Objectives: Endoscopic variceal ligation is well established metbod of treatment for esophageal varices whereas for gastric varices there has not been any systematic report of its use as a method of treatment. To evaluated its possible clinical application, the band ligation(banding) and the method of band ligation in conjuction with submucosal ethanolamine injection(banding with sclero) were tested on canine stomach, and results were assessed.
Esophageal and Gastric Varices ; Ethanolamine ; Ligation* ; Rubber* ; Stomach

A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.
Animals ; Antineoplastic Agents ; administration & dosage ; chemistry ; Cell Line, Tumor ; Deoxycholic Acid ; chemistry ; Drug Carriers ; chemistry ; Humans ; Male ; Mice ; Neoplasms ; drug therapy ; Phospholipids ; chemistry ; Solubility ; Triterpenes ; administration & dosage ; chemistry

OBJECTIVETo study the selective dilatation effects of iptakalim (Ipt) on basilar and pulmonary arterioles, and endothelial cell function of these arterioles in hypoxic rats.

METHODSSD male rats were divided into 2 groups:control and hypoxic group fed in normobaric hypoxic environment (O2 7.8%, 8 h). Arteriole rings about (204 + 5) pm were isolated and the tension of hypoxic arterioles pre-contracted by 6 nmol/L endothelin-1 (ET-1) was observed with wire myograph system model (DMT 610 m). The relaxing response of hypoxic arterioles induced by different concentration of Ipt were detected and endothelial activity was also tested by acetylcholine.

RESULTS10(5) mol/L acetylcholine (ACh)-mediated vasodilatation of basilar and pulmonary arterioles was greatly reduced in the hypoxic group than those in control group (P < 0.05). Compared with normal group, a novel ATP-sensitive potassium channel opener Ipt at the concentration ranging from 10(-11) mol/L to 10(3) mol/L, caused stronger dose dependent vasodilatation on hypoxic pulmonary arterioles, and there was no significant difference between control and hypoxic basilar arterioles.

CONCLUSIONThe endothelial function of basilar and pulmonary arterioles was damaged under hypoxic state, and Ipt selectively increased dilatation effects on hypoxic pulmonary arterioles, but not on hypoxic basilar arterioles which could improve high altitude pulmonary edema pathological state and be the novel drug in the treatment of pulmonary hypertension.

Acetylcholine ; pharmacology ; Altitude ; Altitude Sickness ; physiopathology ; Animals ; Arterioles ; drug effects ; Dilatation ; Endothelin-1 ; pharmacology ; Hypoxia ; KATP Channels ; drug effects ; Male ; Propylamines ; pharmacology ; Rats ; Vasodilation ; Vasodilator Agents ; pharmacology

Liquid chip technology have been licensed to be used in clinic because of its advantage of high-throughput, high-sensitivity, good signal to noise ratio, reaction in liquid phase, convenient operation and short time consuming, etc. The optimization of a liquid chip system for the detection of serum biomarkers of colorectal tumour and initial application in the detection of CEA were studied. The optimized reaction conditions of liquid chip were determined through orthogonal design after it was prepared. The results showed that the consuming reaction time of the coated antibody and the antigen was 1hour. The microspheres, biotinylated detecion antibody and the consuming complexes and avidin-PE time of the microspheres and the biotinylated tested antibody was 1hour, 1hour and 15minutes respectively.the consuming time of the complexes and avidin-PE was fifteen minutes, The optimized dilution of the biotinylated tested detection antibody was 1∶300 and the optimized concentration of avidin-PE was 12?g/ml. Totally 55 clinical samples were detected by the liquid chip and by Enzyme-Linked Immunosorbent Assay (ELISA) simultaneously and the results of the two methods were compared. The results of the two methods showed good correlation between positive and negative samples but the detection limits and the dynamic ranges of the liquid chip method were more sensitive and wider than those of the ELISA. The multiple tumour biomarkers may be detected simultaneously and the time of clinical test and manpower requirements were reduced by the liquid chip method.

To investigate the absorption kinetics of Cu B-SDC/PLC-MMs in rat different intestinal segments and compared with the absorption of Cu B suspension. The in vitro everted gut sacs model was established to study the absorption characteristics of Cu B-SDC/ PLC-MMs in rat duodenum, jejunum, ileum and colon, and the content of cucurbitacin B was detected by HPLC method, and the effects of concentrations on intestinal absorption were evaluated as well. The results showed that the absorption of Cu B-SDC/PLC-MMs was linearity at different intestine segment and different concentrations (R2 > 0.9), which was consistent with zero order rate process. The Ka of different intestine segments showed a concentration-dependent increasing along with the raised concentration of Cu B-SDC/ PLC-MMs, indicating that it was likely to be a mechanism of passive absorption. The best absorption site of Cu B-SDC/PLC-MMs was ileum, and its absorptions in different intestinal segments were superior to cucurbitacin B suspension. SDC/PLC-MMs could significantly enhance the intestinal absorption of cucurbitacin B, and the study of intestinal absorption kinetics of Cu B-SDC/PLC-MMs had gave a support to its further reasonable solidfication.
Animals ; Deoxycholic Acid ; administration & dosage ; Female ; Intestinal Absorption ; Kinetics ; Male ; Micelles ; Nanoparticles ; Phospholipids ; administration & dosage ; Rats ; Rats, Wistar ; Triterpenes ; administration & dosage ; pharmacokinetics

