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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 4 (1987), S. 490-494 
    ISSN: 1573-904X
    Keywords: tissue tolerance ; intramuscular ; injection ; rat ; plasma enzyme activity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The local tissue damage after intramuscular injection caused by various commercially available injection solutions was determined in the albino rat, by measuring plasma activities of creatine phosphokinase, aspartate aminotransferase, and lactic dehydrogenase, the tissue activity of creatine phosphokinase, and macroscopic changes in the muscle at the injection site (gastrocnemius muscle). The plasma enzyme activities were determined 2, 6, 18, and 28 hr after the injection. After 28 hr the animals were sacrificed for macroscopic inspection of the injection site and for the determination of tissue enzyme activity. The tissue injury caused by the test substances correlated well with the elevated creatine phosphokinase activity (2 hr). The elevations of aspartate aminotransferase (18 hr) and lactate dehydrogenase (2 hr) activity as well as the loss of tissue creatine phosphokinase activity were less indicative of differences between test preparations. The i.p. administration of some of the test preparations caused increased enzyme activity without muscle damage, which could interfere with the test results. The creatine phosphokinase determination indicates the damage occurring immediately after the administration of the test solution, and the macroscopic inspection offers the possibility to obtain some information on the evolution of the muscular lesion.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 5 (1988), S. 677-679 
    ISSN: 1573-904X
    Keywords: Ciclosporin ; intestinal absorption ; lipid vehicle ; in vivo model ; lipid digestion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The influence of lipid vehicles on the intestinal absorption of Ciclosporin was studied in vivo. The model takes into account the effect of the intestinal lipid digestion on the absorption after intraduodenal administration of [3H]Ciclosporin in olive oil or middle-chain triglyceride (MCT) to the bile duct-cannulated rat. Digested vehicles significantly promoted the absorption compared to nondigested vehicles. In the nondigested state, olive oil was a significantly better vehicle than MCT, whereas the difference between both lipids was only a trend in the digested state. Further studies with variants of this in vivo model should determine the influence of abnormalities of fat digestion and absorption on the pharmacokinetics and pharmacodynamics of a drug with a low therapeutical index.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 5 (1988), S. 673-676 
    ISSN: 1573-904X
    Keywords: Ciclosporin ; intestinal absorption ; lipid vehicle ; in vitro model ; lipid digestion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The influence of lipid vehicles on the intestinal absorption of Ciclosporin was studied in vitro. The effect of the intestinal lipid digestion was considered on the partition of the drug from olive oil or middle-chain triglyceride (MCT) into phases of simulated intestinal content. The phases obtained after ultracentrifugation were analyzed for their Ciclosporin content and characterized for their lipid classes. For both lipid vehicles the presence of lipolysis products did not promote the partition of the drug into the aqueous phase. The absorption in vivo was not related to the drug amount in the aqueous phase and in the oil phase. Therefore, phase quantification in vitro cannot simulate the dynamics of in vivo absorption events following application of a poorly water-soluble drug in a lipid vehicle.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 6 (1989), S. 958-960 
    ISSN: 1573-904X
    Keywords: sugar esters ; solubilizers ; solid surfactant solution ; surfactants, biodegradable ; ciclosporin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract This paper describes the preparation of solid solutions of ciclosporin as model solubilizate in water-soluble sugar esters, which are solid, biodegradable, and nontoxic surfactants. Sugar esters were found to be excellent solubilizers for poorly water-soluble drugs such as ciclosporin. Such systems are suitable for the preparation of solid dosage forms for the purpose of oral administration. Addition of water to the solid solutions yields clear solutions of the solubilizate.
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  • 5
    ISSN: 1573-904X
    Keywords: Arrhenius equation ; bioindicator ; propylene glycol ; propylene glycol–water mixtures ; thermodynamic data ; Z value
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Our interest in calculating the thermodynamic data by means of the Arrhenius equation was based on two observations: (a) the thermal death time increases considerably when the bioindicators Bacillus subtilis var. niger and Bacillus stearothermophilus are sterilized in nonaqueous hydrophilic solutions as found in propylene glycol (PG) with low water concentrations; and (b) the inactivation kinetics of Bac. stearothermophilus does not follow a first-order reaction. The frequency factor A and the entropy of activation ΔS* have the highest values in water and the lowest value in PG; ΔS* for Bac. stearothermophilus in water is 812 J/mol K; however, in PG it is −9.6 J/mol K. A good correlation between ΔS* and the enthalpy ΔH* is found, indicating possible protein denaturation during thermal inactivtion. The moderate positive and negative ΔS* values in PG and PG with low water concentrations might be explained by (a) rigid conformation of proteins due to stabilization and (b) slow reaction, making the complex a less probable structure, when the activated complex is built only under considerable rearrangement of the structure of the reactant molecules. The opposite was observed with the Z and Z* values, the latter being defined as Z values of nonlogarithmic survival curves. The Z values increase with increasing concentrations of PG, i.e., for Bac. subtilis of Z = 8°C in water up to Z = 23°C in PG and for Bac. stearothermophilus of Z = 6°C up to Z* = 27°C. The calculated free enthalpy of activation ΔG* is about 100 kJ/mol for both spore formers tested in the mentioned suspending medium. The ΔG* values found are similar to literature data of the denaturation of most proteins. These thermodynamic data do not explain the enormous increase of resistance in PG–water mixtures.
