Scientific Program

Conference Series Ltd invites all the participants across the globe to attend 16th International Conference and Exhibition on Pharmaceutical Formulations Rome, Italy.

Day 1 :

Keynote Forum

Heiko Briesen

Technical University of Munich, Germany

Keynote: A multiscale perspective on crystal growth and dissolution

Time : 10:00-10:30

Conference Series Formulations 2018 International Conference Keynote Speaker Heiko Briesen photo
Biography:

Heiko Briesen holds the Chair for Process Systems Engineering at Technical University of Munich (TUM). He studied Chemical Engineering in Karlsruhe at the currently named Karlsruhe Institute of Technology (KIT) and the University of Cincinnati. During his academic career at RWTH Aachen, the Max-Planck-Institute in Magdeburg and Technical University of Munich (TUM) he worked on several aspects of modeling, simulation and mathematical optimization for different applications spanning petrochemical, bio engineering, food and pharmaceutical processes. One of the focal applications for many years is the formulation of crystals. To achieve predictive modeling tools for crystal formulations a wide range of tools on various scales from molecular dynamics, via Monte-Carlo-simulations and population balance models, to final process flow sheeting are employed.

 

 

Abstract:

Many pharmaceutical formulations employ active pharmaceutical ingredients (APIs) in crystalline form. The growth behavior of the different facets of a crystal affects the morphology and consequently the further processing e.g. in filtration, drying or tableting steps. In the final product formulation the dissolution behavior is of paramount importance for the bioavailability of the drug. There is not only the thermodynamics in terms of the solubility which is important but also the dynamics, i.e. the dissolution rate in a certain environment. A fundamental understanding of crystal growth and dissolution leading to a predictive modeling and simulation thereof would aid product and process design alike. Although being fundamentally governed by the molecular interactions such molecular scale of investigation alone does not provide feasible concepts for process stimulation at an actual batch crystallization scale. For the predictive simulation of crystal growth or dissolution a multiscale simulation approach is needed, in which molecularlevel behavior is used to parametrize methods capable of simulating up to the microscale and beyond, where the theoretical results would be industrially relevant and easily comparable to experimental results. By spanning the range from Molecular Dynamics (MD) simulation via Monte-Carlo (MC) simulations and continuum based transport models towards Population Balance Models (PBM) such multiscale strategy is presented. For exemplary test cases this strategy has already proven to be successful. Key elements of the transition between the different scales and the experimental validation will be presented.

 

 

Conference Series Formulations 2018 International Conference Keynote Speaker Joel Richard photo
Biography:

Richard J pursued PhD in Materials Science. He is currently Senior Vice President, Peptides Development in IPSEN (France). He is globally leading all the pharmaceutical development activities of both injectable and oral peptide and small molecule-based products, including APIs and drug products, with major franchises in Oncology, Neurology and Rare Diseases. He has more than 25 years of experience in chemistry and biopharmaceutical R&D, including several global senior positions in various biotech and pharma companies. He has published 67 peer-reviewed scientific papers, 8 book chapters and 2 review editorials in various fields (colloids and interfaces, drug delivery, supercritical fluids, protein formulations, nanoparticles, sustained-release formulations). He is the author of more than 120 international communications and 53 patent families.

 

 

Abstract:

Peptides have become very attractive drugs in the last decades, due to their selectivity, their high bioactivity and low toxicity. These drugs have been successfully developed for the treatment of major diseases like type 2 diabetes and cardiovascular disorders, various types of cancer and multiple sclerosis. Due to their poor stability in extreme pH conditions, their enzymatic degradation and poor absorption across epithelial membranes, as well as their short plasma half-life, peptides remain difficult-to-administer drugs. At the present time, they are predominantly administered via injection, using sustained-release (SR) formulations mainly based on polymer matrices slowly releasing the peptide over months. These formulations have become the most successful injectable peptide formulations on the market. However, the use of alternative routes of administration, like the oral route or the transmucosal route, is likely to increase in the future, due to the pain and invasiveness of injections, as well as disposal issues associated with used needles and relatively complicated injection protocols. Low bioavailability due to limited permeability through the membranes remains a key challenge for these alternative delivery routes. In addition, new challenges have emerged recently, related to the need for intracellular delivery of peptides to new targets in cancer treatment and to the crossing of the blood-brain barrier (BBB) for peptide delivery to the brain. Then, in this context, nanodelivery systems (e.g. nanotubes, nanoparticles or nanocapsules) can provide appropriate solutions to address present and future challenges of peptide delivery, especially as regards SR formulations and delivery systems crossing cellular membranes (either intestinal epithelium or BBB) or entering cells to target intracellular receptors. This paper will present various successful nanosystems for peptide delivery that have entered the clinic or even progressed to the market, and discuss prospective approaches mainly focused on the crossing of membranes.

