1.Cytochrome P450 and genetic polymorphism
Chinese Pharmacological Bulletin 2001;17(1):21-25
Cytochrome P450 enzyme are an important enzyme family in drug metabolism. Human cytochrome P450 enzymes have been studied entensively about their polymorphism in recent years. polymorphism of CYP2C19 and CYP2D6 have been detected at both phenotypic and genotypic level, and their molecular mechanism have been studied entensively, however, the molecular mechanism of other enzymes for exzample CYP2C9,CYP1A1,CYP2E1 et al) is being discussed, though these enzymes possiblely exist polymorphism. The article summarizes the substrates of P450, molucular mechanism of polymorphism, and paticular reference to the effects of this variation on drug metabolism and susceptibility to chemically-induced diseases.
2.Application of nickel titanium compression anastomosis clip in gastrointestinal anastomosis
Liangqing LI ; Muhai FU ; Dun PAN
Chinese Journal of Digestive Surgery 2013;(7):504-507
Objective To investigate the efficacy and safety of nickel titanium compression anastomosis clip (CAC) in gastrointestinal anastomosis.Methods The clinical data of 413 patients who received gastrointestinal anastomosis with nickel titanium CAC or curved stapler at the First Affiliated Hospital of Fujian Medical University from January 2007 to December 2011 were retrospectively analyzed.All the patients were divided into the CAC group (227 patients) and the curved stapler group (186 patients).The time for gastrointestinal anastomosis,anastomotic bleeding,complications,condition of the incision sites,the first postoperative flatus and time for the excretion of the CAC between the 2 groups were compared.All data were analyzed using the t test or chisquare test.Results The time for gastrointestinal anastomosis of the CAC group was (8.3 ± 2.5) minutes,which was significantly shorter than (18.7 ± 3.6) minutes of the curved stapler group (t =5.74,P < 0.05).There were no significant difference in the time of postoperative flatus,duration of hospital stay and costs between the 2 groups (t =0.27,1.32,3.11,P > 0.05).No patients in the CAC group had anastomotic bleeding,while the incidence of anastomotic bleeding of the curved stapler group was 3.23 % (6/186),with a significant difference between the 2 groups (x2=7.43,P < 0.05).The incidences of gastric emptying dysfunction of the CAC group and the curved stapler group were 0.88% (2/227) and 1.08% (2/186),with no significant difference between the 2 groups (x2=0.04,P > 0.05).The incidences of postoperative anastomotic stricture and anastomositis were 0 (0/227) and 11.01% (25/227) in the CAC group,and 2.15% (4/186) and 21.50% (40/186) in the curved stapler group,with significant differences between the 2 groups (x2 =4.93,8.49,P < 0.05).No anastomotic fistula was detected in the 2 groups.The CAC was excreted at postoperative day 12-26.Conclusion CAC is safe and effective for gastrointestinal anastomosis.
3.Pharmacokinetic study of bifonazole in human
Liangqing FU ; Dezheng WU ; Chuanhuan LUO ; Rong SHU
Chinese Pharmaceutical Journal 2001;(1):43-45
OBJECTIVE To study the pharmacokinetics of bifonazole in healthy human,in order to evaluate the safety of bifonazole.METHODS 8 healthy volunteers were given single dose of 300 mg bifonazole solution and cream preparation respectively in a cross-over design.Blood samples were collected at the designed time,and the concentrations of bifonazole in plasma were determined by means of GC-MS(SIM) quantitative method.The pharmacokinetic parameters were calculated with the 3P87 software.RESULTS The plasma concentration-time curves of the two preparations were fitted to two-compartment open model.The tmax of the solution and cream preparations were 2.91 h and 5.62 h,cmax 713.46 ng.mL-1 and 410.70 ng*mL-1,respectively.The cream preparations absorption,distribution and clearance was a little slower than that of the solution preparation.However,no significant difference in their AUC.CONCLUSION Bifonazole is a safe drug,and clinical use of the solution and cream preparation in turn is suggested to improve its therapeutic efficacy.
4.The plasma concentration of omeprazole and metabolites 5′-hydroxy omeprazole, omeprazole sulphone are determinated by HPLC
Liangqing FU ; Feng HUANG ; Dezheng WU ; Junhua GUO ;
Chinese Pharmacological Bulletin 1987;0(03):-
AIM To set up a method which can determining the blood concentration of omeprazole and its metabolite 5′ omeprazole, omerpazole sulphone in order to study its cinical pharmacokinetics. METHODS The blood concentration of omerpazole was determinated by HPLC. RESULTS Calibrated standard curve of omeprazole in blood is Y=-0 004 499+0 001 909X (r =0 9990), the recoveries of three concentrations 50, 500, 2 000 mg?L -1 are 90 36, 109 62, 108 91%, respectively; and the precisions are 9 86,7 86, 15 52% , respectively. Calibrated standard curve of its metabolite 5′ OH omeprazole in plasma is Y=-0 003 659+0 001 328X(r =0 9970), the recoveries of three concentrations 20, 200, 1 000 mg?L -1 are 79 42%, 96 49%, 95 04%, respectively; and the precisions are 8 95%, 4 52%, 9 73%, respectively. Calibrated standard curve of its another metabolite omeprazole sulphone in plasma is Y=0 009 248+0 001 765X (r =0 999 2), the recoveries of three concentrations 20, 200, 1 000 mg?L -1 are 94 44%, 105 59%, 104 26%, respectively; and the precisions are 8 72, 8 58, 9 60%, respectively. After 20 mg omeprazole were administered by a voluteer via oral, C max of 5′ OH omeprazole, omeprazole, and omerpazole sulphone were 14 622 7, 408 433 2, 454 363 7 mg?L -1 . CONCLUSION The method is good enough to study pharmacokinetics of omeprazole.
