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  • 2000-2004  (27)
  • 1995-1999  (7)
  • 1985-1989  (15)
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 31 (1986), S. 95-99 
    ISSN: 1432-1041
    Keywords: glipizide ; Type 2 diabetes ; dosing frequency
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Two cross-over studies were carried out in 23 patients with Type 2 diabetes, to examine whether glipizide, a potent sulphonylurea with fast and complete absorption and rapid elimination (t1/2〈5 h), can be given once-daily without loss of therapeutic effect. In both studies, patients were randomly assigned to an initial dose of 7.5 mg once daily or 2.5 mg three-times daily, which was increased to 15 mg o.d. or 5 mg t.i.d. if the fasting plasma glucose remained over 10 mmol/l on the lower dosage. In Study 1 (n=11), administration once a day before breakfast was compared with intake before breakfast, lunch and early dinner (5 p.m.) and in Study 2 (n=12) the comparison was between intake once-daily before breakfast and dosing before breakfast, lunch, and at bedtime (10 p.m.). Neither the 24-hour urinary glucose excretion nor HbA1, fasting plasma glucose, insulin or C-peptide levels differed between the once and three times daily administration with the third dose given before early dinner. The nadir plasma levels of glipizide were not significantly different and were often too low to be detected. Postponing the third dose until 10 p.m. did not produce any improvement in HbA1 or in fasting plasma glucose, insulin or C-peptide. The mean nadir glipizide levels following this schedule were twice as high as those after once-daily administration. As expected, the plasma glipizide after breakfast was higher when the whole dose was taken before breakfast than when it was divided. The corresponding plasma level of insulin was higher and that of plasma glucose was lower. The after-lunch levels of glipizide did not differ significantly, and there was no after-lunch difference in plasma insulin or glucose. It appears that the major effect of glipizide is to augment insulin availability following meals, whilst it has little influence on nocturnal glucose control. In a daily dose of 7.5 mg or more, glipizide can be taken once daily without loss of efficacy, at least in areas with Northern European meal schedules.
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  • 2
    ISSN: 1432-1041
    Keywords: indomethacin ; diflunisal ; pharmacokinetics ; drug interaction ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The single-dose pharmacokinetics of indomethacin following 100 mg rectally was measured in two groups of 8 healthy subjects before and after diflunisal 500 mg p.o. once daily, or 500 mg in the morning and 1000 mg in the evening, until steady state conditions were reached. A further group of 8 healthy subjects was given 50 mg indomethacin rectally before and after diflunisal 500 mg p.o. twice daily. High dose diflunisal (1500 mg/day) decreased the renal clearance of indomethacin from 21.9 to 1.8 ml/min (92%) and reduced the renal excretion of both unchanged (63%) and conjugated (82%) indomethacin. The apparent total body clearance (0.12 l/h/kg), apparent volume of distribution (0.98 l/kg), and volume of distribution at steady state (0.80 l/kg) were decreased by 47%, 35% and 30%. The maximum plasma concentration (2.4 µg/ml) and total area under the curve (13.0 µg × h/ml) were increased by 40% and 119%, respectively. The terminal elimination half-life (5.7 h) and mean residence time (6.7 h) were slightly prolonged (7.0 h and 8.8 h) in the presence of diflunisal. The contribution of metabolism to the overall elimination of indomethacin was increased by only 2%. Similar results were obtained when the subjects were challenged with the low dose of diflunisal (500 mg/day), although the magnitude of the changes were smaller. The interaction between indomethacin and diflunisal may be due to competition both at the metabolic (conjugation) and the excretory (tubular secretion) levels. When the subjects were given 50 mg indomethacin and diflunisal 1000 mg/day simultaneously, the achieved maximum plasma concentration of indomethacin (2.53 µg/ml) was comparable to that seen after 100 mg in the absence of diflunisal (3.1 µg/ml), but the AUC was greater (21.7 µg × h/ml vs 13.0 µg × h/ml). Adverse central nervous reactions were more frequent and more pronounced at higher plasma indomethacin concentrations.
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  • 3
    ISSN: 1432-1041
    Keywords: glibenclamide ; glipizide ; pharmacokinetics ; metabolic effects ; Type 2 diabetes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Fifteen Type 2 diabetics were treated for 4-week periods with once daily (10 mg) glibenclamide, glipizide and placebo according to a double-blind cross-over protocol. Post-dose glipizide concentrations were three times higher than those of glibenclamide, due to the incomplete bioavailability of the latter. On the other hand, pre-dose drug levels were similar, as an expression of the slower absorption and/or elimination of glibenclamide. Both active treatments reduced postprandial blood glucose concentrations and 24-hour urinary glucose excretion to a similar degree, but fasting blood glucose concentrations were slightly lower during glibenclamide treatment. Both active treatments enhanced fasting and postprandial insulin and C-peptide concentrations, the C-peptide response being greater after glipizide than after glibenclamide. Plasma glucagon and GIP concentrations were not significantly affected. Insulin sensitivity was increased by glibenclamide but not by glipizide. Neither therapy affected insulin binding to erythrocytes. It appears that both glibenclamide and glipizide improved glucose metabolism by sustained stimulation of insulin secretion, which was most pronounced with glipizide. Only glibenclamide improved insulin sensitivity and was slightly more active than glipizide on fasting blood glucose levels. The differences may be consequences of the pharmacokinetics, but differences in pharmacodynamics cannot be excluded.
