Day 2 :
Keynote Forum
Arik Dahan
Ben-Gurion University of the Negev, Israel
Keynote: Developing better formulations for oral lipophilic drugs by accounting for both the solubility and the intestinal permeability
Biography:
Arik Dahan is an Associate Professor of Pharmaceutics and Biopharmaceutics at the Department of Clinical Pharmacology and the School of Pharmacy, Ben-Gurion University of the Negev in Beer-Sheva, Israel. He is also an Adjunct Professor of Pharmaceutical Sciences at the College of Pharmacy, University of Michigan, USA. He received his PhD (2007) from the Hebrew University of Jerusalem. From 2007 until 2009, he was a Post-Doctoral Research Fellow at the University of Michigan College of Pharmacy with Professor Gordon Amidon. Hiss research interest is the integration of up-to-date molecular and cellular mechanistic investigations of drug disposition in the context of the human body, in order to enable successful drug delivery and therapy. In implementing this molecular biopharmaceutical approach to ADME research, he is seeking to enable mechanistic-based successful solutions to drug delivery, especially (but not only) oral, in challenging scenarios e.g. low-solubility, low-permeability, efflux transport, extensive metabolism, poor site targeting, various pathophysiological conditions (e.g. obesity, inflammatory bowel disease), and pediatrics patient care. He has authored over 70 top-notch journal papers, and contributed chapters to 7 books.
Abstract:
Poor aqueous solubility is a major challenge in today's biopharmaceutics. While solubility-enabling formulations can significantly increase the apparent solubility of the drug, the concomitant effect on the drug's apparent permeability has been largely overlooked. The mathematical equation to describe the membrane permeability of a drug comprises the membrane/aqueous partition coefficient, which in turn is dependent on the drug's apparent solubility in the GI milieu, suggesting that the solubility and the permeability are closely related, exhibit a certain interplay between them, and treating the one irrespectively of the other may be insufficient. In this lecture, an overview of this solubility-permeability interplay will be provided, and the available data will be analyzed in the context of the effort to maximize the overall drug exposure. Overall, depending on the type of solubility-permeability interplay, the permeability may decrease, remain unchanged, and even increase, in a way that may critically affect the formulation capability to improve the overall absorption. Therefore, an intelligent design of solubility-enabling formulation needs to consider both the solubility afforded by the formulation and the permeability in the new luminal environment resulting from the formulation.
Keynote Forum
Arik Dahan
Ben-Gurion University of the Negev, Israel
Keynote: Developing better formulations for oral lipophilic drugs by accounting for both the solubility and the intestinal permeability
Time : r564564
Biography:
Arik Dahan is an Associate Professor of Pharmaceutics and Biopharmaceutics at the Department of Clinical Pharmacology and the School of Pharmacy, Ben-Gurion University of the Negev in Beer-Sheva, Israel. He is also an Adjunct Professor of Pharmaceutical Sciences at the College of Pharmacy, University of Michigan, USA. He received his PhD (2007) from the Hebrew University of Jerusalem. From 2007 until 2009, he was a Post-Doctoral Research Fellow at the University of Michigan College of Pharmacy with Professor Gordon Amidon. Hiss research interest is the integration of up-to-date molecular and cellular mechanistic investigations of drug disposition in the context of the human body, in order to enable successful drug delivery and therapy. In implementing this molecular biopharmaceutical approach to ADME research, he is seeking to enable mechanistic-based successful solutions to drug delivery, especially (but not only) oral, in challenging scenarios e.g. low-solubility, low-permeability, efflux transport, extensive metabolism, poor site targeting, various pathophysiological conditions (e.g. obesity, inflammatory bowel disease), and pediatrics patient care. He has authored over 70 top-notch journal papers, and contributed chapters to 7 books.
