AIMTo explore the causes of the difference in spermatogenic suppression between responders and non-responders in Chinese men treated with levonorgestrel (LNG) implants plus testosterone undecanoate (TU) injectable.

METHODSThe 16 Chinese volunteers treated were divided into two groups in regard to the sperm count during the treatment period, 7 men in the responder group (Group R), including 6 azoospermia and one severe oligozoospermia, and the remaining 9 in the non-responder group (Group N), including 4 oligozoospermia and 5 with sperm counts greater than 20 x 10(6)/mL. The differences in serum profiles of FSH, LH, T, LNG and T/LH ratio were compared between the two groups and the correlation between the seminal fluid parameters and serum reproductive hormones was analyzed.

RESULTSThe serum FSH level was lower in Group R than that in Group N (P<0.05), while the serum LH and LNG levels were higher in Group R than those in Group N (P<0.05). The sperm density (P<0.01, r=0.235), motility(P<0.01, r=0.326) and vitality (P<0.01, r=0.219) showed significantly positive correlation with the serum FSH level.

CONCLUSIONThe blood LNG and T levels, the degree of FSH inhibition and/or the sensitivity of the pituitary-testis axis to exogenous steroids, as well as the individual spermatogenetic potential and the functional status of the Leydig cells may be factors bringing about individual differences in spermatogenic suppression in Chinese men treated with LNG and TU.

Adult ; Contraceptive Agents, Male ; administration & dosage ; Drug Implants ; Follicle Stimulating Hormone ; blood ; Humans ; Injections ; Levonorgestrel ; administration & dosage ; pharmacokinetics ; Leydig Cells ; physiology ; Luteinizing Hormone ; blood ; Male ; Sperm Count ; Spermatogenesis ; drug effects ; Testosterone ; administration & dosage ; analogs & derivatives ; blood

The aim of this thesis is to prepare etoposide submicro-emulsion (ESE) for intravenous injection and investigate its characteristics in vitro and in vivo. High-pressure homogenization was used to prepare ESE, using 10% (w/w) soybean oil and 10% (w/w) medium-chain triglyceride as mixed oil phase, and 1.8% (w/w) fabaceous lecithin as emulsifier. The pH was adjusted to 5.5 with 0.1 mol x L(-1) NaOH to keep the most stability of ESE. The particle size distribution and zeta potential were measured using photon correlation spectroscopy. Ultrafiltration was used to estimate the relative percentages of etoposide in each phase. Long-term storage test and accelerated isothermal test-Weibull distribution method were used to estimate the physical and chemical stability of ESE. Plasma pharmacokinetics in rats was monitored by high performance liquid chromatography by comparison with etoposide nonaqueous solution at the same time. The mean particle size, zeta potential and entrapment efficiency of ESE were (189.9 +/- 54.6) nm, - 32.6 mV and 91.7%, respectively. The emulsion was stable during 9 month storage at 4 degrees C. The shelf life (T0.9) of etoposide in lipid emulsion was estimated to be about 665 days at 4 degrees C. The drug concentration-time curves of ESE and solution were similar and could be described by two compartment model. The area under the curve of concentration versus time from zero to the last time point and the mean residence time of ESE and solution were (18.30 +/- 8.74) and (19.32 +/- 6.45) microg x h x mL(-1), and (1.46 +/- 0.32) and (1.71 +/- 0.52) h, respectively. Etoposide was incorporated in submicro-emulsion to improve its physical and chemical stability without addition of organic solvents with insignificant different characteristics in vivo when compared with solution.
Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; pharmacokinetics ; Area Under Curve ; Drug Carriers ; Drug Compounding ; Drug Stability ; Drug Storage ; Emulsions ; Etoposide ; administration & dosage ; pharmacokinetics ; Female ; Hydrogen-Ion Concentration ; Injections, Intravenous ; Lecithins ; chemistry ; Male ; Particle Size ; Random Allocation ; Rats ; Rats, Wistar ; Solubility ; Soybean Oil ; chemistry ; Technology, Pharmaceutical ; methods ; Triglycerides ; chemistry

ObjectiveTo study an application of a method of improving the quality of sampling in review to determine the light areas of endemic fluorosis(referred to as endemic fluorosis) in quality control. Methods Of 15 light endemic fluorosis township(town), six were randomly sampled, and the prevalence of dental fluorosis in 22 village primary school children aged 8 to 12 were reviewed to determine the improved quality of sampling in Xuyong county Sichuan province. ResultsSix townships(towns) were selected by simple random sampling from 15 endemic fluorosis townships(towns) for review inspection in Xuyong country. A total of 22 villages were verified, accounting for 22.7％ of the total 97 villages verified. Of the 416 children for review inspection of dental fluorosis, 383 children were positive. The consistent rate of children' s dental fluorosis was 92.07％, and the verification to be slight villages was up to 21 endemic villages, accounting for 95.45％. ConclusionsThe application of a method of improving the quality of sampling can improve the efficiency of quality control, and improve the accuracy. It is a novel quality control method.

