Single-Step Granulation Method with Microwaves: Preliminary Studies and Pilot Scale Results

Common pharmaceutical excipients and compounds were dried either by a simple convection method or by a combined convection and microwave method in a static bed or by a combined microwave and vacuum method in a mixed bed. A simple placebo granulation was dried by an exclusive vacuum method and by a combined microwave and vacuum method in a mixed bed. The results were compared.     

Treatment with alendronate prevents fractures in women at highest risk: results from the Fracture Intervention Trial

BACKGROUND: The efficacy of antiresorptive therapy in preventing fractures in women at highest fracture risk, such as very elderly women or those with severe osteoporosis, is uncertain. PARTICIPANTS AND METHODS: Using data from a double-blind, randomized, placebo-controlled clinical trial that enrolled 2027 postmenopausal women aged 55 to 81 years with low femoral neck bone mineral density (BMD) and existing vertebral fractures, we examined the consistency of the effect of treatment with alendronate sodium in preventing fractures within a priori-specified risk subgroups defined at baseline by age, bone density, number of preexisting vertebral fractures, and history of postmenopausal fracture. The women were randomized to oral administration of alendronate or placebo and followed up for an average of 2.9 years. The initial dose of alendronate sodium was 5 mg/d; the dosage was increased from 5 to 10 mg/d at 24 months. New vertebral fractures, the primary end point of this arm of the trial, were defined by morphometry as a decrease of 20% and at least 4 mm in any vertebral height between baseline and a follow-up radiograph at 36 months. Incident clinical fractures, the secondary end point, included nonspine and clinical (symptomatic) vertebral fractures. All clinical fractures were confirmed with x-ray film reports or, in the case of clinical vertebral fractures, x-ray films. RESULTS: Overall, there was a 47% significant reduction in risk of new vertebral fractures in the alendronate group compared with the placebo group. The reduction in risk of new vertebral fracture was consistent across fracture risk categories including age (relative risk [RR], 0.49 in women < 75 years compared with 0.62 in those > or = 75 years), BMD (RR, 0.54 in women with a femoral neck BMD < 0.59 g/cm2 [median] compared with 0.53 in those with a BMD > or = 0.59 g/cm2), and number of preexisting vertebral fractures (RR, 0.58 in women with 1 vertebral fracture compared with 0.52 in those with > or = 2). The overall significant 28% reduction in risk of incident clinical fractures in the alendronate group compared with the placebo group was also observed within these subgroups. Compared with the number of lower-risk women, a similar or smaller number of high-risk women needed to be treated to prevent 1 fracture. For example, 8 women aged 75 years or older compared with 9 women younger than 75 years, or 4 women with 2 or more existing vertebral fractures compared with 16 women with 1 existing vertebral fracture, needed to be treated with alendronate for 5 years to prevent 1 new vertebral fracture. CONCLUSIONS: Alendronate effectively reduces fracture risk in postmenopausal women with vertebral fractures and low BMD, including those women at highest risk because of advanced age or severe osteoporosis. Since the risk reductions observed with alendronate treatment were consistent within fracture risk categories, more fractures were prevented by treating women at highest risk.     

Biocide polymers

Summary Potential polymeric herbicides have been synthesized by reacting poly(acrylic acid)s with 3-aniino-1,2,4-triazole and 1-acetyl-5-amino-1,2,4-triazole, respectively. The produced copolymers contained the active moieties as pendant groups in the range of 3 to 27 per cent of weight and with a content of carboxyl groups up to 95 mol-%. The hydrolytic release of 3-amino-1,2,4-triazole was investigated.Part 12: M. Hartmann, H,-J. Bauer, A. Pritzsche and K. Wermann, Makromol. Chem., in press     

An analytical reflection and emission UHV surface electron microscope

An UHV surface electron microscope is described which allows the study of surfaces under vacuum conditions common in surface science with the following techniques: LEERM; LEED; photo, thermionic, secondary emission microscopy; absolute micro area work function measurements. In particular, the first LEERM of Mo(110) and Si(111) surfaces are presented. They show monoatomic steps with high contrast due to Fresnel diffraction and structural differences, respectively. Condensed silver crystallites are imaged. Gold adsorption layers on Si(111) show strong contrast in photoemission; the layer thickness is deduced from LEED.     