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  • 6
    ISSN: 0075-4617
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Aus dem wäßrigen, gepufferten Extrakt von acetongetrockneter Bäckerhefe wird, nach Vorfällung inaktiven Materials mit Essigsäure, durch Ammonsulfat-und Acetontrennung sowie Chromatographie an DEAE-Sephadex eine Proteinfraktion mit Acetokinase- und Phosphotransacetylase-Aktivität gewonnen. Die Acetokinase ist Mg2⊕- oder Mn2⊖-Ionen bedürftig; sie wird durch Fluorid gehemmt. Die Phosphotransacetylase zeigt keine Arsenolyse-Reaktion; sie ist frei von Myokinase und Acetylphosphatase. Durch fraktionierte Säurefällung wird die durch Fluorid nicht hemmbare Acetthiokinase gewonnen. Während diese die Energie von ATP auf Acetylcoenzym A überträgt, wird die Bedeutung des Systems Phosphotransacetylase + Acetokinase darin gesehen, daß sie die Energie von überschüssigem Acetylcoenzym A auf ATP zurück zu übertragen vermag.
    Additional Material: 13 Tab.
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  • 7
    ISSN: 0009-286X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Process Engineering, Biotechnology, Nutrition Technology
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 601 (1956), S. 202-215 
    ISSN: 0075-4617
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: In ruhenden Bakterien ist die pantothensäurebedürftige Acetylcholinbildung auf den Zusatz von Acetat angewiesen. Glucose kann nicht durch ATP ersetzt werden. In einfacher Weise läßt sich aus acetongetrockneten Bakterien ein aktiver Extrakt bereiten. Für die Acetylcholinbildung in diesem Extrakt ist entweder Coenzym A zusammen mit ATP oder Acetylphosphat erforderlich oder Coenzym-A-acetat. Morin ist ein Hemmstoff für die Acetylcholinbildung sowohl im Extrakt als auch in ruhenden oder wachsenden Bakterien.
    Additional Material: 1 Ill.
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  • 9
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 601 (1956), S. 216-232 
    ISSN: 0075-4617
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Aus dem Extrakt von acetongetrockneten Bakterien wird bei pH 4,5 Acetataktivierendes Enzym zusammen mit Myokinase ausgefällt. Aus der Restlösung wird durch Ammonsulfat bei pH 6,8 das Acetylcholin-synthetisierende Ferment in einem anderen Konzentrationsbereich gefällt als Cholinacetylase aus Nervengeweben. Das Acetylcholin-synthetisierende Ferment benötigt Coenzym A und Acetylphosphat, keine Kaliumionen oder andere Kationen und besitzt ein scharfes Wirkungsoptimum bei pH 6.7. Durch fraktionierte Fällungen, Elektrophorese oder durch Hemmstoffe kann die Cholinacetylase-Aktivität nicht von der Phosphotransacetylase-Aktivität getrennt werden, die zur Arsenolyse Kalium-oder Ammonium-Ionen erfordert. Das Ferment wird als Acetylcholinsynthetisierende Transacetylase angesehen, die den Acetylrest, dem Energiegefälle folgend, sowohl von Acetylphosphat auf Coenzym A als auch von Coenzym A-acetat auf Cholin zu übertragen vermag.
    Additional Material: 3 Ill.
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  • 10
    Electronic Resource
    Electronic Resource
    Weinheim : Wiley-Blackwell
    Chemie Ingenieur Technik - CIT 52 (1980), S. 609-609 
    ISSN: 0009-286X
    Keywords: Granulieren ; Leistungsaufnahme ; Flüssigkeitsbedarf ; Pulverhaufwerk ; Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Process Engineering, Biotechnology, Nutrition Technology
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
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