Objective:To determine the equilibrium solubility and the apparent oil/water partition coefficient of nebivolol hydrochloride to provide experimental basis for the development of new preparations.Methods:The concentration of nebivolol hydrochloride was determined by an HPLC method,and a saturated solution method and a shake-flask method were respectively applied to determine the equilibrium solubility and the apparent oil/water partition coefficient of nebivolol hydrochloride in water,0.1 mol·L-1 HCl solution and phosphate buffer solution with different pH values(pH2.0,pH6.8,pH7.4 and pH8.0).Results:At (37±0.5)℃,the equilibrium solubility of nebivolol hydrochloride in water and in 0.1 mol·L-1 HCl solution was 722.53 μg·ml-1and 56.07μg·ml-1,respectively.The apparent oil/water partition coefficient (Log P) of nebivolol hydrochloride was 1.17 and 1.32,respectively.Within the pH range of 2.0-7.4,with the increase of pH value, the equilibrium solubility and the Log P decreased and increased,respectively,while pH value increased from 7.4 to 8.0,the equilibrium solubility of nebivolol hydrochloride increased and Log P decreased.Conclusion:The method is accurate and reliable.Nebivolol hydrochloride has poor water solubility,and the equilibrium solubility and the Log P are both influenced by pH values.

Objective To observe the expressions of transforming growth factor-?1(TGF-?1) and plasminogen activator inhibitor-1(PAI-1) mRNA in tubulointerstitial fibrosis( TIF ) rats,and explore the effects of TGF-?1 and PAI-1 on TIF and the interaction between TGF-?1 and PAI-1.Methods Sixty male SD rats were randomly divided into sham operation group (SOR group,n=30) and unilateral urethral obstruction group(UUO group,n=30).TIF model was established via UUO.At d 7,d 14,d 21 after operation,10 rats of every group were killed to obtain renal samples.Histological changes were observed in tubulointerstitium injury under microscope;mRNA and proteins of TGF-?1 and PAI-1 were detected by real-time PCR assays and Western blotting respectively at d 7,d 14,d 21 after experiment onset.SPSS 10.0 software was used to analyze data.Results 1.HE,Masson staining of renal tissues of all groups indicated that there were no fibrosis in SOR rats,there were vacuole degeneration in tubular epithelial cells and inflammatory cell infiltration in tubulointerstitial in UUO rats at d 7,fibrosis aggravated gradually and became severe fibrosis at d 21.2.The expression locations of TGF-?1 and PAI-1 were renal sites of fibrosis by immunohistochemical staining.The mRNA and proteins of TGF-?1 in rats from SOR groups were lower than those of UUO groups at d 7,d 14,d 21(P

Humans ; Hyperphosphatemia ; diagnosis ; drug therapy ; Kidney Failure, Chronic ; diagnosis ; therapy ; Medicine, Chinese Traditional ; methods ; Phytotherapy ; methods

Antibodies, Monoclonal ; therapeutic use ; Antibodies, Monoclonal, Humanized ; Antineoplastic Agents ; therapeutic use ; Breast Neoplasms ; drug therapy ; metabolism ; Carcinoma, Ductal, Breast ; drug therapy ; metabolism ; Drug Delivery Systems ; Female ; Humans ; Nitriles ; therapeutic use ; Receptor, ErbB-2 ; metabolism ; Survival Rate ; Tamoxifen ; therapeutic use ; Trastuzumab ; Triazoles ; therapeutic use

Adolescent ; Adult ; Cleft Lip ; surgery ; Female ; Humans ; Lip ; injuries ; surgery ; Male ; Middle Aged ; Postoperative Complications ; Reconstructive Surgical Procedures ; methods ; Surgical Flaps ; Young Adult

Biopsy, Needle ; Breast ; pathology ; Breast Neoplasms ; classification ; metabolism ; pathology ; Carcinoma, Ductal, Breast ; metabolism ; pathology ; Carcinoma, Intraductal, Noninfiltrating ; metabolism ; pathology ; Carcinoma, Papillary ; metabolism ; pathology ; Diagnosis, Differential ; Female ; Humans ; Hyperplasia ; Keratin-14 ; metabolism ; Keratin-5 ; metabolism ; Keratin-6 ; metabolism ; Membrane Proteins ; metabolism ; Papilloma, Intraductal ; metabolism ; pathology ; Receptors, Estrogen ; metabolism

Objective To investigate the acute phase adverse effects and influencing factors of adverse effects of diphosphonate treatment in the elderly patients with primary osteoporosis.Methods A total of 208 patients [male 25 patients,female 183 patients,age 60 ～ 93 with a average of (75.51 ± 7.73) years] with primary osteoporosis were selected from 1 Jan 2012 to 30 Nov 2015,admitted to Department of Geriatrics.According to the serious condition of osteoporosis and willingness of patients,208 patients were divided into zoledronic acid treatment group,alendronate treatment group,and pamidronic acid group,and received corresponding diphosphonate treatment.All kinds of adverse reactions of diphosphonate in each treatment group were closely to be observed after administration of diphosphonate in 3 days and 7 days.Results The incidence rate of adverse reactions in the zoledronic acid treatment group (59/134,44.03％;60/134,44.78％) was obviously higher than that in the alendronate treatment group (1/57,1.75％;1/57,1.75％),and the pamidronic acid group (3/17,17.65％;3/17,17.65％) after treatment of diphosphonate in three and seven days (P ＜ 0.05).In different generations,the incidence rate of adverse reactions in the zoledronic acid group and the pamidronic acid group after treatment of diphosphonate in three and seven days was not statistically significant (P ＞ 0.05).There were three patients suffering from severe acute kidney injure (AKI) and three patients suffering from hypokalemia in the 134 patients treatment with zoledronic acid.Conclusions There are obvious differences in the incidence rate of acute phase adverse reactions in the osteoporosis patients who received different treatment policy (P ＜ 0.05).The safety issues in the kidney function and electrolyte abnormality (such as hypokalemia) should be paid much enough attention in the primary osteoporosis patients who receive zoledronic acid treatment.

Animals ; Guanylate Cyclase ; metabolism ; Hypercapnia ; metabolism ; Hypoxia ; metabolism ; Lung ; metabolism ; physiopathology ; Male ; Rats ; Rats, Sprague-Dawley ; Receptors, Cytoplasmic and Nuclear ; metabolism ; Soluble Guanylyl Cyclase

Aged ; Aged, 80 and over ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Fibrin Fibrinogen Degradation Products ; metabolism ; Fibrinolysis ; drug effects ; Glycoproteins ; blood ; Humans ; Injections ; Male ; Middle Aged ; Phytotherapy ; Plasminogen Activator Inhibitor 1 ; blood ; Platelet Aggregation ; drug effects ; Pulmonary Heart Disease ; blood ; drug therapy ; Tissue Plasminogen Activator ; blood