 

 

Keynote Forum

Masatomo Yashima

Tokyo Institute of Technology, Japan

Keynote: Visualization of the ion-diffusion path and chemical bonding in inorganic materials

Time : 11:20-11:50

Conference Series Formulations 2018 International Conference Keynote Speaker Masatomo Yashima photo
Biography:

Masatomo Yashima obtained his PhD in Materials Science and Engineering from Tokyo Institute of Technology, Japan in 1991. He has been a Full Professor at the institute from April 2011 to present. He was also a Research Associate and an Associate Professor at the same institute. He has published over 500 papers, including over 212 original research papers (cited over 10297 times (Google Scholar, Feb. 28, 2018). He has received over 28 awards including CSJ Award for Creative Work (2018), Award of the Ceramic Society of Japan (2009), the Award of the Crystallographic Society of Japan (2008).

 

 

Abstract:

Peptides have become very attractive drugs in the last decades, due to their selectivity, their high bioactivity and low toxicity. These drugs have been successfully developed for the treatment of major diseases like type 2 diabetes and cardiovascular disorders, various types of cancer and multiple sclerosis. Due to their poor stability in extreme pH conditions, their enzymatic degradation and poor absorption across epithelial membranes, as well as their short plasma half-life, peptides remain difficult-to-administer drugs. At the present time, they are predominantly administered via injection, using sustained-release (SR) formulations mainly based on polymer matrices slowly releasing the peptide over months. These formulations have become the most successful injectable peptide formulations on the market. However, the use of alternative routes of administration, like the oral route or the transmucosal route, is likely to increase in the future, due to the pain and invasiveness of injections, as well as disposal issues associated with used needles and relatively complicated injection protocols. Low bioavailability due to limited permeability through the membranes remains a key challenge for these alternative delivery routes. In addition, new challenges have emerged recently, related to the need for intracellular delivery of peptides to new targets in cancer treatment and to the crossing of the blood-brain barrier (BBB) for peptide delivery to the brain. Then, in this context, nanodelivery systems (e.g. nanotubes, nanoparticles or nanocapsules) can provide appropriate solutions to address present and future challenges of peptide delivery, especially as regards SR formulations and delivery systems crossing cellular membranes (either intestinal epithelium or BBB) or entering cells to target intracellular receptors. This paper will present various successful nanosystems for peptide delivery that have entered the clinic or even progressed to the market, and discuss prospective approaches mainly focused on the crossing of membranes.

 

 

Keynote Forum

Richard Bone

Florida International University, USA

Keynote: Comparison of diacetate esters of macular carotenoids with lutein: Effect of supplementation on macular pigment

Time : 11:50-12:20

Conference Series Formulations 2018 International Conference Keynote Speaker Richard Bone photo
Biography:

Richard Bone completed his PhD in 1972 from the University of the West Indies, Kingston, Jamaica. He is currently a Full Professor in the Department of Physics at Florida International University in Miami, Florida, USA. He has published more than 45 papers in peer-reviewed journals and 5 book chapters. He serves on the Scientific Advisory Board of Guardion Health Sciences Inc. and as a Consultant to Beneseed Co. Ltd., Japan.

 

 

Abstract:

The carotenoids lutein, zeaxanthin and meso-zeaxanthin accumulate in the center of the human retina where they are known collectively as the macular pigment. The carotenoids are believed to protect the retina from age-related macular degeneration. Because macular pigment is obtained via the diet, nutraceutical products containing the macular carotenoids, particularly lutein, are readily available over-the-counter. We have conducted a 24 week supplementation study in which we compared changes in macular pigment in the retina for two groups of 24 subjects each. One group received 20 mg/day of lutein, the most commonly available macular carotenoid. The other group received a combination of diacetate esters of lutein, zeaxanthin and meso-zeaxanthin, equivalent to 20 mg/day of free carotenoids. Macular pigment in the retina was assessed using heterochromatic flicker photometry, which measures its optical density. The diacetate group had a significantly larger (p=0.0287) increase (0.0666±0.0481) in macular pigment optical density compared with the lutein group (0.0398±0.0430), due largely to the older subjects. Generally there were smaller increases for those subjects whose baseline optical density was high. The trend, however, was only significant (p<0.05) for subjects in the diacetate group. We also found that there were no differences, on average, in macular pigment response between male and female subjects. Neither did we observe that the use of statin drugs, which lower LDL and HDL carriers of carotenoids in the blood serum, had any measurable effect on carotenoid uptake in the retina.

