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OBJECTIVE To establish a method for the determination of propofol concentration in human plasma and apply it in patients with lymphedema. METHODS The concentration of propofol was determined by UPLC-MS/MS after protein precipitation of plasma samples using thymol as internal standard. The sample was eluted on a Kinetex C18 column with a mobile phase consisting of acetonitrile （A）-water （B） for gradient elution at the flow rate of 200 μL/min. The sample size was 5 μL， and the column temperature was set at 40 ℃. The sample chamber temperature was 15 ℃. Using multi-reaction monitoring mode， the ion pairs for quantitative analysis were m/z 177.0→161.2 （propofol） and m/z 149.0→133.1 （internal standard）， respectively. The above method was used to determine the plasma concentration of propofol in 6 patients with lymphedema. RESULTS The linear range of propofol was 50-5 000 ng/mL （r＝0.995 0）. RSDs of within- and between-batch precision were not more than 8.08%； no endogenous interference， carryover effect， or dilution effect was observed in blank plasma. The extraction recovery ranged from 89.80% to 93.73%， and matrix effects were within the range of 97.93%-101.73%. RSDs of the stability test were all lower than 3.27%. During intraoperative TCI 2-30 min， the plasma concentration of propofol in 6 patients was maintained in the range of 1 865.3-6 056.2 ng/mL， and the propofol was almost excreted within 4-8 h after operation. CONCLUSIONS The established UPLC-MS/MS method in this study can achieve the determination of propofol and a simple and fast sample pretreatment process without derivatization； it is proved to be suitable for the concentration monitoring of propofol in plasma samples of patients with lymphedema.
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OBJECTIVE To study the components of ethyl acetate fraction in Qubai tablet ，and its pharmacodynamics on de melanocyte model ，and explore the material basis for anti-vitiligo effect of Qubai tablet. METHODS The ethyl acetate fraction of Qubai tablets was obtained by extraction ，and its components were analyzed by ultra performance liquid chromatography-mass spectrometry（UPLC-MS）. Model control group ，vehicle control group and 8-methoxypsoralen（8-MOP）administration groups （10，50，100，150，200 μmol/L），ethyl acetate fraction administration groups of Qubai tablet （10，50，100，150，200 μg/mL） were set up in the experiment. By establishing the de melanocyte model ，the effects of ethyl acetate fraction of Qubai tablet on de melanocyte were studied from four aspects ：cell number ，cell viability ，melanin formation and tyrosinase activity. RESULTS UPLC-MS component analysis preliminarily determined the structure of 64 compounds in the ethyl acetate fraction of Qubai tablet ， of which 14 compounds were detected in positive and negative ion mode ；psoralen compounds accounted for the largest proportion ， and the content of psoralen chromone chalcone was the highest in positive and negative ion mode. The results of pharmacodynamic study showed that the ethyl acetate fraction of Qubai tablet could increase the number of de melanocytes ，and significantly improve the cell proliferation rate ，the rate of promoting melanin formation and the rate of promoting tyrosinase activity in the process of melanin formation （P＜0.01）. CONCLUSIONS Psoralen compounds may be the material basis for the anti-vitiligo effect of ethyl acetate fraction of Qubai tablet ；good anti-vitiligo effect of ethyl acetate fraction of Qubai tablet may be related to the promotion of tyrosinase activity.
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AIM: To provide reference for the clinical application of tigecycline and subsequent population pharmacokinetic-pharmacodynamics study in the future. METHODS: The Chinese and English keywords of "Tigecycline", "population pharmacokinetics", "population pharmacokinetic model", "pharmacodynamics" or "Tigecycline" pharmacokinetics "were used to search the relevant references published from the time of self-establishment to June 1, 2021 in PubMed, China Knowledge Infrastructure, Wanfang and other databases. The research progress of population pharmacokinetics and pharmacodynamics of tigecycline was reviewed. RESULTS & CONCLUSION: A total of 73 relevant references were retrieved, including 8 tigecycline PPK studies and 7 tigecycline PK/PD studies. At present, tigecycline PPK models had been established in patients with complex intra-abdominal infections, skin and skin and soft tissue infections, community-acquired pneumonia, nosocomial pneumonia, septic shock and other severe infections, including 8 two-compartment models. The main covariates affecting tigecycline plasma clearance were weight-related, liver function and renal function-related parameters. Body weight was also an important factor influencing the apparent volume of distribution. The effect of different disease types on the pharmacokinetics of tigecycline was different, and it needed to be considered and selected in combination with the specific circumstances of patients when formulating clinical dosing regimens. Pharmacodynamics studies should consider not only the type of disease, pathogens and patient factors themselves, but also the characteristics of atypical nonlinear plasma protein binding of tigecycline. In order to accurately understand the efficacy of different dose regimens, it was necessary to monitor the therapeutic drugs of tigecycline.