5.Comparison of genotype polymorphism of cytochrome CYP2C19 between Chinese Han subjects and Chinese Meng subjects
Liangqing FU ; Feng HUANG ; Dezheng WU ; Junhua GUO ;
Chinese Journal of Clinical Pharmacology and Therapeutics 2002;0(05):-
AIM: To compare genotype polymorphism of cytochrome CYP2C19 between Chinese Meng subjects and Chinese Han subjects. METHODS: The genotype polymorphism was analyzed by PCR RFLP (Restriction Fragment Length Polymorphism) in 74 subjects of healthy Chinese Han and 6 subjects of Chinese Meng. RESULTS: Of the 74 genotyped healthy subjects, 31 ( 41.9 %) were homozygous for wildtype (wt/wt), 9 ( 12.2 %) were homozygous for CYP2C19m1 and CYP2C19m2 (m1/m1 or m1/m2 or m2/m2), and 34 ( 45.9 %) were heterozygous for CYP2C19m1 or CYP2C19m2 (m1/wt or m2/wt). Among the 6 genotyped Chinese Meng, 1 ( 16.7 %) was homozygous for wildtype (wt/wt), 2 ( 33.3 %) were homozygous for mutant allele CYP2C19m1 and CYP2C19m2 (m1/m1 or m1/m2 or m2/m2), and 3( 50.0 %) were heterozygous for CYP2C19m1 or CYP2C19m2 (m1/wt or m2/wt); no homozygous genotype for CYP2C19m2(m2/m2)was found in this study. CONCLUSION: There is no statistical difference in occurrence of wt/wt and m1/m1 between in 74 subjects of healthy Chinese Han and 6 subjects of Chinese Meng.
6.Bioequivalence of Metoprolol Tartrate Tablets in healthy volunteers
Jing WANG ; Liangqing FU ; Yongbiao GUAN ; Yi FANG ; Zeyuan LIU
Chinese Journal of Clinical Pharmacology and Therapeutics 2004;0(09):-
AIM: To study the bioequivalence of domestic and imported Metoprolol Tartrate Tablets in Chinese healthy volunteers.METHODS: According to the rule published by SFDA,the serum concentration of 20 selected volunteers among 18 to 40 years old was determined by HPLC-fluorescence detection after giving domestic and imported Metoprolol Tartrate Tablets 0.1g,and the pharmacokinetic parameters were calculated by DAS software.RESULTS: The method of HPLC-fluorescence detection to study the pharmakokinetics of Metoprolol Tartrate was sensitive,reliable,accurate and reasonable.The main pharmakokinetics parameters of domestic and imported Metoprolol Tartrate Tablets were T_(max):(1.11)?(0.36 h) and(1.39)?(0.65 h) respectively;C_(max):(269.20)?(87.15)(?g?L~(-1)) and(262.03)?(75.52)(?g?L~(-1)) respectively;AUC_(0-12h):(1088.91)?(510.52)(?g?L~(-1)?h) and(1098.29)?5(55.14)(?g?L~(-1)?h) respectively.The relative bioavailability of domestic Metoprolol Tartrate Tablets was(100.09)%.CONCLUSION: The domestic and imported Metoprolol Tartrate Tablets was bioequivalents.
7.Comparison of clinical efficacy between robotic and laparoscopic low anterior resection for rectal cancer:a Meta analysis
Junye LIU ; Ping FU ; Huazhang HONG ; Xihong YUAN ; Jian LI ; Liangqing LIN ; Kai ZHOU
Chongqing Medicine 2017;46(29):4088-4092
Objective To compare the clinical efficacy of robotic low anterior resection (R-LAR) and laparoscopic low anterior resection(L-LAR) for rectal cancer.Methods The case-control studies for comparing the clinical efficacy of R-LAR and LLAR for rectal cancer were retrieved from databases,including PubMed,OVID,Springer,Wanfang and VIP,till June 2016.The studies were selected in accordance with inclusion and exclusion critera,and the data were extracted and evaluated by two researchers.The RevManS.3 software was used for Meta-analysis.Results A total of 7 studies including 1 126 patients with rectal cancer were included,592 cases in the R-LAR group and 534 cases in the L-LAR group.Compared with the L-LAR group,in the R-LAR group the operation time was longer (MD=33.84,95% CI:4.25-63.43,P =0.03),the conversion rate was lower (OR =0.10,95%CI:0.03-0.36,P=0.000 5),and more lymph nodes were dissected (MD=1.24,95%CI:0.31-2.17,P=0.009).No statistically significant difference was found in length of hospital stay,intraoperative blood loss,distance from distal margin to tumor and incidence rate of postoperative anastomotic leakage between the two groups (P > 0.05).Conclusion Compared with L-LAR,RLAR is characterized by longer operation time,lower conversion rate and more thoroughly removing lymph nodes.And the length of hospital stay,intraoperative blood loss,distance from distal margin to tumor and incidence rate of postoperative anastomotic leakage of R-LAR are similar to those of L-LAR.