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Article in Chinese | WPRIM | ID: wpr-804552


@#To investigate the effects of clinical P-glycoprotein inhibitors on oral bioavailability and brain penetration of gefitinib, 16 inhibitors and gefitinib were co-administered orally to ICR mice. The suspension of gefitinib and CMC-Na were co-administered to the control group. The suspension of gefitinib and clinical P-glycoprotein inhibitors were co-administered to the control group. Blood samples and brain homogenate samples were extracted by protein precipitation with acetonitrile and determinated by LC-MS/MS. It was found that ritonavir can significantly increase the oral bioavailability of gefitinib, and the area under the plasma concentration-time curves(AUC)of gefitinib was increased by 2 times; while brain exposure was increased, there was no increment in brain penetration. Some other drugs can also increase the plasma AUC of gefitinib, but can not enhance the brain penetration; After we corrected brain concentration with fraction of unbound drug in brain, it was found that the brain concentration of gefitinib in both control group and ritonavir group did not achieve the in vitro IC50 of inhibiting non-small cell lung cancer(NSCLC)cell growth. Our results suggest that clinical doses of the 16 clinical P-glycoprotein inhibitors can not specifically increase brain tissue exposure, more specific and safer P-gp inhibitors are required. After we corrected brain concentrations with fraction of unbound drug in brain, our preclinical studies found that insufficient brain exposure may be one of the reasons for the unsatisfactory efficacy of gefitinib in the treatment of brain metastases.

China Pharmacy ; (12): 1281-1287, 2018.
Article in Chinese | WPRIM | ID: wpr-704784


OBJECTIVE:To evaluate the efficacy and safety of Yupingfeng powder combined with second- generation antihistamines versus second-generation antihistamines for chronic urticaria(CU)systematically,and to provide evidence-based reference for clinical treatment for CU. METHODS:Retrieved from PubMed,Embase,The Cochrane Library,CJFD,VIP and CBM,RCT about therapeutic efficacy(total response rate,cure rate,recurrence rate)and safety(the incidence of ADR)of Yupingfeng combined with second-generation antihistamines(trial group)versus second-generation antihistamines(control group) in the treatment of CU were collected. The data extraction was performed for included clinical studies,and Meta-analysis was performed by using Rev Man 5.3 statistical software after quality evaluation with Cochrane Handbook 5.1.0 evaluation criteria. RESULTS:A total of 34 RCTs were enrolled,involved 3 405 patients in total. Results of Meta-analysis showed that the total response rate [OR=4.02,95%CI(3.03,5.34),P<0.001],cure rate [OR=2.25,95%CI(1.95,2.60),P<0.001] and recurrence rate [OR=0.33,95%CI(0.26,0.42),P<0.001] of trial group were significantly better than those of control group,with statistical significance. There was no statistical significance in the incidence of ADR between 2 groups [OR=0.98,95%CI(0.71,1.37),P=0.92]. CONCLUSIONS:For CU therapy,Yupingfeng powder combined with second-generation antihistamines is better than second-generation antihistamines alone in improving total response rate and cure rate,reducing recurrence rate,both have similar safety.

Article in Chinese | WPRIM | ID: wpr-694394


Objective To investigate the effects of the third-generation mechanical chest compressor on outcomes of cardiopulmonary resuscitation in patients with out-of-hospital cardiac arrest.Methods The patients with out-of-hospital cardiac arrest from October 2015 to September 2017 in the Yuyao peoples' hospital were included and divided randomly into 2 groups:manual chest compression group and mechanical chest compression group.The duration of resuscitation,the rate of restoration of spontaneous circulation (ROSC),4-h survival rate and the rate of survival getting to hospital discharge with favorable neurological status of two groups were analyzed.Results A total of 95 patients with out-of-hospital cardiac arrest were included.The rate of ROSC and 4-h survival was significantly increased in the mechanical chest compression group compared with the manual chest compression group (P<0.05).There was no remarkable difference in the duration of resuscitation and the rate of survival getting to hospital discharge with favorable neurological status between 2 groups.Conclusions The thirdgeneration mechanical chest compressor significantly improves the rate of ROSC and the shout-term survival in patients with out-of-hospital cardiac arrest.

