To prepare rivastigmine liposome, rivastigmine was loaded into liposome via ammonium sulfate gradient method. Its pharmacokinetic profile in rats was evaluated after intranasal administration. The size, zeta potential, entrapped efficiency and release of rivastigmine from the liposome in vitro were determined. Plasma concentration of rivastigmine was determined by high performance liquid chromatography-tandem mass spectrometry (HPLC/MS) using antipyrine as internal standard. The pharmacokinetic parameters were calculated by DAS 2.0. The entrapped efficiency of rivastigmine liposome was (33.41 +/- 6.58) %, with the mean diameter of 154-236 nm and zeta potential of (-10.47 +/- 2.41) mV. The release behavior of rivastigmine was fitting the first order equation in vitro. The pharmacokinetic studies indicated that the C(max), T(max) and AUC(0-infinity), of rivastigmine liposome were (1.50 +/- 0.15) mg x L(-1), 15 min and (89.06 +/- 8.30) mg x L(-') x min, respectively. Rivastimine liposome was absorbed rapidly, and could reach a certain concentration in rat plasma after intranasal delivery.

Chronic Disease ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Liver Diseases ; drug therapy

Objective Study the diagnostic value of CT to assess the transfer of right recurrent nerve nodes(RRNN) on the thoracic esophageal squamous carcinoma,so as to provide reference for thoracic segment esophageal surgery way.Methods A retrospective analysis from January 2011 to February 2014 in the first affiliated hospital of zhengzhou university at the records of 132 cases of thoracic segment esophageal thoracic surgery with preoperative CT image data,recorded each patient's right recurrent nerve nodes in the largest length to diameter and the average CT number,and compared with postoperative pathologic results.Results With the ROC curve analysis,considering transfer when the length of RRNN' s diameter 8.5 mm or more in CT,the area under the curve is 0.911,the sensitivity is 85.7％,specificity is 78.8％.Considering transfer when the RRNN average CT number acuity 32.50 HU,the area under the curve is 0.815,the sensitivity is 85.7％,specificity is 76.9％.Whether RRNN transfer has significant correlation(P ＜ 0.05) with the length of tumor,tumor location and whether lymph node of other station transfer,doesn' t have significant correlation (P ＞ 0.05)with patients'age,sex,tumor differentiation degree and the T stage.Conclusion When the RRNN length to diameter 8.5 mm or RRNN average CT numberr acuity 32.50 HU,right recurrent nerve nodes should be considered lymph node metastasis,and choose chest conclusion laparoscopic radical prostatectomy.The upper thoracic portion esophageal tumor's length is 5 cm or more,or clinical suspected lymph node metastasis of other station is the risk factor for metastasis of RRNN.

Objective To summarize the placement, maintenance, and safety of a high-pressure resistant peripherally inserted central catheter. Methods Ten patients were peripherally placed with this catheter (included 4Fr-single lumen, 5Fr-dual lumen, and 6Fr-three lumen) using ultrasound-guided Seldinger technique in Peking Union Medical College Hospital in August 2010. The therapeutic effectiveness and safety were evaluated. Result Ten catheters were inserted successfully into the upper arms, with few complications noted during routine maintenance. Conclusions This peripherally inserted central catheter can be used for high-pressure injection, central venous pressure monitoring, and fast flow-speed transfusion. Therefore, it can be successfully applied for contrast-enhanced CT angiography and massive fluid infusion.

OBJECTIVETo study the correlation between TCM syndrome type and liver tissue pathological changes in patients with chronic hepatitis B (CHB) in order to provide evidence for syndrome differentiation.

METHODSSyndrome typing as well as liver pathological grading and staging of liver biopsy were performed on 260 patients with CHB, then the relationship between them was analyzed.

RESULTS(1) The grade of liver inflammation was mainly G1 and G2 in patients of Gan-qi stagnation and Pi-deficiency type (type 1); G2 in patients of inner damp-heat retention type (type II); G3 in patients of Gan-Shen yin-deficiency type (type lII) and Pi-Shen yang-deficiency type (type IV); while G4 occurred mainly in patients of blood stasis blocking collateral type (type V), showing significant difference as compared with other syndrome types. (2) The liver pathological stage in patients of type I and II was mainly S1 and S2, while S3 and S4 occurred mainly in patients of type III and type IV. (3) The pathological change was mainly G3-G4 and S3-S4 in blood stasis syndrome, while it was mainly G1-G2 and S1-S2 in non-blood stasis syndrome.

