The 2nd Electronic Conference on Pharmaceutical Sciences
1–31 May 2012
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Welcome from the Chairs
Welcome from the Chair of the Forum
Welcome to the 2nd Electronic Conference on Pharmaceutical Sciences (ECPS 2012). The Conference covers research in key areas of opportunity and challenge in pharmaceutical sciences, including:
Participants in this multidisciplinary conference will be able to examine, explore and critically engage with issues and advances in these and related areas. We hope to facilitate debates on these topics from academic and industrial perspectives, which will contribute to making drug development globally more successful and efficient.
A special feature of the Conference is that it is an electronic conference. This type of conference is particularly appropriate and useful for pharmaceutical research because the area is progressing rapidly, while activities in industry and academia are simultaneously becoming increasingly globalized. Successful research therefore requires interaction with individuals and groups around the world, demonstrating the need for new types of communication within our community. An electronic conference provides a platform for rapid and direct exchanges about the latest research findings, as well as a possibility for global meetings with no limitations related to traveling. To further remove barriers to "attendance", participation in the Conference as an author or other participant is free of charge.
The 2nd Electronic Conference on Pharmaceutical Sciences will be held at https://www.sciforum.net/conference/ecps2012, on a platform developed by MDPI to organize electronic conferences.
The 2nd Electronic Conference on Pharmaceutical Sciences is sponsored by MDPI and the scientific journal Pharmaceutics. Accepted papers will be published in the proceedings of the Forum, and selected papers will be published in Pharmaceutics.
I am very grateful to attendees, in particular authors, members of the Scientific Advisory Committee, session chairs and organizers.
I hope that your participation in the 2nd Electronic Conference on Pharmaceutical Sciences will prove to be interesting, enjoyable and above all beneficial.
Dr Clare Strachan
Dr Clare Strachan completed a PhD in 2005 at the University of Otago (in collaboration with the University of Cambridge) and subsequently became a post doctoral researcher and then group leader at the Centre for Drug Research, University of Helsinki, Finland. She is currently a Senior Lecturer at the School of Pharmacy, University of Otago and has recently accepted a position at the Faculty of Pharmacy, University of Helsinki as an Assistant Professor. She has supervised numerous postgraduate researchers, including six PhD researchers to completion and another seven currently. She has published over 60 articles in international peer-reviewed scientific journals, and has active collaborations with researchers at various universities in Europe and the USA. She has been invited to present at pharmaceutical and spectroscopic conferences around the world. In 2011, she was awarded a University of Otago 2011 Early Careers Award for Distinction in Research.
Dr Clare Strachan’s main research interests involve the physico-chemical characterisation of solid drugs and dosage forms. In particular she has used traditional and novel spectroscopic methods to understand solid state forms of drugs and excipients and changes during manufacturing, storage and dissolution. The main spectroscopic techniques she has used are infrared, near-infrared, Raman, terahertz pulsed spectroscopy. Spatially resolved analysis has involved Raman mapping and coherent anti-Stokes Raman microscopy. Analysis of these data is supported by various chemometrics approaches, both qualitative and quantitative, and computational chemistry methods including ab initio calculations.
Call for Papers
- Advances in the solid state field
- Nanotechnology for drug delivery
- Design and processing of protein and peptide formulation
- Innovations in pharmaceutical manufacturing
- Imaging in drug and dosage form development
- Physiologically Relevant in Vitro Models
Instructions for Authors
- Full author names
- Affiliations and authors' e-mail addresses
Videos are highly encouraged where they enhance scientific understanding and may be submitted as supplementary material attached to the abstract website of the pdf file main text. Video files may be submitted as .flv (preferred) or .avi formats.
Authors are encouraged to preare a couple of slides in PowerPoint or similar software, to be displayed online along with the Communication. Slides, if available, will be displayed directly in the website using Sciforum.net's proprietary slides viewer. Slides can be prepared in exactly the same way as for any traditional conference where research results can be presented. Slides should be converted to the PDF format before submission so that our process can easily and automatically convert them for online displaying.
Submissions should be done by the authors online by registering with www.sciforum.net, and using the "new submission" function once logged into system.
MDPI AG, the publisher of the Sciforum.net platform, is an open access publisher. We believe that authors should retain the copyright to their scholarly works. Hence, by submitting a Communication paper to this conference, you retain the copyright of your paper, but you grant MDPI AG the non-exclusive right to publish this paper online on the Sciforum.net platform. This means you can easily submit your paper to any scientific journal at a later stage and transfer the copyright to its publisher (if required by that publisher).
