als PDF - ECV Editio Cantor Verlag
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als PDF - ECV Editio Cantor Verlag
APV – Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e. V. APV NEWS Nachrichten und Mitteilungen MAKING SCIENCE WORK Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V. Gemeinnütziger wissenschaftlicher Verein International Association for Pharmaceutical Technology 06 • 2014 1st 1ST EUROPEAN CONFERENCE on Pharmaceutics – Drug Delivery European Conference on Pharmaceutics 13 to 14 April 2015 Reims, France • Oral Short Lectures • Poster Presentations • Industrial Exhibition Drug Delivery • Hot Topics • • • • • • • • Drug Targeting Liposomes and Nanoparticles Oral Drug Delivery Pulmonary Drug Delivery Skin / Vaginal / Rectal / Nasal / Ear / Ocular Drug Delivery Smart Drug Delivery Systems Transdermal Drug Delivery Vaccine Delivery www.europeanmeeting.org 10th World Meeting onPharmaceutics, Biopharmaceutics and Pharmaceutical Technology 4 to 7 April 2016, SECC, Glasgow, Scotland • Industry Focus Sessions • Poster Presentations • Accompanying Exhibition ResearchPharm® SEE YOU IN GLASGOW IN 2016 Find out more www.worldmeeting.org APV NEWS – Aus der Geschäftsstelle Neues Angebot unseres Finanzierungsund Leasingpartners Leasing und Finanzierung von Investitionsgütern im Pharmabereich, z.B. Fertigungslinien, Laborgeräte, Neu- und Gebrauchtmaschinen, bietet zahlreiche Vorteile für Hersteller/Lieferanten und Endkunden. Gerne senden wir Ihnen weitere Informationen zu. Bitte fordern Sie weitere Informationen unter [email protected] an. APV NEWS – Aus dem Vereinsleben Lokale Gruppen Montag, 24. November 2014 Lokale APV-Gruppe Westfalen ab 19:30 Uhr am Hauptausgang des Dortmunder Bahnhofes als Startpunkt zum gemütlichen Bummel über den Weihnachtsmarkt. Anmeldung erforderlich bis zum 23. November 2014 bei Dr. Kathrin Bartscher. Mittwoch, 26. November 2014 Lokale APV-Gruppe Nord ab 18:30 Uhr im Hofbräuhaus (Esplanade 6, 20354 Hamburg) Anmeldung erforderlich bis zum 20. November 2014 bei Birgit Mootz. Mittwoch, 26. November 2014 Lokale APV-Gruppe Rhein-Main ab 19:30 Uhr. Ort wird noch bekanntgegeben. Weitere Informationen erhalten Sie bei Cathrin Pauly. Montag, 12. Januar 2015 Lokale APV-Gruppe Bonn/Köln/Aachen ab 19:30 Uhr im Restaurant Rietbrocks Weinhaus (Königstrasse 84, 53115 Bonn) Anmeldung erforderlich bis zum 10. Januar 2015 bei Dr. Michael Horstmann. Dienstag, 13. Januar 2015 Lokale APV-Gruppe Berlin um 19:00 Uhr, in den Räumen der CPL - Chemisch-pharmazeutisches Labor Rolf Sachse GmbH, Stieffring 14, Berlin. Anmeldung erforderlich bis zum 10. Januar 2015 bei Dr. Andreas Sachse. Liebe APV-Mitglieder, nach der erfolgreichen Gründung mehrerer lokaler Gruppen würden wir das Konzept der lokalen APV-Gruppen gerne auch in weiteren Regionen etablieren. Bitte sprechen Sie uns an, wenn Sie Interesse an einer Teilnahme an einer lokalen Gruppe in Ihrer Region haben oder als Ansprechpartner, unterstützt durch die APV-Geschäftsstelle, für eine neue lokale Gruppe zur Verfügung stehen würden. Wir freuen uns auf Ihre Rückmeldung! Ansprechpartner: Dr. Martin Bornhöft, Email: [email protected], Tel: + 49 6131 9769-30 APV NEWS 6-2013 APVnews – Infos aus der Hochschule What’s hot in European Journal of Pharmaceutics and Biopharmaceutics? Stefanie Funke, Ludwig-Maximilians-Universität, D-München A. Fortuna et al./European Journal of Pharmaceutics and Biopharmaceutics 88 (2014) 8–27 Intranasal delivery of systemic-acting drugs: Small-molecules and biomacromolecules Ana Fortuna, Gilberto Alves, Ana Serralheiro, Joana Sousa, Amílcar Falcão abstract As a non-invasive route, intranasal administration offers patient comfort and compliance which are hurdled in parenteral drug therapy. In addition, the current recognition that the high permeability and vascularization of nasal mucosa coupled to the avoidance of the first-pass elimination and/or gastrointestinal decomposition ensure higher systemic drug absorption than oral route has