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  • 4
    ISSN: 1432-1041
    Keywords: glipizide ; plasma lipoproteins ; HDL ; LDL ; cholesterol ; triglycerides ; blood glucose ; Type 2 diabetes ; insulin-dependent diabetes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A double-blind, placebo-controlled investigation has been made into the effects of 8 weeks of glipizide treatment in diabetics previously classified as Type 2 but with subsequent attenuation of insulin secretion and thence maintained on exogenous insulin. Although all patients were exposed to therapeutic plasma concentrations of glipizide, fasting blood glucose, haemoglobin A1 and plasma lipoproteins (HDL, LDL, total cholesterol and triglycerides) did not show any consistent improvement following this treatment. It appears unlikely that SU (glipizide) has any primary effect on insulin action or on plasma lipoproteins. Its primary action is to augment insulin release and availability, so, its use should be restricted to Type 2 diabetics who retain insulin secretion.
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  • 5
    ISSN: 1432-1041
    Keywords: glipizide ; diabetes mellitus ; NIDDM ; insulin release ; glucose disposal
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary An early defect in subjects with non-insulin-dependent diabetes mellitus (NIDDM) and the preceding phase of impaired glucose tolerance (IGT) is a reduction in early insulin release and hence a prolonged elevation of postprandial blood glucose. We therefore assessed whether a rapidly acting sulphonylurea (glipizide 5 mg 0.5 h before a test meal) could correct these disturbances in 38 IGT/NIDDM subjects, whose early insulin release and postprandial blood glucose elevations remained unimproved after 10 weeks of dietary regulation. We also assessed whether the efficacy of glipizide was dependent upon the ambient blood glucose concentration, and if early systemic availability of the drug was important for the blood glucose lowering effect. A single dose of glipizide normalized early insulin release and hence reduced the postprandial blood glucose increase that was not lowered by dietary regulation. The efficacy of glipizide was dependent upon the early systemic availability of the drug, but early systemic availability and efficacy were independent of the extent of blood glucose elevation, at least within a range of 6–12 mmol·l−1 of fasting blood glucose.
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  • 6
    ISSN: 1432-1041
    Keywords: diflunisal ; pharmacokinetics ; healthy volunteers ; kidney failure ; rheumatoid arthritis ; aged subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The single-dose plasma kinetics of diflunisal was studied in healthy young and old subjects, in patients with rheumatoid arthritis, and in patients with renal failure. The plasma and urine kinetics of the glucuronidated metabolites of diflunisal were studied in the healthy elderly subjects and in the patients with renal failure. In addition, the multiple-dose plasma kinetics of diflunisal was assessed in healthy volunteers and in patients with rheumatoid arthritis. After a single dose of diflunisal the terminal plasma half-life, mean residence time and apparent volume of distribution were higher in elderly subjects than in young adults. No difference was observed in any pharmacokinetic parameter between age-matched healthy subjects and patients with rheumatoid arthritis. The elimination half-life of unchanged diflunisal was correlated with the creatinine clearance (r=+0.89) and its apparent total body clearance exhibited linear dependence on creatinine clearance (r=+0.78). In patients with renal failure, the terminal plasma half-life and mean residence time of diflunisal were prolonged. The renal and apparent total body clearances were lower, the mean apparent volume of distribution was higher and the mean area under the concentration-time curve extrapolated to infinity (AUC) was greater in the renal failure patients than in controls. The plasma concentration of the glucuronidated metabolites rapidly rose to levels above those of unchanged drug in renal patients, whereas they were lower than those of unchanged diflunisal in controls. The AUC (0–96 h) of diflunisal glucuronides in the patients was four-times that in controls, and the terminal elimination half-life of the glucuronides was prolonged in them. The renal excretion and clearance of diflunisal glucuronides were reduced when renal function was impaired. After multiple dosing, the pre-dose steady-state plasma-concentration increased with decreasing creatinine clearance (r=-0.79). When the plasma concentration exceeded 200 µmol·1−1, the elimination half-life was doubled, due to partial saturation of diflunisal conjugation. This finding suggests that lower doses could be used in long-term treatment. Thus, old age and arthritic disease appear to have little influence on the kinetics of diflunisal in the absence of renal functional impairment. Ordinary doses can be given for short term treatment of elderly patients with or without RA. In patients with renal failure, however, reduced doses of diflunisal are recommended.
