Objective To establish an UPLC method for determination of Triptolide in serum and explore its pharmacokinetics in patients with rheumatoid arthritis after oral administration of tripterygium glycosides tablet. Methods Three patients with rheumatoid arthritis were enrolled. Using Estazolam as internal standard, serum was extracted with acetic ether, and determination was performed on column of Waters Acquity C18 (2.1 mm×100 mm, 1.7 μm) with mobile phase consisted of acetonitrile-0.1% glacial acetic acid (30∶70) at the flow rate of 0.2 mL/min. The column temperature was 30 ℃, and the detection wavelength was set at 220 nm. The serum concentration of Triptolide was processed by DAS 2.1.1 computer program. Results Triptolide was well-separated from internal standard, and the retention time were about 4.9 min and 8.9 min, respectively. Linear range of Triptolide was 13.13-840.00 ng/mL. RSD of intra-day and inter-day were lower than 15%and the recoveries were 88.25%-99.33%. Pharmacokinetic parameters were as follows:Cmax was (159.97±42.43) ng/mL, Tmax was (1.33±0.58) h, T1/2βwas (7.51±2.26) h, and AUC0-12 h was (1131.12±89.20) mg?h/L, respectively. Conclusion Pharmacokinetics of Triptolide conformed to two compartment model. Triptolide can be quickly absorbed, and exists differences among individuals.

Objective To explore whether major depressive disorder（MDD）and the therapeutic effect of fluoxetine are related to a functional polymorphism-1019C/G in the promoter region of the 5-HT1A receptor（HTR1A）gene.Methods Genotype and allele frequencies of HTR1A receptor gene-1019C/G polymorphism in MDD patients and healthy subjects（control）were examined by PCR-RFLP technique.Before and after the MDD patients accepted fluoxetine treatment for 6 weeks,17-item Hamilton depression rating scales（HAMD）were made to determine the severity of the symptoms,the outcome and remission status.Results There were significant differences in-1019C/G gene genotypes and alleles distribution between the patients and the healthy control,G allele frequency of the MDD patient was higher than that of the healthy control（P 0.05）.There were significant differences in HAMD scores among the patients with different genotypes in MDD group（P 0.05）,the score of C/C genotype patient was especially higher than that of C/G genotype（P 0.05）and G/G genotype patient（P =0.008）.There was no statistical difference in the therapeutic effect of fluoxetine among the patients with different genotypes in MDD group（P =0.761）.Conclusion HTR1A gene-1019C/G genetic polymorphism might related to MDD,especially G allele might be the possible risk factor of MDD.C allele might be correlated with the degree of pathogenetic severity,especially patients with the-1019C/C carriers.-1019C/G genetic polymorphism was not related to the clinical outcome of MDD patients treated with fluoxetine.

Objective To study the mRNA expression of myelin basic protein (MBP) and myelin oligodendregha glyeoprotein (MOG) in hippocampus of rats following global brain ischemia.Method The four- vessel occlusion animal model in the Sprague-Dawley rats was used in this study.The mRNA expression levels of MBP and MOG in the hippocampus of rats were analyzed by reverse transcription polymerase chain reaction (RT- PCR) at day 2,4,7,14 and 28 days after global brain ischemia.There were eight rats at each time-point and sham operated group.Results The mRNA expression of both MBP and MOG in hippocampus of rats decreased at 2 days after global brain ischemia.The gene expression of myelin gene decreased significantly at 7 days and it reached to the lowest level at 28 days.Compared with sham operated group,the gene expression of MBP and MOG in hippocampus of rats decreased significantly at 7,14 and 28 days after global brain ischemia (P

