AIMTo establish a RP-HPLC method for determination of diphenytriazol (DL111-IT) in rat hepatic microsomes.

METHODSDL111-IT in rat hepatic microsomal incubates was extracted with chloroform, using diazepam as internal standard. The determination was performed on a Lichrospher ODS-C18 reversed column (25 cm x 0.46 cm ID) with mobile phase of methanol-pH 7.5 phosphate buffer (70:30) at a flow-rate of 1.0 mL.min-1. A UVVIS detector was operated at 235 nm.

RESULTSThe assaywas linear from 1.01-101.0 micrograms.mL-1 for DL111-IT. The limit of detection was 0.15 microgram.mL-1 (signal-to-noise ratio 3) and the limit of quantification was 1.01 micrograms.mL-1(RSD < 10%, n = 4). The method afforded average recoveries of (100.3 +/- 1.9)% (n = 5), and intra-day and inter-day RSD were less than 5.0%(n = 5). The method allowed study of the in vitro phase I metabolism of DL111-IT in rat liver microsomal incubates. The microsomes induced by beta-naphthoflavone showed high enzymatic activity for DL111-IT phase I metabolism.

CONCLUSIONThe method is simple, accurate and can be used to study the metabolism of DL111-IT in rat hepatic microsomes.

Abortifacient Agents, Nonsteroidal ; analysis ; metabolism ; Animals ; Cell Separation ; Chromatography, High Pressure Liquid ; methods ; Female ; Microsomes, Liver ; metabolism ; Rats ; Rats, Sprague-Dawley ; Triazoles ; analysis ; metabolism

Objective To study effectiveness of System intervention to occupation burnout of medical staff.Methods Specimens were classified as interventional group and control group by 1:1 partnership rule.Systemic intervention,which came from organization,family and individual,was only applied to interventional group.The objective was to establish requirement and resource mechanism,continually increase response resource,and improve matching state of individual & job.It allowed full play to the first grade prevention(development intervention),the second grade prevention(symptom intervention)and the third grade prevention(burnout intervention).It determined effectiveness of intervention via indexes of occupation burnout,mental health and satisfaction within group or internal groups.Results Before systemic intervention,there was no significant difference between intervention group and control group(P＞0.05).After systemic intervention,the scores of burnout(emotion exhaustion(17.54±9.97)vs(14.30±11.87),P＜0.01;depersonalization(5.29±5.01)vs(4.63±5.65),P＜0.05;low personal accomplishment(6.47±4.89),(5.61±5.10),P＜0.01),check list-90(SCL-90),personal satisfaction in intervention group showed apparent difference compared with that in control group.But there was no significant difference in control group before and after intervention.Conclusion On the whole systemic intervention to health care staff obtains obvious achievement,effectively reduces emotional exhaustion,obsessive symptom and terror emotion,and enhances individual satisfaction.

Adult ; Female ; Forearm ; surgery ; Free Tissue Flaps ; Humans ; Male ; Middle Aged ; Oral Surgical Procedures ; methods ; Reconstructive Surgical Procedures ; methods ; Skin Transplantation

Objective To evaluate the feasibility of composite material of bone morphogenetic protein (BMP) and PLGA/TCP in repair of peri-porous-titanium bone defects in adult rabbits.Meth- otis The composite of PLGA/TCP scaffold with bovine BMP was made and implanted in distal bone de- fects peri-porous-titanium in femur of adult rabbits.The effect of BMP with PLGA/TCP on peri-prosthesis was evaluated by means of scanning electron microscope (SEM),energy dispersive X-ray analysis (EDX) and biomechanics.Results BMP with PLGA/TCP showed obvious peak of Ca and P of EDX in the pores of titanium in experiment group six weeks after operation and higher than that in control group (P＜0.05).Push-out test demonstrated that the bonding strength between the composite of HA coating/ porous titanium and bone was increased significantly with time (P＜0.05).In experiment group,at 6 and 12 weeks,peri-porous-titanium had higher shearing force compared with control group (P＜0.05). Conclusion BMP loaded with PLGA/TCP is a promising bone graft for bone defects in revision arthro- plasty,as indicates that bone induction of BMP plays an important role in biological stabilizaiton.