 

 

  • Pharmaceutical Formulations | Solid Dosage Forms | Semi-Solid Dosage Forms | Liquid Dosage Forms Gaseous Dosage Forms | Types of Formulations | Novel Drug Delivery Systems | General Considerations in Dosage Forms | Drug Formulation Procedures
Location: Meeting Hall: Olimpica 1
Speaker

Chair

Richard Bone

Florida International University, USA

Speaker

Co-Chair

Joel Richard

IPSEN, France

Session Introduction

Vivek Puri

Chitkara University, India

Title: Importance of mental symptoms in homoeopathy prescribing

Time : 12:20-12:50

Speaker
Biography:

Vivek Puri has completed his education in Chitkara University in India.

Abstract:

Mental illness refers to a wide range of mental health conditions, disorders that affect your mood, thinking and behaviour. Many people have mental health concerns from time to time. But a mental health concern becomes a mental illness when ongoing signs and symptoms cause frequent stress and affect your ability to function. A mental illness can make you miserable and can cause problems in your daily life, such as at school or work or in relationships. In most cases, symptoms can be managed with a combination of medications and talk therapy (psychotherapy). But the most efficacious and effective medicine is homoeopathic Medicines. In homoeopathic medicine physician read the mind of the patient and find the medicine that suites best for the patient. The mental symptoms are of special importance in homoeopathic prescribing. Peculiar mental symptoms and special sensations are given primary importance in homoeopathic treatment. As we know that diseases originate in the vital molecular processes, obviously, mental and physical symptoms, whether subjective or objective, are the expressions of these molecular errors. Mind, consciousness, feeling, emotions, understandings, thought, sensations, mental symptoms etc., are the functions of a complex material system, known as brain and nervous system. Homeopathy treats the patient as a whole (in mental and physical plane together) on symptoms’ similarity. Homoeopathy always gives more importance to patient’s subjective feelings and sensations and for their betterment. The unique characteristic symptoms of mind will always be considered as peculiar and characteristic symptom of the patient or individual (individualization). This striking symptom helps in finding out the right remedy for easy cure. Homoeopathy makes an attempt to judge the situation quite differently, homeopathy try to use his intellectual image and select the remedy accordingly. The homoeopathic prescription has the ability to liberate vital energies locked up in the body, so that a healthier self is experienced with a greater sense of vitality, energy and well-being. In all the cases, the homoeopath avoids suppression because this does not cure but simply pushes problems deeper.

 

 

Speaker
Biography:

Mehran feizi dehnayebi has completed his education in University of Sistan and Baluchestan, Iran.

Abstract:

Alzheimer’s disease is the main cause of death in the old people which is caused by amyloid beta aggregation (Aβ) in the brain. Human serum albumin (HSA) is the carrier protein in the body which forms the most of the blood plasma proteins. The rational design of drugs is a crucial dispute in pharmaceutical industry. In-silico drug design and discovery studies can be performed by using molecular docking simulation. In this approach, a lead compound is proposed and developed from the discovery stage to the clinical usage. In this study, in order to choose the lead compound the interaction of two anti-Alzheimer drugs (galantamine and tacrine) with HSA is investigated by molecular docking simulation. Based on the lead, ten new compounds are designed. Afterwards, the pharmaceutical properties and toxicity of these new compounds are estimated by using OSIRIS DataWarrior software. Beside molecular docking simulation, the prediction of their pharmaceutical properties assists to discover the new potential drugs. Docking results represent galantamine compared to the tacrine gives not only more stable interaction energy (-112.18 vs -106.45 kcal/mol), but also shows higher ligand efficiency (-6.02 vs -5.22). So, galantamine is chosen as a lead molecule due to the interaction energy. Furthermore, docking results indicate that the new compounds B, G, H and J, compared to the other designed compounds, have the highest interaction energy with HSA (-130.061, -113.086, -119.584, -118.735 kcal/mol). On the other hand, OSIRIS Data Warrior results provide that the compound J lacks the effects of mutagenic, tumorigenic, sterility and irritant. Moreover, for this compound, clogP, drug likeness and drug score are equal to 0.623, 4.761 and 0.892, respectively. So, based on the aformentioned results, compound J in terms of computational results can be used as a potential drug for the treatment of Alzheimer’s disease. To ensure the medicinal effect of this compound, the biological and laboratory tests should be performed.

 

 

 

 

 

Christopher F Tirotta

Nicklaus Children’s Hospital, USA

Title: Liposomal bupivacaine: A novel, long acting local anaesthetic

Time : 14:30-15:00

Speaker
Biography:

Christopher F Tirotta received his BA from Cornell University (USA) in 1982 and his MD from New York University School of Medicine (USA) in 1986. He also received an MBA Degree from Columbia University (USA) in 1999. He completed his internship in Internal Medicine at State University of New York, Stony Brook in 1987. He completed his residency training in Anaesthesiology at the University of Miami/Jackson Memorial Hospital in 1990; he sub specialized in pediatric and cardiovascular anesthesia, including heart transplantation has been an active member of Nicklaus Children’s Hospital medical staff since 1991, practicing in the Department of Anaesthesiology; he has served as the Director of Cardiac Anesthesia since 2002. He also has a clinical appointment with the Department of Anaesthesiology at the University of Miami Leonard M Miller School of Medicine, USA.

