Four constitunets were isolated from the flower of Rhododendron molle ( BI. ) G. Don. One of these was named Rdl.The acute LD50 of Rdl in mice ( iv ) was found to be 4742 ug/kg.The hypotensive effect of Rdl was studied in various anesthesized animals. In cats, the dosage of 100, 300 and 500 Hg/kg of the Rdl ( iv ) reduced the blood pressure by 10:9% ( P

Objective To develop a new method with using surgical procedures for multiple correction of nasal deformity with cleft lip and palate.Methods Our operation procedures included elevation of the nasal floor depression in cleft side with the transplantation of autogenous cancellous bone, frustration and elevation of the nasal bone and part of the frontal process of maxilla, and replacement of septum between alar cartilages.Through these procedures, the nasal deformity could be multiply corrected.Results Postoperative follow up for 1～8years in 45 patients demonstrated satisfactory results. Conclusion Multiple correction is a new method of treatment for nasal deformity with cleft lip and palate.

Objective To identify the expressions and distributions of aquaporin-1(AQP 1) and microvessel density(MVD) in human cervical carcinomas and their relationship,and investigate the roles of AQP1 and MVD in human cervical carcinomas. Methods The expressions of AQP1 and MVD in 74 cases of cervical carcinoma(46 cases of squamous-cell carcinoma of the uterine cervix,28 cases of in adenocarcinoma of the uterine cervix),in 34 cases of cervical intraepithelial neoplasia(CIN) and in 15 cases of normal cervices by immunohistochemical technique.Results The expression of AQP1 was found in vascular endothelial cell of CIN,squamous-cell carcinoma and adenocarcinoma of the uterine cervix,with the largest amount in adenocarcinoma and a same amount in CIN and squamous-cell carcinoma of the uterine cervix.There was distinct difference in the intensities of squamous-cell carcinoma,adenocarcinoma of the uterine cervix and control groups.The expression rates of MVD gradually increased with the progress of cervical lesion.There were significant differences between the above 4 groups for MVD(P

Objective To assess the feasibility,safety and efficacy of endoscopic papillectomy (EP) for tumors at the ampulla of Vater (AV).Methods A total of 15 patients with tumor at AV that were indicated for EP were included in this prospective study.Their clinical profiles,procedural parameters and outcome were evaluated.Results All patients underwent EP procedure successfully.Four patients who were diagnosed as having chronic inflammation in the reference endoscopy were confirmed as having adenoma after EP.Out of the 11 patients who were previously diagnosed as andenoma on biopsy,2 of low differentiated adenocarcinoma,1 of well differentiated adenocarcinoma and 1 malignant transformation were pathologically confirmed after EP.Stents were implanted in 8 patients with dilated pancreatic and/or common bile duct.Except for 2 cases of melena and 2 transient elevated level of blood amylase after EP,no other major complications occurred.Three patients,including 1 case of low-differentiated adenocarcinoma,1 case of malignant transformation and 1 case of lesion residual,were referred to surgery,another patient with low-differentiated adenocarcinoma declined any additional intervention because of old age.In the remaining 11 cases ( 11/15,73.3％ ) including one well differentiated adenocarcinoma,no recurrence was observed during a follow-up period of 23.4 (5 to 47) months.Conclusion EP is a minimal invasive,safe and effective treatment for tumors at AV,which also can provide an accurate staging of the lesion.

OBJECTIVETo construct the ferulic acid loaded chitosan microspheres containing liposomes.

METHODFerulic acid was selected to be the model drug. Liposomes were prepared by calcium acetate gradient method. The entrapment efficiency of liposomes was(79.97 +/- 0.54)%, the average size was (187.6 +/- 11.9) nm and the Zeta potential was -12.67 +/-1.78. The chitosan microspheres, whose entrapment efficiency was (57.89 +/- 1.72)%, were prepared by onic gelation method after liposomes were mixed with chiotosan solution. Ferulic acid was entrapped in liposomes in amorphous form and then liposomes were distributed in microspheres intactly.

RESULTThe 80.97% liposomes were released from microspheres and the 32.33% ferulic acid was released from microspheres at 12 h, which was much slower than simple chitosan microspheres.

CONCLUSIONThis study demonstrated that chitosan microspheres containing liposomes have good sustained-releasing property in vitro.