CONCLUSIONThe TCM syndrome type is correlated with liver tissue pathological change to certain extent, among them, syndrome with or without blood stasis showed the closest correlation. The syndrome type of CHB patients developed, along with the aggravating of liver pathological injury, from sthenia to asthenia, from qi to blood, and finally to the blood stasis blocking collateral. So the treatment should be lay stress on activating blood circulation to remove stasis, and be implemented by 3 stages.

Adult ; Diagnosis, Differential ; Female ; Hepatitis B, Chronic ; diagnosis ; pathology ; Humans ; Liver ; pathology ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Syndrome ; Yang Deficiency ; pathology ; Yin Deficiency ; pathology ; Young Adult

Objective To investigate the sensitizing effects and the mechanisms of selective cyclooxygenase-2(COX-2)inhibitor celecoxib on radiotherapy of pancreatic cancer.Methods Radiosen- sitization of celecoxib in pancreatic cancer cell SW1990 in vivo and in vitro were investigated by colony forming assay and xenograft tumor model.Expressions of proliferating cell nuclear antigen(PCNA)and Cyelin D1 were assessed by Western Blot.Effect on apoptosis was studied by TUNEL.Expression of bcl-2 and bax was assayed by RT-PCR.Expression and secretion of matrix metalloproteinases(MMPs) and tissue inhibitors of metalloproteinases(TIMPs)were assessed by RT-PCR and zymography.Results Celecoxib enhanced the effect of radiotherapy on pancreatic cancer in vitro and in vivo.TUNEL demonstrated a significant increase of apoptotic cells in vitro after treatment with celecoxib alone or com bined with radiation,but no change after radiation.Expression of bcl-2 was decreased by celecoxib;radi- ation induced the expression of bcl-2;combination of celecoxib and radiation significantly suppressed the expression of bcl-2.In vitro,angiogenesis and cell invasion potential of pancreatic cancer cells were in- hibited by celecoxib,and celecoxib combined with radiation,but without significant change in radiation group compared with the control group.Expression and secretion of MMP-2 and MMP-9 were closely related to the changes in angiogenesis and cell invasion potential,while the expressions of TIMP-1 and TIMP-2 did not alter significantly in all groups.Conclusions The selective eyclooxygenase 2 inhibitor celecoxib potently enhances the effect of radiation on the treatment of pancreatic cancer. Induction of apoptosis,inhibition of angiogenesis and invasion are involved in the mechanism of cele- coxib treatment.

Objective To investigate the clinical value of Hangzhou Criteria in selection of patients with hepatocellular carcinoma(HCC)for living donor liver transplantation(LDLT)and their effects on recipient's post-transplant survival.Methods A retrospective analysis was conducted on 43 patients with HCC who underwent LDLT in our center.All of the recipients were classified into subgroups according to Milan Criteria,Up-to-Seven Criteria and Hangzhou Criteria,and post-transplant total survival rate and tumor-free survival rate were compared among the criteria.Results The number of patients within Hangzhou Criteria was 61.5 %(8/13)more than that within Milan Criteria and 23.5 %(4/17)more than that within Up-to-Seven Criteria.The 1-,and 3-years total survival rate and tumor-free survival rate of the recipients within Milan Criteria(n=13)were 100 %,80.0 % and 84.6 %,84.6 %,those of the recipients within Up-to-Seven Criteria(n=17)were 100 %,75.2 % and 87.5 %,81.2 %,and those of the recipients within Hangzhou Criteria(n=21)were 100 %,80.0 % and 89.5 %,84.2 %,respectively.There was no significant difference among the three criteria in total survival rate and tumor-free survival rate(P>0.05).Conclusion Hangzhou Criteria further enrolled more liver transplantation candidates without decline of total survival rate and tumor-free survival.It is a more effective selection of HCC recipients for LDLT.

