Four salts of ticagrelor, ticagrelor-3,5-dinitrobenzoic acid, ticagrelor-pyrazinamide, ticagrelor-D-proline and ticagrelor-L-proline were prepared by solvent suspension and liquid-assisted grinding to improve the solubility of ticagrelor. The compounds were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, nuclear magnetic resonance spectroscopy, elemental analysis, and the intermolecular salt-bonding forces were analyzed. The equilibrium solubility of salts and pure drug in hydrochloride buffer pH 1.2 and phosphate buffer pH 6.8 were measured by high-performance liquid chromatography. Ticagrelor was salted with 3,5-dinitrobenzoic acid, pyrazinamide, D-proline, L-proline all in a stoichiometric ratio of 1∶1; with the exception of ticagrelor-D-proline, the solubility of the other three salts provided significantly improved solubility in hydrochloride buffer pH 1.2, and the equilibrium solubility of ticagrelor-3,5-dinitrobenzoic acid was increased by approximately 1.7 folds as compared to pure drug. Salt-forming technology is convenient and can improve the solubility of ticagrelor.

OBJECTIVETo explore the expression and clinical significance of T cell immunoglobulin mucin (TIM)-1, TIM-3 and T cell-specific transcription factors T-bet and GATA-3 in spleen mononuclear cells in patients with primary immune thrombocytopenia (ITP).

METHODSThe spleen samples were obtained from 17 active ITP patients and 10 controls with spleen traumatic rupture. By using real-time quantitative polymerase chain reaction, the mRNA expressions of TIM-3, TIM1, T-bet and GATA-3 were studied in all subjects.

RESULTSTIM-3 mRNA levels of active ITP patients were significantly decreased to (29 ± 16)% of that of control, TIM-1 mRNA levels of active ITP patients increased to (3.20 ± 2.18) folds of that of control, but the difference was not significant. The ratio of TIM-1/ TIM-3 was elevated in active ITP patients. T-bet mRNA levels were up-regulated in ITP patients by (2.82 ± 1.57) folds (P<0.05) and the expression of GATA3 was decreased by 14% folds (P<0.05) compared to controls. The ratio of T-bet/GATA3 were significantly elevated in ITP patients.

CONCLUSIONThe imbalance between TIM-3 and TIM-1 expression might play an important role in pathogenesis of ITP.

Adolescent ; Adult ; Aged ; Aged, 80 and over ; Case-Control Studies ; Female ; Flow Cytometry ; GATA3 Transcription Factor ; metabolism ; Hepatitis A Virus Cellular Receptor 1 ; Hepatitis A Virus Cellular Receptor 2 ; Humans ; Male ; Membrane Glycoproteins ; metabolism ; Membrane Proteins ; metabolism ; Middle Aged ; Purpura, Thrombocytopenic, Idiopathic ; immunology ; metabolism ; RNA, Messenger ; genetics ; Receptors, Virus ; metabolism ; Spleen ; metabolism ; Th1 Cells ; immunology ; Th2 Cells ; immunology ; Young Adult

Cerebellum ; surgery ; Cystadenoma, Papillary ; complications ; pathology ; surgery ; Epididymis ; pathology ; surgery ; Follow-Up Studies ; Genital Neoplasms, Male ; complications ; pathology ; surgery ; Humans ; Keratin-7 ; metabolism ; Kidney ; surgery ; Male ; Middle Aged ; Mucin-1 ; metabolism ; Vimentin ; metabolism ; von Hippel-Lindau Disease ; complications ; metabolism ; pathology ; surgery

Objective To investigate the characteristic,diagnosis,clinical staging, treatment and clinical prognosis of occult breast carcinoma (OBC). Method Forty-six cases of OBC were analyzed retrospectively with the clinical and follow-up information that were confirmed by postoperative pathologic diagnosis from November 1981 to November 2005. Results All patients showed axillary node enlargement as the first sign and were operated.The operation included axillary node excision in 2 patients,radical mastec-tomy or modified radical mastectomy in 44 patients. Forty-five cases got follow-up for 1-22 years,33 cases had existed 3 years,18 cases had existed 5 years,8 cases had existed 10 years. Conclusions For axillary mass which causes are uncertain ,the possibility of OBC should be considered .Meanwhile excision and pathological examination is necessary.The metastatic histological structure and immunohistochemical index of the axillary nodes usually provide important clue for the source of this tumor.Radical or modified mastectomy is the best method, and pest-operative chemotherapy and/or radiotherapy should be done. It has been showed that targeted therapy is very important to breast cancer with C-erbB-2 positive recently.To the cases that neck lymphatic metastasis is M4G3 positive by immunohistochemical examination and no primary focus clinically, the diagnosis of OBC should be considered. The cases without primary focus have better prognosis than those with primary focus.

Diagnosis, Differential ; Endometrial Stromal Tumors ; metabolism ; pathology ; surgery ; Female ; Follow-Up Studies ; Gastrointestinal Stromal Tumors ; pathology ; Humans ; Leiomyoma ; metabolism ; pathology ; Middle Aged ; Neprilysin ; metabolism ; Receptors, Estrogen ; metabolism ; Receptors, Progesterone ; metabolism ; Rectal Neoplasms ; metabolism ; pathology ; surgery ; Rectum ; surgery ; Solitary Fibrous Tumors ; metabolism ; pathology

OBJECTIVETo evaluate clinical efficacy of electroacupuncture at Changqiang (GV 1) and Chengshan (BL 57) 30 min before surgery on postoperative pain and discomforts in patients with mixed hemorrhoids.

