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OBJECTlVE To estabIish a simpIe,sensitive and quick method for determination of B7011 in rat pIasma. METHODS The method of protein precipitation with methanoI was used for pre-treatment of pIasma sampIes determined by Iiquid chromatography mass spectrometer. The Iinear reIa-tionship,intra-batch and inter-batch precision,specificity,matrix effect,recovery rate,the accuracy and stabiIity of the pIasma sampIes were vaIidated. The concentration of B7011 in pIasma was determined by LC-mS/ mS foIIowing a singIe intravenous injection of B7011 0.5 mg·kg-1 to rats. RESULTS The Iinear range of B7011 was 30-20 000 μg·L-1 ,the Iower Iimit of quantification was 30 μg·L-1 in pIasma,the in-tra-batch precision of 60,1000,16 000 and 10 000 ng·mL-1 was 5.61% -13.31%,2.31% -8.35%, 2.02%-9.47% and 4.0%-15.0% respectiveIy,and inter-batch precision was 10.05%,2.55%,3.75% and 8.58% respectiveIy. The recovery of 60,1000,and 16 000 μg·L-1 was 114.12%,109.2% and 101.06%respectiveIy. The average peak concentrations were 8373.28 and 8564.59 μg·L-1 ,the mean AUC was 98 400 and 104 000 μg·L-1·h and the t1/ 2z for B7011 was 41.7 and 63.6 h in bIood of maIe and femaIe rats, respectiveIy. CONCLUSlON The estabIished method is sensitive, fast and simpIe and concentration of B7011 in pIasma is determined by LC-mS/ mS foIIowing a singIe intravenous injection of B7011 0.5 mg·kg-1 to rats. It can satisfy the requirements of pharmacokinetic and toxicokinetic studies.
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ObjectiveTo study the changes and clinical significance of vascular endothelial growth factor (VEGF) in sputum of patients with pulmonary arterial hypertension associated with chronic obstructive pulmonary disease (COPD).MethodsThe sputum VEGF levels of 52 cases with pulmonary arterial hypertension associated with COPD during stable period (group A),60 cases with COPD during stable period (group B) and 50 normal persons (group C) were detected by enzyme linked immunosorbent assay (ELISA)method.The pulmonary function,arterial blood gas analysis and pulmonary artery systolic pressure (PASP)were detected.ResultsThe sputum VEGF levels of group A,B and C were (4.30±0.93),(2.64±0.57)and ( 1.48±0.32 ) μ g/L respectively,which had significant difference ( F =31.612,P ＜ 0.01 ).The percentage of forced expiratory volume in the first second (FEV1) in predicted value (FEV1％) of group A,B and C were (48.68±10.53 )％,(67.56±14.61 )％,( 101.60±21.97 )％ respectively,which had significant difference (F =28.983,P ＜ 0.01 ),as well as PASP had [ (55.02±11.90),(23.50±5.08 ),(16.16±3.49) mm Hg (1 mm Hg =0.133 kPa),F=34.887,P＜ 0.01 ].The arterial partial pressure of oxygen (PaO2) and carbon dioxide(PaCO2) of three groups had no significant difference (F=2.159,3.167,P ＞ 0.05).The sputum VEGF level had significantly negative correlation with FEV1％ (r =-0.562,P ＜ 0.05),and positive correlation with PASP(r =0.783,P＜0.05),while had no correlation with PaO2,PaCO2(r =-0.318,0.275,P＞0.05).ConclusionsThe sputum VEGF level of patients with pulmonary arterial hypertension associated with COPD expresses high level,which has significant correlation with pulmonary function and PASP.Therefore,VEGF plays an important role in the pathogenesis of pulmonary arterial hypertension associated with COPD.
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The module design of pharmaceutical superfine pulverization matched up GMP was attempted. The integral of mechanism and electricity into the whole pulverization process was designed and established.
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Objective:To study the influence of some process parameters on the product granularity in pharmaceutical air jet pulverization process.Methods:The method of quadratic regressive orthogonal experiment was used.Results:The mathematics model describing the relationship between the parameters studied and product granularity was established.Conclusion:The conclusions in the experimental study have instructional significance for pharmaceutical production.