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21.
The in vitro capacity of sympathetic superior cervical ganglia (SCG) to take up [3H]choline from the extracellular medium, to synthesize acetylcholine from [3H]choline, and to release [3H]acetylcholine in response to a high K+ concentration, were examined in rats throughout a 24-h cycle. Both the release of [3H]acetylcholine and the synthesis of [3H]acetylcholine from [3H]choline exhibited significant diurnal variations, showing maxima during the first half of the night. After these maxima, nocturnal acetylcholine release and synthesis decayed to daytime levels and remained low until the end of the night. [3H]Choline uptake by rat SCG did not vary significantly throughout a 24-h period. A 1.5-h exposure of rats to darkness at the 5th hour of light phase of the daily photoperiod did not change significantly any parameter studied. A 20-min, 5-Hz, electrical stimulation of the preganglionic trunk of SCG excised from rats at noon increased significantly subsequent K+-induced [3H]acetylcholine release but did not change [3H]acetylcholine synthesis. In decentralized SCG of rats subjected to a unilateral SCG decentralization and a contralateral sham-operation 7 days earlier, [3H]acetylcholine release and synthesis were highly reduced or abolished at the decentralized side, while [3H]choline uptake remained unaltered. The present results suggest that an activation of preganglionic rat SCG neurons takes place during the first half of the scotophase. 相似文献
22.
Formulation and in Vitro-in Vivo Evaluation of Sustained-Release Lithium Carbonate Tablets 总被引:1,自引:0,他引:1
Çiftçi Kadriye Çapan Yilmaz Öztürk Orhan Hincal A. Atilla 《Pharmaceutical research》1990,7(4):359-363
The release of lithium carbonate incorporated into polymethylmethacrylate, poly vinyl chloride, hy-drogenated vegetable oil, and carbomer matrix tablets was studied in vitro. The formulation containing 10% carbomer showed a sustained-release profile comparable to that of a standard, commercially available, sustained-release preparation containing 400 mg lithium carbonate embedded in a composite material. In vivo the newly formulated and standard sustained-release lithium carbonate tablets were compared to an oral solution and conventional lithium carbonate tablets in 12 healthy subjects. These crossover studies showed that the sustained-release tablets produced a flatter serum concentration curve than the oral solution and conventional tablet, without loss of total bioavailability. 相似文献
23.
Devi Kanikanti Padmalatha Rao Kanikanti V. Ranga Baveja Srikrishan Fathi Marc Roth Marc 《Pharmaceutical research》1989,6(4):313-317
Zero-order release of oxprenolol hydrochloride was obtained by controlling the swelling and erosion of the matrix. This formulation involves only mixing of drug, hydroxypropylmethylcellulose (HPMC), and sodium carboxymethylcellulose (Na CMC) at the ratio of 1:0.4:1.6, respectively, and compressing the mixture directly into tablets. The in vitro release pattern from this optimized matrix tablet was reproducible. Accelerated stability studies revealed that the optimized formulation remains stable for an approximately 2-year shelf life. This sustained-release (SR) tablet was evaluated in dogs, and for comparison a conventional (CV) formulation was also given at the same dose level. Plasma oxprenolol levels were monitored by a sensitive and specific high-performance liquid chromatographic (HPLC) method. Significant differences in the pharmacokinetic parameters, i.e., lower C
max, higher values of t
max, MRT, AUC, and plasma concentration at 24 hr, and nearly constant plasma levels over 12 hr, indicated that the SR matrix tablet is superior to the CV rapid-releasing formulation. The in vitro release parameters and in vivo pharmacokinetics correlated well. 相似文献
24.
It has been suggested that reward dependence, as measured by the Tridimensional Personality Questionnaire (TPQ), is related to central noradrenergic activity, a proposition supported by two studies of urinary norepinephrine metabolite. In the current investigation, 190 normal young Han Chinese were examined, with genetic polymorphisms determined for the norepinephrine transporter (1287G/A) and the α2c‐adrenoceptor (Del322–325) to test the association with TPQ personality traits. No significant association was demonstrated for these two polymorphisms and any of the TPQ personality‐factor scores, including reward dependence and its subscales. Our negative findings suggest that the investigated polymorphisms of the norepinephrine transporter and the α2c adrenoceptor do not play a major role in the reward‐dependence personality trait as assessed by TPQ. © 2002 Wiley‐Liss, Inc. 相似文献
25.
