OBJECTIVE: To establish a HPLC method for the determination of content of entecavir and its related substances. METHODS: The HPLC condition was consisted of a Luna C18 column with a column temperature at 25 ℃, using gradient eluate method, the mobile phase was acetonitrile,with a flow rate of 1.0 mL?min-1 and detection at 254 nm. RESULTS: The calibrated linear curve of entecavir was within 0.033 45～0.167 2 mg?mL-1(r=0.999 98). The average recovery was 100.09%,RSD=0.20%, The content of related substance was 0.54%～1.48%. CONCLUSION: This accurate and reliable HPLC method is applicable for the quality control of entecavir and its related substances.

Objective To examine HOXA11,ER and PR expression in human endometrial hyperplasia and adenocarcinoma.Methods The immunohistochemistry was applied to analyze the level of HOXA11、ER and PR expression in the proliferative endometria,simple hyperplasia and endometrial adenocarcinoma.Results The expression level of HOXA11 in the endometrial hyperplasia and adenocarcinoma was significantly higher than that of proliferative endometrium(P

Aim To determine whether AngⅡin para-ventricular nucleus (PVN)was involved in the chronic intermittent hypoxia (CIH ) induced-hypertension in rats.Methods Male Sprague-Dawley rats were ran-domly divided into Sham and CIH groups,the Sham rats were exposed to continuous normoxia,while the CIH rats were submitted to CIH (8 h per day for 15 days).The conscious noninvasive method with tail cuff was performed in rats to record the systolic blood pres-sure during establishing the model of CIH induced hy-pertension.Mean arterial pressure (MAP)and heart rate (HR)were recorded in vivo on a PowerLab data acquisition system after CIH.Rats were fixed on the stereotaxic instrument to conduct microinjection in the PVN.We used Western blot to measure Ang Ⅱ level and AngⅡtype 1 receptor (AT1 R)protein expression in PVN.Results The level of PVN Ang Ⅱin CIH rats was significantly higher than that in Sham rats,a-long with increased AT1 R protein expression.Microin-jection of Ang Ⅱ(0.03,0.3,3 nmol)in bilateral PVN dose-dependently increased MAP in both CIH and Sham rats,and this response was significantly augmen-ted in CIH rats.Losartan (50 nmol),AT1 R antago-nist,had no effect on MAP in Sham rats,but caused significant MAP decreases in CIH rats,and prevented Ang Ⅱ-induced increases in MAP in both CIH and Sham rats.Conclusion The results suggest that the increased AngⅡrelease and enhanced AT1 R activation in the PVN contribute to CIH induced-hypertension in rats.

OBJECTIVE:To establish an RP-HPLC method for content determination of s-omeprazole sodium and its related substances.METHODS:The separation of s-omeprazole sodium and the related substances was carried out on a Phenomenex Luna C18 column,the mobile phase consisted of methanol-0.033 mol?L-1 ammonium dihydrogen phosphate-triethylamine (58∶41.8∶0.2,adjusted to pH 7.0 by phosphate acid).The detection wavelength was 302 nm,the flow rate was 1.0 mL?min-1,the column temperature was 25 ℃,and the sample size was 20 ?L.RESULTS:The linear range of omeprazole sodium was 10～500 mg?L-1 (r=0.999 7).The average recovery rate was 100.27% (RSD=0.74%).The average content of the related substances in samples was 0.42%.CONCLUSION:This method is simple,accurate,specific and applicable for content determination of s-omeprazole sodium and its related substances.

OBJECTIVE:To establishment the method for the determination of content of vitamin A palmitate(VAP) and its related substances by HPLC. METHODS:The HPLC conditions were consisted of Phenomenex Luna C18 column with a mobile phase of a mixture of acetonitrile-isopropanol (90∶10) ,the detection wavelength of 328 nm,the column temperature of 30 ℃ and the flow rate of 1.0 mL?min-1. RESULTS:VAP was completely separated from impurities,the linearity range was 90～400 mg?L-1(r=0.999 2). The average recovery rate was 99.60% (RSD=1.32%). The average content of the related substances were lower than 2.53% . CONCLUSION: This accurate and reliable HPLC method is applicable for the quality control of VAP.

Aim To study the effect of pectin-adriamy-cin conjugate ( PAC) on cardiac toxicity .Methods 50 female SD rats were randomly divided into 5 groups with 10 animals in each group .Adriamycin ( ADM ) group received 3 mg? kg -1 , ip, every other day for 6 times.PAC group received ADM equivalent 1.5,3 and 6 mg? kg -1 , ip, every other day for 6 times.Control group received normal saline parallel to ADM .Rats were sacrificed and the echocardiogram , cardiac en-zymes , the oxidative stress levels in myocardial cells and histopathological changes after 48 h administration were detected.S180 ascites tumor bearing mice models were established to investigate the antitumor activity of PAC.Results The survival rate of ADM group was 50% and that of PAC each group was 100%.PAC could significantly increase body weight ,heart index and immune index and increase HR ,EF,FS,reduce LVIDd, LVIDs.PAC could also significantly increase the AST , LDH, CK, CK-MB level in serum .GSH-Px and SOD activities of PAC group were significantly increased and MDA contents were reduced , and histopathological changes decreased .PAC could effectively inhibit the growth of tumor cells and extend the survival period of mice.Conclusion PAC induces a significant reduc-tion in cardiotoxicity by increasing survival rate , im-mune and cardiac function , improving cardiac en-zymes ,oxidative stress and myocardial cell injury , and also PAC has obvious antitumor effect .

Pectin, a polysaccharide extracted from the cell wall of plants, was used as the drug carrier to synthesize the pectin-adriamycin conjugates (P(A)n). The structure of the conjugates was confirmed by UV and IR. The degree of esterification (DE) of the pectin was assessed, and it was found that DE significantly influenced the carboxy group contents, inherent viscosity and galacturonic acid contents of the pectin. The results of drug release test in vitro showed that the conjugate was stable in normal saline, but was gradually enzymolyzed to release the adriamycin in blood plasma and in lymph nodes. The results of lymphatic targeting study of P(A), demonstrated that the modification of DE or drug coupling capacity of pectin significantly influenced the lymphatic targeting characteristics of P (A)n. The adriamycin concentration of lymph nodes was 208 times higher than that of plasma after local injection of the P(A)n, of which the adriamycin content was 27.9% and the pectin was deesterificated 120 minutes by the use of hypothermy alkaline deesterification method.
Animals ; Antibiotics, Antineoplastic ; administration & dosage ; pharmacokinetics ; Doxorubicin ; administration & dosage ; pharmacokinetics ; Drug Carriers ; chemistry ; Esterification ; Lymph Nodes ; metabolism ; Pectins ; administration & dosage ; pharmacokinetics ; Rabbits

Bupivacaine is a long-acting local anesthetic widely used clinically,but its 6-8 hours duration is insufficient for postoperative analgesia.Designing drug dosage forms to prolong the action time of local anesthetics is the research content of local anesthetics.In 2011,the FDA approved a bupivacaine liposome preparation based on DepoFoam TM technology:Exparel,which can be used for more than 72 hours.This article reviewed the clinical safety research of Exparel and the research progress of its application in clinical postoperative analgesia.