contributed to the growing interest for intranasal delivery of drugs that require considerable systemic exposure to exert their therapeutic actions (systemic-acting drugs). Nevertheless, several features may hamper drug absorption through the nasal mucosa, particularly the drug molecular weight and intrinsic permeability, and, therefore, several strategies have been employed to improve it, propelling a constant challenge during nasal drug (formulation) development. This review will firstly provide an anatomical, histological and mechanistic overview of drug systemic absorption after nasal administration and the relevant aspects of the therapeutic interest and limitations of the intranasal systemic delivery. The current studies regarding the nasal application of systemic-acting small drugs (analgesic drugs, cardiovascular drugs and antiviral drugs) and biomacromolecular drugs (peptide/protein drugs and vaccines) will also be outlined, addressing drug pharmacokinetics and pharmacodynamic improvements. R.M. Dutescu et al./European Journal of Pharmaceutics and Biopharmaceutics 88 (2014) 123–128 Semifluorinated alkanes as a liquid drug carrier system for topical ocular drug delivery R.M. Dutescu, C. Panfil, O.M. Merkel, N. Schrage abstract Semifluorinated alkanes (SFA, e.g. perfluorobutylpentane F4H5, perfluorohexyloctane F6H8) are inert, non-toxic fluids capable of dissolving lipophilic drugs. The aim of this study to assess the bioavailability and safety of SFAs as drug solvents for the topical ocular application of Cyclo- APV NEWS 6-2014 sporin A (CsA). A commer-cially available CsA formulation (Restasis®, 0.05% CsA in castor oil) was tested against two novel formulations of 0.05 % CSA in (a) F4H5 containing Ethanol (0.5 w/w %) and (b) F6H8 containing Ethanol (0.5 w/w %) with 0.05 % CsA. Formulations were tested on rabbit corneas cultured on an artificial anterior chamber with a constant flow of an aqueous humour supplement (Ex Vivo Eye Irritation Test (EVEIT) system). Anterior chamber fluids were sampled at multiple time points to analyse the CsA concentration following single and repeated application regimes by HPLC. Photographs of fluorescein sodium-stained corneas were recorded for corneal toxicity evaluation. The impact of the formulations on the integrity of the corneal barrier function was tested after drug application by fluorescein sodium corneal diffusion experiments. The influence on the corneal metabolism was evaluated by analysis of the metabolic markers glucose and lactate. Restasis® did not pass the corneal barrier after short term application, CsA in ethanolic F4H6 reached a maximum of 152.95 ng/ml in anterior chamber fluid samples whilst CsA in ethanolic F6H8 reached a maximum of 15.12 ng/ml. After repeated applications for 8 h, Restasis® reached 21.07 ng/ml compared to 247.62 ng/ml and 174.5 ng/ml for F4H5 and F6H8, respectively. No corneal toxicity was observed in following application of any of the formulations. In contrast to the commercially available castor oil-based formulation, CsA dissolved in SFAs reached therapeutic inner ocular concentrations after topical administration, possibly leading to the replacement of systemic applications of CsA for inflammatory ocular disease. D. D’Sa et al./European Journal of Pharmaceutics and Biopharmaceutics 88 (2014) 129–135 Predicting physical stability in pressurized metered dose inhalers via dwell and instantaneous force colloidal probe microscopy Dexter D’Sa, Hak-Kim Chan, Wojciech Chrzanowski abstract Colloidal probe microscopy (CPM) is a quantitative predictive tool, which can offer insight into particle behavior in suspension pressurized metered dose inhalers (pMDIs). Although CPM instantaneous force measurements, which involve immediate retraction of the probe upon sample contact, can provide information on inter-particle attractive forces, they lack the ability to appropriately imitate all critical particle pMDI interactions (e.g., particle re-dispersi- APVnews – Infos aus der Hochschule on after prolonged pMDI storage). In this paper, two novel dwell force techniques – indentation and deflection dwell – were employed to mimic long-term particle interactions present in pMDIs, using particles of various internal structures and a model liquid propellant (2H,3H perfluoropentane) as a model system. Dwell measurements involve particle contact for an extended period of time. In deflection dwell mode the probe is held at a specific position, while in indentation dwell mode the probe is forced into the sample with a constant force for the entirety of the contact time. To evaluate the applicability of CPM to predict actual pMDI physical stability, inter-particle force measurements were compared with qualitative and quantitative bulk pMDI measurement techniques (visual quality and light scattering). Measured instantaneous attractive (snap-in) and adhesive (max-pull) forces decreased as a function of increasing surface area, while adhesive forces measured by indentation dwell decreased as a function of dwell contact time for particles containing voids. Instantaneous force measurements provided information on the likelihood of floccule formation, which was predictive of partitioning rates, while indentation dwell force measurements were predictive of formulation re-dispersibility after prolonged storage. Dwell force measurements provide additional information on particle behavior within a pMDI not obtainable via instantaneous measurements. F. Danhier et al./European Journal of Pharmaceutics and Biopharmaceutics 88 (2014) 252–260 Nanosuspension for the delivery of a poorly soluble anti-cancer kinase inhibitor Fabienne Danhier, Bernard Ucakar, Marie-Lyse Vanderhaegen, Marcus E. Brewster, Tina Arien, Véroni-que Préat abstract We hypothesized that nanosuspensions could be promising for the delivery of the poorly water soluble anti-cancer multi-targeted kinase inhibitor, MTKi 327. Hence, the aims of this work were (i) to evaluate the MTKi 327 nanosuspension for parenteral and oral administrations and (ii) to compare this nanosus-pension with other nanocarriers in terms of anti-cancer efficacy and pharmacokinetics. Therefore, four formulations of MTKi 327 were studied: (i) PEGylated PLGA-based nanoparticles, (ii) self-assembling PEG750 p-(CL co TMC) polymeric micelles, (iii) nanosuspensions of MTKi 327; and (iv) Captisol solution (pH = 3.5). All the nano-formulations presented a size below 200 nm. Injections of the highest possible dose of the three nano-formulations did not induce any side effects in mice. In contrast, the maximum tolerated dose of the control Captisol solution was 20-fold lower than its highest possible dose. The highest regrowth delay of A-431-tumor-bearing nude mice was obtained with MTKi 327 nanosuspension, administered intravenously, at a dose of 650 mg/kg. After intravenous and oral administration, the AUC0∞ of MTKi 327 nanosuspension was 2.4-fold greater than that of the Captisol solution. Nanosuspension may be considered as an effective anticancer MTKi-327 delivery method due to (i) the higher MTKi-327 maximum tolerated dose, (ii) the possible intravenous injection of MTKi 327, (iii) its ability to enhance the administered dose and (iv) its higher efficacy. Impressum: Redaktion Prof. Dr. Jörg Breitkreutz (Präsident) Dr. Martin Bornhöft (Leiter Geschäftsstelle) Vorstand der APV Dr. Rainer Alex · Dr. Hermann Allgaier · Dr. Kathrin Bartscher · Prof. Dr. Jörg Breitkreutz · Prof. Dr. Heribert Häusler · Prof. Dr. Sandra Klein · Dr. Andreas Rummelt · Dr. Alexandra Steckel Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e. V. (APV) Kurfürstenstraße 59 55118 Mainz (Germany) Telefon +49 6131 9769-0 Telefax +49 6131 9769-69 e-mail: [email protected] http://www.apv-mainz.de Verlag ECV · Editio Cantor Verlag für Medizin und Naturwissenschaften GmbH Baendelstockweg 20 88326 Aulendorf, Germany Telefon +49 7525 940-0 Telefax +49 7525 940-180 e-mail: [email protected] http://www.ecv.de Alle Rechte bei APV e. V. All rights reserved Printed in Germany Jede Form des Nachdrucks verboten Druck Holzmann Druck GmbH & Co. KG Gewerbestr. 