1.EFFECT OF MICROENVIRENMENT ON LIPASE-CATALYZED ENANTIOSELECTIVE ESTERIFICATION OF KETOPROFEN
Wei DU ; Minhua ZONG ; Rong YANG ; Qiong LI ; Yong GUO
Microbiology 1992;0(05):-
The effect of reaction media cosolvent water activity, temperature and pH on Novozym 435-caulyzed enantioselective esterification of ketoprofen was systematically explored. Novozym 435 showed high catalytic activity and enantioselectivity in cyclohexane; E value increases markedly by addition of toluene to cyclohexane; the optimum temperature and the initial water activity were found to be 30℃ and 0.09 respectively; pH shows little effect on enzymatic reaction wilson the scope studied.
2.Determination of pirfenidone and its majormetabolite in human plasma by LC-MS/MS analysis
Changyin LI ; Huiting SONG ; Yang ZONG ; Jun ZHANG ; Wenzheng JU
Chinese Pharmacological Bulletin 2017;33(5):696-703
Aim To establish a LC-MS/MS method for the determination of pirfenidone(BT)and its major metabolite 5-carboxy-pirfenidone(SBT)in human plasma.Methods Human plasma samples containing BT and SBT,as well as their corresponding deuterium-labeled internal standards pirfenidone-d5(dBT)and 5-carboxy-pirfenidone-d5(dSBT),were precipitated using methanol.Chromatographic separation was carried out on an Agilent ZORBAX SB C18(3.0 mm×100 mm,3.5 μm)column with the mobile phase of water(0.5%formic acid)and acetonitrile(50/50).The detection of analytes was performed on a tandem mass system equipped with an electrospray ionization source in positive ion mode using multiple-reaction monitoring.The MS/MS ion transitions monitored were m/z 185.958→77.1 for BT,m/z 215.944→77.0 for SBT,m/z 190.965→81.1 for dBT and m/z 220.948→99.1 for dSBT.Results There was no remarkable interference in blank solvent,plasma,and there was no mutual interference between analytes or internal standards.The proposed method showed good linearity over the concentration range of 0.020 59~25.14 mg·L-1 for BT and 0.016 73~20.42 mg·L-1 for SBT.The intra-batch and inter-batch precision and accuracy were proved to be acceptable.Human samples kept stable after 4 h at room temperature,the three freeze-thaw cycles and 10,29 and 52 days at-70 ℃,and the processed samples remained stable after 24 h in the autosampler.The average extraction recovery and matrix effect were precise,reproducible and acceptable.Conclusion Our current LC-MS/MS method is proved to be sensitive,accurate and convenient,and could be suitable for the clinical pharmacokinetic studies of BT-related preparations.
3.Discussion on Medical Costs Control in China from the Perspective of the Relationship among Doctors, Hospitals and Health Insurance Institutions in the United States
Maomao ZONG ; Xiaomin YOU ; Rui ZHAO ; Li YUAN ; Yue YANG
China Pharmacy 2016;27(16):2172-2176
OBJECTIVE:To provide reference for medical costs control in China. METHODS:Based on main characteristics of the United States health service system,information asymmetry,principal-agent theory and Freedman’s consumption theory were used to analyze the advantages of restrictive relationship among doctors,hospitals and health insurance institutions in control-ling medical costs and improving the quality of diagnosis and treatment. The growth rate of medical cost,the percentage of drug ex-penditure and other aspects were compared between China and the United States;the effect of restrictive relationship on medical cost control was demonstrated. RESULTS & CONCLUSIONS:In the United States,there are hierarchical medical system and two-way referral system;for-profit hospitals and non-profit hospitals are mutually complementary;different natures of health insur-ance system,different payment methods and strict“commercial bribe”monitoring system are carried out;doctors,hospitals and health insurance restrict each other. Not only there are many advantages in theory,but also in practice the growth rate of medical cost and the percentage of drug expenditure are superior to our country. Finally it controls the rapid growth of medical cost to a cer-tain extent. Combined with our national conditions,learning from the United States experience,restrictive relationship among doc-tors,hospitals and health insurance institutions is established to control the increase of medical cost in China through reducing infor-mation asymmetry and standardizing payment audit;establishing a scientific pattern of mixed payment;strengthening the indirect impact of the health insurance institutions on doctors and hospitals,etc.
4.Study of lumbar spinal stability after laminectomy in the treatment of lumbar intraspinal tumors
Taihang GAO ; Shaohui ZONG ; Bing LI ; Ran ZHANG ; Shuzhen LI ; Yuan YANG ; Kun YANG
Journal of Medical Postgraduates 2014;(9):949-951
Objective Laminectomy is destructive to bone structure in spine , which affect spinal stability .This article was to investigate the effect on spinal stability after laminectomy in different segments of vertebral plate in the treatment of lumbar intraspinal tumors. Methods Retrospective analysis were made on the data of 143 patients with lumbar intraspinal tumors from January 2009 to June 2012 in 6 hospitals.All the patients underwent laminectomy with no use of inner regular apparatus during the operation .JOA evalu-ation was applied to observe short-term efficacy , while ASIA scale for long-term efficacy .Comparison was made on lumbar spinal stability before operation and in the last visiting . Results From the observation of short-term efficacy, JOA evaluation score rised from (1.12 ± 0.65)to (1.97 ±0.71).Form the observation of long-term efficacy, ASIA scale classification was as follows:4 cases of Grade I, 6 cases of Grade II, 14 cases of Grade III, 53 cases of Grade IV and 66 cases of Grade V.In the following 12-30 months′visiting, all patients were covered.In the last postoperative visiting, patients suffering spinal instability after laminectomy were as follows:2 of 45(one seg-ment), 9 of 47(two segments), 5 of 27 (three segments) and 2 of 14 (four segments).From the observation on the postoperative spinal sta-bility and the segments in laminectomy , spinal stability of one-segment group was significantly higher than that of multi-segment group ( P=0.047).No significant difference exist between the groups of less than 2 segments and more than 3 segments as well as the groups of less than 3 segments and more than 4 segments. Conclusion A single seg-ment laminectomy on lumbar intraspinal tumors showed good postopera-tive spinal stability .But laminectomy in two or more segments implied greater risk of postoperative spinal instability .
