In vitro study of dual drug-eluting stents with locally focused sirolimus and atorvastatin release

Within the context of novel stent designs we developed a dual drug-eluting stent (DDES) with an abluminally focussed release of the potent anti-proliferative drug sirolimus and a luminally focussed release of atorvastatin with stabilizing effect on atherosclerotic deposits and stimulating impact on endothelial function, both from biodegradable poly(l-lactide)-based stent coatings. With this concept we aim at simultaneous inhibition of in-stent restenosis as a result of disproportionally increased smooth muscle cell proliferation and migration as well as thrombosis due to failed or incomplete endothelialisation. The especially adapted spray-coating processes allowed the formation of smooth form-fit polymer coatings at the abluminal and luminal side with 70 % respectively 90 % of the drug/polymer solution being deposited at the intended stent surface. The impacts of tempering, sterilization, and layer composition on drug release are thoroughly discussed making use of a semi-empirical model. While tempering at 80 °C seems to be necessary for the achievement of adequate and sustained drug release, the coating sequence for DDES should be rather abluminal–luminal than luminal–abluminal, as reduction of the amount of sirolimus eluted luminally could then potentially minimize the provocation of endothelial dysfunction. In vitro proliferation and viability assays with smooth muscle and endothelial cells underline the high potential of the developed DDES.     

Area postrema mediates the formation of rapid, conditioned palatability shifts in lithium-treated rats.

The rapid acquisition and subsequent retention of lithium-induced conditioned changes in taste reactivity responses to sucrose were examined in rats with the area postrema (AP) either ablated or intact. On 2 conditioning days, a series of brief intraoral sucrose infusions was paired with the effects of LiCl or NaCl injections. Repeated associations of the sucrose taste with the effects of lithium significantly reduced ingestive responses and increased aversive responses only in the AP-intact group. AP-ablated rats treated with LiCl and rats injected with NaCl displayed an ingestive pattern of responses. Only the AP-intact rats, previously injected with LiCl, subsequently displayed evidence of a conditioned taste aversion. We conclude that toxin activation of the AP is required to produce the conditioned shift in taste reactivity responses and subsequent expression of a taste aversion in rats treated with lithium. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Das Oxitron-System,ein neues biologisches Abwasserreinigungs-Verfahren für den BSB5-Abbau sowie zur Nitrifikation und Denitrifikation

The oxitron system: a new biological sewage treatment process for reducing BOD₅ and for nitrification and denitrification . In the oxitron process, the waste water passes through a fluidized sand bed. As in the case of droplets, a stable biological slime is formed on the sand particles. The particular efficacy of the process can be explained in terms of the high specific surface, of the order of more than 3000 m² per m³ reactor volume. This leads to a particularly effective use of available space. The high content of biomass makes the process largely insensitive to fluctuations in feed rates and toxic effects. The oxitron process is used as a biological purification stage for reducing BOD₅ or as the third purification stage for nitrification and denitrification. The reactor can be operated at particularly high solids concentrations (ca. 20 g/l). The correspondingly high oxygen consumption of this process requires the use of pure oxygen in the aerobic step; over 90% of the oxygen supply is utilized. The special advantages of the oxitron process are: (1) 30% lower capital costs than for conventional processes (operating costs are comparable); (2) space requirements are some 80% lower than for the best conventional technology presently available, facilitating expansion; (3) the mode of operation is extremely simple and is not subject to interference by blockages, etc. Design data and results for large scale test plant are reported.     

In vitro degradation and drug release of a biodegradable tissue adhesive based on functionalized 1,2-ethylene glycol bis(dilactic acid) and chitosan

Biodegradability and adhesive-associated local drug release are important aspects of research in tissue adhesive development. Therefore, this study focuses on investigating the in vitro degradation and drug release of a tissue adhesive consisting of hexamethylene diisocyanate functionalized 1,2-ethylene glycol bis(dilactic acid) and chitosan chloride. To prevent infections, ciprofloxacin hydrochloride (CPX·HCl) was incorporated into the adhesive. The influence of CPX·HCl on the adhesive reaction and adhesive strength was analyzed by FTIR-ATR-spectroscopy and tensile tests. The CPX·HCl release was investigated by HPLC. The degradation-induced changes at 37 °C were evaluated by gravimetric/morphological analyzes and micro-computer tomography. The antibiotic potential of the CPX·HCl loaded adhesive was determined by agar diffusion tests. The degradation tests revealed a mass loss of about 78 % after 52 weeks. The adhesive reaction velocity and tensile strength were not influenced by CPX·HCl. Using a 2 mg/g CPX·HCl loaded adhesive an inhibition of all tested bacteria was observed.     

