To characterize the pharmacokinetic behavior of the Sitagliptin/Metformin extended-release tablets (50/1000 mg and 100/1000 mg), we conducted four independent, single-center, single-dose, open-label, randomized, two-period, two-sequence (2 × 2) crossover trials under both fasting and fed conditions.；A total of 46 healthy volunteers were randomized in each study.
核心结论
To formally assess bioequivalence, 90% confidence intervals (CIs) were calculated for the geometric mean ratios (Test/Reference) of the log-transformed parameters (Cmax, AUC0–t, and AUC0-∞).；For sitagliptin, the 90% CIs across the fasting and fed studies ranged from 89.35% to 106.72% for Cmax, from 94.27% to 102.58% for AUC0–t, and from 94.13% to 102.49% for AUC0-∞.；Similarly, for metformin, the corresponding 90% CIs ranged from 94.09% to 116.05% for Cmax, from 94.92% to 112.80% for AUC0–t, and from 94.63% to 112.70% for AUC0-∞. ‖ 结论：In conclusion, the generic sitagliptin/metformin extended-release (ER) fixed-dose combinations (50/1000 mg and 100/1000 mg) successfully demonstrated bioequivalence to the reference innovator products under both fasting and fed conditions in healthy Mexican volunteers.
局限
While the present study robustly establishes pharmacokinetic bioequivalence, several avenues for future research remain available to further characterize these formulations’ clinical profile in real-world settings.；Within this context, future studies should evaluate these FDCs in patients with T2D, particularly those with varying degrees of renal function, to confirm broader clinical applicability.
对本项目的价值
★★★☆☆ 干预证据决定参照标准效应量——任何抗衰干预的收益至少应对标该基线。最大样本量约 46。
全文来源
PMC JATS 全文（正文 54,669 字符，已过标题/DOI 逐字归属校验）
原文题录
- 英文标题：Bioequivalence Assessment of Sitagliptin/Metformin Extended-Release Fixed-Dose Combinations in Healthy Mexican Subjects Under Fasting and Fed Conditions.
- 期刊与标识：Pharmaceuticals (Basel) · PMID 42943229 · DOI 10.3390/ph19101532**
A 级证据分级：A 级（同行评议人体研究）
本文属人体研究证据，但需注意：观察性或小样本干预的结论不等于已证实临床获益；效应量与长期安全性仍需更大规模、更长随访的试验验证。
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