AIMTo observe the metabolic interaction between diphenytriazol and steroid hormone drugs, and provide some useful information for clinical medication.

METHODSThe steroid hormone drugs which may be co-administrated with diphenytriazol were selected, such as mifepriston, estradiol, medroxyprogesterone acetate, progesterone, norethisterone and so on. Diphenytriazol was incubated with each drug in rat liver microsome. The residual concentration of diphenytriazol or steroid hormone drugs in the microsomal incubates was determined by reversed-phase high-performance liquid chromatography, separately. The inhibition constants (K(i)) for each of them were calculated.

RESULTSThe inhibition constant K(is) of diphenytriazol for the metabolism of mifepristone, estradiol, medroxyprogesterone acetate, progesterone and norethisterone were (201.3 +/- 1.0), (94 +/- 4), (128.7 +/- 2.2), (64 +/- 5) and (80 +/- 4) micromol x L(-1), respectively. The inhibition constants K(i) of steroid hormone drugs for the metabolism of diphenytriazol was (66.9 +/- 2.2) micromol x L(-1) for estradiol, (60.0 +/- 2.3) micromol x L(-1) for medroxyprogesterone acetate, (163 +/- 10) micromol x L(-1) for progesterone and (88 +/- 5) micromol x L(-1) for norethisterone, respectively.

CONCLUSIONDiphenytriazol shows metabolism interaction with steroid hormone drugs such as estradiol, medroxyprogesterone acetate, progesterone and norethisterone.

Abortifacient Agents, Nonsteroidal ; metabolism ; pharmacology ; Abortifacient Agents, Steroidal ; metabolism ; Animals ; Contraceptives, Oral, Synthetic ; metabolism ; Drug Interactions ; Estradiol ; metabolism ; Female ; In Vitro Techniques ; Medroxyprogesterone ; metabolism ; Microsomes, Liver ; metabolism ; Mifepristone ; metabolism ; Rats ; Rats, Sprague-Dawley ; Triazoles ; metabolism ; pharmacology

OBJECTIVETo study the effect of Tongluo Xingnao effervescent tablets on learning and memory capacity and expression of Na(+)-K(+)-ATPase in hippocampus of rats with chronic cerebral ischemia-induced learning and memory dysfunction model.

METHODThe 2-VO method was used to establish sd rat model learning and memory dysfunction induced by chronic cerebral ischemia. The 50 rats in the successfully established model were randomly divided into the model control group, the Dihydroergotoxine Mesylate tablets group (0.7 mg x kg(-1), Tongluo Xingnao effervescent tablets high dose (7.56 g x kg(-1)), middle dose (3.78 g x kg(-1)) and low dose (1.59 g x kg(-1)) groups and the sham operation group (n = 10) as the control group. The groups were orally given 10 ml x kg(-1) x d(-1) drugs for consecutively 90 days. On the 86th day, Morris water maze was adopted for them. On the 90th day, a leaning and memory capacity test was held. The brain tissues were fixed with 10% formaldehyde and observed for pathomorphism after routine slide preparation and staining. The expression of hippocampal Na(+)-K(+)-ATPase was detected with immunohistochemistry and image quantitative analysis.

RESULTCompared with the model group, all of Tongluo Xingnao effervescent tablets groups showed significant decrease in the escape latency at the 5th day in the Morris water maze, and notable increase in the frequency of the first quadrant dwell, the frequency passing the escape platform and the frequency entering effective area (p < 0.05). According to the pathomorphological detection, the control group showed a significantly higher pathological score than the sham operation group (p < 0.01), the middle dose group showed a significantly lower pathological score than the model group (p < 0.05). According to the immunohistochemistical detection, the model control group showed a remarkably lower mean OD value of Na(+)-K(+)-ATPase than the sham operation group (p < 0.05), high and middle dose groups showed a significantly higher mean od value than the model control group (p < 0.01).

CONCLUSIONTongluo Xingnao effervescent tablets can improve the learning and memory capacity, reduce pathological changes of hippocampal tissues of rats with chronic cerebral ischemia-induced learning and memory dysfunction model, and promote the expression of Na(+)-K(+)-ATPase in hippocampus.