Abstract:
Poor aqueous solubility is a major challenge in today's biopharmaceutics. While solubility-enabling formulations can significantly increase the apparent solubility of the drug, the concomitant effect on the drug's apparent permeability has been largely overlooked. The mathematical equation to describe the membrane permeability of a drug comprises the membrane/aqueous partition coefficient, which in turn is dependent on the drug's apparent solubility in the GI milieu, suggesting that the solubility and the permeability are closely related, exhibit a certain interplay between them, and treating the one irrespectively of the other may be insufficient. In this lecture, an overview of this solubility-permeability interplay will be provided, and the available data will be analyzed in the context of the effort to maximize the overall drug exposure. Overall, depending on the type of solubility-permeability interplay, the permeability may decrease, remain unchanged, and even increase, in a way that may critically affect the formulation capability to improve the overall absorption. Therefore, an intelligent design of solubility-enabling formulation needs to consider both the solubility afforded by the formulation and the permeability in the new luminal environment resulting from the formulation.
- Types of Pharmaceutical Formulations | Hospital Pharmacy | Pharmacognosy and Phytochemistry
Location: LEON
Co-Chair
Arik Dahan
Ben-Gurion University of the Negev, Israel
Session Introduction
Irina Ermolina
De Montfort University, UK
Title: Characterization of mechanical properties of freeze-dried cake in vial: Application for Pharmaceutical formulation development
Biography:
Irina Ermolina obtained her PhD degree in molecular physics and after 15 years of work in biophysics she expanded her interests into the pharmaceutical science. After post-doc positions at University of Jerusalem and University of Glasgow she got a senior lectureship at De Montfort University, UK. Irina Ermolina has her expertise in Pharmaceutical and Biological Materials Science (especially. amorphous materials); Drug Delivery Systems (hydrogels); Process Analytical Technologies for Pharmaceutical Manufacture (esp. Freeze-Drying and Roller Compaction); and different analytical techniques (Dielectric Relaxation Spectroscopy, Terahertz Imaging and Terahertz Spectroscopy, Thermoanalytical methods). She has published 48 articles and book chapters.
Abstract:
Freeze-drying (FD), or lyophilisation, is a standard commonly used method for the production of long-term stable solid products. The most frequently used containers for freeze-drying are glass vials and blister packs. The aim of this study was to develop and optimize a Texture Analysis (TA) technique to study the compressive mechanical properties of FD cakes directly in glass vials using a standard commercially available texture analyser. Examining the cakes in glass vials has many advantages as it allows studying the intact FD cakes minimizing the bias from texture distortion during samples preparation, and reducing the moisture uptake. The mechanical properties of the FD cakes can provide valuable information on the strength and susceptibility to breakage of the FD cakes, in particular, when developing the formulation for the orally disintegrating tablets. Besides, analysis of the mechanical properties and the texture of the FD cakes can help improve the freeze-drying protocols as the properties of FD cakes (in particular, the pore size and the wall thickness of FD solids) depend on the FD cycle parameters. The application of a standard texture analysis (TA) technique to study the mechanical properties of the freeze-dried cakes directly in glass vials used for freeze-drying has been demonstrated. A procedure allowing quantitative assessment of the strength, fracturability, and elastic properties of the FD cakes using TA has been developed. The results show that the TA method is sensitive to the variations in cake materials, storage conditions (temperature, excessive moisture), and cake quality. The results also show that TA can also be applied for optimization and improvement of the freeze-drying protocols and rapid disintegrating tablet formulation development.
Jitka RychlÃÄková
Hospital Na Bulovce, The Czech Republic
Title: Clinical pharmacy service at orthopedic department in the Czech Republic
Biography:
Jitka RychlíÄková works as a Clinical Pharmacist at Hospital Na Bulovce, Prague, she has been assigned to Orthopedic Department for four years. She is a PhD candidate in the field of Safety and Quality of Drugs where she deals with economic evaluation of clinical pharmacy services. As a member of the board of the Czech Society of Clinical Pharmacy, she contributes to clinical pharmacy developing in the Czech Republic. She is interested in teaching and is a Lecturer in Continuous Pharmacy and Clinical Pharmacy Education, as well as she teaches Pharmacology to Under-graduate Medical students.