6.The report of success sequential therapy for ectopic pregnancy with fetal cardiac activity
Lin ZONG ; Jun MENG ; Jing-Yi YANG ; Xiao-Yun DAI ; Li-Li SHAN ; Yi YU ;
Chinese Journal of Primary Medicine and Pharmacy 2006;0(08):-
Objective To investigate the effects and safety of sequential treatments with methotrexate and mifepristone for ectopic pregnancy with fetal cardiac activity.Methods 4 cases of ectopic pregnancy with fetal car- diac activity in our hospital were given by sequential therapy with methotrexate and mifepristone.Serum?-HCG,liv- er function and renal function,blood routine and gastrointestinal response were observed.Results 4 cases of ectopic pregnancy with fetal cardiac activity with 1~4 periods of sequential treatments were cured.Except light gastroin- testinal response,and one had slight rise of serum ALT level and AST level,no one had rnyelosuppression and heavy hepatic injury.Conclusion The sequential therapy with methotrexate and mifepristone is an effective and safe method for the treatment to ectopic pregnancy with fetal cardiac activity.
7.Evaluation of Clinical Detection Methods for Detection of Helicobacter Pylori Infection in Children
zong-ping, JIN ; yu-hua, LIU ; li, LI ; ai-jun, YANG
Journal of Applied Clinical Pediatrics 2006;0(19):-
Objective To explore the optimal methods to detect helicobacter pylori(Hp)antigen in children.Methods 13C labeled urea breath test(13C-UBT)was performed on 937 children of alimentary department from Sep.2000 to Feb.2006.Gastric mucosa biopsy of 96 children was detected.Hp stool antigen(HpSA)status of the 557 children were evaluated.Both 13C-UBT and HpSA were assayed in 105 children from Apr.2003 to Apr.2004.Method of 13C-UBT was taken as the golden standard on diagnosis of Hp infection.Results Forty-one point seven percent children was positive for 13C-UBT.Forty point six percent children was positive for gastric mucosa biopsy.Thirty-eight point two percent was positive for HpSA.The difference was not significant.2.Among the 105 children performed by both 13C-UBT and HpSA,41.9% was positive for 13C-UBT and 39.0% for HpSA.Taking 13C-UBT as the golden standard,sensitivity of HpSA to diagnose Hp infection was 91.8%,and its specificity was 81.8%.Consistency Kappa coefficient was 0.743(P=0),which denoted that there was no significant difference on the positive detection rate between 13C-UBT and HpSA(P=0.388).Conclusions 13C-UBT and HpSA as non-invasive technique is effective to detect the Hp antigen.Compared to 13C-UBT,as a convenient,noninvasive,economical method,HpSA detection is much more acceptable to children and their patients.
8.Chitosan nanoparticles as gene vector: effect of particle size on transfection efficiency.
Xiao-rong YANG ; Li ZONG ; Xi-ying YUAN
Acta Pharmaceutica Sinica 2007;42(7):774-779
The aim was to investigate the effect of particle size on transfection efficiency of chitosan (CS)-based nanoparticles. Nanoparticles were synthesized through complex coacervation CS with plasmid DNA (pDNA). Three kinds of pDNA/CS nanoparticles with different sizes (250, 580 and 1300 nm) were prepared by altering the adding rate and the vortexing time. The particle size, zeta potential and the stability in cultural medium were evaluated by zetasizer. The association efficiency was determined by spectrofluorophotometer. The combination of chitosan with pDNA as well as the ability to protect pDNA from nuclease degradation was analyzed by gel electrophoresis. The transfection efficiency of pDNA/CS nanoparticles in HEK293 cells was investigated by flow cytometry. Using CS grafted fluorescein isothiocyanate as a fluorescent marker, the adsorption features of the nanoparticles were visualized by fluorescence microscopy and the cellular uptake percent was quantitated by flow cytometry. The internalization process of the nanoparticles was visualized by confocal laser scanning microscopy (CLSM) using nanoparticles of the size of 250 nm. Results showed that the three kinds of pDNA/CS nanoparticles had no differences in zeta potential, association efficiency, protection ability, stability and transfection efficiency in HEK293. The nanoparticles were all adsorbed on cell surface in the form of aggregates, and similar cellular uptake percent as well as quantities were observed 4 h post-incubation with HeLa cells. CLSM images showed that the aggregates below 2 microm could be internalized by endocytosis. These results suggest that the transfection efficiency of pDNA/CS nanoparticles does not depend on particle size in the range from 250 nm to 1300 nm.
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chemistry
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Genetic Vectors
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HeLa Cells
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