METHODSOne hundred and twenty cases of mixed hemorrhoids who received Milligan-Morgan operation were randomly divided into an electroacupuncture group, a sham electroacupuncture group and a blank group, 40 cases in each one. At the same time of basic treatment, the electroacupuncture was applied at Changqiang (GV 1) and Chengshan (BL 57) 30 min before surgery in the electroacupuncture group, while shallow needling without electrical stimulation at sham acupoint (1 cm next to acupoint) was applied 30 min before surgery in the sham electroacupuncture group, while no treatment was given before the surgery in the blank group. The total dose of painkillers in the first 24 h after operation, the number of cases who received additional anesthetic in the operation, the self-score of most severity pain in the first 24 h after operation and sleeping time in the night of surgery were observed.

RESULTSThe differences of the numbers of cases who received additional anesthetic in the operation had no statistical significance among the three groups (all P > 0.05), but compared with the sham electroacupuncture group and blank group, the total dose of painkillers in the first 24 h after operation was reduced in the electroacupuncture group [(2.43 +/- 1.08) tablets vs (3.23 +/- 1.33) tablets, (3.10 +/- 1.22) tablets], and the score of most severity pain was also decreased (6.65 +/- 1.00 vs 7.48 +/- 0.96, 7.25 +/- 1.19), besides, the sleeping time in the night of surgery was increased [(220.63 +/- 85.50) min vs (162.00 +/- 92.69) min, (151.50 +/- 80.01) min, all P < 0.05].

CONCLUSIONThe electroacupuncture at Changqiang (GV 1) and Chengshan (BL 57) 30 min before surgery has effects of preemptive analgesia on postoperative pain for patients with mixed hemorrhoids.

Acupuncture Points ; Adult ; Aged ; Electroacupuncture ; Female ; Hemorrhoids ; surgery ; Humans ; Male ; Middle Aged ; Pain, Postoperative ; therapy ; Young Adult

Piroxicam has polymorphism. Different crystalline forms can exhibit different physicochemical properties and biological activities. Analysis of the intermolecular interactions is essential to reveal the formation mechanism and differences of polymorphs. In this paper, Hirshfeld surface analysis and semi-empirical methods were used to calculate and analyze the intermolecular interactions in seven polymorphic forms of piroxicam. The results show that the Hirshfeld surface analysis method can clearly and intuitively reveal the intermolecular interactions, among which H…H, O…H/H…O and N…H/H…N interactions account for 95% of the total energy. There are differences in the proportion and distribution of the forces of different crystal forms. The energy calculation shows that the lattice energy of the hydrate is significantly lower than that of the anhydrous forms, and in the specific energy distribution, the contribution of the dispersion force is the most prominent. Further interaction energy analysis was found that within the distance of 3.8 Å from the center of the piroxicam molecule, different crystalline forms of piroxicam molecule have different interaction energies with surrounding molecules.

OBJECTIVETo investigate the effects of catecholamine hormone on the blood and brain of heroin addicts.

METHODSRats were divided into three groups and treated with the glucose (control group), the heroin (im) (heroin group), and the combination of the intramuscular injection of reserpine and heroin (reserpine group). Changes in the levels of the dopamine (DA), cAMP, and cGMP were detected by the radioimmunoassay (RIA) method in the blood and brain tissue.

RESULTSNo significant withdrawal symptoms were observed in the reserpine group. Compared with the control and heroin groups, the blood cAMP levels were increased by 35.36% and 15.53% in the reserpine group, respectively; the cAMP levels in the midbrain ventral tegmental area (VTA), prefrontal cortex (PFC), and hippocampus (Hipp) were increased by 24.08% & 8.53%, 15.66% & 8.13%, and 21.95% & 8.40%, respectively. While compared to the control and heroin groups, the DA levels of the PFC, Hipp, striatum, and nucleus accumbens (NAc) were significantly reduced in the reserpine group, decreasing by 74.09% & 82.86%, 81.06% & 82.23%, 91.62% & 86.55% and 84.35% & 90.63%, respectively. The concentrations of cGMP of the brain tissues in the reserpine group were lower than those in the control group. In addition, the neural electrophysiological testing showed that the electroencephalogram (EEG), electrocardiogram (ECG), and muscle spindle discharge diagram of rats in both the reserpine and heroin groups were apparently changed.

CONCLUSIONCatecholamine hormone plays an important role in heroin addiction.

Animals ; Brain ; drug effects ; metabolism ; Catecholamines ; physiology ; Cyclic AMP ; blood ; metabolism ; Cyclic GMP ; blood ; metabolism ; Dopamine ; blood ; metabolism ; Heroin Dependence ; metabolism ; physiopathology ; Male ; Rats ; Rats, Wistar

Abstract?AIM:To study the Influence and outcomes of eye healthcare information teaching for the visual development of children under“combination of medicine and education” in kindergartens.?METHODS:The children(5-6 years old) were randomly selected from 6 kindergartens in Nanjing, 3 in Yuhua District as the experimental group, and the other 3 in Jianye District as the control group.A one-year follow-up was conducted to evaluate the difference of visual development, including the rate of low vision, rate of referral caused by refractive abnormality, rate of astigmatism, the average of the equivalent spherical lens and the rate of lacking physiological hypermetropia, between the experimental group and the control group children.?RESULTS:One school year later,the rate of low vision, rate of referral caused by refractive abnormality and the rate of astigmatism, were significantly lower (P<0.05)in the experimental group under the mode of“combination of medicine and education”, which were also lower than those before experiment(P<0.05).The average of the equivalent spherical lens of experimental group increased and the rate of lacking physiological hypermetropia decreased significantly, compared with the control group ( P <0.05 ) and with those before experiment(P<0.05).?CONCLUSION:Using “combination of medicine and education” eye health care model,is good for children's visual development,so as to reduce the rate of low vision and delay the occurrence of myopia.

Adult ; Humans ; Lateral Ventricles ; pathology ; Male ; Neurocytoma ; pathology