2 86825 Bad Wörishofen, Germany Satz Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e. V. (APV) Kurfürstenstraße 59 55118 Mainz (Germany) APV NEWS 2-2012 APV NEWS – Leasing-Highlights zu Sonderkonditionen Kfz-Leasing: Vorteile für APV-Mitglieder Die APV hat für ihre Mitglieder einen Rahmenvertrag mit einem bekannten Leasing-Unternehmen geschlossen. Als Kooperationspartner der APV bietet das Unternehmen Leasing von Neu- und Gebrauchtfahrzeugen zu Sonderkonditionen. Alle Marken und Modelle sind lieferbar. Die nachfolgende Tabelle gibt nur wenige aktuelle Beispiele möglicher Modelle und Marken wieder. NEU: Vorführwagen (VFW) aus dem Leasing-Pool und Dienst-/Werkswagen (DW) zu attraktiven Konditionen erhältlich. Alle Preise in Euro zuzüglich gesetzlicher Mehrwertsteuer. Beschaffung durch die Leasing-Gesellschaft. 36 Monate Laufzeit, 15.000 km pro Jahr, Angebote freibleibend. Der Nachlass auf den Listenpreis ist in die ermäßigte Rate einkalkuliert. Anfragen bitte an [email protected], das Leasing-Unternehmen wird sich dann mit Ihnen in Verbindung setzen. JETZT NEU: Leasing auch für andere Investitionsgüter Leasing und Finanzierung zu günstigen Konditionen sind auch für Investitionsgüter wie Walzenpressen, Verpackungsmaschinen, Laboreinrichtungen etc. über die APV möglich. Sprechen Sie uns an. Hersteller/Typ Listenpreis mtl. Rate Audi Q5 2.0 TDI 120kW/163PS S tronic inkl. Radioanlage Chorus, Klimaautomatik, 17"LM-Felgen im 7-Speichen-Design etc. 35.042,00 € 389,00 € Audi A6 Avant 3.0 TDI quattro 160kW/218PS inkl. Komfortklimaautomatik, Xenon plus, LM-Felgen 6-Arm-Design, Tempomat, Glanzpaket etc. 44.832,00 € 409,00 € BMW 114i 3-Türer inkl. Klimaautomatik, Radio Professional, Lichtpaket, Ablagenpaket, Armauflage vorn verschiebbar etc. 19.647,00 € 215,00 € BMW 218i Active Tourer 100kW/136PS inkl. Radio/CD, Bluetooth Audiostreaming, Klimaanlage, Sport-Lederlenkrad, 16" LM-Räder etc. 22.958,00 € 289,00 € Jaguar XF Sportbrake „Vfw“ 2.2 L Diesel 147kW/200PS inkl. Automatik, Navi, Leder, Einparkhilfe mit Rückfahrkamera, Sitzheizung etc. 48.739,00 € 329,00 € Mazda CX-5 „Sendo“ Skyactiv-Diesel 110kW/150PS inkl. Automatik, Metallic, Navi, Klimaautomatik, LM-Felgen, Bi-Xenon, Spurhalteassistent etc. 28.840,00 € 449,00 € MINI One Countryman 100kW/136PS inkl. Klimaanlage, Radio MINI CD, Auto Start Stop Funktion, Fussmatten Velours, Armauflage vorn etc. 17.336,00 € 215,00 € Porsche Boxster „Vfw“ 195kW/265PS inkl. PDK, PCM-Navi, Sportsitze, Bi-Xenon, ParkAssistent, 2-Zonen-Klimaautomatik, Sitzheizung etc. 64.814,00 € 699,00 € Porsche Cayenne Diesel Tiptronic S 193kW/262PS inkl. Metallic, PCM, Leder, BOSE Surround Sound-System, Luftfederung, Panoramadach etc 88.834,00 € 1.059,00 € Skoda Fabia (neues Modell !) 1.0 MPI Active 44kW/60PS inkl. Klimaanlage, Skoda Surround Soundsystem DAB+, Reifendrucküberwachung etc. 10.739,00 € 115,00 € Skoda Octavia Combi 1.2 TSI Active 63kW/86PS inkl. Musiksystem, Klimaanlage, elektrisch einstell- und beheizbare Außenspiegel etc. 15.613,00 € 149,00 € Toyota Yaris 5-Türer Hybrid Comfort 55kW/77PS inkl. Klimaautomatik, Multimedia-Audiosystem Touch2 mit Rückfahrkamera, USB, Bluetooth etc. 15.462,00 € 149,00 € Toyota Verso „Skyview“ 5-Sitzer 1,6l Diesel 82kW/112PS inkl. PanoramaGlasdach, Navi, Klimaautomatik, LM-Felgen, Rückfahrkamera etc. 23.773,00 € 259,00 € Volvo XC60 D3 Kinetic 100kW/136PS inkl. Audiosystem Performance Sound, Klimaautomatik, Einparkhilfe hinten, LM-Felgen „SEGIN“ etc. 29.714,00 € 369,00 € VW Polo 1,0l 3-Türer 44kW/60PS 5-Gang inkl. Klimaanlage, Radio „Composition Colour“, Reifenkontrollanzeige etc. 11.563,00 € 99,00 € VW Tiguan Trend & Fun 1,4l BMT 6-Gang 90kW/122PS inkl. Leichtmetallräder „Portland“, Radio/CD „RCD 310“, Klimaanlage etc. 21.130,00 € 155,00 € Vfw = Vorführwagen zu Sonderkonditionen, DW = Dienst-/Werkswagen (genannter Listenpreis=Kaufpreis)