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 apv@apv-mainz.de 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: mb@apv-mainz.de, 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: apv@apv-mainz.de
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: info@ecv.de
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 apv@apv-mainz.de, 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)