The pharmacokinetics and comparative bioavailabilty of oral and subcutaneous semaglutide in healthy volunteers.

Q3 Pharmacology, Toxicology and Pharmaceutics
Mohammed Bouhajib, Zia Tayab, Chantal Di Marco, Dennis Dong-Kyun Suh
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引用次数: 0

Abstract

Objectives: In this study, the comparative bioavailability of semaglutide following the administration of oral (PO) and subcutaneous (SC) doses in healthy subjects was evaluated. The pharmacokinetics of semaglutide of these formulations at lower doses (SC dose of 0.25 mg; PO dose of 3 mg) was examined by utilizing a sensitive bioanalytical method.

Methods: Twenty-two subjects were administered either 0.25 mg SC or 3 mg PO and blood samples were taken up to 504 h. The samples were assayed for semaglutide with an analytical range of 0.05-50 ng/mL. The pharmacokinetic parameters were estimated using a non-compartmental approach and were used to evaluate the comparative bioavailability of semaglutide.

Results: The pharmacokinetics of semaglutide was characterized following the administration of low subcutaneous and oral doses. The comparative bioavailability (PO relative to SC) was 0.66 % at the doses administered. Overall, the study drug was well tolerated, and no serious adverse events were reported.

Conclusions: The bioavailability of semaglutide following oral and subcutaneous administrations has been determined using a validated bioanalytical method. This method will enable more investigations into the pharmacokinetics of all formulations of semaglutide at lower doses, which will enable a better understanding of its' disposition in healthy subjects and in patients.

健康志愿者口服和皮下注射西马鲁肽的药代动力学和比较生物利用度。
目的:在本研究中,对健康受试者口服(PO)和皮下(SC)给药后的西马鲁肽的比较生物利用度进行了评估。低剂量(SC剂量为0.25 mg;采用灵敏的生物分析方法检测PO剂量(3 mg)。方法:22名受试者分别给予0.25 mg SC或3 mg PO,采集血样至504 h。检测样品的semaglutide,分析范围为0.05-50 ng/mL。使用非室室方法估计药代动力学参数,并用于评估semaglutide的比较生物利用度。结果:低剂量皮下和口服给药对西马鲁肽的药代动力学有明显影响。在给药剂量下,比较生物利用度(PO相对于SC)为0.66 %。总的来说,研究药物耐受性良好,没有严重不良事件的报道。结论:用一种有效的生物分析方法测定了口服和皮下给药后的西马鲁肽的生物利用度。该方法将使我们能够在低剂量下对所有西马鲁肽制剂的药代动力学进行更多的研究,从而更好地了解其在健康受试者和患者中的倾向。
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
Journal of Basic and Clinical Physiology and Pharmacology
Journal of Basic and Clinical Physiology and Pharmacology Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
3.90
自引率
0.00%
发文量
53
期刊介绍: The Journal of Basic and Clinical Physiology and Pharmacology (JBCPP) is a peer-reviewed bi-monthly published journal in experimental medicine. JBCPP publishes novel research in the physiological and pharmacological sciences, including brain research; cardiovascular-pulmonary interactions; exercise; thermal control; haematology; immune response; inflammation; metabolism; oxidative stress; and phytotherapy. As the borders between physiology, pharmacology and biochemistry become increasingly blurred, we also welcome papers using cutting-edge techniques in cellular and/or molecular biology to link descriptive or behavioral studies with cellular and molecular mechanisms underlying the integrative processes. Topics: Behavior and Neuroprotection, Reproduction, Genotoxicity and Cytotoxicity, Vascular Conditions, Cardiovascular Function, Cardiovascular-Pulmonary Interactions, Oxidative Stress, Metabolism, Immune Response, Hematological Profile, Inflammation, Infection, Phytotherapy.
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