Bioanalysis
·
2025
·
IF 1.8
Kaiwei Luo,Danrui Liu,Shengshuo Zhang,Xin Zhang,Qunan Cheng,Jie Lin,Yonghua Yu
Aims This study aimed to establish a robust LC-MS/MS method for quantifying trazodone in human plasma and investigate its pharmacokinetic profile in healthy Chinese subjects under fasting and fed conditions.Materials & methods A validated LC-MS/MS method using protein precipitation was applied to analyze trazodone in 68 healthy subjects (34 fasting/34 fed), with full method validation performed.Results This method exhibited high selectivity, precision, and accuracy. The results showed good linearity in the range of 5–3000 ng/mL and matrix effect results showed no matrix interference. The pharmacokinetic data revealed notable differences between the fasting and postprandial states.Conclusions The validated LC-MS/MS method proved reliable for trazodone quantification. The observed food effects on absorption suggest clinical dosing should consider administration conditions to ensure optimal therapeutic outcomes.
研究领域:
分析化学
·
药理学
·
临床医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Pharmaceutics
·
2026
·Vol. 18
·期 8
·1010
·
IF 6.9
Zeyu Wen,Xilu Sun,Sumeng Chen,Jinyan Meng,Runlin Yu,Shuyan Guo,Xingyuan Cao
Background: The Biopharmaceutics Classification System (BCS) classifies drug substances according to their aqueous solubility and intestinal permeability; however, its application to veterinary drugs should account for species-specific gastrointestinal physiology. Grapiprant is a selective prostaglandin E2receptor subtype 4 (EP4) antagonist approved as an oral tablet to control pain and inflammation associated with osteoarthritis in dogs, but its properties within the BCS framework remain unclear.Methods: This study evaluated the equilibrium solubility of grapiprant across pH conditions relevant to the canine gastrointestinal tract and calculated the dose number (D0) based on different gastric fluid volumes. A Caco-2 cell monolayer model was used to assess grapiprant intestinal permeability and the effects of time, concentration, pH, and efflux transporter inhibitors on its transepithelial transport.Results: Grapiprant showed relatively small changes in solubility across the tested pH range. D0varied with pH and gastric fluid volume and approached or fell below 1 at larger fluid volumes. In the Caco-2 model, grapiprant showed generally limited apparent absorptive permeability, with permeability varying with pH. Efflux ratios were greater than 1, and verapamil reduced the efflux ratio, suggesting possible P-glycoprotein (P-gp) involvement.Conclusions: These findings suggest that both solubility and apparent intestinal permeability may limit the oral absorption of grapiprant under certain canine-relevant conditions. Accordingly, this study provides a biopharmaceutical characterization of grapiprant within the BCS framework rather than a definitive canine BCS classification, highlighting the importance of considering canine gastrointestinal conditions when interpreting its solubility and permeability. The results may support future optimization of dosing conditions and oral formulations.
✓ 已验证
产品关联
DOI
高影响因子
MICROCHEMICAL JOURNAL
·
2025
·
IF 5.1
Moying Yang,Yan Yao,Haotian Shen,Fei Teng,Yunuo Liu,Yuyang Ma,Bin Di,Mengxiang Su
Depression has gradually become a serious public health problem. Traditionally, data on depression are mainly derived from questionnaires or antidepressant prescriptions, and these methods may suffer from update delays and survey bias, resulting in a low actual prevalence of depression. To monitor the prevalence of depression in near real-time, this study developed an analytical method of UPLC-MS/MS by wastewater-based epidemiology to detect 10 typical antidepressants and metabolites in four provinces of China. The method has high sensitivity in that the lower limit of quantification was 2 ng/L. And the method provides recoveries and matrix effects ranging from 85.12 % to 102.98 % and 84.95 % to 112.75 %, respectively. The results showed that among the four provinces, the highest average detected concentration of antidepressants was in Jiangsu (91.82 ± 150.46 ng/L), followed by Guangxi (76.06 ± 130.44 ng/L), Anhui (61.53 ± 94.09 ng/L), and Hainan (27.87 ± 28.33 ng/L). Most wastewater treatment facilities had antidepressants such as venlafaxine, fluvoxamine, and agomelatine. The average back-calculated consumption of venlafaxine and fluvoxamine was 815.88 ± 2015.96 mg/day/1000 inh and 497.02 ± 405.21 mg/day/1000 inh, respectively. Based on this study, the estimated prevalence in the population over 15 in Jiangsu, Anhui, and Hainan was finally determined to be 4.90 %, 5.36 %, and 2.93 %, indicating regional diversity. This study offered a workable way to track the prevalence of depression using wastewater-based epidemiology, which aided public health agencies in comprehending the state of depression prevalence.
研究领域:
环境科学
·
分析化学
·
流行病学
·
公共卫生
·
药物监测
✓ 已验证
产品关联
DOI
高影响因子
Biomaterials Advances
·
2023
·
IF 0
Fengying Dai,Kepeng Lv,Bo Zhang,Junqiang Zhao,Shaoteng Wang,Ke Lan,Yiping Zhao,Xiaolei Zhang,Bohong Kan
Tannic acid (TA) shell is of great interest for nanodrug design due to its versatile application such as antioxidant, antibacterial, anti-inflammatory. However, evidence is emerging that TA air oxidation in storage stage and unfavorable interactions of TA with electrolyte or protein in drug delivery could bring great challenge for the structure stability of nanodrug. In this study, a smart TA shell of nanomicelles was constructed through phenolic hydroxyl protection strategy, and the antioxidant capacity of nanomicelles maintain stable after 24 days storage. The phenolic hydroxyl protective tannic acid micelles (PHPTA micelles) show excellent performance for combination delivery of azoramide (Azo), dantrolene (Dan), Trazodone (Tra) in accelerated senescence (SAMP8) mice. This study may pave the way for the fabrication of nanodrugs with stable and smart TA shell for oxidative stress relevant diseases.
研究领域:
药学
·
生物医学工程
·
神经科学
✓ 已验证
产品关联
DOI
PubMed
危险品化学品经营许可证（带存储）