Abstract:
Statement of the Problem: In the Czech Republic the clinical pharmacy is a young and rapidly growing field. One of the Czech clinical pharmacy authorities predefined some general procedures how to provide clinical pharmacy; three levels of clinical pharmacy services were predefined. Previously published data to the topic of clinical pharmacy services in orthopedics and traumatology departments are very scarce. The aim is to present results of clinical pharmacy service at orthopedic/traumatology department as an example of application of predefined procedures.
Methodology & Theoretical Orientation: We have been collecting data during four years of continuous cooperation. At the department (with 7 units) the combination of all three levels of clinical pharmacy services was applied.
Findings: Our results provide an evidence of increasing orthopedists’ adherence to newly introduced clinical pharmacy service during four years as well as provide an evidence of professional growth of clinical pharmacist herself. On the first level of clinical pharmacy services the clinical pharmacist does an intervention in 17% of admitted patients at this type of department, the most interventions are associated with antithrombotics and the recommendation to continue the unchanged therapy is becoming the most common intervention during the four-year period. On the second level of clinical pharmacy services the analgesic therapy was improved by elimination of an off-label drug, moreover hydration regimen and prevention of chemotherapy induced nausea and vomiting was optimized. On the third level some rules for prescription were established.
Conclusion & Significance: There is evidence how the general predefined procedures work, their application to the orthopedic/ traumatology department is shown and their efficacy in here is presented. There is enough space for clinical pharmacy services even in orthopedics/traumatology.
Tuba Aydin
Agri Ibrahim Cecen University, Turkey
Title: Effects of some natural compounds on the glutathione reductase enzyme
Biography:
Tuba Aydin is currently working as an Assistant Professor in the Faculty of Pharmacy at the Agri Ibrahim Cecen University, Turkey where she has been a faculty member since 2013. She completed her PhD at Ataturk University, Turkey. She has expertise in isolation and characterization of phytochemicals from natural products.
Abstract:
Discovery of Glutathione Reductase (GR) inhibitors has become very popular recently due to antimalarial and anticancer activities. In this study, GR inhibitory capacities of some natural compounds, β-sitosterol, β-stigmasterol, diosgenin and jervine, which have steroidal skeleton, were reported. While β-stigmasterol was isolated from Artemisia dracunculus, β-sitosterol, diosgenin and jervine were isolated from rhizomes of Veratrum album. The chemical structures of the compounds were confirmed by IR, 1H-NMR, 13C-NMR, 1D and 2D NMR methods. The tested molecules were exhibited much potent inhibitory activities against GR at low micromolar concentrations with IC50 values ranging from 0.1916 to 5.2116 μM as compared with well-known agents. In this study first time, the inhibition effects of β-sitosterol, β-stigmasterol, diosgenin and jervine were determined on glutathione reductase enzyme.
Fatma Tugce Guragac
Gazi University, Turkey
Title: Insights into research on the anti-inflammatory and antinociceptive activities of Scandix iberica Bieb.
Biography:
Abstract:
It is thought that bioactive compounds from plant foods may have beneficial health effects and decrease the risk of chronic inflammatory diseases. In Turkish folk medicine, flowers of the Scandix iberica Bieb. (Apiaceae) have been used to combat rheumatic pain. The aim of this study is to appraise the anti-inflammatory and antinociceptive activities of the different types of extracts prepared from S. iberica carrageenan, Prostaglandin E2 (PGE2) and serotonin-induced hind-paw oedema, acetic acid-induced capillary permeability and 12-O-tetradecanoyl-phorbol-13-acetate (TPA)-induced mouse-ear oedema models were used to appraise anti-inflammatory activity. Antinociceptive activity was tested using a p-benzoquinone induced abdominal constriction method. Among the extracts, only the n-Hexane extract was shown to possess a noticeable anti-inflammatory and antinociceptive activity in mice without inducing any gastric damage at 100 and 200 mg/kg doses, while the rest of the extracts were entirely inactive. The activity of the n-Hexane extract led to a greater appreciation of some phenylpropanoids, mainly estragole (88.90 %), through Capillary Gas chromatography-Mass Spectrometry (GC-MS).