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

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

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

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

Two regression models, based on panel data over the period of 2000-2011, are built and used to analyze what factors determine China's exports of primary and semi-finished products of traditional Chinese medicine to ASEAN. The results indicate that, China GDP, the ratio of ASEAN to China GDP per capita, average export price, the ratio of state-owned assets to total assets, have a significant positive influence on the export volumes of primary products of Chinese medicine. At the same time, RMB appreciation, the ratio of three kinds of foreign-invested assets to total assets, China-ASEAN Early Harvest Program, ASEAN-China Free Trade Area have a significant negative influence. In respect of the export volumes of semi-finished products of Chinese medicine, the significant influential factors are ASEAN GDP and the ratio of ASEAN to China GDP per capita. The former is positive and the latter is negative. In order to optimize the commodity composition of experts, it is needed to increase export volumes of both primary and semi-finished products of Chinese medicine. According to the analysis above, some proposals are put forward, such as, improving the performance of foreign capital, playing an exemplary and leading role in technological innovation by state-owned enterprises, taking advantage of bargaining power of suppliers, increasing outward foreign direct investment.
China ; Commerce ; Drugs, Chinese Herbal ; chemistry ; economics ; Europe, Eastern ; Medicine, Chinese Traditional ; economics ; standards ; Quality Control

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

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