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OBJECTIVE To investigate the effects of omeprazole on pharmacokinetic parameters of imatinib in rats. METHODS According to body weight， the rats were divided into imatinib+low-dose， medium-dose， and high-dose omeprazole groups， imatinib group， with 6 rats in each group. They were given omeprazole suspension at the doses of 1.8， 3.6 and 7.2 g/kg， or 0.5% sodium carboxymethyl cellulose solution intragastrically respectively； one hour later， imatinib suspension was administered by oral gavage at a the dose of 10 mg/kg. Blood sample （100 μL） was taken from the orbit before and 0.5， 1， 2， 2.5， 3， 4， 5， 6， 8， 12， 24 and 36 hours after intragastric administration of imatinib. Using imatinib-d3 as internal standard， the plasma concentrations of imatinib and its metabolite N-desmethyl imatinib in rat were determined by high performance liquid chromatography-tandem mass spectrometry. The pharmacokinetic parameters were calculated by DAS 2.0 software and compared. RESULTS Compared with imatinib group， AUC0－∞ and AUMC0－∞ of imatinib in rat plasma of imatinib+medium-dose omeprazole group， cmax， t1/2， AUC0－∞ and AUMC0－∞ of imatinib in rat plasma of imatinib+high-dose omeprazole group were all increased or prolonged significantly （P＜0.05）. Compared with imatinib group， AUC0－∞ and AUMC0－∞ of N-desmethyl imatinib in rat plasma of imatinib+medium-dose omeprazole group， and cmax and AUC0→∞ of N-desmethyl imatinib in rat plasma of imatinib+high-dose omeprazole group were decreased significantly （P＜0.05）. CONCLUSIONS Omeprazole may increase the plasma concentration of imatinib in rats and reduce the plasma concentration of N-desmethyl imatinib in rats， which may be associated with inhibiting the metabolism of imatinib.
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OBJECTIVE：To establish a method for the determination of pyrrotinib concentration in plasma ，and apply it in clinic. METHODS ：After precipitated with methanol ，the plasma sample was determined by LC-MS/MS using imatinib as internal standard. The determination was performed on Ultimate AQ-C 18 column with mobile phase consisted of methanol （containing 0.1％ formic acid ）and water （containing 0.1％ formic acid ）（gradient elution ）at the flow rate of 0.4 mL/min. The column temperature was 40 ℃，and the sample size was 5 µL. The ion source was electrospray ionization source ，and the positive ion scanning was carried out in multiple reaction mode. The ion pairs for quantitative analysis were m/z 583.4→138.3（pyrrotinib）and m/z 494.5→ 393.4（internal standard ），respectively. Thirty breast cancer patients taking pyrrotinib were collected from the Affiliated Hospital of Qingdao University during Jun.-Nov. 2020 to determine their steady-state trough concentrations of pyrrotinib after a week of treatment. RESULTS ：The linear range of pyrrotinib were 5-300 ng/mL（r＝0.999 3）. The lower limit of quantification was 5 ng/mL. RSDs of intra-day and inter-day were not higher than 9.30％，and relative errors （REs）ranged －6.70％-5.04％. REs of stability tests were in the range of －1.92％-5.42％. The extraction method ，matrix effect and residual effect did not affect the quantitative analysis of the substance to be tested. The steady-state trough concentrations of pyrrotinib were 32.6-82.8 ng/mL，with an average plasma concentration of 53.8 ng/mL；there was about 2.54 fold individual difference. CONCLUSIONS ：Established LC-MS/MS method is simple ，sensitive and accurate ，and can be used for the plasma concentration monitoring of pyrrotinib in breast cancer patient.
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Objective:To explore the of short-term psychodynamic psychotherapy on anxiety and depression of gout patients and its influence on well-being index, family function and compliance.Methods:60 gout patients were selected from June 2018 to December 2019 in the outpatient department of rheumatism and immunity department of Dongguan Kanghua Hospital by prospective case-control study. They were randomly divided into control group and treatment group, 30 cases respectively. Both groups were given gout related clinical treatment and routine nursing, and the treatment group was given short-term dynamic orientation psychotherapy. The treatment compliance, the psychological status, well-being index and blood uric acid (UA) level of the two groups were compared before intervention, immediately after intervention and 3 months after intervention.Results:The scores of Patient Health Questionnaire-9 (PHQ-9) and the generalized anxiety disorder 7-item scale (GAD-7) in the two groups were gradually decreased immediately and 3 months after intervention ( P<0.05), and the scores of well-being index were gradually increased ( P<0.05); Compared with the control group, the scores of PHQ-9 and GAD-7 in the treatment group decreased more significantly ( P<0.05), and the score of well-being index increased more significantly ( P<0.05); The scores of communication, behavior control and total function of family function in the treatment group decreased gradually immediately after intervention and 3 months after intervention ( P<0.05), and were significantly lower than those in the control group ( P<0.05); The level of serum UA in the two groups decreased gradually immediately after intervention and 3 months after intervention ( P<0.05), but there was no significant difference in UA level at each time point between the two groups. The treatment compliance of the treatment group was significantly better than that of the control group ( P<0.05). Conclusions:The short-term dynamic orientation psychotherapy for gout patients has obvious effect in improving the state of anxiety and depression, improving the index of well-being, family function and treatment compliance.