To detect the in vitro probe microdialysis recoveries based on an HPLC-DAD method for simultaneous quantification of nine active ingredients (ephedrine, pseudoephedrine, methylephedrine, amygdalin, liquiritin, cinnamyl alcohol, cinnamic acid, cinnamaldehyde and glycyrrhizic acid) in Mahuang decoction, which provides reference for in vivo pharmacokinetic study. The concentrations of nine active ingredients in dialysate were detected by HPLC-DAD, to investigate the effect of flow rates (incremental method and subtraction method) and intraday stability of the probe recoveries and medium concentrations on the recoveries. Nine active ingredients could be well separated in 52 min. At the perfusion rate of 1.0 μL x min(-1), the relative recoveries of ephedrine, pseudoephedrine, methylephedrine, amygdalin, liquiritin, cinnamyl alcohol, cinnamic acid, cinnamaldehyde and glycyrrhizic acid were (50.95 ± 0.82)%, (52.74 ± 1.13)%, (51.29 ± 0.51)%, (32.56 ± 0.84)%, (45.36 ± 0.83)%, (70.94 ± 0.99)%, (69.98 ± 2.30)%, (71.68 ± 0.63)%, and (22.14 ± 0.48)%, respectively. And the probe kept steady in 7 hours. At the same medium concentration, the probe recoveries decreased exponentially with the increase in flow rates. The recoveries of seven ingredients detected by these two methods were similar at certain flow rates, except for amygdalin and cinnamaldehyde. At the same flow rate, the relative recoveries of cinnamyl alcohol, cinnamic acid and cinnamaldehyde changed greatly (9.55%-16.2%) and the others six ingredients had less change (3.27%-5.71%) with the changes in medium concentrations. Microdialysis method could be used to detect the in vitro recoveries of nine ingredients in Mahuang decoction. Reverse dialysis method could be used for the in vivo probe recovery calibration of ephedrine, pseudoephedrine, methylephedrine, liquiritin, cinnamyl alcohol and cinnamic acid at the flow rate of 2.0 μL x min(-1).
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Ephedra sinica ; chemistry ; Microdialysis ; methods ; Molecular Structure

To compare the microcalorimetric fingerprint profiles of Lonicerae japonicae Flos (Lj.F) and Lonicerae Flos (L.F), microcalormietry was applied to find the heat change regularity of Bacillus shigae (B. shigae) metabolism affected by Lj.F and L.F (we choose Lonicera macranthoides Hand.-Mazz in this paper) with different concentrations. The thermogenic curves and thermodynamics parameters were investigated as evaluation index, and then the date of experiment was studied by similarity analysis. All the results indicated that the Lj.F and Lonicera macranthoides Hand.-Mazz (L.m.H-M) significantly impacted the microbial growth and had good similarity in its inhibitory activities. The combination approach of chemical analysis with bioassay was developed and employed to ensure the safety and efficacy of Chinese herbal medicines.
Anti-Bacterial Agents ; isolation & purification ; pharmacology ; Bacillus ; drug effects ; growth & development ; Calorimetry ; methods ; Chemical Safety ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Flowers ; chemistry ; Lonicera ; chemistry ; classification ; Plants, Medicinal ; chemistry ; classification ; Quality Control ; Thermodynamics ; Thermogenesis