Objective To investigate whether leukotriene D4 (LTD4) regulates eotaxin-3 (Eot-3) expression in bronchial epithelial cells, and study effect of pranlukst on the regulation.Methods BEAS-2B cells and normal human bronchial epithelia cells were pre- treated with LTD4 for 1 hour,stimulated with interleukin-4, the cells were incubated for 24 hours. Eot-3 protein in supernatant were measured by enzyme linked immunosorbent assay(ELISA). The cells were pretreated with pranlukast in different concentration, then the above procedure was repeated. Results The untreated bronchial epithelial cell expressed Eot-3 protein on a very low level. After stimulating with IL-4 and incubating for 24 hours, Eot-3 production increased significantly. Pretreating the cells with LTD4 enhanced the inducing effect of IL-4. Pranlukast inverted the upregulation of LTD4. Conclusions Upregulating the expression of Eot-3 induced by IL-4 on bronchial epithelial cells may explain partially the mechanism of leukotrienes involving airway allergic inflammation of asthma. The invertion impact on upregulation of LTD4 by pranlukast may be one of mechanisms that leukotrienes receptor antagonist cure asthma.

Objective To explore the changes of the plasma motilin(MTL)and serum gastrin(GAS)levels and their relationship with course of disease,the severity,the complication of digestive system in neonates with intracranial haemorrhage(ICH).Methods The objects were 26 cases of term newborns with ICH,the healthy control group contained 30 cases of healthy term newborns.Plasma motilin and serum gastrin concentration were measured by radioimmmunoassay in 26 cases of newborns with ICH in the 2 d,3-5 d,7-10 d,and 12-15 d after birth,and compared with the healthy control group.Results Compared with healthy control group,the blood GAS and MTL levels of neonatal ICH group increased dramatically(Pa

Objective To explore the prognostic value of albumin/globulin(AGR)in patients with stage Ⅲ-Ⅳ non-small cell lung cancer(NSCLC)treated with first-line chemotherapy.Methods From January 2016 to December 2020,288 patients with ad-vanced NSCLC initially diagnosed in the Affiliated Hospital of Xuzhou Medical University were selected.AGR critical value was deter-mined by receiver operating characteristic(ROC)curve,patients were divided into high AGR group(n=104)and low AGR group(n=184).Survival curve was plotted using Kaplan-Meier method,overall survival(OS)and progression-free survival(PFS)were com-pared between the two groups.COX proportional risk regression model was used to analyze the factors affecting prognosis of NSCLC pa-tients.Results The critical value of AGR was 1.5,the area under the curve of AGR was 0.693,the sensitivity was 76.8％,and the specificity was 58.3％.AGR was correlated with age,pathological type and curative effect(P＜0.05).The high AGR group had longer PFS and OS than the low AGR group(9 months vs 5months,25months vs 19months).Multivariate COX regression analysis showed that low level of AGR was an independent risk factor for NSCLC patients(P＜0.05).Conclusion AGR can be used as an effective prognos-tic indicator for patients with stage Ⅲ-Ⅳ NSCLC treated with first-line chemotherapy,and low levels of AGR suggest poor prognosis.

AIMTo prepare nifedipine (NP) rapid release mini-tablet, sustained release mini-tablets, pulsed release mini-tablets and delayed-onset sustained release mini-tablets and develop multiplied pulsed drug delivery system (DDS), site-specific DDS, zero-order DDS and quick/slow DDS by various ways.

METHODSVelocity-time (v-t) equation of each mini-tablet was deduced by non-linear least square model fit. The difference of combinations in v-t profiles between theoretical value and test value was compared.

RESULTSAccording to the v-t equations, the combined release behaviors were observed directly from v-t profiles and the test values coincided with the theoretical profiles.

CONCLUSIONThe programmed DDS, which consist of a variety of mini-tablets with different dosages and combinations in capsules, could be predicted by summing up the v-t equation of each tablet.

Capsules ; Delayed-Action Preparations ; Drug Delivery Systems ; Models, Chemical ; Nifedipine ; administration & dosage ; chemistry ; Polyethylene Glycols ; administration & dosage ; chemistry ; Povidone ; administration & dosage ; analogs & derivatives ; chemistry ; Solubility ; Starch ; chemistry ; Tablets

OBJECTIVETo study the effects of hermap gene on kinases in erythroid signal transduction pathway and investigate the mechanism of hermap on erythroid differentiation.