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OBJECTIVE： To study the effects of Wuzhi soft capsule and imatinib mesylate tablet on the pharmacokinetics of imatinib in rats. METHODS： The rats were divided into single administration group and consecutive administration group. The single administration group was divided into imatinib group one （ig administration of blank soybean oil+imatinib suspension 10 mg/kg）， low-dose， medium-dose and high-dose of Wuzhi soft capsule+imatinib group （ig administration of Wuzhi soft capsule solution 134， 268， 536 mg/kg+imatinib suspension 10 mg/kg）， with 6 rats in each group. Each group was given imatinib suspension intragastrically 30 min after intragastric administration of blank soybean oil/Wuzhi soft capsule solution. The consecutive administration group was divided into imatinib group two （ig administration of blank soybean oil+imatinib suspension 10 mg/kg）， Wuzhi soft capsule low-dose+imatinib group （ig administration of Wuzhi soft capsule solution 134 mg/kg+imatinib suspension 10 mg/kg）， with 6 rats in each group. Each group was given blank soybean oil/Wuzhi soft capsule solution intragastrically for consecutive 14 d， once a day； 30 min after last administration， ig imatinib suspension. About 100 μL blood was collected before imatinib， 0.5， 1， 2， 2.5， 3， 4， 5， 6， 8， 12， 24 and 36 h after medication. The plasma concentration of imatinib was determined by HPLC-MS/MS. The pharmacokinetic parameters were fitted by using DAS 2.0 software. RESULTS： After single administration， compared with imatinib group one， cmax， t1/2， AUC0-36 h and AUMC0-36 h in low-dose， medium-dose and high-dose of Wuzhi soft capsule+imatinib group were increased significantly （P＜0.05 or P＜0.01）. After consecutive administration， compared with imatinib group two， cmax， t1/2 and AUMC0-36 h of imatinib+low-dose of Wuzhi soft capsule group were increased significantly （P＜0.05 or P＜0.01）. CONCLUSIONS： Single administration and consecutive administration of Wuzhi soft capsule influence the pharmacokinetics of imatinib， increase plasma concentration of imatinib and prolong half-time.
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OBJECTIVE:To evaluate the clinical efficacy of Shuanghuanglian injection in the treatment of acute exacerbation of chronic obstructive pulmonary disease (AECOPD),and to observe its effects on the plasma levels of C-reactive protein (CRP),procalcitonin(PCT)and interleukin-6(IL-6). METHODS:A total of 100 AECOPD patients were randomly divided into observation group and control group,with 50 cases in each group. Control group received routine treatment,such as controlled oxygen therapy,intravenous dripping of moxifloxacin,bronchodilator for relieving asthma,mucolytic for eliminating phlegm,nu-tritional support. Observation group was additionally given Shuanghuanglian injection 1 ml/(kg·d)added into 5% Glucose injec-tion 250 ml intravenously,qd,on the basis of control group. Treatment course of 2 groups lasted for 10 d. Clinical efficacies of 2 groups were compared as well as the changes of serum levels of CRP,PCT and IL-6 before and after treatment and the occur-rence of ADR. RESULTS:After treatment,total effective rate of observation group was 96.0%,which was significantly higher than 82.0% of control group,with statistical significance(P0.05). After treatment,serum levels of CRP,PCT and IL-6 were de-creased significantly in 2 groups,and those of observation group were significantly lower than those of control group,with statis-tical significance (P0.05). CON-CLUSIONS:Shuanghuanglian injection can effectively improve serum inflammatory factors of AECOPD patients,and shows good clinical efficacy and safety.
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<p><b>OBJECTIVE</b>Alpha-2 macroglobulin (alpha2M) is a proteinase inhibitor found in association with senile plaques in Alzheimer's disease (AD). Also alpha2M has been implicated in several pathophysiological processes in AD. In view of the recent contradictory reports on the relationship between AD and a common polymorphism I1000V in A2M gene, the present authors studied a relatively large sample, determined the genotype of the I1000V polymorphism in A2M gene in sporadic AD patients and age-matched controls with normal cognition, and examined the possible association of the polymorphism with AD.</p><p><b>METHODS</b>Genotypes of A2M and apolipoprotein E (apoE) were detected by polymerase chain reaction combined with restriction fragment length polymorphism in 257 patients and 242 controls in Guangzhou, and 112 patients and 113 controls in Chengdu.</p><p><b>RESULTS</b>The 1000Val allele frequencies in the merged AD and control groups were 7.7% and 8.7%, respectively. The differences of allelic and genotypic frequencies between the patients and control subjects were not statistically significant, even after stratification by apoE epsilon4 status or by age-of-onset of the disease.</p><p><b>CONCLUSION</b>The results of this study revealed no association between the I1000V polymorphism of A2M and Chinese sporadic AD in Guangzhou and Chengdu.</p>
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Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Doença de Alzheimer , Etnologia , Genética , Apolipoproteínas E , Genética , Povo Asiático , Genética , China , Frequência do Gene , Predisposição Genética para Doença , Genótipo , Reação em Cadeia da Polimerase , Polimorfismo Genético , Genética , Polimorfismo de Fragmento de Restrição , alfa-Macroglobulinas , GenéticaRESUMO
Objective:To explore the mental health status of the first-degree relatives of the heroin addicts. Methods: Three hundred twenty first-degree relatives of the heroin addicts were evaluated with SCL-90. Results: The scores of somatization, depression, anxiety, paranoia, and psychiatric factor among the first-degree relatives were significantly higher than the national norm. The first-degree relatives of heroin addicts who had addicted more than 5 years had significantly higher score than the relatives of heroin addicts who had addicts less than 5 years. Conclusion: The mental health condition of the first-degree relatives of heroin addicts was poor, especially those relatives of heroin addicts who have addicted for more than 5 years.