新型肌酸制剂在健康成人中表现出与一水肌酸相似的血清肌酸浓度和药代动力学。
摘要
背景：一水肌酸（CrM）是研究最广泛的肌酸形式，已证明具有稳健的功效、生物利用度和安全性。随着肌酸日益普及，已开发出替代性肌酸制剂，旨在改善溶解度、优化吸收药代动力学（PK），并减少胃肠道（GI）不耐受。本研究旨在评估新型一水肌酸（OptiCreatineTM；CrO）与CrM相比，在健康成人中对血清肌酸药代动力学和胃肠道耐受性的急性影响。…
正文 待译
BACKGROUND: Creatine monohydrate (CrM) is the most widely studied creatine form, demonstrating robust efficacy, bioavailability, and safety. With creatine growing in popularity, alternative formulations of creatine have been developed to target solubility and to optimize absorption pharmacokinetics (PK), as well as to reduce gastrointestinal (GI) intolerability. The purpose of the current study was to evaluate the acute effects of a novel creatine monohydrate (OptiCreatineTM; CrO) compared to CrM on serum creatine PK and GI tolerability in healthy adults. METHODS: Healthy, recreationally active adults (age: 22 ± 3 years; males n = 8, females n = 9) consumed a single 5-gram dose of CrM or CrO across two separate visits following an overnight fast, in a randomized, double-blind, crossover design. Venous blood samples were collected at baseline and 30, 60, 90, 120, 180, 240, and 300 mins post-ingestion of their assigned treatment to assess serum creatine concentrations. PK parameters including peak concentration (Cmax), time to peak (Tmax), absorption rate constant (ka), elimination rate constant (kel; h-1), and area under the curve (AUC₀-T) were derived using nonlinear regression modeling. GI symptoms were assessed using validated questionnaires. RESULTS: There was no difference in serum creatine concentrations between CrM or CrO across all participants (p = 0.707), males (p = 0.318), or females (p = 0.996) at any time point. Serum creatine increased over time regardless of treatment (p < 0.0001). No differences were observed between CrM and CrO for Cmax (mean difference ± standard deviation (MD ± SD): 7.66 ± 50.37μM; p = 0.82), Tmax (MD ± SD: -0.04 ± 0.13 h; p = 0.54), ka (MD ± SD: -0.15 ± 0.45 h-1; p = 0.51), kel (MD ± SD: 0.01 ± 0.03 h-1; p = 0.61), or AUC₀-T (MD ± SD: 22.09 ± 160.57 μM·h; p = 0.74), with no sex × treatment interactions (p ≥ 0.05). Descriptive evaluation showed similar GI symptom profiles between conditions, with low frequency and minimal severity reported across both treatments. CONCLUSIONS: A single 5-gram dose of CrO produced similar serum creatine and PK characteristics to CrM in healthy adults. These findings support CrO as a viable delivery option, with no significant differences in acute pharmacokinetic profiles or GI tolerability compared to CrM.
English
BACKGROUND: Creatine monohydrate (CrM) is the most widely studied creatine form, demonstrating robust efficacy, bioavailability, and safety. With creatine growing in popularity, alternative formulations of creatine have been developed to target solubility and to optimize absorption pharmacokinetics (PK), as well as to reduce gastrointestinal (GI) intolerability. The purpose of the current study was to evaluate the acute effects of a novel creatine monohydrate (OptiCreatineTM; CrO) compared to CrM on serum creatine PK and GI tolerability in healthy adults.…