Article in Chinese | WPRIM | ID: wpr-711313


Objective To explore the effect of radiofrequency-induced hyperthermia on the morphology of articular cartilage and any changes in serum-1 interleukin-1 (IL-1β) and tumor necrosis factor-alpha (TNF-α) in the process of knee osteoarthritis in rabbits.Methods Fifty-four male rabbits were selected and knee osteoarthritis was introduced to their right hind limbs using the modified Huhh model.They were then randomly divided into a model group,a cervus and cucumis polypeptide (CCP) group and a radiofrequency thermotherapy (RT) group,each of 18.The CCP group was injected with deer melon peptide intramuscularly.The RT group was given radiofrequency hyperthermia treatment.The model group was not provided with any special treatment.On the 7th,13th and 19th day of the treatment,6 rabbits in each group were sacrificed to resect the right medial femoral condyle cartilage.The morphological characteristics of the cartilage were evaluated using the modified Mankins score,while the content of IL-1βand TNF-α in the serum were detected using enzyme-linked immuno-sorbent assays (ELISAs).Results At the same time points,the average Mankins score and the average content of IL-1βand TNF-α in the serum of the model group were significantly higher than in the CCP group,with the values in the latter group significantly higher than in the RT group.In the RT group,the average Mankins score,as well as the IL-1 beta and TNF-alpha levels in the serum,decreased significantly with longer treatment.Conclusion Radiofrequency-induced hyperthermia is superior to deer melon polypeptide in treating knee osteoarthritis,at least in rabbits.Its therapeutic mechanism may be related to the control of serum IL-1 beta and TNF-alpha levels.

Article in Chinese | WPRIM | ID: wpr-711265


Objective To explore the effect of radiofrequency heating on type Ⅱ collagen expression in a rabbit model of osteoarthritis.Methods Knee osteoarthritis was induced in the right hind legs of 54 male rabbits using modified Hulth modeling.The rabbits were randomly divided into a model group which was not given any special treatment,a Lugua polypeptide group and a radiofrequency hyperthermia group.The Lugua polypeptide group was injected with Lugua polypeptide;the radiofrequency hyperthermia group was treated with radiofrequency irradiation.Six,12 and 18 days after the treatment,the morphological condition of the rats' right femoral medial condyle cartilages were evaluated using modified Mankins scoring and the type Ⅱ collagen content of the cartilage was detected using a quantitative PCR technique.Results At the same time points after treatment,the average Mankins scores were decreased in all the 3 groups,with that of the model group was significantly higher than those of both of the other groups,and the radiofrequency hyperthermia group's average score was significantly better than that of the Lugua polypeptide group.The average type Ⅱ collagen content was significantly increased in all the 3 groups to various extent (the radiofrequency hyperthermia group > Lugua polypeptide group > model group).For the radiofrequency hyperthermia group,the average Mankins score decreased significantly and the average type Ⅱ collagen content increased significantly as the treatment continued.Conclusion Radiofrequency hyperthermia is superior to Lugua polypeptide for treating knee osteoarthritis,at least in rabbits.Its therapeutic effectiveness may be related to a significant increase of type Ⅱ collagen in the cartilage.

Article in Chinese | WPRIM | ID: wpr-790581


Objective To determine the concentration of eupatilin and arteanoflavone in A rtemisia anomala by high per-formance liquid chromatography (HPLC).Methods A rtemisia anomala was extracted by ultrasonic for 60 minutes with 10 times volume of methanol.The HPLC was performed on a SHISEIDO MG-C18 column (3.0 mm × 100 mm,3μm).The mobile phase was a mixture of acetonitrile (ACN) and 0.1% formic acid (40:60,V/V ).The detection wavelength was 350 nm,the column temperature was 25 ℃ and the injection volumn was 5μl.Results Eupatilin and arteanoflavone were separated at base-line within 15min with good linearity.The method validation results show that the precisions,repeatability and stability were all in the normal range.The low,medium and high level recoveries of eupatilin were 100.26%,99.58%,102.24%,and those of arteanoflavone were 99.09%,101.12%,101.43%,respectively.Conclusion The method was rapid,simple,reproductive and accurate.It can be used to control the quality of Artemisia anomala.