Verbesserung des Vakuums in Isoliergefäßen aus Glas

Improving the vacuum would increase the insulation capacity of commercially available glass containers by a factor of about two. To do this, pressures of 10^?4 mbar must be attained. Different approaches were taken to meet this objective. As an alternative to today's commonly practiced sealing method, three possibilities are introduced which eliminate the necessity of pump stub narrowing which causes reduced conductance. Furthermore, depending on the sealing process used, the gases occuring during sealing are either avoided completly or they can at least be reduced by having the chance of exact temperature control resp. by a lower separation temperature. A completly different approach was taken by using Getters, of which a metal hydride on a TiVMn base proved especially suitable. It is activated by heat and can be integrated into the normal production process without any problem. Aside from a shorter pump period, the added advantage here is the containment of the gasses occuring during sealing as well as that of the longterm gasses.     

Penicilloyl peptides are recognized as T cell antigenic determinants in penicillin allergy

Although hapten immune responses have been intensively studied in the mouse, very little is known about hapten determinants involved in human allergic reactions. Penicillins, as chemically reactive compounds of low molecular weight, constitute typical examples of hapten allergens for humans. Penicillins become immunogenic only after covalent binding to carrier proteins and in this form frequently induced IgE-mediated allergic reactions in patients subjected to antibiotic treatment. However, our previous data strongly indicated that penicillins also form part of the epitopes contacting the antigen receptors of beta lactam-specific T cells in allergic individuals. We have therefore investigated the molecular constraints involved in the T cell immune response to penicillin G (Pen G). Designer peptides containing a DRB1*0401-binding motif and covalently modified with Pen G via a lysine epsilon-amino group were found to induce proliferation of Pen G-specific T cell clones. A precise positioning of the hapten molecule on the peptide backbone was required for optimal T cell recognition. Furthermore, we extended these observations from our designer peptides to show that a peptide sequence derived from a natural DRB1*1101-binding peptide modified in vitro with Pen G, also acquired antigenic properties. Our data for the first time provide insight into the manner in which allergenic haptens are recognized by human T cells involved in allergic reactions to drugs and suggest possible mechanisms leading to the onset of these adverse immune responses.     

Lipasekatalysierte Triglyceridumesterung in einem lösungsmittelfreien Prozeß I: Analytik und Umesterungskinetik

Lipase-Catalyzed Interesterification of Triglycerides in a Solvent-Free Process I: Analytics and Kinetics of the Interesterification The interesterification of lipids catalyzed by immobilized lipases is an interesting substitute to the chemical interesterification. Studies using an industrial manufactured biocatalyst in a solvent-free process were performed. The kinetics of the interesterification were examined as a function of temperature and water content of the reaction system. The reaction rate of the interesterification can be described with reversible first order reaction kinetics. A part of the triglycerides of the substrate is hydrolyzed by a lipasecatalyzed lipolysis. Hydrolysis products are 1,2(2,3) and 1,3-diglycerides. This shows that an unspecific interesterification is catalyzed if the residence time is extended.     

Design aspects of MOS-controlled thyristor elements: technology,simulation, and experimental results

2.5-kV thyristor devices have been fabricated with integrated MOS controlled n⁺-emitter shorts and a bipolar turn-on gate using a p-channel DMOS technology. Square-cell geometries with pitch variations ranging from 15 to 30 μm were implemented in one- and two-dimensional arrays with up to 20000 units. The impact of the cell pitch on the turn-off performance and the on-state voltage was studied for arrays with constant cathode area as well as for single-cell structures. By realizing MOS components with submicrometer channel lengths, scaled single cells are shown to turn off with current densities of several kiloamperes per square centimeter at a gate bias of 5 V. In the case of multi-cell ensembles, turn-off performance is limited due to inhomogeneous current distribution. Critical process parameters as well as the device behavior were optimized through multidimensional numerical simulation