目的 通过¹⁴C同位素标记技术研究[¹⁴C]玛舒拉沙韦混悬液在男性健康受试者中的放射性药动学行为、物质平衡和代谢转化途径。方法 采用单中心、开放、非随机、单剂量、空腹状态下的口服给药试验。6名健康男性受试者空腹服用40 mg（约100 μCi）[¹⁴C]玛舒拉沙韦混悬液，采集全血、血液、尿液、粪便，根据总放射性、玛舒拉沙韦及其代谢产物的血药浓度，通过非房室模型估算药动学参数；通过尿样和粪样中的浓度，计算药物累积排泄量，提供物质平衡数据。结果 血浆中未检测到玛舒拉沙韦，血浆中主要放射性物质为代谢产物GP1707D07，其暴露量占总放射性物质的95.4%。GP1707D07与总放射性物质的药动学特征相近。在0～336 h时段，尿和粪中放射性物质总回收率为90.1%，其中粪样中总放射性占84.1%。除原形药外，在人体内共鉴定了8个代谢产物。在人体内最主要代谢途径是经O-去烷基化生成代谢产物M2。结论 在健康受试者中玛舒拉沙韦原药在体内快速代谢，血浆中主要成分为其活性代谢产物GP1707D07，其代谢产物不倾向分布于血细胞，且在全血中的消除比血浆中的稍慢，玛舒拉沙韦及其代谢产物主要经粪便排泄。

Objective To study the radiopharmacokinetic behavior, mass balance, and metabolic transformation pathway of [¹⁴C] Suraxavir Marboxil Suspension in healthy male subjects by ¹⁴C isotope labeling technique. Methods A single-center, open, nonrandomized, single-dose, fasting oral administration trial was designed. Six healthy male subjects were po administered with 40 mg (approximately 100 µCi)[¹⁴C] Suraxavir Marboxil Suspension on an empty stomach. The whole blood, blood, urine, and stool were collected. The pharmacokinetic parameters were estimated by non-atrioventricular model according to total radioactivity and the blood concentration data of Suraxavir Marboxil and its metabolites. The cumulative excretion of drugs was calculated by the concentration data in urine and stool samples obtained to provide material balance data. Results Suraxavir marboxil was not detected in the plasma, and the main radioactive substance in the plasma was the metabolite GP1707D07, and its exposure accounted for 95.4% of the total radioactive substance. The pharmacokinetic characteristics of GP1707D07 were similar to those of total radioactive material. During the 0 — 336 h period, the total recovery rate of radioactive substances in urine and feces was 90.1%, with 84.1% of the total radioactivity in fecal samples. In addition to the original drug, a total of 8 metabolites were identified in the human body. The main metabolic pathway in the human body was the generation of metabolite M2 through O-dealkylation. Conclusion In healthy subjects, the suraxavir marboxil original drug is rapidly metabolized in the body, and its main component in plasma is its active metabolite GP1707D07. Its metabolite does not tend to be distributed in blood cells and its elimination in whole blood is slightly slower than those in plasma. Suraxavir marboxil and its metabolites are mainly excreted through feces.

R969.1