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1.
The acute influences of arsenic compounds on the metabolism of porphyrins and heme in various organs of rats after oral or intratracheal administration of disodium arsenate (Na2HAsO4) and gallium arsenide (GaAs) were examined and compared. For the oral administration experiments, 21 or 84 mg of Na2HAsO4, or 2 or 4 g of GaAs, per cm3 saline per kg body weight of each animal was administered to Jcl: Wistar male rats and the organs were removed after exsanguination from the vein of the right axilla under anesthesia with ether, 16 h after administration. In the case of intratracheal administration, rats given 8.2 or 16.4 mg of Na2HAsO4, or 0.2 or 0.4 g GaAs per cm3 saline per kg body weight were examined under the same experimental conditions as for the administration route. Increase in the body weight of rats was suppressed after intratracheal administration of the two arsenic compounds. In these rats the hematocrit value increased significantly. These changes were not shown by the orally administered rats. Elevation in δ-aminolevulinate synthase (ALA-S, EC 2.3.1.37) activity in erythroblasts by Na2HAsO4 was much higher after intratracheal administration than after oral administration. Suppression in the activities of δ-aminolevulinate dehydratase (ALA-D, EC 4.2.1.24) and porphobilinogen deaminase (PBG-D, EC 4.3.1.8) in peripheral erythrocytes by Na2HAsO4 and GaAs were stronger by intratracheal administration than by the oral route. Influences of GaAs on the activity of PBG-D in rat liver were shown to be more effective by oral administration than by the intratracheal route. Oral administration of Na2HAsO4 and GaAs had a stronger suppression effect on the activities of ALA-D and PBG-D in rat kidney. It seems from these results that the different extents of the influence of arsenic compounds might depend on the routes of intake. 相似文献
2.
B. Evrard P. Bertholet M. Gueders M. Piette G. Piel D. Cataldo L. Delattre 《Journal of inclusion phenomena and macrocyclic chemistry》2007,57(1-4):303-308
Ro 28-2653 is a new synthetic inhibitor of matrix metalloproteinases. The ability of these enzymes to degrade various components
of the extracellular matrix seems to play a major role in tumors progression and is potentially effective against bronchial
remodeling in asthma and BPCO. Ro 28-2653 is very poorly soluble in water. This low solubility estimated at about 0.56 μg/ml
in water at 25 °C gives rise to difficulties in pharmaceutical formulation of oral, injectable or nebulizable solutions. The
purpose of our study is to prepare and to characterize inclusion complexes between Ro 28-2653 and cyclodextrins and to investigate
the biopharmaceutical repercussion of the inclusion of the active substance.
The complex formation was investigated by phase solubility studies. 1H-NMR spectroscopy and molecular modeling studies were carried out to elucidate the structure of the inclusion complex between
Ro 28-2653 and cyclodextrin. Oral, intravenous and nebulizable solutions of Ro 28-2653 were developed with cyclodextrin. The
in vivo studies were performed on healthy sheep for the pharmacokinetic evaluation of the oral and intravenous formulations
while the nebulization of the complex solution was studied by using an asthma model in mouse. 相似文献
3.
Peng Lu Yue Xing Zhifeng Xue Zhe Ma Bing Zhang Hui Peng Qi Zhou Hongfei Liu Zhidong Liu Jiawei Li 《Biomedical chromatography : BMC》2019,33(8)
A sensitive and accurate LC–MS/MS method was established for quantifying salvianolic acid B (Sal B), rosmarinic acid (Ros A) and Danshensu (DA) in rat plasma. Salvia miltiorrhiza polyphenolic acid (SMPA), active water‐soluble ingredients isolated and purified from Salvia miltiorrhiza Bge included Sal B, Ros A and DA. The pharmacokinetic analysis of Sal B, Ros A and DA after pulmonary administration of SMPA solution to rat was performed by LC–MS/MS. Results from the pharmacokinetic studies showed that the peak concentration of DA was 21.85 ± 6.43 and 65.39 ± 3.83 ng/mL after pulmonary and intravenous administration, respectively. DA was not detected at 2 h after administration. The absolute bioavailabilities of Sal B and Ros A were respectively 50.37 ± 27.04 and 89.63 ± 12.16% after pulmonary administration of 10 mg/kg SMPA solution in rats. The absolute bioavailability of Sal B increased at least 10‐fold after pulmonary administration, compared with oral administration. It was concluded that the newly established LC–MS/MS method was suitable for describing the pharmacokinetic characteristics of Sal B, Ros A and DA in rat after pulmonary administration of SMPA solution. The data from this study will provide a preclinical insight into the feasibility of pulmonary administration of SMPA. 相似文献
4.
