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  • healthy volunteers  (17)
  • Bone  (16)
  • Springer  (33)
  • 1980-1984  (33)
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  • Springer  (33)
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Year
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 21 (1982), S. 433-441 
    ISSN: 1432-1041
    Keywords: antipyrine ; antipyrine metabolites ; drug metabolism ; route of administration ; healthy volunteers ; urinary excretion ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of antipyrine in plasma and saliva, and urinary excretion of its major metabolites, were studied following i.v. and oral administration of antipyrine 500 mg to 6 healthy volunteers. Data from both plasma and saliva showed that the oral bioavailability of antipyrine given as an aqueous solution was complete. The saliva/plasma concentration ratio was constant with time from about 3 h onwards, with a mean value of 0.87 after oral and 0.91 after i.v. administration. It is concluded that the pharmacokinetic parameters of antipyrine can be satisfactorily established on the basis of salivary data, although the volume of distribution and clearance values are then slightly too high. After i.v. administration, 3.8±1.9% of the dose was excreted in urine as unchanged antipyrine in 48h, 24.9±6.3% as 4-hydroxyantipyrine, 16.5±3.2% as norantipyrine, 13.0±2.2% as 3-hydroxymethyl-antipyrine and 5.8±1.0% as 3-carboxy-antipyrine. No significant differences were observed following oral administration. The half-lives calculated from the linear part of the urinary excretion rate curves of the metabolites were about the same for oral and i.v. administration, and were of the same order of magnitude as the elimination half-life of parent drug in plasma and saliva. It is important for determination of the ultimate metabolite ratio that urine is collected for at least 36h, because there is a delay in the excretion of 3-hydroxymethyl-antipyrine in urine.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 27 (1984), S. 447-452 
    ISSN: 1432-1041
    Keywords: alaproclate ; antipyrine clearance ; serotonin reuptake inhibitor ; healthy volunteers ; antipyrine metabolism ; metabolite clearance ; alaproclate kinetics ; inhibition of drug metabolism
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Alaproclate, a selective serotonin reuptake inhibitor, presently undergoing clinical trial for the treatment of major depressive disorders, has been shown to inhibit hexobarbital metabolism in mice. In the present study the influence of oral alaproclate on the total plasma clearance of antipyrine and on the formation of its metabolites was investigated in 10 healthy volunteers. The peak level of alaproclate was reached after about 1.5 h, and after a distribution phase, its plasma elimination half-life was between 3.0 and 3.5 h. Antipyrine tests were performed before treatment, during the first four doses and after the seventh dose of alaproclate 200 mg/day. During treatment, total plasma antipyrine clearance and the clearance for production of all antipyrine metabolites were reduced by 30%, indicating non-selective inhibition of oxidative drug-metabolizing enzyme activity in man by alaproclate. After the last dose of alaproclate, antipyrine plasma clearance and the clearance to its metabolites returned to control values. In order to allow more detailed evaluation of the results, the time course of the clearances for production of metabolites was investigated. This revealed that the extent of inhibition of metabolite formation by alaproclate was dependent on the plasma alaproclate level, indicating a rapidly reversible inhibition.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 33 (1981), S. 369-374 
    ISSN: 1432-0827
    Keywords: Histomorphometry ; Bone ; Reproducibility
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary To study bone histomorphometry reproducibility in normal subjects, we performed during orthopedic surgery bone biopsies in 16 post-menopausal women. Each woman had four bone biopsies, two at the usual site in the iliac crest, one on the left and one on the right side, and two other biopsies just behind the usual site, one at each side. We performed measurements of trabecular bone volume, relative osteoid volume, osteoid surfaces, osteoclastic resorption surfaces and calcification front. The average values of the 16 patients were compared, on the one hand, two by two, by a student test, and on the other hand, by a variance analysis. By these two methods the results showed no significant difference between the average values of the 16 patients at each location for any of the histomorphometric parameters studied. However, there was a location variation which was estimated by the intra-individual variation for a given patient. On the other hand, we calculated from the variance analysis the location variance for a group of 10 to 100 patients. In any case all the parameters had a location variation which was high for osteoclastic resorption surfaces and relative osteoid volume when expressed in % of the absolute value of these parameters. The variation of the trabecular bone volume was 0–46. 15% (95% confident limit interval) in a single patient and the hypothetical value of the location variation was 41.6% for a group of 10 patients and 13.0% for a group of 100 patients.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 36 (1984), S. S7 
    ISSN: 1432-0827
    Keywords: Bone ; Mechanical function
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary The variety of different mechanical functions required of whole bones is discussed. Often, the design optimizing the structure for one function is not optimal for another function.