Chemistry, Pharmaceutical ; Chitosan ; chemistry ; Coumaric Acids ; chemistry ; pharmacokinetics ; Delayed-Action Preparations ; chemistry ; pharmacokinetics ; Drug Compounding ; Kinetics ; Liposomes ; chemistry ; Microspheres ; Particle Size

OBJECTIVETo study the pharmacokinetics of tetramethylpyrazine (TMP), ferulic acid and their compatibility.

METHODTwenty-four Sprague-Dawley rats were randomly divided into 3 groups: TMP 20 mg x kg(-1), ferulic acid 20 mg x kg(-1) and TMP 20 mg x kg(-1) + ferulic acid 20 mg x kg(-1). All the rats were given intragastric administration then blood samples were obtained from fossa orbitalis at several time points. All the plasmas concentrations were analyzed by HPLC method and the data were treated by DAS 2.0 program.

RESULTThe main pharmacokinetics parameters of TMP 20 mg x kg(-1) group, ferulic acid 20 mg x kg(-1) and TMP 20 mg x kg(-1) + ferulic acid 20 mg x kg(-1) were as follows: t(max) 0.5 h, t1/2 0.856 h,MRT 1.321 h, AUC 5.112 microg x h(-1) x L(-1), C(max) 2.834 microg x L(-1); t(max) 0.083 h, t1/2 1.024 h, MRT 1.324 h, AUC 1.581 microg x h(-1) x L(-1), C(max) 1.492 microg x L(-1); t(max) 0.583 h, t1/2 37.901 h, MRT 3.798 h, AUC 4.097 microg x h(-1) x L(-1), C(max)1.571 microg x L(-1); t(max) 0.6 h, t1/2 7.860 h, MRT 2.894 h, AUC 1.984 microg x h(-1) x L(-1), C(max) 1.03 microg x L(-1), respectively.

CONCLUSIONThe experiments suggested that the compatibility of TMP and ferulic acid had interaction in pharmacokinetics; all the t1/2 and MRT were prolonged and had the effect of lente liberates.

Animals ; Area Under Curve ; Calibration ; Coumaric Acids ; pharmacokinetics ; Female ; Linear Models ; Pyrazines ; pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Reproducibility of Results

In this paper, the pharmacokinetics of ferulic acid loaded liposome-in-chitosan-microspheres was investigated. Eighteen Sprague-Dawley rats were divided into 3 groups randomly. Each group was administered orally of ferulic acid, ferulic acid loaded chitosan microspheres and ferulic acid loaded liposome-in-chitosan-microspheres, respectively. Then blood samples were obtained from fossa orbitalis at different time points. The concentration of ferulic acid in blood was analyzed by a HPLC method using coumarin as internal standard. The data were analyzed by DAS program. The t(max), MRT and t(1/2beta) of liposome-in-chitosan-microspheres were 2.500, 7.487 and 7.818 h, respectively, which were much longer than crude drug and chitosan microspheres. This results demonstrated that liposome-in-chitosan-microspheres had better sus-tained-releasing property. The AUC of liposome-in-chitosan-microspheres was 6.08 times higher than crude drug and 1.21 times higher than chitosan microspheres, which verified that liposome-in-chitosan-microspheres could enhance oral absorption.
Absorption ; Administration, Oral ; Animals ; Anticoagulants ; administration & dosage ; blood ; pharmacokinetics ; Biocompatible Materials ; Chitosan ; Coumaric Acids ; administration & dosage ; blood ; pharmacokinetics ; Delayed-Action Preparations ; Liposomes ; Male ; Microspheres ; Orbit ; blood supply ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Time Factors

