Object To develop a method for the quantitative determination of salvianolic acid A in rat plasma. Methods HPLC method and Hypersil ODS column (4 6 mm?200 mm, 10 ?m) were used, the mobile phase was acetontrile water (1∶2 65, adjusted pH to 2 5 with formic acid), at a flow rate of 0 9 mL/min, the UV detection wavelength was 285 nm. Cinnamic acid was used as internal standard. Results The recovery of the method was in the range of 98 9%～106 9%, the recovery of the extraction was over 83%. The within day precision and the day to day precision were both lower than 8 4%. Conclusion The method is appropriate for the determination of salvianolic acid A when pharmacokinetics of salvianolic acid A is studied in rat plasma.

Objective To explore the correlation between obstructive sleep apnea hypoventilation syndrome (OSAHS)and glucose metabolism disorders in patients without diabetes mellitus.Methods A total of 88 patients with OSAHS but without diabetes mellitus from 2009 to 2011 in our hospital were selected and the pulse oximeter were used to measure the oxygen saturation.Patients were divided into 2 groups:the mild OSAHS group (n=46) and the severe OSAHS group (n=42).The age-and body mass index (BMI) matched control patients without OSAHS (control group,n =48) were randomly selected.The medical history,age,body height and BMI were recorded.The levels of fasting blood glucose,glycated hemoglobin (HbA1c),cholesterol,triglyceride and low density lipoprotein cholesterol were determined.Results There were significant differences in the numbers of respiratory disorders,respiratory disturbance index,average length of apnea,the longest apnea time,low-oxygen frequency,oxygen index,the time of oxygen saturation (SaO2) below 90％,minimum SaO2 and mean SaO2 between the OSAHS group and the control group (F=2.71,2.89,1.94,2.30,2.93,2.27,3.66,3.06,1.82,respectively,all P＜0.05).There were differences in the levels of fasting blood glucose,postprandial blood glucose,HbA1c,cholesterol,triglycerideand low density lipoprotein cholesterol between the three groups(F=1.81,1.85,2.16,1.77,2.24,2.19,respectively,all P＜0.05).Conclusions The severe degree of OSAHS has the correlation with the levels of glycated hemoglobin and blood glucose,which can provide a basis to observe the duration of diabetes mellitus and to predict the risk of cardiovascular diseases.

The anti-tumor activity of folate receptor targeting docetaxel-loaded membrane-modified liposomes (FA-PDCT-L) was investigated in vitro and in vivo. FA-PDCT-L was prepared by organic solvent injection method. Transmission electron microscope, dynamic light scattering and electrophoretic light scattering were employed to study the physicochemical parameters of FA-PDCT-L. The inhibitory effects of docetaxel injection (DCT-I), non-modified DCT liposomes (DCT-L) and FA-PDCT-L on the growth of MCF-7 and A-549 cells at different incubation times were detected by CCK-8 assay; and the hemolytic test was employed in vitro. Tumor mice were randomized into 4 groups: DCT-I, DCT-L, FA-PDCT-L and control group (normal saline), and given drugs at 10 mg x kg(-1) x d(-1) through tail vein. The tumor volume, mice weight, inhibition rate of tumor and life span were measured at the end of experiments. The IC50 of the FA-PDCT-L for MCF-7 and A549 cell lines were significantly lower than that of DCT-I and DCT-L, without hemolysis reaction observed. Compared with control group, the weights of tumor in DCT-I, DCT-L and FA-PDCT-L were decreased, especially for FA-PDCT-L, with inhibitory rates at 79.03 % (P < 0.05). The life span and median survival time of FA-PDCT-L treated mice were significantly higher than that of DCT-I and DCT-L. In conclusion, FA-PDCT-L shows a good anti-tumor activity, indicating that it is potential carriers for DCT in the treatment of tumor.

The clinical trials of gossypol at the dosage of 15 mg and 22.5 mg per day were carried out in the city and the rural area respectively. The results of cytological, cytochemical as well as ultrastructural studies of the semen obtained before and during gossypol administration were as follows:1. It was shown that a decrease in sperm count and the occurrence of abnormal sperm in semen was detectable 4 weeks after gossypol administration. By the 8th week the sperm count being reduced markedly in semen, while exfoliated spermatogenic cells (including mainly spermatids and spermatocytes) increased concomitantly, the date indicated that the site of gossypol action was at the spermiogenic spermatids as well as the mid-and late stage spermatocytes.2. Decrease in the activity of SDH in the middle piece of the sperm and damage to the spiral mitochondrial sheath including derangement, vacuolation, and loss of mitochndrial cristae were observed following gossypol treatment. Such changes suggested that gossypol might suppress the energy matoblism of sperm. The effect of gosspol on the PLE of acrosome system appeared to be secondary.3. The ultrastructural changes of sperm nuclear chrmatin after gosspol treament suggested the possibility that gosspol might exert effect on the matoblism of the nuclic acid.

Objective To investigate the expression of endothelin-1 (ET-1 ), nitrogen monoxidium (NO), vascular endothelial growth factor (VEGF) and brain tissue VEGF induced by chronic intermittent hypoxia (CIH) in aged rats. Methods The CIH model of aged rat was established by using intermittent hypoxia. The levels of ET-1, NO and VEGF in the plasma were detected at 3, 6 and 9 weeks after experiment in each group. The expression of VEGF in brain tissues and the pathological changes of the vessels of the cerebra and the ratio between the thickness of vessel wall and external diameter (WT%) were observed. Results In CIH group, the ET-1 and VEGF levels increased, however NO level decreased. The levels of ET-1 and VEGF were higher at 3 weeks in CIH group than in UC group (t=2.47 and 2.38, both P<0.05), however NO level was lower in CIH group than in UC group (t=2.39, P<0.05). VEGF levels increased significantly at 9 weeks in CIH as compared with UC group [(171.1±13.5) pg/ml vs. (109.8±8.6) pg/ml, t = 3.46, P< 0.01]. The levels of VEGF in CIH group increased remarkably at 9 weeks as compared with 3 weeks [(129.3±12.3) pg/ml, t=2.38, P<0.053. VEGF levels in CIH group showed positive correlation with the time of intermittent hypoxia. The changes of cerebral vessels in UC group were not found, while the aged rats in CIH group showed cerebral neuron cells swelling and blood vessel hyperplasia. The WT% of cerebral small artery was more apparent in CIH group than in UC group at 3 weeks (t=2.34,P<0.05). The expression of VEGF in cerebra was higher in CIH group than in UC group in the three stages (r=2.37, P<0.05). There was an aggravated tendency in the change of the expression of brain tissue VEGF and WT% over time. The change was more apparent at 9 weeks than at 3 weeks (t=2.32 and 2.35, both P<0.05). Conclusions CIH can induce an increase in the expression of ET-1 and VEGF, a decrease in the expression of NO in aged rats. The over expression of VEGF and the disbalance of ET-1 and NO levels can cause brain cellular swelling, arteriola vessel wall thickening,lumens stenosis.

The purpose of this study is to design push-pull osmotic pump (PPOP) tablets of famotidine using the expert system for the formulation design of osmotic pump of poor water-soluble drug which had been established by the authors. Firstly, the parameters which were requisite of the system input were obtained from literatures and experimental tests. Then the parameters were input into the system, and the program was run. The system displayed the designed formulations sequential. Finally, famotidine PPOP was prepared according to the designed formulations and the in vitro dissolution was carried out. It was found out that the target formulation of famotidine PPOP which could release for 24 hours was obtained in a very short period. Meanwhile, the practicability of the established expert system was proved.