Thermostabile, basische Proteinaseinhibitoren aus Kartoffeln isolierung und charakterisierung

Zusammenfassung Aus Kartoffeln (SorteMaritta) wurden durch Ammoniumsulfatf?llung, Hitzebehandlung, Ionenaustauscherchromatographie und pr?parative Polycrylamidgel-Elektrophorese vier basische Proteinaseninhibitoren isoliert. Die isoelektrischen Punkte der Inhibitoren liegen zwischen pH 9,2 und 9,8. über Sephadex Gelfiltration wurden für den Inhibitor K 1 ein MG von 8500 und für die Inhibitoren K 3, K 4 und K6 ein MG von 22000 bestimmt. Unterschiede bei den Inhibitoren in der AS-Zusammensetzung und in den spezifischen Aktivit?ten gegenüber sechs verschiedenen Proteinasen werden diskutiert. Vergleiche mit früher beschriebenen Inhibitoren werden vorgenommen. Eine Korrelation zwischen hohem Cystin-Gehalt und Thermostabilit?t bei den Inhibitorproteinen wird aufgezeigt.

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Thermostable basic proteinase inhibitors from potatoes isolation and characterization

Summary Four basic proteinase inhibitors were isolated from potato tubers (var.Maritta) by ammonium sulfate precipitation, heat treatment, chromatography on CM-cellulose and preparative polyacrylamide gel electrophoresis. Their isoelectric points are in the pH range 9.2–9.8. The molecular weights, as estimated by Sephadex gel filtration, were 8500 for inhibitor K 1 and 22 000 for the inhibitors K3, K4, and K6. Differences in inhibitors regarding amino acid composition and specificic activity against six different proteinases are discussed. Comparisons with previously described inhibitors are given. A correlation between high cystine content and thermostability of the inhibitor proteins is indicated.

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Wir danken Frau Christine Kmita-Dürrmann für technische Assistenz. Prof. Dr. H.-D. Belitz danken wir für die Unterstützung unserer Arbeit, u. a. durch Mittel der Deutschen Forschungsgemeinschaft (DFG)     

Leistungsgrenzen,Technologie und Anwendungen von Niedertemperatur-Wärmerohren

Zusammenfassung In jüngster Zeit fanden W?rmerohre im Bereich niedriger, Temperaturen (etwa−50°C bis 300°C) gesteigerte Aufmerksamkeit und ein immer breiter werdendes Anwendungsgebiet. Gegenüber den schon l?nger untersuchten Mittel- und Hochtemperatur-W?rmerohren treten verschiedene anders geartete Probleme auf. Gemessene Leistungen und errechnete Leistungsgrenzen, einige wichtige technologische Probleme sowie verschiedene Anwendungsbeispiele von Nieder-, Mittel- und Hochtemperatur-W?rmerohren werden besprochen.     

Proteaseinhibitors in potatoes Protein-, Trypsin- und Chymotrypsininhibitorenmuster durch isoelektrisches Fokussieren in Polyacrylamidgel. Eine Schnellmethode zur Identifizierung von Kartoffelsorten

Summary By applying iscelectric focusing in polyacrylamide gel, 42 proteins and 21 inhibitors were detected in 12 potato varieties. The protein- and inhibitor-patterns are very characteristic, and can be used for rapid variety identification. The protein distribution is not the same in the whole tuber. Germination tests showed a smaller inhibitor content in sprouts than in tubers. The alkaline and neutral inhibitors decreased, whereas more acidic inhibitors appeared.

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Proteaseinhibitoren in Kartoffeln Protein-, trypsin- and chymotrypsininhibitor patterns by isoelectric focusing in polyacrylamidegel. A rapid method for identification of potato varieties

Zusammenlassung Durch isoelektrisches Fokussieren in Polyacrylamidgel wurden in 12 Kartoffelsorten 42 Proteine und 21 Inhibitoren nachgewiesen. Die Protein- und Inhibitormuster sind sehr charakteristisch und können zur schnellen Sortendiagnose heraugezogen werden.Die Proteinverteilung ist nicht über die gesamte Knolle gleich. Keimversuche ergaben eine Verminderung des Inhibitorgehalts in Keimen gegenüber der Knolle. Während die basischen und neutralen Inhibitoren abnehmen, treten zusätzlich saure Inhibitoren auf.

     

Zur Erstellung einer computerunterstützten Grammatik “Flexionsmorphologie des Frühneuhochdeutschen”

The inflectional morphology of Early New High German is the subject of research at the Forschungsvorhaben Grammatik des Frühneuhochdeutschen at the University of Bonn. Because the High German of the period 1350–1700 shows strong graphemic and morphemic variation, we could not use improved computational lemmatizing alogorithms for computer-assisted analysis. Instead, the data base was extended by philological information manually analyzed. To illustrate our proceeding in setting up the paradigms requires explaining the different algorithms for analyzing verb and noun inflection. The numerous grammatical positions, for most of which little evidence is given, and the prevailing inflected structure precluded an automatic segmentation of verb forms. The program for establishing verb paradigms is based on extended informations (for instance, those about endings, historical inflection classes, preterite suffixes, etc.), and consists of steps for sorting, collecting, and printing. For nouns, the automatic segmentation can be carried out by using as a word-stem the nominative singular form, which always shows a zero-morpheme. In a lemmatizing procedure different from those already in use, the nominative plural form (singular stem + plural formative) is taken as word-stem in order to segmentize the plural cases, and thus avoid the problem of stem variation which is due to the “Pluralumlaut.” A noun class is defined by the combination of a singular paradigm, which is characterized by a genitive formative and a plural formative.