To explore the new pattern of Chinese medicine solid preparations (CMSP) in vitro dissolution, a method testing the bio-thermal activity in combination with UPLC was used. Microcalorimetry was used to obtain the characteristic metabolic growth power-time curves and a series of biothermodynamic parameters of the inhibition of Staphylococcus aureus by Yinhuang tablet dissolving solutions at the pH 6.8 (phosphate buffer) dissolution medium at different times. From these results, the cumulative dissolution of Yinhuang tablet based on bio-thermal activity was obtained. The dissolution rates of two components of chlorogenic acid and baicalin were determined by UPLC method. Then f2 similar factor method was used to evaluate the relevance of these two methods. The result showed that f2 values all were more than 50, indicating that there is a good correlation between the two methods of measuring the dissolution rate. It is feasible to determine CMSP in vitro dissolution by using bio-thermal activity, and to provide new evaluation methods for controlling the quality of CMSP.
Calorimetry ; methods ; Chlorogenic Acid ; chemistry ; pharmacology ; Chromatography, Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Flavonoids ; chemistry ; pharmacology ; Quality Control ; Solubility ; Staphylococcus aureus ; drug effects ; physiology ; Tablets ; Thermodynamics

OBJECTIVETo study the effect of Modified Guipi Decoction (MGD) on blood pressure and quality of life (QOL) in hypertension patients complicated depression.

METHODSTotally 245 hypertension patients complicated depression were randomly assigned to the treatment group (125 cases, treated with MGD) and the control group (120 cases, treated with Sertraline). Final recruited qualified patients were 117 cases in the treatment group and 111 cases in the control group. The therapeutic course for all was 4 weeks. Changes of blood pressure, scores rated by Hamilton Depression Scale-17 (HAMD-17), Hamilton Anxiety Rating Scale (HAMA), short-form 36 health survey questionnaire (SF-36), and Treatment Emergent Symptom Scale (TESS) were observed before and after treatment, thereby judging their efficacies.

RESULTS(1) Compared with before treatment in the same group, systolic and diastolic blood pressures significantly decreased in the treatment group after 2 weeks of treatment; systolic blood pressure significantly-decreased after 2 weeks of treatment and diastolic blood pressure significantly decreased after 3 weeks of treatment in the control group (all P < 0.05, P < 0.01). Decreased valley values of systolic and diastolic blood pressures at week 2, 3, and 4 after treatment were obviously higher than those at week 1 after treatment in the two groups (P < 0.05, P < 0.01). Compared with the control group at week 4 after treatment, valley value of systolic blood pressure obviously decreased in the treatment group (P <0. 01). Decreased valley values of systolic and diastolic blood pressures in the treatment group were higher than those of the control group (P <0. 01). The success rate of target blood pressure was 60. 7% (71/117 cases) in the treatment group and 42. 3% (47/111 cases) in the control group, with statistical difference (χ² = 7.6781, P < 0.01). (2) Compared with before treatment in the same group, the score of HAMD-17 at week 2, 3, and 4 after treatment all decreased in the two groups (P < 0.01). Compared with the control group, the score of HAMD-17 at week 4 after treatment decreased more obviously in the treatment group, with higher difference in decreased value (P < 0.05). The effective rate was 79.5% (93/117) in the treatment group, higher than that in the control group [66.7% (74/111); χ² = 4.7741, P < 0.05]. (3) Compared with before treatment in the same group, the score of HAMA at week 1, 2, 3, and 4 after treatment all obviously decreased in the two groups (P <0. 05, P <0. 01). Compared with the control group, the score of HAMA at week 3 and 4 after treatment decreased more obviously in the treatment group, with higher difference in decreased value (P < 0.05, P < 0.01). (4) After 4 weeks of treatment, except physical function in the control group, SF-36 total score and the score for each factor were obviously higher in the two groups (P < 0.05, P < 0.01). MGD showed superior effect in improving physical function, physical activity, overall health, emotion activity, and health changes to that of Sertraline (P < 0.05, P < 0.01). (5) The incidence of insomnia, tremor, liability to agitation, dizziness was obviously less in the treatment group than in the control group (P < 0.05).

CONCLUSIONSMGD had favorable clinical effect on hypertension patients complicated depression. Meanwhile, it also could improve their blood pressure and QOL.

Antidepressive Agents ; therapeutic use ; Blood Pressure ; drug effects ; Depression ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Hypertension ; complications ; Phytotherapy ; Psychiatric Status Rating Scales ; Quality of Life ; Sertraline ; therapeutic use ; Surveys and Questionnaires

OBJECTIVETo explore the apoptosis resistance induced by Leptin and its mechanism in breast cancer cells in vitro.

METHODSThe leptin-mediated reduction of docetaxel-induced apoptosis in human breast cancer T47D cells was evaluated by TransAM ELISA, MTT and caspase-9 assay. The leptin-promoted survivin expression was analyzed by Western-blot and RT-PCR. The reversing effect of STAT3 knockdown on leptin-induced survivin upregulation was measured by Western-blot and RT-PCR.