ObjectiveTo observe the treatment effects in 48 cases of advanced lung cancer patients,with the immune therapy of the dendritic cells loading of tumor autologous antigen (DCTAA) combining with the cells induced factor of the killer cells(CIK)from the matched umbilical cord blood cells.MethodsThe peripheral blood mononuclear cell(PBMC)from the matched umbilical cord blood cells was seperated,and induced to CIK and DC with some cytokines in vitro, such as CD3McAb, IL-2, IFN-γ IL-1α, etc. After 12 to 15 days, the amplified CIK cells obtained were obtained, with the strict quality control, infused the CIK cells to the patients body back in six times,about(5-8)×109 CIK cells in each time.In the fifth day of the cultivation,DETAA cells were loaded and DCTAA cells were collected in the eighth day,and then hypodermic injection was done. The patient' s general situation after the immune treatment was observed, such as the size of the tumors, clinical symptom score, the quality of life and immune indexes. Karnofsky score, weight, toxic side effects and the patient's survival were also studied.ResultsIn the 48 cases with the DCTAA-CIK treatment, complete remission (CR), partial remission (PR)was 37 cases, the overall remission rate was 77.1％. The improvement rate of clinical symptom scores was from 78.9 ％ to 84.7 ％, the increasing rate of Karnofsky score was 89.6 ％ (43/48). 1-year survival reached to 80.6 ％. There were significant difference in little toxic side effects(P ＜ 0.01). The proportion of CD3, CD4 and NK cells in peripheral blood cells increased significantly (P ＜ 0.01) after DCTAA-CIK cells treatment[(42.21±6.12)％, (24.42±3.01)％, 0.99±0.34, (24.98±3.02) ％; (71.58±7.64) ％, (37.25±2.13) ％, 1.62±0.45, (35.23±4.11) ％](t = 6.34, 5.67, 0.25, 4.43, P ＜0.01).ConclusionThe DCTAA-CIK immune therapy is benefit for advanced lung cancer,not only improve the immune function but also ameliorate the clinical symptoms.

OBJECTIVETo study the pharmacokinetics of single administration and different compatibility of tetramethylpyrazine (TMP) in rats.

METHODThirty two Sprague-Dawley rats were randomly divided into 4 groups: the TMP (30 mg x kg(-1)) group, the TMP+FA (30 mg x kg(-1) + 50 mg x kg(-1)) group, the TMP+TET (30 mg x kg(-1) mg x kg(-1)) group and the TMP+FA+TET (30 mg x kg(-1) + 50 mg x kg(-1) + 20 mg x kg(-1)) group. After the oral administration, their blood samples were collected to detect plasmas concentrations by HPLC method and to calculate pharmacokinetic parameters DAS 2.0 program.

RESULTIn compatibility with FA, AUC(0-t), Cmax and Tmax showed no significant difference with the single administration of TMP, but t(1/2) and MRT,, were obviously longer than the single administration. In compatibility with TET and FA + TET, AUC (0-t), Cmax and Tmax showed significant increase than the single administration of TMP, whereas t(1/2) and MRT0, did not notably vary from the single administration.

CONCLUSIONFA can prolong TMP's action time in rats, and TET can accelerate TMP's absorption in rats.

Animals ; Chromatography, High Pressure Liquid ; Coumaric Acids ; pharmacokinetics ; Diterpenes ; pharmacokinetics ; Drug Interactions ; Female ; Pyrazines ; pharmacokinetics ; Random Allocation ; Rats ; Rats, Sprague-Dawley

The valaciclovir was used as the model drug, the bovine serum albumin nanoparticles (BSA-NP) were prepared by desolvation process. Glycyrrhizin (GL) was oxidized by sodium periodate to be conjugated to surface reactive amino groups (SRAG) of the VACV-BSA-NP. Gel filtration method combined with HPLC method verified that GL was covalent coupling to the surface of VACV-BSA-NP with mean 9 GL residues per albumin molecule. The mean diameter of the VACV-BSA-NP-GL was 268 +/- 23 nm, the drug loading was 1.35%, and embedding ratio was 68.76%. The characteristics of release in vitro were in accord with two-phase kinetics. The uptake amount of VACV-BSA-NP-GL by primary cultured rat hepatocytes in vitro was higher, compared to the control-VACV-BSA-NP. 69.89% and 64.82% of the VACV were concentrated in liver at 15 min after i.v. VACV-BSA-NP-GL and VACV-BSA-NP, respectively. There is a significant difference between surface-modified group and control group (P<0.10). VACV-BSA-NP-GL was successfully prepared, which is considered to be a novel drug delivery system for targeting to hepatocytes.
Acyclovir ; analogs & derivatives ; pharmacology ; Cells, Cultured ; Drug Delivery Systems ; Glycyrrhizic Acid ; pharmacology ; Hepatocytes ; cytology ; metabolism ; Humans ; Microspheres ; Nanostructures ; Nanotechnology ; Particle Size ; Serum Albumin, Bovine ; pharmacology ; Technology, Pharmaceutical ; methods ; Valine ; analogs & derivatives ; pharmacology