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Shock waves 7 (1997), S. 343-350 
    ISSN: 1432-2153
    Keywords: Key words: Holographic interferometry, Two-reference beam holography, Shock wave focusing
    Source: Springer Online Journal Archives 1860-2000
    Topics: Physics , Technology
    Notes: Abstract. Transient shock waves in a confined elliptical chamber are experimentally investigated. Quantitative results of the pressure distribution are obtained for an air-filled cavity. Lower bounding surfaces of different geometrical shapes can be inserted making it possible to get chambers with varying height. An electrical discharge across a pair of electrodes inside the cavity gives rise to the shock waves. Double pulsed holographic interferometry is used to study the propagation and focusing process of the waves. The results are quantitatively evaluated by using the method of two-reference-beam holography. The angular pressure distribution behind the converging wave front is presented for different geometries of an air-filled cavity. The pressure distribution is non-homogeneous but symmetric along the wave front. The pressure level is higher for the geometry where the height of the chamber decreases with the radial distance from the outgoing focus and lower for increasing height of the chamber. In addition, shock waves in a water-filled cavity are studied. In this case qualitative results are obtained.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Irrigation and drainage systems 12 (1997), S. 23-34 
    ISSN: 1573-0654
    Keywords: flow measurement ; irrigation flow measurement ; adjustable-throated flume ; portable flumes ; adjustable weir ; canal flow measurement ; portable flow meter for small canals
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition
    Notes: Abstract The utility of developing vertically-adjustable flumes for canal flow measurement systems, is important to several problems in field practice. One involves the perception by some canal water users that flumes and weirs significantly and harmfully restrict flow. These perceptions, correct only sometimes, occur often enough to cause resistance to flow measurements and impedance to proper irrigation management. Parshall flumes and Cutthroat flumes require ponding depths upstream equal to about 40% of head reading while long-throated flumes and the related broad-crested weirs require only 10 to 15%. The actual head drop through all of these flumes is greater than hydraulically necessary for all but the maximum design discharge. The highly obvious excessive ponding is often misunderstood as a harmful restriction to flow. Also, the velocities at the low flows are reduced by this excessive ponding, which can aggravate sediment accumulation. The system described herein allows control of the ponding restriction from nearly zero to just enough restriction to gain measurement control of the flow at nearly all flow rates in the design range of a particular size. This reduces the amount of visible restriction. For a small structure size, with a control section less than 1 m wide and flowing under a head of less than about 25 to 30 cm, this restriction is about 10% to 15% of the head reading, or about 3 to 5 cm at maximum head. This maintains relatively high velocities in the approach channel for assisting sediment movement. The device is applicable to measuring flow rates in unlined and lined canals. The system described permits adjustment of the canal flow levels, reduces the perception of ponding, and minimizes the induced sediment problems.
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  • 9
    ISSN: 1432-1955
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Immune responses to the repeat regions of the Plasmodium falciparum antigen Pf155/RESA have been extensively studied, and antibodies to the repeats are known to interfere with parasite growth both in vitro and in vivo. Less is known with regard to the effect on parasites of antibodies to the nonrepeat regions of the antigen. In the present study, rabbits were immunized with synthetic peptides corresponding to three different nonrepeated sequences of antigen Pf155/RESA. The reactivity of the antibodies with the particular peptides was analyzed by enzyme-linked immunosorbent assay (ELISA) and that with the parasite antigen, by immunoblotting and immunofluorescence. Although all antisera reacted strongly with the corresponding synthetic peptides, they reacted only weakly with full-length Pf155/RESA in either of the methods used. The specificity of the antibodies for Pf155/RESA was confirmed by their failure to stain Pf155/RESA-deficient parasites in erythrocyte membrane immunofluorescence, a method mainly detecting this antigen. Antibodies to the nonrepeat sequences also efficiently inhibited the merozoite invasion in vitro of Pf155/RESA+ parasites. However, these antibodies also inhibited Pf155/RESA-deficient parasites, indicating the presence of an antigen exhibiting a high degree of homology with Pf155/RESA. The results indicate that nonrepeat sequences of Pf155/RESA are immunogenic and may serve as targets for parasite-neutralizing antibodies, and, thus, the potential of the antigen as a vaccine candidate is emphasized.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Experimental mechanics 29 (1989), S. 378-387 
    ISSN: 1741-2765
    Source: Springer Online Journal Archives 1860-2000
    Topics: Mechanical Engineering, Materials Science, Production Engineering, Mining and Metallurgy, Traffic Engineering, Precision Mechanics
    Notes: Abstract Propagating bending waves are studied in plates made of aluminum and wood. The waves are generated by the impact of a ballistic pendulum. Hologram interferometry, with a double pulsed ruby laser as the light source, is used to record the out of plane motion of the waves. Elliptic-like fringes visualize differences in wave speed for different directions in the anisotropic plate and circular ones are obtained for the isotropic plate. The experimental data for the isotropic plate compare favorably with analytical results derived from the Kirchhoff-plate equation with a point impact of finite duration. A similarity variable is found when starting conditions are modeled as a Dirac pulse in space and time, that brings new understanding to the importance of specific parameters for wave propagation in plates. A formal solution is obtained for a point force with an arbitrary time dependence. For times much larger than the contact time, the plate deflection is shown to be identical to that from a Dirac pulse applied at the mean contact time. A method for determining material parameters, and the mean contact time, from the interferograms is hence developed.
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