5.
《Biomedical chromatography : BMC》2017,31(12)
A highly sensitive liquid chromatography tandem mass spectrometry (LC–MS/MS) method for simultaneous determination of glycyrrhizin (GL) and its active metabolite, glycyrrhetinic acid (GA), from human plasma was validated and applied to a human pharmacokinetic study. The analytes were extracted from human plasma using an Oasis MAX cartridge and chromatographic separation was performed on an Inertsil ODS‐3 column. The detection was performed using an API 4000 mass spectrometer operating in the positive electrospray ionization mode. Selected ion monitoring transitions of m /z 823 → 453 for GL and m /z 471 → 149 for GA were obtained. The response was a linear function of concentration over the ranges of 0.5–200 ng/mL for GL and 2–800 ng/mL for GA (both R 2 > 0.998). Using this method, the pharmacokinetics of GL after single oral administration of a clinical dose (75 mg) to six healthy male Japanese volunteers were evaluated. GL was detected in the plasma of all subjects and the average peak concentration was 24.8 ± 12.0 ng/mL. In contrast, peak concentration of GA was 200.3 ± 60.3 ng/mL, i.e. ~8‐fold higher than that of GL. This is the first report clarifying pharmacokinetic profiles of GL and GA simultaneously at a therapeutic oral dose of a GL preparation. 相似文献
6.
D. Chirio M. Trotta M. Gallarate E. Peira M. E. Carlotti 《Journal of Dispersion Science and Technology》2013,34(3):320-325
In the present work, thermosensitive systems were prepared, characterized, and proposed for diltiazem administration in the topical treatment of anal fissures. Methylcellulose and PluronicF127 were used as gelling polymers. Some low-toxicity molecules, such as sodium glycocholate, citric acid, and lactic acid, were added to gel formulations as counterions to enhance diltiazem lipophilicity. The systems were characterized by sol-gel transition temperature, viscosity, and rheological studies. The resulting data allowed us to determine which systems presented sol-gel transition. A change from Newtonian to plastic behavior at sol-gel transition temperature was observed. An increase in diltiazem pig skin permeability and two-fold skin accumulation was observed in the presence of citric acid. 相似文献
7.
CI战略成功导入的关键,是对企业内部CI作业群体的行为进行系统、科学的管理。本文在首先提出企业内部群体行为管理假说的基础上,借鉴系统科学的相关思想,就CI作业过程中群体行为管理的基本方法,作了较为深入,全面的探讨。 相似文献
8.
The research was conducted to know the effect of amikacin administrations to the concentration of drug in reptile. The 16 sanca batik snakes (Broghammerus reticulatus) were adapted then divided into four groups of which each was administered5 mg · kg–1 body weight of amikacin by posterior and anterior intravenous and intramuscular injection, respectively. The blood collection was done by cardio-puncture to each group at minute 1, 60 and 24, 48 h after drug injection and the drug concentration was analysed by High Performance Liquid Chromatography. The result showed that the drug by i.v. or i.m. administration routes (t1,t48) from posterior region had higher concentrations (81.90 ± 23.1) mg · mL–1, (17.23 ± 5.29) mg · mL–1) compared to the anterior injection (P < 0.01). The other concentration comparisons between regions resulted in no significant difference. 相似文献
9.
应用直接标化法计算病种构成变化对医疗质量综合评价指标的影响程度并算出标化值。1991年病种构成变化对治愈率、病死率、平均住院日变化的影响程度分别为69.91%,84.96%,86.77%,表明病种构成变化对医疗质量综合评价指标的影响不容忽视,未经标化的指标无可比性 相似文献
10.
Chenglong Sun Jiuming He Hongbo Wu Xiaowei Song Jiangshuo Li Luojiao Huang Xiaoyu Xu Manjiangcuo Wang Ruiping Zhang Zeper Abliz 《中国化学快报》2018,29(8):1284-1286
A rapid and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC–MS/MS) method was developed and fully validated for determination of arformoterol in rat plasma, lung and trachea tissues. 相似文献