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BACKGROUND:Psychological disorder and behavior disorders can affect the development of behavior and personality in children.OBJECTIVE:To investigate the behavior disorders and the personality in children with tic disorders (TD).DESIGN:A comparative investigation between TD children and the healthy controls.SETTING:It was conducted at the Department of Pediatrics,Daqing Oil Felid General Hospital in Heilongjiang ProvincePARTICIPANTS:Totally 110 outpatients including 92 males and 18females, diagnosed as TD at the Department of Pediatrics, Daqing Oil Felid General Hospital,were selected (TD group) from February 2003 to December 2004.According to the clinical manifestations,they were divided into transient tic disorder group (46 cases),chronic motor/vocal tic disorder group (34 cases) and Tourette Syndrom (TS) group(30 cases).All the patients were newly diagnosed without any medication and intracranial organic diseases. Meanwhile,30 children with normal physical examination findings, between the ages of 7 and 14,24 males and 6 females, were selected as controls. Informed consents were obtained from guardians of all the participants.used to measure the children's social skills and behaviors (It contains a 113-item behavior problems scale. According to the children's ages,the items were classified into 9 factors,including somatic complains,poor social skills,compulsions,undisciplined,hyperactivity,Asperger syndrome,immaturity,hostility and aggressiveness.The scores of referring items constitute the total score of each factor).Comparison of these scores between patients and healthy controls is helpful to determine if a factor in affected children is abnormal. The closer the relationship between the patients and the controls is, the less behavioral problems Personality Questionnaire (EPQ) was adopted in this study to evaluate the personality in the patients compared to healthy controls.{There were four major dimensions of personality including introversion/extraversion,neuroticism,psychoticism and validity questionnaire (construct validity).When the validity score was over 70,it represented that the EPQ was invalid.An over-61.5 neuroticism score represented an apparent neuroticism tendency. Once the neuroticism score and introversion/extraversion score were over 56.7,mental instability or instable tendency could be suspected. When introversion/extraversion score was over 56.7and the neuroticism (extraversion) score was less than 43.3,it represented a sanguine personality or such tendency. When both of the neuroticism score and introversion/extraversion score were less than43.3 (introversion),it revealed a phlegmatic personality or such tendency. And when the introversion/extraversion score was less than43.3 with neuroticism score over 56.7,it represented a melancholic personality or such tendency.}MAIN OUTCOME MEASURES:Comparison of Achenbach's CBCLand EPQ between patients and healthy controls .RESULTS:Totally 110 TD patients and 30 healthy children completed the control group (t=3.12-8.60, P ＜ 0.01).The hyperactivity score in the transient tic group was significantly higher than that in the control group (t=2.01, P ＜ 0.05). In the chronic motor tic disorder group and the TS group,the scores of depression/anxiety,poor social skills,compulsions,social withdrawal,hyperactivity and aggression were all higher than those in the control group(t=2.11-7.65, P ＜ 0.05-0.01).In all of these three TD groups, score factors relating to social functions,such as movements, social skills and school life were apparently lower than those in the control group (t= 1.97-7.31, P ＜ 0.05-0.01).(t=2.76-4.32, P ＜ 0.05-0.01), while the score of validity questionnaire was lower than that in control group (t=3.49-6.38, P ＜ 0.05).CONCLUSION:It reveals that TD patients have many behavioral problems,personality defects and poor social skills. Of all the TD groups,the transient tic group has a higher occurrence rate of disease and only one abnormal factor, hyperactivity. While,the chronic motor tic disorder group and the TS group have more abnormal behavioral factors.
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AIM: To set up population pharmacokinetics/pharmacodynamics (PPK/PD) model of valproate (VPA) in children with epilepsy in China, and promote reasonable use of antiepileptic drugs(AEDs)in clinical practice. METHODS: Sparse data of VPA serum concentrations from 246 pediatric children were collected. These patients were divided into three groups: PPK-Model group ([WTBX]n=146), to calculate PPK parameter values of VPA and set up a PPK model; PPK-Valid group ([WTBX]n=100), to valid the PPK model; and PPD group ([WTBX]n=69), to set up PPK/PD model. Based on the data of PPK-Model group and PPK-Valid group, a PPK model of VPA in children with epilepsy in China was successfully set up by using NONMEM software by ourselves. Now, using the data of 69 patients in PPD group who were on VPA monotherapy and this PPK model, we set up PPK/PD model by NONMEM software. Efficacy of epilepsy treatment was divided into 5 grades according to the percentage of seizure frequency decreased (PSFD%): grade 1: PSFD% was 100%; grade 2: PSFD% was 75%-100%; grade 3: PSFD% was 50%-75%; grade 4: PSFD% was 25%-50%; grade 5: PSFD% was less than 25%. The quantitive relationship between the VPA serum concentrations and the probability for its efficacy score was characterized by Logistic regression analysis with NONMEM. RESULTS: Logistic regression analysis showed that, VPA serum concentrations and the probability for its efficacy grades 5, 4, 3, 2, and 1 were (23 ?g?ml -1, 5, 50%), (30 ?g?ml -1, 4, 32.3%), (50 ?g?ml -1, 3, 26.3%), (65 ?g?ml -1, 2, 36.5%), (78 ?g?ml -1, 1, 50%), and (100 ?g?ml -1, 1, 84.2%)respectively. CONCLUSION: A PPK/PD model of VPA in children with epilepsy in China is successfully established by using NONMEM software, and the probability of efficacy grade for any concentration can be calculated. It will be valuable to facilitate individualized dosage regimen.
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OBJECTIVE: To probe into the medication status of the elder patients in community so as to provide reference for pharmacists to promote rational medication for the elderly people in community. METHODS: The medication status of 484 cases in the community was investigated through questionnaire and interview. RESULTS: The principal diseases affecting the health of the elder people included hypertension, diabetes mellitus, coronary heart disease, cerebrovascular disease. The average number of drugs they used totaled 2.92 kinds; the higher the educational background, the higher proportion of the elder people who read drug package instruction but the lower ratio of medication compliance. The elder people commonly had poor knowledge about the drugs and adverse drug reactions(91.74% and 60.74%);21.11% responded that they had ever received medication guidance from pharmacists, only 3.10% responded that they had once consulted pharmacists about medication problems. CONCLUSION: The medication of the elder people in community is characterized by multiple drug varieties, poor ADR knowledge and lower cognition on pharmacists. It is urgent to improve the pharmaceutical care ability of medical institution and enhance the social influence of pharmacists.