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AIM: To evaluate the pharmacokinetics, bioequivalence, and safety of capecitabine tablet in cancer patients following single oral administration. METHODS: Based on an open-randomized two-period crossover designation, subjects were orally given capecitabine tablet (test or reference products, 0.6 g single dosage). Blood samples were then collected and the plasma concentrations of capecitabine and its active metabolite, 5-fluorouracil (5-FU) were examined by HPLC-MS/MS. The bioequivalence between the test and reference formulations were evaluated with the pharmacokinetic parameters determined by the Phoenix WinNonlin 7.0 software. RESULTS: The numbers of the major pharmacokinetic parameters in patients treated with test and reference products were similar. To analyze the numbers of Cmax, tmax, AUC0-t, AUC0-∞, the 90% confidence interval (CI) for Cmax, AUC0-t and AUC0-∞ were 84.48-106.70, 93.03-96.54 and 96.34-102.84, respectively. For the 5-FU, the 90%CI of the for Cmax, AUC0-t and AUC0-∞ were 84.32-99.67, 90.55-98.76 and 96.99-103.48, respectively. Both sets of numbers fell within the bioequivalent limit ranges of 80.00%-125.00%. No serious adverse event was observed. CONCLUSION: The current data indicate that the test and reference formulations of capecitabine tablets were bioequivalent in cancer patients.
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To explore the influence of zinc supplementation on irbesartan treatment for atherosclerosis of ApoE gene-deleted mice. Atherosclerosis model mice induced by normal feed were randomly divided into ApoE[-/-] control group, irbesartan group and zinc sulfate+ irbesartan group, 6 mice each group; C57BL/6J mice with normal feed were regarded as blank control group [n=6]. Blank control group and ApoE[-/-] control group were not given any medical treatment, and irbesartan group were treated with irbesartan [50mg/kg/d], and zinc sulfate+irbesartan group were given zinc sulfate [25mmol/L] treatment besides the administration of irbesartan group. The blood pressure of each mouse was recorded and the blood lipid level was detected after 15 weeks' treatment. The internal inflammatory reaction of the mice was evaluated according to IL-6 and TNF-alpha level. The oxidative stress was evaluated according to MDA and SOD levels. And the atherosclerosis plaque was analyzed with immunohistochemistry. After 15 weeks of drug administration, it showed that the total cholesterol level, LDL-C, HDL-C and blood pressure level [P<0.05] of the mice were improved significantly with the administration of zinc sulfate+irbesartan compared with irbesartan group, and the oxidative stress response and inflammatory reaction of mice in zinc sulfate+irbesartan group decreased more significantly than those of irbesartan group [P<0.05]. In the detection of atherosclerosis plaque, the ratio of plaque area and tube area as well as the improvement degree of mean aortic IMT in zinc sulfate+irbesartan group were superior to those of irbesartan group [P<0.05]. Zinc supplementation has certain therapeutic effect on the advanced atherosclerosis of ApoE gene-deleted mice, which can significantly improve the efficacy of irbesartan
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OBJECTIVE:To systematically review the effect of CYP2C19 genetic polymorphism on lansoprazole pharmacoki-netics,and provide evidence-based reference for clinical individualized medication of lansoprazole. METHODS:Retrieved from PubMed,EMBase,Web of science,Cochrane Library and CJFD,retrospective studies about the effect of CYP2C19 genetic poly-morphism on lansoprazole pharmacokinetics were collected,Meta-analysis was performed by Rev Man 5.2 software after data ex-tract and quality evaluation. RESULTS:Totally 11 retrospective studies were included,involving 200 patients. The gene type in-cluded homozygote express metabolizers (EM),heterozygous express metabolizers (HEM) and slow metabolizers (PM). Results of Meta-analysis showed CYP2C19 polymorphism significantly affected cmax,AUC,t1/2,tmax and CL/F. The cmax and AUC in group PM were higher than group HEM and group EM;CL/F in group EM was higher than group HEM and group PM;t1/2 in group PM was higher than group HEM and group EM,while there was no significant difference in the t1/2 between group HEM and group EM;tmax in HEM and group PM were higher than group EM,while there was no significant difference in the tmax between group PM and group HEM. CONCLUSIONS:CYP2C19 genetic polymorphism shows obvious effect on lansoprazole pharmacokinetics, which is the key factor for causing efficacy of lansoprazole and individual differences among adverse reactions,and clinic should take into account individualized dose regimen of lansoprazole.
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OBJECTIVE:To explore regularity and characteristics of ADR in our hospital,and to provide reference for ratio-nal drug use in the clinic. METHODS:A total of 368 ADR collected from Zhengzhou People's Hospital during 2013-2014 were an-alyzed statistically in respects of patient's gender,age,drug types,route of administration,dosage form,organs or systems in-volved in ADR,clinical manifestations,ADR outcome,etc. RESULTS:Of 368 ADR reports,female was more than male (52.99% vs. 47.01%);the number of patients aged more than 50 years was the most(36.14%);most of ADR cases were induced by antibiotics and TCM preparations,accounting for 40.22%,21.47%,respectively;among route of administration,most of ADR cases were induced by intravenous administration (85.60%);main clinical manifestations were lesion of skin and its appendants (39.95%),followed by digestive system (21.47%). After treatment,all patients were cured or improved,no death case was found. CONCLUSIONS:Clinic should strengthen ADR monitoring and analysis and evaluarion,strengthen the rational use of anti-biotics and TCM injections and adopt measures to reduce drug risk.
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AIM:The polysaccharides of Hedyotis difusa Willd of different sources were extracted and its content and composition of the polysaccharide was analyzed. METHODS: The microwave was employed for the aqueous extract of Hedyotis difusa Willd and the content of total sugar was determined by phenol-sulfur test,the monosaccharides composition was determined by HPLC with pre-column derivatization. RESULTS: The polysaccharide obtained from the samples of Guangdong Province had the highest content.The analytic data showed that the composition of monosaccharides in hydrolytic polysaccharides of Hedyotis difusa Willd were mannose,glucose,galactose,arabinose and rhamnose,the average content of polysaccharides was 9.82%. CONCLUSION: The HPLC method with pre-column derivatization is appropriate for the analysis of monosaccharide composition of Hedyotis difusa Willd polysaccharides and the method is simple,quick and accurate.