1.Dose-dependent pharmacokinetic study of genistein in Beagle dogs.
Si-Yuan ZHOU ; Qi-Bing MEI ; Ru-Tao WANG ; Qing-Wei WANG ; Zhi-Fu YANG ; Si-Wang WANG
Acta Pharmaceutica Sinica 2005;40(6):553-556
AIMTo study the pharmacokinetics of genistein at different doses in Beagle dogs.
METHODSSuspended in 0.5% CMC-Na solution, genistein was orally administered to Beagle dogs at doses of 2.67, 5.34 and 10.68 mg.kg(-1). At various time intervals, 1.5 mL of blood was drawn from the femoral vein of dogs in their front legs. The plasma was treated with beta-glucuronidase. The genistein in plasma was extracted twice by vortexing with 2.0 mL mixture of methyl tert-tubtyl ether and pentane (v/v = 8:2). The organic phase was removed into the tubes and then evaporated in ventilation cabinet. The residue was dissolved in 50 microL of methanol. 20 microL solution was drawn and detected by high-performance liquid chromatography. The pharmacokinetic parameters were calculated by 3P97 software.
RESULTSThe plasma drug concentration-time data were fitted to the two-compartment model. When the dose was 2.67 mg.kg(-1), the MRT and AUC of parent compound were 52.9 min and 6.7 mg.min. L(-1), respectively. When the dose rose to 5.34 mg.kg(-1), the MRT and AUC of parent compound became 224.8 min and 26.1 mg.min.L(-1), respectively. However, when the dose increased to 10.68 mg .kg(-1), the MRT and AUC of parent compound increased to 267.7 min and 33.2 mg.min L(-1), respectively. The AUC of glucuronidated genistein was 33.9, 70.1 and 140.5 mg.min.L(-1) at the dose of 2.67, 5.34 and 10.68 mg.kg(-1), respectively.
CONCLUSIONDue to significant first pass metabolism, the drug was mainly existed in the form of glucuronidated genistein in the plasma. With the increase of dose, the absorption of genistein became saturated and the half life prolonged.
Animals ; Anticarcinogenic Agents ; administration & dosage ; blood ; pharmacokinetics ; Area Under Curve ; Dogs ; Dose-Response Relationship, Drug ; Female ; Genistein ; administration & dosage ; blood ; pharmacokinetics ; Glucuronides ; blood ; pharmacokinetics ; Male
2.Autopsy study for maxillary nerve and its artery supply
Yuan-Xin ZHANG ; Kui-Qi ZHANG ; Si-Jia QIN ; Fu WANG
Chinese Journal of Otorhinolaryngology Head and Neck Surgery 2012;47(10):836-840
Objective To observe the travel,divisions,and the lengths,diameters,branches,artery supplies of the main segments of maxillary nerve.Methods Fifty formalin-preserved adult half-head specimens with intravascular injection of red color emulsion were used for the gross and microanatomical studies of maxillary nerve.The lengths,diameters,branches and artery supplies of four main segments of maxillary nerve were observed.SPSS 11.5 software was used to analyze the data.Results The length and diameter of cranial middle fossa segment of maxillary nerve were ( 10.70 ± 1.31 ) mm and (4.01 ± 0.52 )mm respectively,which was supplied by inferior-lateral cavernous sinus artery.The length and diameter of pterygopalatine fossa segment were (16.21 ± 1.80) mm and (3.27 ±0.62) mm respectively,in which one zygomatic branch, one to three posterior superior alveolar nerves, two ganglion branches and tuberal descending branches; were given off,and the segment was supplied by foramen rotundum artery.The length and diameter of infraorbital segment were ( 25.73 ± 2.03 ) mm and ( 3.30 ± 0.52 ) mm and it gave off middle superior alveolar nerve (64%) and anterior superior alveolar nerve and was supplied by infraorbital artery.Facial segment gave off superior labial branches,internal and external nasal branches,inferior palpebral branches,buccal branch and zygomatic branch and these branches were supplied by infraorbital artery and superior labial and angular artery originating from facial artery.Conclusions Understanding of travel and artery supply of maxillary nerve is helpful to regional anaesthesia and surgery for maxillary nerve.Foramen rotundum,sphenopalatine foramen and infraorbital nerve are important marks for endoscopic surgery in pterygopalatine fossa.
