Objective: To investigate the effects of AG, an iNOS inhibitor on microcirculation of the septic shock rabbits. Method: The white rabbits were infused endotoxin(LPS, 300?g. kg~(-1)in lh. Two hours after the MAP de creased to 60% of the baseline, the rabbits were grouped randomly as L-NAME(n=6.30 mg. kg~(-1))I. V. group and AG(n=6,20 mg. kg~(-1)) I. V. group. Result: Two hours after MAP decreased, the blood velocity decreased, the arterio lar of mesenterium dilated by 18%(P

Objective: To investigate the effects of selective NOS inhibitor aminoguanidine (AG) on endotoxintreated rat aorta (AO) and pulmonary artery (PA) in vitro. Method: The reaction to noradrenaline (NE) (10~(-9)-10~(-4)mmol/L) was measured in the vessels with complete endothelium, then the vessels were divided into 8 groups after incubated in LPS(300ng/ml)for 4 hours. Each group was incubated with AG(100?mol/L)or L-NAME (300?mol/L)for 20, or 60min, respectively. Result: Both AO and PA showed hyporeaetivity to NE after incubated in LPS. and the reactivity of AO and PA to L-NAME and AG increased significantly after incubated in them for 60min or 20min. The sen sitivities of AO to AG,AO and PA to L-NAME increased greatly. AO had a higher reactivity to AG in 60min than in 20min. L-NAME caused earlier and greater contraction than AG in both 60 min and 20 min groups. Conclusion: LNAME and AG can both increase the decreased reactivities of AO and PA to NE. AG only increases the AO sensitivity.

To enhance the quality and efficiency of ozagrel by investigating the differences between the ozagrel polymorphs in bioavailability. Solid ozagrel in different polymorph forms were orally administered to SD rats. An HPLC method was established to determinate plasma level of ozagrel. The bioavailabilities of two polymorph forms were calculated and compared. The pharmacokinetic parameters of ozagrel, were as follows: Cmax was 32.72 ± 17.04 and 34.01 ± 19.13 mg · L(-1), respectively; AUC0-t was 61.14 ± 14.76 and 85.56 ± 18.08 mg · L(-1) · h, respectively; t½ was 1.53 ± 0.51 and 4.73 ± 3.00 h, respectively. There was no significant difference in pharmacokinetic parameters between form I and II polymorphs of ozagrel while the t½ of form II is longer, which indicates that the use of form II polymorph as pharmaceutical product may prolong the effective action time in clinics. This would help the polymorph quality control in drug production.

Salvianolic acid A (Sal A) is one of the most effective compounds isolated from the root of Salvia miltiorrhiza. Up to now, several studies regarding the pharmacokinetic profiles of Sal A have been reported, however there is no such study reported in monkeys, the species which is more similar to human. The aim of this study is to develop a LC-MS method for the determination of Sal A in monkey plasma and apply it to the pharmacokinetic studies of monkeys. After single intravenous administration of Sal A, the plasma concentration-time curves were observed and the main pharmacokinetic parameters were calculated. The plasma concentration at 2 min (C2 (min)) values were (28.343 ± 6.426), (45.679 ± 12.301) and (113.293 ± 24.360) mg x L(-1) for Rhesus monkeys treated with Sal A at 2.5, 5 and 10 mg x kg(-1). The area under the concentration-time curve (AUC(0-∞)) values were (3.316 ± 0.871), (5.754 ± 2.150) and (13.761 ± 2.825) μg x L(-1) x h, respectively. Furthermore, this method was improved and applied to the simultaneous determination of Sal A, Sal B and Sal C, which provided useful information for preclinical studies and clinical trials of Sal A, Sal B and Sal C.

Objective: To compare hemodynamic effects of infusion of diethylamine/nitric oxide (DEA/NO)and sodium nitroprusside(SNP)during controlled hypotension. Method: General anesthesia was induced in dogs. The twelve healthy adult dogs were randomly assigned into one of two groups. 0.00l％ DEA/NO or 0.01％ SNP was infused to induce mean arterial pressure(MAP) to decrease to 60％ of baseline and be maintained for 30 min. During hypotension, MAP,central venous pressure (CVP), mean pulmonary artery pressure (MPAP)and cardiac output (CO) were measured and recorded. Arterial blood gas, blood lactate and urine output were also measured. Result: HR,CVP and CO were unchanged during hypotension period in both groups, MPAP decreased correspondently with MAP. There were no significantly changes in arterial blood gas,blood lactate and urine output in both groups during hypotension. Conclusion: Controlled hypotension achieved with infusion of DEA/NO has a rapid onset and short duration of action.The hemodynamics were similar to those of SNP.