List of accepted submissions (27)
Laminar Dispersive and Distributive Mixing with Dissolution and Applications to Hot-melt Extrusion
Submitted: 27 Feb 2012
Abstract: Show Abstract
|Hot Melt Extrusion (HME), a novel and potentially disruptive process for manufacturing oral dosage pharmaceutical products, has been explored and studied in recent times, by both industrial and academic investigators, because of its potential of rendering poorly water-soluble active pharmaceutical ingredients (APIs) readily bioavailable to patients through oral dosages. This article presents a brief review of HME from the "elementary steps of polymer processing" perspective: handling of particulate solids, melting, mixing, devolatilization and stripping, pressurization, pumping, as well as dissolution of the API in molten polymeric excipient processed stream. In contrast to traditional polymer processing, the dissolution of the API in the molten excipient during HME is the most important, key, elementary step. The main focus of this article is to discuss the physico-chemical and transport phenomena involved in dissolution and the material, equipment design, and HME process variables which affect it. The main task of the dissolution is to completely dissolve APIs in polymeric melt within the shortest possible residence time, without raising the processed stream melt temperature, and eliminating the possibility of degradation of heat sensitive APIs. We concluded from our work that the dissolution process is a laminar forced convective diffusion process. We will also present results on how to promote the dissolution rate through three categories of variables: process variables (screw speed, feeding rate, barrel temperature,), equipment variables (screw elements and configurations) and material variables (viscosity ratio, solubility parameters and particle sizes of API and excipient particulates). A novel viscometric method for the determination of the solubility of APIs in polymeric melts will also be discussed.|
Preparation and characterization of carbamazepine-polyethylene oxide hot-melt extruded solid dispersions
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Submitted: 29 Feb 2012
Abstract: Show Abstract
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|The aim of the presented study was to investigate the possibility of usage of polyethylene oxide polymer (PEO, Polyox® WSR 301, DOW, USA) in the preparation of carbamazepine hot-melt extruded solid dispersions. Hot-melt extrusion (HME) is a simple, solvent free and continuous processing technique used to produce variety of dosage forms. Thermoplastic materials, such as PEO polymers, are required for the process feasibility. Poloxamer 407 (Lutrol® F127, BASF, Germany) was used as a plasticizer to facilitate the HME process, by reducing the processing temperature and lowering the monitored torque. Physico-chemical properties of carbamazepine and polymers, their physical mixtures and dispersions made by melt-mixing or HME were characterized in detail. A hot-melt extruder with one rotating screw was used for the preparation of solid dispersions by HME technique (RCP-0250 Microtruder, Randcastle extrusion systems, USA). Samples were analyzed by differential scanning calorimetry (DSC), thermo-gravimetric analysis (TGA), FT-IR spectroscopy and hot-stage microscopy (HSM) methods. Obtained results indicate that the addition of plasticizer enables preparation of carbamazepine-PEO hot-melt extrudates using a single-screw extruder configuration. It was demonstrated that there is no degradation of CBZ upon heating in the HME processing temperature range (90-110°C). Furthermore, the crystalline form of CBZ was not altered during the HME processing. The presence of CBZ form III crystals, homogeneously dispersed in the hot-melt extrudates, was confirmed. Dispersion of CBZ crystals in the polymers mixtures was visualized using the polarizing HSM technique. Presented study demonstrates the potential of PEO WSR 301 application in the preparation of carbamazepine hot-melt extruded solid dispersions.|
The Artificial Stomach and Duodenum (ASD): A physiologically relevant in vitro dissolution tool
Submitted: 05 Mar 2012
Abstract: Show Abstract
|The artificial stomach and duodenum (ASD) is a physiologically relevant in vitro dissolution tool that simulates the pH, mixing conditions, fluid composition and fluid flow in the gastric and duodenum compartments. This tool is designed to generate gastric and duodenal concentration profiles to capture dissolution, precipitation and supersaturation phenomena under conditions that simulate the in vivo environment. Duodenal concentration profiles generated from ASD experiments have the potential to provide a rank order prediction of in vivo absorption of compounds as a function of formulation, gastric pH, or gastric emptying time. In this work, we report the IVIVC we established between ASD duodenal concentration profiles generated in our lab, and human in vivo duodenal concentration profiles that were obtained upon oral administration of solution doses of ketoconazole and dipyridamole to healthy volunteers. As an example that demonstrates the application of this tool, we also report on the rank order IVIVC we established between the plasma exposure of dipyridamole and ASD duodenal concentration profiles we generated, under standard and elevated gastric pH conditions. Carino, S. et al. 2006; Relative bioavailability estimation of carbamazepine crystal forms using an artificial stomach-duodenum model. J. Pharm Sci 95(1), 116-125.  Psachoulias, D., et al. 2011; Precipitation in and Supersaturation of Contents of the Upper Small Intestine After Administration of Two Weak Bases to Fasted Adults. Pharm. Research, 28(12): 3145-3158  Russell, T. L., et al. 1994; pH-Related Changes in the Absorption of Dipyridamole in the Elderly. Pharm. Research 11 (1): 136-143|