3.Application of percutaneous needle aspiration biopsy by the simulator guided to the diagnosis for pulmonary focus in coal miners' pneumoconiosis.
Si-hai LIU ; Cheng-dong QI ; Wen-shou XU ; Rui-xia ZHU ; Qin YAN ; Wen FENG ; Rong-xia SUN ; Yan-fang ZHANG ; Xiao-fu WU ; Zheng-chuan FU
Chinese Journal of Industrial Hygiene and Occupational Diseases 2004;22(1):72-73
Aged
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Biopsy, Needle
;
methods
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Coal Mining
;
Humans
;
Lung
;
pathology
;
Lung Neoplasms
;
complications
;
diagnosis
;
Middle Aged
;
Pneumoconiosis
;
complications
4.Metabolic kinetics of MN9202 in Beagle dog liver microsomes.
Zhi-fu YANG ; Si-yuan ZHOU ; Qi-bing MEI ; Tie-hong YANG ; Zhen-guo LIU
Acta Pharmaceutica Sinica 2005;40(11):1019-1023
AIMTo study the metabolic kinetics of MN9202 in Beagle dog liver microsome.
METHODSBeagle dog liver microsomes were prepared by using ultracentrifuge method. After incubating 0.4 micromol x L(-1) MN9202 with 1 g x L(-1) microsomes for 30 min at 37 degrees C, the reaction was terminated by adding 0.5 mL alkalization. The RP-HPLC was used to determine the drug in the incubation mixture. The Michaelis-Menten parameters Km, and Vmax in Beagle dog liver microsomes were initially estimated by analyzing Lineweave-Brurk plot. Various selective CYP inhibitors were used to investigate their inhibitory effect on the metabolism of MN9202.
RESULTSThe Km, Vmax and CLint of MN9202 were (22.6 +/- 8.0) micromol x L(-1), (0.54 +/- 0.17) micromol x g(-1) x min(-1) and (0.0242 +/- 0.0009) L x g(-1) x min(-1), respectively. The metabolism of MN9202 was significantly inhibited by ketoconazole (Ket) and troleandomycin (Tro) in Beagle dog liver microsomes. Tranylcypromine (Tra) could inhibit the metabolism of drug as well. While other inhibitors showed little inhibitory effect on the metabolism of MN9202.
CONCLUSIONIt was shown that CYP3A and CYP2C19 were involved in MN9202 metabolism. The inhibitors of human CYP3A and CYP2C19 may have potential interaction with MN9202, and this can reduce the metabolism rate and increase the toxicity of MN9202.
Animals ; Aryl Hydrocarbon Hydroxylases ; antagonists & inhibitors ; Calcium Channel Blockers ; metabolism ; pharmacokinetics ; Cytochrome P-450 CYP2C19 ; Cytochrome P-450 CYP3A Inhibitors ; Dihydropyridines ; metabolism ; pharmacokinetics ; Dogs ; Ketoconazole ; pharmacology ; Microsomes, Liver ; metabolism ; Mixed Function Oxygenases ; antagonists & inhibitors ; Nitrobenzenes ; metabolism ; pharmacokinetics ; Tranylcypromine ; pharmacology ; Troleandomycin ; pharmacology
5.Establishment of a human CD30+ anaplastic large cell lymphoma cell line and its biological characteristics.
Hua JIANG ; Jian HOU ; Wei-Jun FU ; Si-Qi DING ; Bo ZHANG
Journal of Experimental Hematology 2003;11(5):490-494
A CD30+ anaplastic large cell lymphoma (ALCL) cell line was established from the mononuclear cells isolated from pleural effusion of a patient with non-Hodgkin's lymphoma. The cell line's biological characteristics were analyzed. The results showed that the established cell line could survive and proliferate in RPIM 1640 medium; the Wright-Giemsa-stained cells were exactly similar to malignant cells of CD30+ ALCL in morphology, with many diffuse virus granules in cytoplasm; the cytochemical staining of the cells showed the following reactivity pattern: positive for acid phosphatase (ACP) and periodic acid-Schiff (PAS), negative for peroxidase (POX), myeloperoxidase (MPO) and platelet peroxidase (PPO). The immunoprofile of the cells was positive for CD45, HLA-DR, CD30 and negative for EMA, CD34, CD38, CD2, CD3, CD4, CD7, CD8, CD10, CD15, CD19 and CD20. The cytogenetic analysis showed complicate d qualitative and quantitative abnormality of chromosomes, without typical t(2;5). It is concluded that the established cell line is CD30+ anaplastic large cell lymphoma cell line.