Animals ; Brain Ischemia ; drug therapy ; enzymology ; genetics ; psychology ; Chronic Disease ; drug therapy ; psychology ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Hippocampus ; drug effects ; enzymology ; Humans ; Learning ; drug effects ; Male ; Memory ; drug effects ; Rats ; Rats, Sprague-Dawley ; Sodium-Potassium-Exchanging ATPase ; genetics ; metabolism ; Tablets ; administration & dosage

OBJECTIVETo develop an analytical method and quality control for determination of zolmitriptan and related substances.

METHODSZolmitriptan and related substances were separated and determined on a shimadzu CLC-C(8) column (150 mm x 6 mm, 10 microm) with a mobile phase of acetonitrile-10 mmol/L phosphate buffer (25:75 pH 7.5) and a flow-rate of 1 ml/min; the UV-VIS detector was operated at 229 nm.

RESULTThe limit of detection for the related substances was 0.5 ng on the zolmitriptan basis (S/N >3). Linear calibration curve was gene rated from 4 - 40 microg/ml with a correlation coefficient of 0.9999. The recovery rate of zolmitriptan was 99.1% with a standard deviation of 0.2%. The results of HPLC method were consistent with those of nonaqueous titration method.

CONCLUSIONHPLC method is a rapid sensitive and accurate method for the determination of zolmitriptan and its related substances.

Chromatography, High Pressure Liquid ; Oxazolidinones ; analysis ; Tryptamines

Objective To report a peliosis hepatic in child and review literature and discuss.Methods Case history was inquired.Physical,labtoratory,imagement and histopathology of liver biopsy(HE staining) were examed.Results A 4-year old girl appeared dermatitis with erythema and herpes at local skin where was bit by insect before onset.The girl appeared fever,cough,then abdominal pain,hepatomegaly,pleural effusion and ascites.Lab examination revealed slight elevation of aspartate transaminase,?-glutamyltranspeptidase and alkaline phosphatase.The liver B-mode ultrasonography and CT scan revealed hepatomegaly with density heterogeneity of the parenchyma.The liver biopsy revealed many small capsule filled with blood cells.Conclusions Clinical characteristics of the disease are fever,upper abdomen pain,janundice,ascites and hepatomegaly.The diagnosis shall be combined with the pathologic biopsy of liver.

AIM: To investigate and analyze the changes of corneal biomechanics of normal eyes,forme frusta keratoconus eyes,subclinical keratoconus eyes and clinical keratoconus eyes by Corneal visualization Scheimpflug technology (Corvis ST),and provide clinical basis for early diagnosis of keratoconus.METHODS: Case-control study.We randomly selected 40 normal eyes as normal group,15 forme frusta keratoconus eyes as forme frusta keratoconus group,23 subclinical keratoconus eyes as subclinical keratoconus group,and 40 clinical keratoconus eyes as keratoconus group.The biomechanical parameters of each group were measured by Corvis ST.The receiver operating characteristic(ROC) curves was plotted to distinguish keratoconus from the normal cornea.RESULTS: There was no significant difference in the parameters of biomechanics between normal group and forme frusta keratoconus group (P>0.05).Compared to normal group and subclinical keratoconus group,the parameters second applanation length(AL2),first velocity of applanation (AV1),central curvature radius at highest concavity (HC-radius),deformation amplitude (DA) were revealed statistically significant differences(P<0.05).The biomechanical parameters of the keratoconic group were significantly different from those of normal group except for the second velocity of applanation (AV2),time from the start until the highest concavity(HC-time),peak distance (PD).ROC curve showed that the DA(area under the curve:0.891±0.028) was the best predictive parameter to distinguish keratoconus from the normal eyes.CONCLUSION: The corneal biomechanical parameters of forme frusta keratoconus group are not changed compared with normal group.The changes between normal group and subclinical keratoconus group should combine with other technology to further improve subclinical keratoconic screening.Compared with normal corneas,keratoconus has a great change in biomechanics,which DA diagnosis of the highest efficiency.

Adult ; Female ; Humans ; Lymphadenitis ; complications ; diagnosis ; pathology ; Positron-Emission Tomography ; Urticaria ; etiology ; Vitiligo ; etiology