J. Boldt H. A. Adams B. Zickmann D. Kling G. Hempelmann 《European journal of clinical pharmacology》1990,38(5):431-436
Summary The release of endogenous catecholamines in aorto-coronary bypass graft patients receiving either 0.5 mg/kg enoximone (n=10), 4.0 mg/kg theophylline (n=10) or saline solution (control,n=10) has been studied, as well as certain haemodynamic parameters. Adrenaline (A) and noradrenaline (NA) concentrations were
not significantly changed by the administration of enoximone. Theophylline caused a small increase in NA (+ 40% in the 1st
min) and a marked increase in A (approximately + 7000% in the 1st min), which still remained elevated at the end of the investigation
period (+ 220% in the 30th min). The major haemodynamic effects of enoximone were a significant increase in cardiac index
(CI; + 35%) and a decrease in pulmonary capillary wedge pressure (PCWP; −27%), pulmonary artery pressure (PAP; −21%), RVEDV
and RVESV, while the heart rate (HR) remained almost unchanged. The dominant haemodynamic effects of theophylline were an
increase in HR (+ 26%; arrhythmia in 3 patients), PAP (+ 22%), and RVEDV (+ 19%), while REVESV (+ 26%), MAP (−16%), CI (−14%),
and RVEF (−15%) fell significantly.
It is concluded that the haemodynamic actions of enoximone are not mediated by catecholamine release, whereas the adverse
cardiovascular effects of theophylline might partly be explained by the significant increase in plasma adrenaline. 相似文献
26.
Purpose. Flexible parametric models describing the input process after extravascular drug administration are needed for the assessment of absorption rate and the use of population methods in bioavailability and bioequivalence studies.
Methods. The oral concentration-time curve modeled as the product of the input and disposition function in the Laplace domain was obtained by numerical inversion methods for parameter estimation. The utility of the inverse Gaussian input density was examined using bioavailability data of an extended-release dosage form. Measures of rate of absorption and the cumulative absorbed amount profile were defined in terms of the estimated model parameters.
Results. Accurate estimation of absorption parameters was achieved by simultaneous fitting of the extravascular and intravascular data (describing the latter by a triexponential function). The new input function allowed a direct estimation of both extent of absorption and mean absorption time.
Conclusions. The findings suggest that the inverse Gaussian density is a useful input function. Its flexibility may reduce the effect of model misspecification in parameter estimation. All parameters can be readily interpreted in terms of the absorption process. 相似文献
27.
目的 通过健康受试者的双交叉试验比较萘普生缓释胶囊与普通片的药物动力学和生物利用度。方法10位健康受试者一次服用这两种制剂500mg,在稳态试验中8位受试者接受两种制剂5天,缓释胶囊500mg每天一次,普通片每天两次,每次250mg。血药浓度用HPLC方法测定。结果 一次服药试验证明该缓释胶囊血药浓度上升缓慢,浓度变化平稳,Gmax为85.9μg/ml,Tpeak为6.0h,而普通片的Cmax为140.4μg/ml,Tpeak为3.2h,两种制剂的生物利用度相当,缓释胶囊与普通片生物等效。通过8位健康受试者交叉连续服用萘普生缓释胶囊与普通片的稳态药代动力学研究表明,到第3天给药后已达到稳态,由第5天给药后的血药浓度测定数据计算其主要的稳态药代动力学参数,缓释胶囊的峰浓度(Cmax)、峰谷比和波动度(DF)明显低于普通片,这些参数分别为73,1μg/ml、1.48和37.7o;而普通片的上述参数分别为 100.8μg/ml、2.51和78.2%。结论 奈普生缓释胶囊具有缓释作用,能较好维持血药治疗浓度。 相似文献
28.
29.
Prof. Dr. W. Bernauer 《Basic research in cardiology》1991,86(1):1-10
Summary In isolated perfused rat hearts global ischemia for 2, 5, and 15 min was produced. Depending on the duration of the ischemia, postischemic reperfusion led to the release of adenosine and its catabolites, and to more or less severe ventricular tachyarrhythmias. When ventricular fibrillation occurred, a highly significant increase in the purine release was observed compared with non-fibrillating hearts. Prevention of fibrillation by antiarrhythmic drugs decreased the purine release in a highly significant way. After only 2 min of ischemia, reperfusion did not lead to ventricular fibrillation. Electrical induction of fibrillation during the reperfusion in these hearts provoked the release of very high amounts of the purine compounds. A similar effect of electrically-induced fibrillation was also obtained in hearts without a previous ischemic period. The findings suggest that ventricular fibrillation is able to induce the release of purine derivatives from the heart. 相似文献
30.
K. S. Us P. M. Klodt V. S. Kudrin A. Ya. Sapronova R. U. Ostrovskaya M. V. Ugryumov K. S. Rayevsky 《Neurochemical Journal》2007,1(2):138-142
The level of spontaneous and K+-stimulated release of endogenous glutamate was studied in experiments on slices of brain cortex of Wistar rats. Pronounced spontaneous release of the neuromediator and its increase under conditions of stimulation were registered by high-performance liquid chromatography with electrochemical detection. The effect of the nootropic and neuroprotective dipeptide Noopept (GVS-111) on release of glutamate was investigated. The peptide in concentrations of 10?5 and 10?6 M caused a statistically significant decrease in spontaneous and K+-stimulated glutamate release. This effect could be the basis of the neuroprotective action of the peptide, suggesting that further studies of Noopept as neuroprotector are very promising. 相似文献