Apoptosis
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Cell Line, Tumor
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Female
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Herpesvirus 4, Human
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isolation & purification
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Humans
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Immunophenotyping
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Karyotyping
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Ki-1 Antigen
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analysis
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Lymphoma, Large B-Cell, Diffuse
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genetics
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immunology
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pathology
;
Middle Aged
6.Pharmacokinetics of m-nifedipine in Beagle dogs.
Zhi-fu YANG ; Si-yuan ZHOU ; Tie-hong YANG ; Qi-bing MEI
Acta Pharmaceutica Sinica 2004;39(8):609-612
AIMTo study the pharmacokinetics of m-nifedipine (m-Nif) in Beagle dogs.
METHODSThe Beagle dogs were divided into two groups. m-Nif was intravenously administered to the Beagle dogs in group 1 at the dose of 0. 288 mg x kg(-1), and it was orally administered to the Beagle dogs in group 2, 3 and 4 at the dose of 1.152, 3.456 and 10.370 mg x kg(-1), respectively. m-Nif in plasma was detected by reversed phase high performance liquid chromatography. The pharmacokinetic parameters were calculated by 3P97 software.
RESULTSWhen m-Nif was intravenously administered, the plasma concentration-time curve was fit to a two-compartment model and T1/2beta was 117 min. When m-Nif was orally administered, the plasma concentration-time curve was fit to a one-compartment model. T1/2 (Ke) and Cmax were 147 min and 20 microg x L(-1); at the low dose of 1.152 mg x kg(-1). T1/2 (Ke) was 122 min and Cmax was 36 microg x L(-1) at the middle dose of 3.456 mg x kg(-1). T1/2 (Ke) was 144 min and Cmax was 69 microg x L(-1) at the high dose of 10.37 mg x kg(-1), respectively.
CONCLUSIONIt was showed that the speed of elimination of m-Nif was high in Beagle dogs. The absolute bioavailability of m-Nif given orally was very low.
Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Calcium Channel Blockers ; administration & dosage ; pharmacokinetics ; Dogs ; Injections, Intravenous ; Isomerism ; Nifedipine ; administration & dosage ; pharmacokinetics
7.Allogeneic leukocyte immunization combined with IVF-ET for treatment of infertility induced by recurrent spontaneous abortion.
Ling-hong KONG ; Zhong LIU ; Hong LI ; Si-mei CHEN ; Fu-qi XING
Journal of Southern Medical University 2008;28(7):1300-1301
OBJECTIVETo investigate the effect of allogeneic leukocyte immunization combined with in vitro fertilization-embryo transfer (IVF-ET) for treatment of infertility induced by habitual abortion.
METHODSAllogeneic leukocyte immunization was performed in 9 patients with infertility induced by habitual abortion, with another 9 patients undergoing IVF-ET without habitual abortion as the control group. All the patients were treated with long GnRH-a protocols. The infertility patients with recurrent spontaneous abortion history were immunized with lymphocytes from the husband for before IVF-ET and after clinical pregnancy.
RESULTSThe fertilization rates of the immunotherapy group and control group were 81.3% and 82.2%, respectively, showing no significant difference (P>0.05). Five patients in each group had clinical pregnancy, and a twin pregnancy occurred in the control group. The embryo implantation rates were also comparable between the two groups (22.7% vs 28.6%, P>0.05). All the fetuses resulted from IVF-ET developed normally and were healthily delivered.
CONCLUSIONAllogeneic leukocyte immunotherapy along with IVF-ET is effective for treatment of infertility resulting from recurrent spontaneous abortion.
