1.Plasma ibuprofen enantiomers and their pharmacokinetics in Beagle dogs determined by HPLC.
Hongyan WANG ; Aiying KONG ; Bo YANG ; Liangping YAN ; Xin DI
Acta Pharmaceutica Sinica 2015;50(12):1607-12
A chiral high-performance liquid chromatography method was developed for the simultaneous determination of ibuprofen enantiomers in dog plasma. It was used to study the pharmacokinetics in the Beagle dog after intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen. Ketoprofen was chosen as the internal standard. After a simple precipitation using methanol as the precipitating solvent, both analytes and IS were separated on a Kromasil 100-5CHI-TBB chiral column (250 mm x4.6 mm, 5 μm) with isocratic elution using acetonitrile - 20 mmol x L(-1) phosphate buffer (pH 3.0, containing 5% methanol) (6 : 4) as the mobile phase. The detection wavelength was 220 nm. Liner calibration curves for both of the ibuprofen enantiomers were over the concentration range from 0.5 to 50 μg x mL(-1) with a lower limit of quantification of 0.5 μg x mL(-1), the accuracies were all in standard ranges. The intra- and inter- assay precisions were all below 7%. The recovery rate was 93.1% to 100.4%. The experiments proved that the method was simple, rapid and sensitive. It can be used in the quantitative determination of ibuprofen enantiomers in dog plasma. The method was used to determine the concentration of ibuprofen enantiomers in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen (9 mg x kg(-1)) and the pharmacokinetics parameters were calculated based on the concentration-time curves. The C(max) of S-ibuprofen in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen were 30.8 ± 4.7, 46.1 ± 5.9 and 20.0 ± 2.6 μg x mL(-1), respectively. In terms of the exposure of active ingredient, it revealed a significant difference between the administration of S-ibuprofen and the other two groups. The systematical R- to S- chiral inversion was discussed. Comparing the pharmacokinetic parameters at different doses, chiral inversion were 70.1% ± 36.6% and 76.4% ± 36.2%, respectively, after intravenous administration of racemic- and R-ibuprofen. This study provides a theoretical basis for the safety of ibuprofen formula of injection drug.
2.Balloon embolization therapy for traumatic carotid cavernous fistula
Hong ZHANG ; Min GUAN ; Chengzhi LI ; Yan ZHANG ; Liangping LUO
Chinese Journal of Trauma 2013;(5):461-464
Objective To analyze effect of balloon embolization therapy for traumatic carotid cavernous fistula (TCCF),so as to provide references for treatment of this disease.Methods A total of 21 patients with TCCF managed with balloon embolization from April 2006 to March 2012 were collected in the study.There were 17 males aged (32.3 ±5.4) years and 4 females aged (40.6 ±5.8)years.Perioperative clinical presentations and imageologic changes were observed as well as operative outcome was evaluated.Results After 3 months of follow-up,20 patients experienced successful detachable balloon embolization,but the other one patient had to have stent angioplasty due to the failure of the procedure.All patients had some improvements on clinical presentations after operation (P < 0.05).Imageologic examination revealed that all patients had complete occlusion of TCCF following operation.In follow-up,one patient had a relapse,with total curative ratio of 95%.Conclusions Detachable balloon embolization is effective in treatment of TCCF.Presently,the technique is an optimal method for such kind of disease and is worthy of wide clinical use.
3.Medical risk management for resident doctors in their standardized training
Liangping YAN ; Jiang ZOU ; Minhui CHEN ; Xiangtao GAO
Chinese Journal of Hospital Administration 2009;25(11):772-774
An analysis of the medical risks exposure for resident doctors in their standardized training,and insights into the risk management measures proposed for this stage.These measures include:1) Pre-control of risks;2) Full-length supervisor of such training stage;3) Systematic education for medical risk exposure;4) Timely guidance on risk identification and response;5) Development of the evidence awareness.
4.Pharmacokinetics of sugammadex in reversal of postoperative residual neuromuscular blockade in obese patients
Zhihao LAI ; Liangping WU ; Jie PENG ; Yan LU ; Bo XU
Chinese Journal of Anesthesiology 2021;41(5):527-531
Objective:To investigate the pharmacokinetics of sugammadex in reversal of postoperative residual neuromuscular blockade in obese patients.Methods:Sixteen patients of both sexes, aged 18-65 yr, of American Society of Anesthesiologists physical statusⅠ or Ⅱ, with body mass index of ≥25 kg/m 2, scheduled for elective laparoscopic bariatric surgery, were selected.The patients were divided into 2 groups ( n=8 each) according to the degree of obesity: group O (25 kg/m 2≤BMI<40 kg/m 2) and group M (BMI≥40 kg/m 2). In group O and group M, vecuronium was administered by closed-loop muscle relaxant injection system to maintain moderate neuromuscular blockade.The administration was stopped at the end of surgery, and sugammadex 2 mg/kg was injected according to corrected body weight (CBW) of patients when the muscle relaxation monitoring T 2 recovered naturally.The recovery time of neuromuscular blockade and the occurrence of residual neuromuscular blockade within 3 h after surgery were recorded.Arterial blood samples were collected at 2, 3, 5, 10, 15, 20, 30, 60, 120, 240, 360 and 480 min after administration of sugammadex.The concentration of sugammadex in plasma was determined by ultra-performance liquid chromatography-mass spectrometry.The pharmacokinetic parameters were calculated with PKSolver software. Results:No residual neuromuscular blockade occurred, and the pharmacokinetics of sugammadex in plasma were consistent with the linear non-compartmental model in the two groups.Compared with group O, apparent clearance was increased ( P<0.05), and no significant change was found in other pharmacokinetic parameters, recovery time of neuromuscular blockade and concentrations of sugammadex in plasma at different time point ( P>0.05) in group M. Conclusion:The pharmacokinetics of sugammadex in reversal of postoperative residual neuromuscular blockade in obese patients are consistent with the linear non-compartmental model, and the clearance of sugammadex is higher in morbidly obese patients.