Aim To investigate the effects of diterpene ginkgolides meglumine injection (DGMI ) on amino acids and monoamine neurotransmitters in rats with cerebral ischemia/reperfusion injury.Methods In-traluminal suture was applied to establish middle cere-bral artery occlusion (MCAO/R)model with ischemia for 1.5 h and reperfusion for 24 h.After the adminis-tration of DGMI (i.v.),the levels of amino acid and monoamine neurotransmitters in brain tissue were de-tected through HPLC-ECD.Results DGMI down-reg-ulated the concentrations of aspartic acid, glutamic acid,glycine and γ-aminobutyric acid which were in-creased in MCAO/R group.DGMI also reduced the levels of norepinephrine epinephrine,glyoxylic acid, serotonin and 5-HIAA in cortex and hippocampus,and increased adrenaline content compared to the model group.Conclusion DGMI exhibits a protective role in rats with cerebral ischemia /reperfusion injury through regulating amino acids and monoamine neuro-transmitters.

With the development of CT and the popularization of health examination, the detection rate of small pulmonary nodules has been improved. Some small pulmonary nodules could be malignant nodules. Surgical resection is the preferred treatment. Therefore, it is an important task for thoracic surgeons to accurately locate pulmonary nodules during surgery and remove nodules accurately on the premise of maximum protection of lung function. At present, the core of preoperative auxiliary localization of pulmonary nodules is the implantation of markers. The commonly used clinical localization methods include hook wire localization, microcoil localization, methylene blue puncture injection localization and biological glue localization. In this paper, the development status, application scope, advantages and disadvantages of existing localization methods are briefly reviewed, which can provide references for clinical application and follow-up research.

Objective To study the gastrointestinal absorption process of three letrozole polymorphs in rats, and evaluate the different pharmacokinetics parameters of different polymorphs. Methods A total of 18 SD rats were given the different letrozole polymorphs. Then the high-performance liquid chromatographic method was used for the determination of plasma concentration of letrozole in these SD rats.Finally the pharmacokinetic parameters among the different polymorphs were calculated. Results Cmax of letrozole crystal form I, crystal form II and crystal form III were (9.247± 4.612) ,(23.387± 9.049) and (15.682±1.589) mg·L-1, respectively, and AUC0→t were(198.115±47.014) ,(476.641±125.467) and (271.817±41.068) mg·L-1·h,respectively. Conclusion The different crystal forms of letrozole result in different plasma concentration in SD rats. Crystal form II may be its preponderant polymorphs which deserves further research and development.

Objective To study the mangiferin absorption process of mangiferin polymorphs in SD rats thus to find out the optimal crystal form and explore the factors that may affect the clinical effects of mangiferin. Methods Each rat was given one of three crystal forms of mangiferin. Plasma concentration of mangiferin were determined by HPLC-MS method. After liquidliquid extraction by ethyl acetate, the chromatographic separation was carried out on an Agilent ZORBAX SB-C18 (2.1 mm× 100 mm,3.5 μm) with a mobile phase consisting of methanol-0.1％ formic acid aqueous solution (30:70) . Mass spectrometry were performed in positive ion mode. Ion mass-to-charge ratio was set at 445 and 447 for mangiferin and, cefuroxime sodium (internal standard) respectivel for quantitive analysis. Results The main pharmacokinetic parameters of mangiferin form II, Ⅴ, Ⅵ were as follows: AUC(0-24 h) were (1323. 27 ± 218. 07) ,(1974. 34 ± 469. 24) ,(1737. 79 ± 623. 06) ng · mL-1 · h, respectively; Cmax were (321.92±85.18) ,(455.83±277.07) ,(319.92±86.07) μg·L-1, respectively; tmax were (0.70±0.45) , (0.50±0.32) ,(0.50± 0.34) h, respectively; t1/2z were (2.78± 1.72) ,(5.29± 2.67) ,(5.31± 2.82) h, respectively. Conclusion The main pharmacokinetic parameters of mangiferin polymorphs in plasma of rats are different, and mangiferin form Ⅴ has the hightest AUC(0-24 h) and Cmax.

The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma drug concentrations were determined by a high performance liquid chromatography-mass spectrometry (LC-MS) method. The pharmacokinetic software Data Analysis System (Version 3.0) was used to calculate the pharmacokinetic parameters. For different i.v. doses of J10688, the mean peak plasma concentration (C 0) values ranged from 11.26 to 50.82 mg/L, and mean area under the concentration-time curve (AUC0-t ) values ranged from 1.75 to 11.80 (mg·h/L). J10688 lacked dose-dependent pharmacokinetic properties within doses between 1 and 10 mg/kg, based on the power model. The method developed in this study was sensitive, precise, and stable. The pharmacokinetic properties of J10688 in SD rats were shown to have rapid distribution and clearance values. These pharmacokinetic results may contribute to an improved understanding of the pharmacological actions of J10688.