Gene Delivery using Non-Viral Vectors (Cyclodextrins) with Pluronic-F127 and Folic Acid
Submitted: 12 Mar 2012
Abstract: Show Abstract
|Over the years, gene therapy has gained much attention across the field of research. The ability to deliver genes into cells offers the opportunities to treat various human genetic disease which results from mutation or deletion of gene(s). Effective gene delivery is highly dependent on its stability and ability to transfect across cell membrane and interferes with the host DNA. However, DNA is easily susceptible to enzymatic degradation and its large size and highly negatively charged surface are barriers towards successful transfection (1). Therefore, DNA has to be protected from degradation, neutralised and condensed into appropriate size for effective gene delivery. Currently, non-viral vectors are the preferred carrier systems as they are safer, and easier to manufacture. In this research, the use of β and γ-cyclodextrin as non-viral vectors with the incorporation of two different excipients (Pluronic-F127 and folic acid) at different concentrations to stabilise the formulation was investigated. These formulations were characterised in fresh and freeze dried forms. The freeze dried and fresh solutions of DNA were prepared with cyclodextrins (β or γ), folic acid and Pluronic-F127 as excipients in different ratios [(3:3:1, 10:10:1 and 20:10:1) excipient : cyclodextrin : DNA]. The DNA stability in the formulations was tested by determining the stability of DNA against enzymatic degradation (DNase test) using ultraviolet-visible spectroscopy. The degree of DNA inclusion into cyclodextrins was investigated using fluorescence spectroscopy. Fourier Transform Infrared Spectroscopy (FTIR) was employed to study the interaction between DNA and excipients. Scanning Electron Microscope (SEM) was used in observing the surface morphology and uniformity of formed freeze dried particles and thermal behaviour was studied using Differential Scanning Calorimetry (DSC).The formulations were also stored in high humidity (RH=76%) over 5 weeks to access storage stability. In addition, charge measurement was conducted to figure out the transfection efficiency in vivo. It was observed that incorporation of Pluronic-F127 produced the most stable formulations regarding enzymatic degradation, particularly in the freeze dried formulations. These formulations also show high percentage inclusion (>40%). Shift of peaks in FTIR data, appearance of uniform particulate as detected by SEM and changing in the denaturation temperature as demonstrated by DSC data for Pluronic-F127 containing formulations confirms clear interaction between Pluronic-F127 and the cyclodextrin/DNA complex which exhibits positive overall charge. DNA/cyclodextrin formulations containing Pluronic-F127 also showed high stability and protection for the DNA after storage at 76%RH. Overall, it was noted γ-cyclodextrin provide better protection and inclusion compared to β-cyclodextrin. In summary, Pluronic-F127 with β or γ -cyclodextrins is a promising combination to improve stability and delivery of DNA. References 1. Anchordoquy JT, Allison SD, Lorinda M, Girouard G 2001. Physical stabilization of DNA-based therapeutics. Drug Discovery Today. 6:463-470|
Development strategies for herbal products reducing the influence of natural variance in dry mass on tableting properties and tablet characteristics
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Submitted: 08 Mar 2012
Abstract: Show Abstract
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|One "Quality by Design" approach is the focus on the variability of the properties of the active substance. This is crucially important for active substances that are obtained from natural recourses such as herbal plant material and extracts. In this paper we present various strategies for the development of herbal products taking into account especially the natural batch to batch variability (mainly of the dry mass) for tablets that contain a fixed amount of tincture. The following steps of the development have been evaluated for the out come of the physico-chemical properties of the resulting tablets and intermediates: Concentration of the tincture extracted from Echinacea fresh plant, loading of the concentrate onto an inert carrier, the respective wet granulation and drying step, including milling, and the adjuvant excipients for tablet compression step. The responses that were investigated are the mean particle size of the dried and milled granulates, compaction properties and disintegration time of the tablets. Increased particle size has been shown to significant increase of the disintegration time and decrease of the compaction properties. In addition, our results exhibited that the particle size has a great dependency on the ratio of liquid to carrier during the wet granulation process. Thus, the performed strategy of the extracted tincture in correlation to its dry mass and its relation to the amount of carrier used influenced the variability on the respective parameters tested. In order to optimize those parameters, a good strategy has to be carefully chosen.|
