OBJECTIVE: To evaluate the bioequivalence of domestic sirolimus capsules and commercially available sirolimus oral solution in healthy Chinese volunteers. METHODS: Twenty-two healthy Chinese male volunteers were enrolled and orally administered 5 mg sirolimus capsules or oral solution randomly. The concentrations of sirolimus in whole blood were determined by LC-MS/MS. RESULTS: The pharmacokinetic parameters of sirolimus capsules and oral solution were as following: ρmax(26.62 ± 9.97) and (25.28 ± 5.98) ng · mL-1; tmax(2.27 ± 0.55) and. (1.91 ± 2.33) h; t1/2 (73.07 ± 13.81) and (65.49 ± 17.00) h; AUC0-t (372.3 ± 146.2) and (368.2 ± 275.0) ng middot; h middot; mL-1, AUC0-∞ (466.8 ± 194.3) and (442.3 ± 324.4) ng middot; h middot; mL-1, respectively. The relative bioavailability F0-t was (112.4 ± 34.61)% and F0-∞ was (117.2 ± 39.93)%. Two-sided t-test of ρmax, AUC0-t and AUC0-∞ indicated that the preparations were equivalent, and non-parametric test showed that sirolimus capsules had larger tmax than the reference preparation with a significant difference (P < 0.05). CONCLUSION: The domestic sirolimus capsule is bioequivalent to the marketed sirolimus oral solution with significantly different tmax. Copyright 2012 by the Chinese Pharmaceutical Association.

By the breeding model of physics mutagenests (60Co,UV light) and re-strong in the body of insects, We obtained a Bt strain Bt99985 with high insecticidal activity. The shake flask and 40t tank fermentation tests showed that, this strain showed special activity against Spodoptera exjgua, Comparing with original Bt strain: 93005, CK strain: HD-1-580 and GC-91, the value of potency increased respectively by 429%, 655% and 114% in shake flask test. Comparing with GC-91, the value of potency increased by 180% in 40t tank fermentation test.

Objective To explore the establishment method of brain ischemia model with blood stasis. Methods The rat models of blood stasis were established by intramuscular injection of dexamethasone 0.2 mg?kg-1?d-1 inside the thigh for successive 10 d. When the blood stasis models were successfully established, the rats were anaesthetized and common carotid arteries in both sides were separated and ligated to make brain ischemia model. Meanwhile the blank control group and Sham-operation to one of the model groups were conducted. Results Compared with the blank control group, the level of whole blood viscosity were obviously increased and TT、PT、APTT markedly decreased in the operation group and pseudo-operation group. Compared with the blank control group and the operation group, the changes of ATP activity,the LD ,LDH ,NO,NOS, SOD,MDA, Glu, T-AA, ET and CGRP levels were significant in the pseudo operation group(P

Objective:To establish an HPLC method to determine the content of schaftoside in Jinshaniu Huashi tablets .Meth-ods:The separation was performed on an Agilent ZORBAX SB-C18 column(150 mm ×4.6 mm, 5 μm)with 0.2% phosphoric acid-acetonitrile as the mobile phase with gradient elution at a flow rate of 1.0 ml· min-1 .The detection wavelength was set at 272 nm, and the column temperature was set at 25 ℃.Results: The calibration curve of schaftoside had a good linearity within the range of 4.58-183.15 μg· ml-1(r=1.000 0).The average recovery was 99.65%with RSD of 1.09%(n=6).Conclusion:The established method is simple and accurate with high repeatability , which can be used for the content determination of schaftoside in Jinshaniu Hua-shi tablets .

Objective:To analyze the role of preoperative circulating tumor cell(CTC) and circulating tumor vascular endothelial cells (CTEC) in the diagnosis of gastric cancer and its correlation with the clinicopathological characteristics of gastric cancer.Methods:Sixty-two gastric cancer patients and 11 patients of benign gastric diseases were enrolled. Subtraction enrichment (SE) and immunofluorescence staining-chromosome fluorescence in situ hybridization (i·FISH) were used to integrate the unique SE-i ·FISH technology platform detecting patients′ CTC and CTEC.Results:The number of CTC in the gastric cancer group was significantly higher than that in the control group ( t=2.693, P=0.009); the number of CTEC in the gastric cancer group was higher than the control group ( t=2.015, P=0.048). With the cut-off value being set at 9 cells/6 ml in blood, the sensitivity of CTC in the diagnosis of gastric cancer is 84%, and the specificity is 82% (AUC=0.876, 95% CI, 0.792-0.963, P<0.01); When set at 6 cells/6 ml, the sensitivity of CTEC in the diagnosis of gastric cancer is 50%, and the specificity is 100%(AUC=0.727, 95% CI, 0.603-0.851, P=0.02). CTC positive is closely related to tumor location(χ 2=4.292, P=0.038 ) and TNM stage(CTC≥10, χ 2=4.848, P=0.028; CTC≥11, χ 2=6.234, P=0.013). CTEC positive is closely related to serum CA19-9(χ 2=4.858, P=0.028) and serum CA724 (χ 2=4.108, P=0.043 ) . Conclusion:SE-i·FISH technology has high sensitivity and specificity in the detection of CTC and CTEC of gastric cancer.

