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 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 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 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

Nitric oxide (NO), which is involved in the regulation of the cardiovascular system, nervous system, immune system, reproductive system, digestive system and other physiological activities, is an important biological substance with activity. Under normal physiological conditions, neuronal nitric oxide synthase (nNOS) can precisely regulate the nervous system NO production, release, diffusion and inactivation processes. But an excess of NO associates with the development of cerebral ischemia, Alzheimer's and Parkinson's psychosis nervous system diseases, while inhibition of nNOS activity can regulate the content of NO in vivo, and produce a therapeutic effect on some of the nervous system diseases. This review mainly describes the structure and regulation of nNOS and recent developments of small molecule inhibitors of nNOS.
Alzheimer Disease ; physiopathology ; Brain Ischemia ; physiopathology ; Humans ; Nitric Oxide ; metabolism ; Nitric Oxide Synthase Type I ; antagonists & inhibitors ; metabolism ; Parkinson Disease ; physiopathology

Objective By observing the effect of Xiaoyuhuatan decoction on insulin resistance in rar with nonalchoholic fatty liver,the author made a reasearch into this herb'S machanism on cambating on nonalchoholic fatty liver.Methods The insulin resistance rat model was fed by high fat forage and Dongbaogantai control group was set up for the sake of comparion.We determined the contents of total cholesterol(TC),triglyceride(TG),free fatty acid(FFA),fasting plasma glucose(FBG),fasting serum insulin(INS)in serum and the contents of TC,TG of liver tissue homogenate of each group,and the degree of hepatocytic steatosis.Results Xiaoyuhuatan decoction could obviously decrease the index of insulin resistance and improve insulin insensitive index.Lipid in blood serum and hepatic tissues were significantly decreased,liver fat cell denaturation was improved.Conclusion The thrapentic eftect of Xiaoyuhuatan Decoction on fatty liver is probably contribute tO this herb's mechanism of improving insulin resistance and increasing insulin insensitive.

To provide the basis for preparation of diagnostic kits and vaccines in Toxoplasma gondii infection, the gene coding for the qualified recombinant p30 protein (SAG1) of this parasite was amplified by PCR, and the amplified gene was cloned into prokaryotic expression vector pET-30a(+) to construct the recombinant plasmid, and then transformed to E.coli DH5α. The positive recombinant plasmid was screened by PCR and double enzymes digestion, and the nucleotide sequence of p30 gene was determined by automated DNA sequencing. Meanwhile, the identified recombinant plasmid was transformed to E.coli BL21(DE3) with the expression of p30 on bacteria induced by IPTG and the expressed protein was identified by SDS-PAGE. The protein obtained was then further purified and refolded, and its biological activity was checked by Western blotting. It was shown that the size of the amplified gene was 750 bp with molecular weight of 30 ku, and this protein could specifically react with monoclonal antibody against p30 protein.

Objective To explore the changes of hydrogen sulfide(H2S) levels in plasma of newborn infants with pulmonary hypertension(PH) and its relationship with pulmonary hypertension,and provide scientific evidence for the decision of treating neonatal PH.Methods Sixteen children with PH and 16 children without PH in ICU from Mar.2005 to Mar.2006 were selected.Ultrasonic cardiogram(UCG) examination was performed for eachpatients.Pulmonary artery pressure(PAP) was measured.The plasma concentrations of H2S,cysteine and PAP of each patient were measured.Results PAP was 4.27-9.73 kPa[(6.49?1.79) kPa] in neonatal PH group,and PAP in control group was normal.The plasma levels of cysteine and H2S in neonatal PH group significantly increased compared with those of control group [(11.94?6.65) ?mol/L vs(6.43?2.08) ?mol/L,t=2.630 P=0.016;(26.99?1.33) ?mol/L vs(24.92?1.36) ?mol/L,t=4.373 P=0].Conclusions Endogenous H2S and cysteine were up-regulated during the development of neonatal PH;it might play an improtant role in the development of PH.H2S possibly depress the PAP by dilating the pulmonary artery to protect the patients with pulmonary hy pertension.