RESULTSLeptin promoted T47D cells proliferation and the inhibitory rate was -63.6%. It reduced docetaxel-induced apoptosis in T47D cells by 31.9%. Leptin at different concentrations promoted survivin protein and mRNA expression in T47D cells. The expression of survivin mRNA was 4.6 fold compared with the T47D cells not treated with leptin(10 nmol/L). The expression of survivin mRNA in T47D cells was 0.55 +/- 0.15 fold after transfected with small interfering RNA (siRNA) of STAT3. The expression of survivin mRNA in STAT3 siRNA group and mock transfected group were 0.56 +/- 0.18 fold and 1.61 +/- 0.22 fold after treated by leptin, respectively. The survivin protein level of T47D mock transfected cells was increased after treated by leptin, but the protein level of T47D transfected with STAT3 siRNA cells were not changed significantly.

CONCLUSIONLeptin/STAT3 signaling is a novel pathway for up-regulation of survivin expression in breast cancer cells.

Apoptosis ; drug effects ; Breast Neoplasms ; metabolism ; pathology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Female ; Humans ; Inhibitor of Apoptosis Proteins ; Leptin ; pharmacology ; Microtubule-Associated Proteins ; genetics ; metabolism ; RNA, Messenger ; metabolism ; RNA, Small Interfering ; STAT3 Transcription Factor ; genetics ; metabolism ; Signal Transduction ; Transfection ; Up-Regulation

OBJECTIVETo assess the features of fluorine-18 fluorodeoxyglucose (FDG) uptake in patients with benign pulmonary nodules.

METHODSFrom October 1998 to July 2004, 47 patients with benign pulmonary nodules were imaged with FDG-positron emission tomography (PET). Diagnoses were confirmed by surgery. FDG-PET data was analyzed by visual method and semi-quantitive method. When pulmonary nodules with abnormal FDG intake appeared in PET scans confirmed by visual method, their maximum and mean standard uptake value (SUVmax and SUVmean) and SUV of normal lung (SUVlung) were measured using semiquantitative method.

RESULTSTwenty-one cases showed nothing abnormal in PET scans, including 17 calcification and fibrosis, 2 hamartomas and 2 sclerosing hemangiomas. 26 pulmonary nodules were detected by FDG-PET (17 active tuberculous, 6 inflammatory pseudotumors, 3 cryptococcosis). FDG uptake of these 26 nodules was higher than that of normal lung (SUVmax, SUVmean and SUVlung were 3.04 +/- 1.65, 2.48 +/- 1.35 and 0.40 +/- 0.07, respectively, P < 0.001). Correlations were not found between FDG uptake and nodule size or SUV of normal lung or age or blood glucose level in these 26 patients (P > 0.05). SUV in 9 cases (9/26, 35%) were beyond 2.5.

CONCLUSIONSSome benign pulmonary nodules were FDG avid.

Adult ; Aged ; Diagnosis, Differential ; Female ; Fluorodeoxyglucose F18 ; pharmacokinetics ; Humans ; Lung Neoplasms ; diagnostic imaging ; Male ; Middle Aged ; Radionuclide Imaging ; Radiopharmaceuticals ; pharmacokinetics ; Retrospective Studies ; Sarcoidosis, Pulmonary ; diagnostic imaging ; Solitary Pulmonary Nodule ; diagnostic imaging ; Tuberculosis, Pulmonary ; diagnostic imaging

Objective To analyze the long-term effect and prognosis of automatic angle measuring instrument in measuring anteversion angle of patients with total hip arthroplasty(THA).Methods A total of 120 patients with THA from June 2012 to January 2017 were divided into two groups by random number table,with 60 cases in each group.The anteversion angle of THA in control group was measured by CT, while the anteversion angle of THA in observation group was measured by automatic angle measuring instrument.The recovery of hip joint, score of living quality,incidence of complications before and after surgery were compared between the two groups. Results After surgery,the score of hip joint recovery in control group was lower than that in observation group,the difference was significant(P<0.05).After surgery, the scores of living quality in two groups increased compared with those before surgery,and the increased range of observation group was lar-ger,the difference was significant(P<0.05).The incidence of complications in control group was 13.33% ,which was higher than 1.67% of observation group,the difference was significant(P<0.05). Conclusion Automatic angle measuring instrument in measuring anteversion angle of THA can increase measuring accuracy,decrease the incidence of complications,increase living quality and promote prognosis,which is worthy of promotion in clinical application.