Abortion, Habitual ; physiopathology ; Adoptive Transfer ; methods ; Adult ; Embryo Transfer ; Female ; Fertilization in Vitro ; methods ; Humans ; Infertility, Female ; physiopathology ; therapy ; Pregnancy ; Pregnancy Outcome ; Treatment Outcome
9.Effects of beta-asarone on expression of c-fos in kindling epilepsy rat brain.
Yong-Qi FANG ; Ruo-Ming FANG ; Geng-Li FANG ; Yong JIANG ; Si-Ying FU
China Journal of Chinese Materia Medica 2008;33(5):534-536
OBJECTIVETo study the effects of beta-asarone on expression of immediately early gene c-fos in kindling epilepsy rat brain.
METHODThe rats were randomly divided in to beta-asarone groups (200, 100, 50 mg x kg(-1) x d(-1)), difetoin control group (36 mg x kg(-1)) and model group. The remedy was administered orally. The effects were observed in kindling epilepsy model induced by penicillin, then the expression of c-fos were determined by western blot (hippocampus) and immunohistochemical techniques (cortex).
RESULTBeta-asarone could significantly increase the expression of c-fos in kindling epilepsy rat brain, and show its quantity-effect relation. The expression of c-fos in hippocampus was (1139.45 +/- 155.56), (1109.56 +/- 134.03), (1103.73 +/- 235.82) CNT x mm2 in beta-asarone groups, 920.54 +/- 203.20 in model control group, and 1106.26 +/- 186.24 in difetoin group, respectively. The number of c-fos positive cell was 87.1 +/- 2.2, 76.3 +/- 1.3 and 59.9 +/- 1.3 in beta-asarone groups, 39.3 +/- 2.6 in model control group, and 95.2 +/- 1.1 in difetoin group, respectively.
CONCLUSIONBeta-asarone can obviously increase the expression of c-fos in epilepsy rat brain. It is one of important response to epilepsy.
Animals ; Anisoles ; pharmacology ; Blotting, Western ; Brain ; drug effects ; metabolism ; Epilepsy ; drug therapy ; metabolism ; Female ; Gene Expression ; drug effects ; Immunohistochemistry ; Male ; Proto-Oncogene Proteins c-fos ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley
10.Clinical trial of Qianlie Yikang capsule in the treatment of patients with nonspecific prostatitis
Guang-Yuan HE ; Jian-Qi ZHAO ; Si-Xi ZHANG ; Ying-Shi SONG ; Fu-Biao LI
The Chinese Journal of Clinical Pharmacology 2017;33(13):1198-1200
Objective To evaluate the clinical effect of Qianlie Yikang capsules on the levels of prostaglandin E2 (PGE2) and interleukin-8 (IL-8) in serum and prostatic fluid in patients with nonspecific prostatitis.Methods Eighty patients with nonspecific prostatitis were randomly divided into control group and treatment group,40 cases in each group.Control group was orally given Pule'an tablets 2.0 g,3 times a day.Treatment group was treated with Qianlie Yikang capsules 1.5 g,3 times a day,orally.Before and after treatment,the levels of serum and prostatic fluid PGE2,IL-8 and clinical efficiency in two groups were compared.Results The clinical efficiency of treatment group was 92.50% (37/40 cases),had significant difference with that in control group,which was 75.00% (30/40 cases,P < 0.05).After treatment,the serum PGE2 of treatment group and control group were (159.76 ± 16.34),(190.65 ± 17.56) ng · L-1,IL-8 were (2.28 ± 0.32),(3.08 ± 0.22) ng· L-1,with significant difference (P < 0.05).After treatment,the prostatic fluid PGE2 of treatment group and control group were (227.46 ±20.84),(309.46 ± 19.39) ng·L-1,IL-8 were (3.12±0.43),(4.77 ± 0.67) ng · L-1,with significant difference (P <0.05).There was no significant adverse reactions in two groups.Conclusion The Qianlie Yikang capsules can significantly reduce the serum and prostatic fluid PGE2,IL-8 levels in patients with nonspecific prostatitis,and have good clinical effect.