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

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

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

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 distribution of etiology and the analysis of drug resistance in the patients with cerebrovascular disease complicated with pulmonary infection.Methods A total of 125 patients' sputum specimens with cerebrovascular disease complicated with pulmonary infection were cuhured.The distribution of pathogens and antibiotic resistance were analyzed.Results The total 591 strains of pathogenic bacteria which isolated and cultivated for this research were taken from 125 patients' 356 sputum specimens.The top five bacteria were Pseudomonas aeruginosa,Acinetobacter Bauman,Klebsiella pneumoniae,Escherichia coli,Proteus mirabilis.12 extended-spectrum β-lactamase (ESBL)-producing Klebsiella pneumoniae,19 ESBL-producing Escherichia coli.56 cases (9.48％) showed Gram positive cocci.424 cases (71.74％) showed Gram negative bacilli.The resistance rate of Pseudomonas aeruginosa was 57.96％ to imipenem and about 30％ to ceftazidime,ciprofloxacin,gentamicin.The resistance rate of Acinetobacter Bauman was above 70％ to ciprofloxacin,ceftazidime,piperacillin/tazobactam,imipenem and gentamicin.The resistance rate of Klebsiellapneumoniae was above 30％ to ciprofloxacin,levofloxacin,ceftazidime,aztreonam.The resistance rate of Escherichia coli was above 50％ to ciprofloxacin,ceftazidime,gentamicin.Conclusion High incidence of pulmonary infection in elderly patients with cerebrovascular disease.Most of the pathogens were multi drug resistant bacteria.

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.

Objective To investigate the roles of matrix metalloproteinases(MMP)and tissue inhibitors of metalloproteinases(TIMP)in dentinogenic ghost cell tumor(DGCT)and ghost cell odontogenic carcinoma(GCOC).Methods The expressions of MMP-2,MMP-9,MMP-14,TIMP-1 and TIMP-2 were examined in 15 DGCT cases and 9 GCOC cases by immunohistochemistry.Their mRNA expression in one DGCT case and one GCOC case were investigated by RT-PCT.MMP-2 and MMP-9 protein activities in the two csses were analyzed by gelatin zymography.Results MMP-9 and TIMP-1 expressions elevated greatly in GCOC,and there was a significant dliferenee(P＜0.05)in TIMP-1 expression between GCOC and DGCT.Pro-MMP-9,MMP-9 activated form,pro-MMP-2,and MMP-2 activated forms were detected in the GCOC case.while pro-MMP-9 and MMP-9 activated form were very faint in the DGCT case.The mRNA level of MMP-9 elevated obviously in the GCOC case,which was similar to that of TIMP-1.Conclusions The elevated expression of MMP-9 and TIMP-1 may influence the behaviour of GCOC.

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