Objective To evaluate the accuracy and clinical application of endoscopic ultrasound guided fine needle aspiration (EUS-FNA) in diagnosis of occupying lesions in upper digestive tract and its pe-ripheral areas. Methods The data of 64 patients who underwent EUS-FNA for occupying lesions in upper di-gestive tract, between July 2006 and December 2007, were retrospectively analyzed. Results EUS-FNA was successfully performed on 62 patients, with a success rate of 96.88%. The overall diagnostic accuracy, sensi-tivity, specificity, positive predictive value and negative predictive value of EUS-FNA for occupying lesions in upper digestive tract and its peripheral areas were 88.71%, 86.54%, 100.00%, 100.00%, and 58.82%, respectively. There was no significant difference between the foei larger and smaller than 3cm (P > 0.05), re-garding the diagnostic accuracy and average puncture numbers. Diagnostic accuracy of those with real-time cy-tolngical evaluation was significantly higher than those without (P=0.029), and the puncture numbers were less (P=0.001). Among the total 99 punctures, the positive diagnostic accuracy of those with 5ml negative pressure suction was significantly higher than those of 10 ml (P = 0.044). Conclusion EUS-FNA is a safe and applicable approach to diagnosis of occupying lesions in upper digestive tract and its peripheral areas with higher diagnostic accuracy, sensitivity, specificity and positive predictive value. Moreover, the real-time cyto-logical evaluation and adequate negative pressure might facilitate the diagnosis accuracy.

OBJECTIVETo study the therapeutic effects and mechanism of Jiechangning (JCN) decoction on carrageenan induced experimental ulcerative colitis (UC).

METHODSAfter sensitizing guinea pigs with carrageenan, we established UC animal models by free drinking water containing 2% acid degraded carrageenan (ADC). JCN decoction was orally administered once a day for 2 weeks after carrageenan treatment. Salicylazosulfapyridine (SASP) and normal saline were given to the other two groups as control. The levels of colon lipid peroxide (LPO), acid phosphatase (ACP) activity and tumor necrosis factor-alpha (TNF-alpha) were measured; colitis activity score (CAS) was carried out for assessment of the degree of tissue inflammation and injury; the colonic pathological changes were examined simultaneously with hematoxylin and eosin (HE) and toluidine blue staining used to evaluate the therapeutic effects of JCN decoction and SASP.

RESULTSExperimental colitis models resembling human UC were successfully induced. The levels of tissue LPO, ACP activity and the content of tissue TNF-alpha were markedly increased in the model group as compared with the normal control group (P < 0.01) and were positively correlated with CAS. JCN decoction could reverse these changes like SASP. HE staining showed that JCN decoction and SASP could reduce CAS and the degree of tissue injury, toluidine blue staining revealed that mucosa and submucosa red metachromasia pellets in JCN group and SASP group were markedly fewer than those in the model group.

CONCLUSIONJCN decoction is effective in treating experimental UC, which provides theoretical basis for its clinical application.

Acid Phosphatase ; metabolism ; Animals ; Carrageenan ; Colitis, Ulcerative ; chemically induced ; metabolism ; pathology ; Colon ; drug effects ; metabolism ; pathology ; Gastrointestinal Agents ; pharmacology ; Guinea Pigs ; Lipid Peroxides ; metabolism ; Male ; Medicine, Chinese Traditional ; Plant Preparations ; pharmacology ; Sulfasalazine ; pharmacology ; Tumor Necrosis Factor-alpha ; metabolism

To prepare rivastigmine liposome, rivastigmine was loaded into liposome via ammonium sulfate gradient method. Its pharmacokinetic profile in rats was evaluated after intranasal administration. The size, zeta potential, entrapped efficiency and release of rivastigmine from the liposome in vitro were determined. Plasma concentration of rivastigmine was determined by high performance liquid chromatography-tandem mass spectrometry (HPLC/MS) using antipyrine as internal standard. The pharmacokinetic parameters were calculated by DAS 2.0. The entrapped efficiency of rivastigmine liposome was (33.41 +/- 6.58) %, with the mean diameter of 154-236 nm and zeta potential of (-10.47 +/- 2.41) mV. The release behavior of rivastigmine was fitting the first order equation in vitro. The pharmacokinetic studies indicated that the C(max), T(max) and AUC(0-infinity), of rivastigmine liposome were (1.50 +/- 0.15) mg x L(-1), 15 min and (89.06 +/- 8.30) mg x L(-') x min, respectively. Rivastimine liposome was absorbed rapidly, and could reach a certain concentration in rat plasma after intranasal delivery.
Administration, Intranasal ; Animals ; Area Under Curve ; Chromatography, Liquid ; Drug Carriers ; Drug Compounding ; Liposomes ; Male ; Neuroprotective Agents ; administration & dosage ; blood ; chemistry ; pharmacokinetics ; Particle Size ; Phenylcarbamates ; administration & dosage ; blood ; chemistry ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Rivastigmine ; Tandem Mass Spectrometry