METHODSThe K562 cells expressing hermap and hermap-siRNA respectively were established for up- and down-regulating the expression of hermap gene. These K562 cells were then induced by Ara-C to erythroid differentiation and analyzed at 0, 24, 48, 72 and 96 h, respectively, for cell morphology and biphenylamine staining positive cells, determination of CD235a, CD36, kinases p-STAT5, p-Akt, p-MAPK and p-c-JUN by FCM; and quantification of hermap gene and γ (Aγ,Gγ) globin gene by FQ-PCR.

RESULTSWith up-regulating hermap gene and inducing by Ara-C, K562 cells were changing to low ratio of nucleus to cytoplasm, cytoplasm colour from basophilic to pinkish or amethyst tinge, increase of number of biphenylamine positive cells and expression of CD235a, CD36, γ (Aγ,Gγ) globin gene, hermap gene and p-STAT5 from 0 to 96 h. At 0, 24, 48, 72 and 96 h of culture, the positive rates of p-STAT5 cells were detected of 0.46%, 4.54%, 20.01%, 23.65% and 33.08%, respectively. This results demonstrated that there was a positive correlation between expression of p-STAT5 and hermap gene expression (P < 0.05).

CONCLUSIONhermap gene can stimulate erythroid differentiation of Ara-C induced K562 cells mainly through JAK/STAT5 signal transduction pathway.

Cell Differentiation ; Erythrocyte Membrane ; Erythrocytes ; cytology ; Erythropoiesis ; Gene Expression ; Humans ; K562 Cells ; Receptors, Erythropoietin ; genetics ; STAT5 Transcription Factor ; metabolism ; Signal Transduction

Objective To analyze and estimate the possibility of early control in Shanghai if COVID-19 had begun in Shanghai. Methods Comparison was made in the processes of early control between H7N9 avian influenza in Shanghai in 2013 and COVID-19 in Wuhan in 2019.The early incidence data of Korean COVID-19 was simulated and analyzed to predict whether the medical resources needed in Shanghai were available. Results If it had occurred in Shanghai, it would have taken 22 days from the first case to the government′s emergency response.It was estimated that there would have been 602-763 patients with cumulative onset and onset after incubation period.At least 500 beds of infectious diseases could have been allocated in Shanghai in case of emergency.Through adding beds and resources reallocation in the whole city, patients could have been fully admitted and treated. Conclusion If COVID-19 epidemic had occurred in Shanghai, it′s early control would have been possible though there might have difficulties.

PURPOSE: To report the 5-year follow-up results of a randomized controlled trial comparing bipolar transurethral resection of the prostate (TURP) with standard monopolar TURP for the treatment of benign prostatic obstruction (BPO). MATERIALS AND METHODS: A total of 220 patients were randomized to bipolar plasmakinetic TURP (PK-TURP) or monopolar TURP (M-TURP). Catheterization time was the primary endpoint of this study. Secondary outcomes included operation time, hospital stay, as well as decline in postoperative serum sodium and hemoglobin levels. All patients were assessed preoperatively and followed-up at 1, 6, 12, 24, 36, 48, and 60 months postoperatively. Parameters assessed included quality of life, transrectal ultrasound, serum prostate-specific antigen level, postvoid residual urine volume, maximum urinary flow rates (Qmax), and International Prostate Symptom Score. Patient baseline characteristics, perioperative data including complications, and postoperative outcomes were compared. Complication occurrence was graded according to the modified Clavien classification system. RESULTS: PK-TURP was significantly superior to M-TURP in terms of operation time, intraoperative irrigation volume, resected tissue weight, decreases in hemoglobin and sodium, postoperative irrigation volume and time, catheterization time, and hospital stay. At 5 years postoperatively, efficacy was comparable between arms. No differences were detected in safety outcomes except that the clot retention rate was significantly greater after M-TURP. CONCLUSION: Our results indicate that PK-TURP is equally as effective in the treatment of BPO, but has a more favorable safety profile in comparison to M-TURP. The clinical efficacy of PK-TURP is long-lasting and comparable with M-TURP.
Aged ; Aged, 80 and over ; Humans ; Male ; Middle Aged ; Prostate/*surgery ; Transurethral Resection of Prostate/adverse effects/*methods ; Treatment Outcome