5.Radiation dose estimation and protective measure discussion of 241Am-Be neutron source logging
Yaping FU ; Yuan YAN ; Zhengwei YU ; Liangping CHEN ; Linghai KONG ; Peng SUN
Chinese Journal of Radiological Health 2022;31(2):167-171
Objective To investigate the radiation dose to operators in the process of 241Am-Be neutron source logging, and discuss neutron source management and protective measures for operators in well logging. Methods Through on-site observation and measurement of 241Am-Be neutron source logging in a company, we obtained the surface γ dose rate and neutron dose rate of the neutron source, as well as the operating time and distance of various processes including source taking, transfer, and loading, calculated the radiation dose to operators in various processes, and analyzed the source and proportion of the personal effective dose to operators. Results The effective doses of neutron irradiation and γ irradiation were 94.17 μSv and 2.72 μSv, respectively, for the combined processes of source tank inspection, transfer, and detection; 36.66 μSv and 24.08 μSv, respectively, for source loading and unloading; and 130.83 μSv and 26.80 μSv, respectively, for the whole neutron source logging process. The total annual effective dose of neutron source logging was 15.78 mSv, as estimated by logging 100 times per year. Conclusion In the process of 241Am-Be neutron source logging in the company, the effective dose to operators mainly arises from neutron irradiation. Therefore, it is necessary to strengthen neutron source management and take effective protective measures against neutron radiation.
6.Effects of increased secretory SERPINE1 expression by dexmedetomidine on the malignant biological behavior of thyroid carcinoma cells
Xueyan TONG ; Wenfeng JIANG ; Liangping ZENG ; Yan LIN
China Pharmacy 2025;36(10):1179-1185
OBJECTIVE To explore the effects of dexmedetomidine (DEX) increasing serpin peptidase inhibitor clade E member 1 (SERPINE1) protein on the malignant biological behavior of thyroid carcinoma (THCA) cells. METHODS THCA cells (KTC-1, TPC-1) were treated with 1, 10 and 100 nmol/L DEX, and their viabilities, clone formation rates, migration rates and invasion number were examined. Potential biological functions of DEX in THCA cells were analyzed through whole genome sequencing and gene ontology enrichment analysis. The core targets of DEX were mined through a protein-protein interaction network. The expression characteristics of DEX core targets and their relationship with patient prognosis were evaluated. The effects of DEX on mRNA and protein expressions of core targets and protein secretion in 2 types of THCA cells were detected, and the effects of this target on DEX-related effects were validated preliminarily by knocking down the core target. RESULTS Compared with the control group (0 nmol/L DEX), DEX at 1, 10 and 100 nmol/L significantly increased the viabilities of 2 types of THCA cells (except for the KTC-1 cells in the 1 nmol/L DEX group at 24 h), concentration-dependently elevated the rates of clone formation, migration rates (except for 2 types of THCA cells in 1 nmol/L DEX group), and the number of invasion (P<0.05). A total of 287 differently expressed genes (75 up- tongxueyan180@163.com regulated and 212 down-regulated) were enriched in signaling pathways such as phosphatidylinositol 3-kinase/protein kinase B, Wnt, and senescence-associated secretory phenotypes in the 2 kinds of DEX-treated or non-treated THCA cells. SERPINE1 was a core target of DEX for THCA, and its mRNA and protein expression in THCA tissues/cells were significantly elevated and associated with poor prognosis of the patients (P<0.05). Compared with the control group, mRNA and protein expression of SERPINE1 was significantly up-regulated in 2 types of cells in the 1, 10 and 100 nmol/L DEX groups, while the secretion of this protein in conditioned medium was also significantly increased, all of which showed concentration-dependence (P<0.05). After knocking down SERPINE1, the promoting effects of DEX on the proliferation, colony formation, migration and invasion abilities of two types of THCA cells were significantly inhibited (P<0.05). CONCLUSIONS DEX can promote the proliferation, migration and invasion of THCA cell, and the above effects may be associated with the expression of increased secretory SERPINE1 protein.