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  • 5
    ISSN: 1432-0827
    Keywords: Bone ; Osteosarcoma ; Matrix vesicles ; Alkaline phosphatase ; Aminopeptidase ; Naphthylamidase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary Extracellular matrix vesicles from bovine fetal alveolar bone and from a dog osteosarcoma were isolated by differential centrifugation and then fractionated on a discontinuous sucrose density gradient. The fractions were examined by electron microscopy and were analyzed for protein, alkaline phosphatase, aminotripeptidase, and four different β-naphthylamidase activities. The low-density peak of enzyme activities was shown by electron microscopy to be much more homogeneous than the crude matrix vesicle fraction. Two major peaks of protein and enzyme activities were present, one in the high and one in the low density layers. There was good correlation between the activities of alkaline phosphatase and the various peptidases in the fractions from the sucrose density gradient. These results indicate a coexistence of peptidase and alkaline phosphatase in matrix vesicles. On the other hand, there was generally no correlation between the peptidase and alkaline phosphatase activities in vesicular specimens from bovine liver obtained in the same way. Most of the peptidase activity and about half of the alkaline phosphatase activity were solubilized from bone matrix vesicles by detergents. The extracted alkaline phosphatase and alanyl β-naphthylamidase activities were separated from each other on a DEAE-cellulose column.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 32 (1980), S. 189-194 
    ISSN: 1432-0827
    Keywords: Bone ; Fluoride ; Strength ; Porosity ; Mineralization
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary Radiographically normal vertebral bone cylinders from 80 male subjects were tested mechanically by static compression and analyzed for porosity, fluoride and ash content. As a group, they had low fluoride content, suggesting little prior intake, consonent with this geographic area. Nevertheless, increasing levels of fluoride were associated with bulkier bone, less porosity, and less mineral per unit of bone, which in direction though not degree suggested changes similar to those of osteomalacia and opposite from those of osteoporosis without apparent threshold. The higher fluoride hard tissue was weaker in static tests than that with less fluoride, but the increased bulk apparently offset this, resulting in bones of unchanged static strength. Hence, water fluoridation should not alter static bone strength. There has, however, been a recent report suggesting that increased mineralization of bone renders it more brittle and thus more likely to fracture on impact. Therefore, the possibility that fluoridation may increase impact resistance by lessening mineralization can be entertained.
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  • 7
    ISSN: 1432-0827
    Keywords: Bone ; Mineral ; Amorphous calcium phosphate ; X-ray diffraction ; Radial distribution function
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary X-ray diffraction radial distribution function analysis was used to determine if a significant amount of an amorphous solid phase of calcium phosphate exists in bone, and if so, whether the amount varies as a function of age and maturation. Unfractionated cortical bone from embryonic and posthatch chicks of various ages and a low-density fraction of embryonic bone were studied. No evidence was found for the presence of an amorphous solid phase of calcium phosphate in any of the samples studied, including the recently deposited bone mineral of the low density fraction of embryonic bone. As little as 12.5% of synthetic amorphous calcium phosphate (ACP) added to bone was readily detected by the radial distribution function technique used. The results clearly indicate that the concept that ACP is the initial solid mineral phase deposited in bone, and the major mineral constituent of young bone is no longer tenable. The concept does not provide an accurate description of the nature of the initial bone mineral deposited, or the changes that occur with maturation, nor can it acount for the compositional and X-ray diffraction changes that the mineral component undergoes during maturation and aging.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 36 (1984), S. S118 
    ISSN: 1432-0827
    Keywords: Bone ; Strain ; Remodeling ; Adaptation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary For bone to remodel adaptively, the cells responsible should follow some algorithm. Nine different loading situations and structures are discussed. It seems that either algorithm must be extremely complex, or cells in different structures must follow different algorithms.
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 34 (1982), S. 337-342 
    ISSN: 1432-0827
    Keywords: Bone ; Histomorphology ; Immobilization ; Quadriplegia ; Multiple sclerosis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary The cortical bone histomorphometrics, total visible osteon density, and mean osteonal cross-sectional area were determined for the major long bones and sixth ribs of two individuals with neurological deficit. One was a multiple sclerosis patient who had been in a wheelchair for 15 years. The other was a quadriplegic as a result of poliomyelitis. Statistically significant differences in osteon densities occurred only in the case of the quadriplegic. Nevertheless, in that subject, the total visible osteon densities for bones of the right arm were not statistically different from those of their age-matched (control) radii. Medical history records revealed that there had been partial use of this limb. These results support the belief that mechanical stress is an important factor in the maintenance of normal cortical bone remodeling. In addition, since there were subnormal osteon densities and normal mean osteonal cross-sectional areas, immobilization appears to be characterized by reduced activation frequency with a normal amount of bone turnover per BMU.
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Calcified tissue international 34 (1982), S. 376-381 
    ISSN: 1432-0827
    Keywords: Matrix vesicles ; Bone ; Actin ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Notes: Summary Preliminary indications of the occurrence of actin and myosin in crude matrix vesicle preparations have been reported previously. In the present study extracellular matrix vesicles from rat alveolar bone were isolated. They were further purified by a sucrose density gradient. SDS-polyacrylamide gel electrophoresis of the purified vesicles revealed the presence of a polypeptide with a molecular weight of 43 K daltons and with electrophoretic mobility identical to that of blood platelet actin. The limited proteolysis of both 43 K dalton vesicular polypeptide and actin byStaphylococcus aureus-V8-protease revealed three fragments with identical electrophoretic mobility. In addition, the vesicular preparations inhibited the activity of DNase I, a property typical of actin monomers. Filamentous material extracted from matrix vesicles showed ultrastructural features of F-actin. Reaction of this material with heavy meromyosin resulted in arrowhead formation, which is characteristic of acto-heavy meromyosin. The occurrence of actin in extracellular matrix vesicles may account for their budding from the osteoblastic plasma membrane, their possible motility in the matrix, and maintenance of the spherical shape.
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