Animals ; Animals, Newborn ; Carbon Monoxide ; metabolism ; Heme Oxygenase (Decyclizing) ; metabolism ; Lung ; metabolism ; Oxygen ; physiology ; Rats

Animals ; Humans ; Influenza A virus ; genetics ; immunology ; Influenza Vaccines ; administration & dosage ; genetics ; immunology ; Influenza, Human ; prevention & control ; virology ; Vaccines, Virus-Like Particle ; administration & dosage ; genetics ; immunology

OBJECTIVETo observe and identify the effect of Jiangya Maijing Liquid (JYMJL) on spontaneous hypertension rats (SHR) fed with high lipid diet in antagonizing hypertension and hyperlipidemia and improving pathological changes of kidney.

METHODSForty-two SHR were divided into 5 groups, except Group A, the Groups B-E were fed with high lipid diet, and Group C, D and E was treated with JYMJL, western drug and Niuhuang Jiangya pill respectively. Besides, Group F was set up for control with normal rats fed by normal diet. The changes of blood pressure (BP), biological indices and renal pathology were observed in the 14 weeks' period of observation.

RESULTS(1) BP raised significantly in Group A and B, it became stable in Group C from the 5th week on and was lower than the BP in other groups (P < 0.01). BP in Group F was not changed; (2) The highest level of nitric oxide (NO) was shown in Group F, and that in Group B and E was lower than that in Group C and D; (3) Level of cholesterol was lower in Group A and F than that in Group C, D and E (P < 0.01), and that in Group C was lower than that in Group B and E (P < 0.01 and P < 0.05 respectively); (4) Pathologic examination on kidney showed that no change was found in Group F, the most severe change was shown in Group B among Group B-E, and the improvement after treatment in Group C was better than that in group B (P < 0.01).

CONCLUSION(1) Condition of disease in rats with hypertension complicated with hyperlipidemia was more severe than that with simple hypertension; (2) JYMJL could restrain the developing of hypertension in SHR, the mechanism may be related with the raising of NO; (3) JYMJL has effect of lowering blood lipid; (4) JYMJL has kidney protective effect, it could alleviate the pathological changes in kidney by way of lowering BP and blood lipid.

Animals ; Antihypertensive Agents ; pharmacology ; Dietary Fats ; administration & dosage ; Drugs, Chinese Herbal ; pharmacology ; Female ; Hyperlipidemias ; etiology ; pathology ; Hypertension ; complications ; pathology ; Hypolipidemic Agents ; pharmacology ; Kidney ; pathology ; Male ; Phytotherapy ; Rats ; Rats, Inbred SHR ; Rats, Inbred WKY

OBJECTIVETo observe the effect of garlicin on adhension molecules CD11a and deformability of peripheral neutrophil in patients with acute cerebral infarction (ACI).

METHODSNeutrophils were separated from peripheral blood of healthy subjects and ACI patients, and incubated in 37 degrees C in vitro. The CD11a expression was detected by antibody fluorescence labeling method and the time of neutrophils passing millipore membrane were measured for calculation of the filter index.

RESULTSCD11a expression rate in healthy subjects was 34.64 +/- 25.34%, while in patients was 55.35 +/- 30.54%, difference between them was significant (P < 0.05). After garlicin treatment, it lowered to 49.16 +/- 31.68%, as compared with untreated group, P < 0.05. The neutrophil filter index in healthy group, untreated group, garlicin treated group and Nimodipine treated group was 0.87 +/- 0.46, 6.42 +/- 6.40, 3.47 +/- 3.67 and 5.03 +/- 3.72 respectively, comparison between that in the garlicin treated group and in untreated group showed significant difference (P < 0.05).

CONCLUSIONGarlicin could effectively inhibit the CD11a expression in peripheral blood neutrophils and improve the deformability of the neutrophils in ACI patients.

Aged ; Allyl Compounds ; pharmacology ; CD11a Antigen ; biosynthesis ; Cell Adhesion ; drug effects ; Cell Separation ; Cerebral Infarction ; blood ; Disulfides ; pharmacology ; Erythrocyte Deformability ; drug effects ; Female ; Garlic ; chemistry ; Humans ; Male ; Middle Aged ; Neutrophils ; physiology

Adult ; Hepatitis, Viral, Human ; complications ; Histiocytic Sarcoma ; complications ; Humans ; Male