List of Authors (67)
Proceedings & Editors
Dr. Clare Strachan
School of Pharmacy
(please direct your e-mails about ECPS 2012
Ms. Kathy Lai
Tel.: +86 10 6280 0830
Ms May Mah
University of Otago, New Zealand
Prof. Dr. Arvind Bansal
National Institute of Pharmaceutical Education and Research (NIPER), India
Prof. Dr. Anne Juppo
University of Helsinki, Finland
Prof. Dr. Peter Kleinebudde
Prof. Dr. Ken Morris
University of Hawaii at Hilo, USA
Prof. Dr. João Pinto
University of Lisbon, Portugal
Prof. Dr. Thomas Rades
University of Otago, New Zealand
Prof. Dr. Jukka Rantanen
University of Copenhagen, Denmark
Prof. Dr, Jean Paul Remon
Ghent University, Belgium
Dr. Axel Zeitler
University of Cambridge, UK
A. Advances in the solid state field
Dr Kirsten Graeser, Hoffman La Roche, Basel, Switzerland
The solid state of drugs remains an area of intensive research and work in this area is largely aimed at improving the process-ability, bioavailability and stability of drugs. The session will highlight recent developments in the solid state field of pharmaceutics such as solid dispersions, co-crystals, amorphous and co-amorphous systems. We also welcome contributions on advances in solid state analytical techniques that help to probe the solid state further.
Dr. Kirsten Graeser
B. Nanotechnology for drug delivery
Dr Leena Peltonen, Division of Pharmaceutical Technology, University of Helsinki, Finland
Modern drug discovery tools are pushing numerous difficult-to-deliver molecules into the development pipeline. Nanoscience based interventions can help in overcoming challenges of drug absorption and targeting. Nanotechnology in the strictest sense refers to structures roughly in 1 - 100 nm size range, however structures up to several hundred nanometer are also included. This session shall focus on cutting edge developments in the field of nano-carriers, nano-particles, nano-crystals and nano-manufacturing.
Dr. Leena Peltonen
C. Design and processing of protein and peptide formulation
Assoc. Prof. Lene Jørgensen, Department of Pharmaceutics and Analytical Chemistry, University of Copenhagen, Denmark
This session will explore recent trends in the development of drug delivery systems suitable for successful delivery of peptide and protein drugs. We welcome contributions that address the key elements in the successful development of a protein drugs such as obtaining a thorough understanding of protein structure and stability, interaction with excipients, design of delivery systems, and on the effect of processing the protein drug into a pharmaceutical dosage form.
Dr. Lene Jorgensen
D. Innovations in pharmaceutical manufacturing
Dr Markus Thommes, Institute of Pharmaceutical Technology and Biopharmaceutics, Heinrich-Heine University Düsseldorf, Germany
In recent years pharmaceutical manufacturing processes has re-entered the focus of pharmaceutical research. This trend is mainly driven by new requisitions of the authorities and evolution of pharmaceutical technologies. Initiatives like “Quality by Design” and “Pediatric Investigation Plan” have triggered the development of continuous processes like extrusion, process analytical technologies like in line probes and new therapeutic concepts like orodispersable minitablets. Contributions are welcome in all areas of the innovative development in pharmaceutical manufacturing processes.
Dr. Markus Thommes
E. Imaging in drug and dosage form development
Prof. Niklas Sandler, Pharmaceutical Sciences, Department of Biosciences, Åbo Akademi University, Finland
This session will explore recent trends and advances in imaging in drug and dosage form development. We welcome contributions on any imaging technique and expect examples of how imaging techniques can help the understanding of drug development, dosage form functionality, properties and quality.
Professor Niklas Sandler, Abo Akademi University
F. Physiologically Relevant in Vitro Models
Assoc. Prof. Anette Mullertz, Department of Pharmaceutics and Analytical Chemistry, University of Copenhagen, Denmark
In order to facilitate the drug development process there is an increasing need for in vitro models able to predict the fate of a dosage form in the gastrointestinal tract and in the end the bioavailability of the drug compound. This section invites contributions dealing with all forms of biorelevant in vitro models, aimed as simulating the environment of the gastro-intestinal tract and the interactions with formulations and drug compound.
Dr. Anette Mullertz, University of Copenhagen