The experiment's aim was to optimize the processing technology of Xanthii Fructus which through comparing the difference of UPLC fingerprint and contents of toxicity ingredient in water extract of 16 batches of processed sample. The determination condition of UPLC chromatographic and contents of toxicity ingredient were as follows. UPLC chromatographic: ACQUITY BEH C18 column (2.1 mm x 100 mm, 1.7 microm) eluted with the mobile phases of acetonitrile and 0.1% phosphoric acidwater in gradient mode, the flow rate was 0.25 mL x min(-1) and the detection wavelength was set at 327 nm. Contents of toxicity ingredient: Agilent TC-C18 column (4.6 mm x 250 mm, 5 microm), mobile phase was methanol-0.01 mol x L(-1) sodium dihydrogen phosphate (35: 65), flow rate was 1.0 mL x min(-1), and detection wavelength was 203 nm. The chromatographic fingerprints 16 batches of samples were analyzed in using the similarity evaluation system of chromatographic, fingerprint of traditional Chinese medicine, SPSS16.0 and SIMCA13.0 software, respectively. The similarity degrees of the 16 batches samples were more than 0.97, all the samples were classified into four categories, and the PCA showed that the peak area of chlorogenic acid, 3,5-dicaffeoylquinic acid and caffeic acid were significantly effect index in fingerprint of processed Xanthii Fructus sample. The outcome of determination showed that the toxicity ingredient contents of all samples reduced significantly after processing. This method can be used in optimizing the processing technology of Xanthii Fructus.
Caffeic Acids ; analysis ; toxicity ; Chemistry, Pharmaceutical ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; toxicity ; Quinic Acid ; analogs & derivatives ; analysis ; toxicity ; Xanthium ; chemistry ; classification

To study the influence of stir-baked with sand on active ingredients, diarrhea and hepatoprotection of Herpetospermum caudigerum, the contents of herperione and herpetin in H. caudigerum before and after stir-baking with sand were analyzed by HPLC. The effect of stir-baked with sand on diarrhea of H. caudigerum TL was evaluated using the mean stool rate (MSR) and mean diarrheal index ( MDI) and the influence of stir-baked with sand on hepatoprotective effect of H. caudigerum TL was examined using a mouse model of CCl4-induced liver injury based on the analysis of serum ALT and AST activities. The results of HPLC analysis showed the content of herperione in H. caudigerum after stir-baking with sand decreased by 40.9% (P < 0.01) and the content of herpetin had no change. Pharmacodynamic results showed that the MSR and MDI of high-dose and middle-dose group of H. caudigerum TL after stir-baking with sand were significantly lower than that of high-dose and middle-dose group of H. caudigerum TL without stir-baking with sand; The high-dose and middle-dose of H. caudigerum TL with/without stir-baking with sand significantly alleviated liver injury as indicated by the decreased levels of serum ALT and AST, but the ALT and AST levels of high-dose and middle-dose group of H. caudigerum TL after stir-baking with sand were higher than that of H. caudigerum TL without stir-baking with sand. The results revealed that the stir-baking with sand could effectively relieve diarrhea effect of H. caudigerum TL, while it also reduces the hepatoprotection of H. caudigerum TL.
Animals ; Chromatography, High Pressure Liquid ; Cooking ; Cucurbitaceae ; chemistry ; Diarrhea ; chemically induced ; Female ; Liver ; drug effects ; Male ; Mice ; Protective Agents ; pharmacology

No abstract available.
Carcinoma, Non-Small-Cell Lung* ; Drug Therapy, Combination*

To study the effect of steaming and baking process on contents of alkaloids in Aconite Lateralis Radix (Fuzi), 13 alkaloids were analyzed by UPLC-MS/MS equipped with ESI ion source in MRM mode. In steaming process, the contents of diester-diterpenoid alkaloids decreased rapidly, the contents of monoester-diterpenoid alkaloids firstly increased, reached the peak at 40 min, and then deceased gradually. The contents of aconine alkaloids (mesaconine, aconine and hypaconine) increased all the time during processing, while the contents of fuziline, songorine, karacoline, salsolionl were stable or slightly decreased. In baking process, dynamic variations of alkaloids were different from that in the steaming process. Diester-diterpenoid alkaloids were degraded slightly slower than in steaming process. Monoester-diterpenoid alkaloids, aconine alkaloids and the total alkaloids had been destroyed at different degrees, their contents were significantly lower than the ones in steaming Fuzi at the same processing time. This experiment revealed the dynamic variations of alkaloids in the course of steaming and baking. Two processing methods which can both effectively remove the toxic ingredients and retain the active ingredients are simple and controllable, and are valuable for popularization and application.
Aconitine ; analogs & derivatives ; isolation & purification ; Aconitum ; chemistry ; Alkaloids ; isolation & purification ; Chromatography, High Pressure Liquid ; Drug Stability ; Drugs, Chinese Herbal ; isolation & purification ; Hot Temperature ; Plant Extracts ; isolation & purification ; Steam ; Tandem Mass Spectrometry ; Time Factors

To explore the feasibility of chemical and biological method in evaluation of the in vitro dissolution rate of Liuwei Wuling tablet (LWT), this experiment investigated the inhibitory effect of LWT dissolving solutions on LX-2 hepatic stellate cells in 0.1% SDS dissolution medium in different dissolving periods. From these results, the cumulative dissolution rate of LWT was obtained based on the cell inhibitory rate. The dissolution rates of deoxyschizandrin, phillyrin, and Specnuezhenide were determined by HPLC method. A novel approach of self-defined weighting coefficient had been created to establish the integrated dissolution rate model. Then f2 similar factor method was used to evaluate the relevance of these two methods. The results showed that f2 values for deoxyschizandrin, phillyrin, Specnuezhenide, and the integrated dissolution were 61, 43, 61 and 75 respectively, indicating that the dissolution of multi-component integration could fully reflect the biological potency of the whole recipe. The dissolution evaluation method for multicomponent integration based on biological activity is expected to be one of the effective means for in vitro dissolution test of LWT.
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; Kinetics ; Quality Control ; Solubility ; Tablets ; chemistry