 

 

 

Abstract:

Post-operative pain control continues to be a problem in surgical patients. A novel formulation of an ultra-long acting local anesthetic is now available in the US: Exparel or liposomal bupivacaine. Liposomal bupivacaine is made up of microscopic polyhedral particles. The liposomes encapsulate the drug, bupivacaine hydrochloride, without altering molecular structure.This provides the reliable low dose release of the bupivacaine over time, providing long-lasting, post-surgical pain relief over the course of 2-3 days. This eliminates the need for titration of a single dose or the need for external devices or pumps to prolong analgesia. Plasma bupivacaine levels may persist for 96 hours after injection. Peak plasma concentrations are lower in magnitude and occur later in time than after a similar injection with bupivacaine HCl. Plasma bupivacaine concentrations are not correlated with local efficacy. Safety profile was evaluated in 10 clinical trials in patients undergoing a variety of surgical procedures. Most common adverse events were nausea, constipation and vomiting. Exparel demonstrated a favourable cardiac profile. There was no cardiac toxicity and no QTc prolongation, even a supra-therapeutic doses. Rate of absorption is dependent on total dose administered, route of administration and vascularity of the surgical site. Efficacy has been established. Multiple trials demonstrated a significant reduction if pain intensity scores and a reduction if overall opioid consumption compared to placebo. Liposomal bupivacaine is a safe and effective novel drug to treat post-surgical pain.

 

 

Ana Maria Ghelidiu

Iuliu Hatieganu University of Medicine and Pharmacy, Romania

Title: The relative bioavailability of two pharmaceutical formulations containing triclabendazole in healthy sheep

Time : 15:00-15:30

Speaker
Biography:

Iuliu Hatieganu University of Medicine and Pharmacy, Romania

Abstract:

A study was carried out to evaluate the pharmacokinetics of triclabendazole sulfoxide, the main metabolite of triclabendazole (6-chloro-5-(2,3-dichlorophenoxy)-2-methylthio-benzimidazole) and to assess the bioequivalence of two formulations of oral suspension containing triclabendazole 50 mg/ml each in 36 healthy sheep. In order to determine the relative bioavailability of the test product with respect to the reference product the study was designed as a randomized, crossover study, with administration of a single-dose, under fasting conditions in each of the two study periods. For the determination of triclabendazole sulfoxide sheep plasma concentrations a rapid, selective high performance liquid chromatography coupled with mass spectrometry (LC-MS/MS) method was developed and validated. The measured plasma concentrations of triclabendazole sulfoxide were used for the determination of bioequivalence between the test product with regards to the reference product. Noncompartmental analysis of the pharmacokinetic data of triclabendazole sulphoxide showed similarity between first-order kinetics of the test and reference product. The relevant pharmacokinetic parameters (Cmax, AUClast, AUCtot) were determined. The mean values for Cmax were 56.0 (+/-17.1) μg/ml for test and 54.4 (+/-20.1) μg/ml for the reference product. The mean values for the AUClast were 1655.6 (+/-443.9) μg/ml x h for test and 1803.3 (+/-750.6) μg/ml x h for reference product. The mean values for the AUCtot were 1702.4 (+/-445.9) μg/ml x h for test and 1847.7 (+/-755.6) μg/ml xh for reference product, respectively. The mean bioequivalence (mean ratio “Test/Reference”) for Cmax and AUClast is 1.05119 and 0.969058 respectively. The 90% confidence intervals for the ratio of means of triclabendazole sulphoxide “Test/Reference” are 98.28-112.44% and 87.97-106.75% for Cmax and AUClast, respectively, which lies within the conventional bioequivalence range of 80-125%. The difference between means is not statistically significant for the Tmax of the test and reference products (Friedman and Kruskal Wallis test). It was thus concluded that the test product is bioequivalent to the reference product with regards to the rate and extent the pharmacokinetics of triclabendazole sulfoxide.

 

 

 

 

 

 

Speaker
Biography:

Berrin Kucukturkmen has graduated from Ankara University, Faculty of Pharmacy. She received her MSc on the subject of ocular in situ gelling systems in 2008, followed by a PhD about polymeric/solid lipid nanoparticles and their interaction with glioblastoma cells in 2014 from Ankara University, under Professor Asuman Bozkır. She is currently working as a postdoctoral research assistant at the same university.

 

Abstract:

New biomaterials applied in guided bone regeneration (GBR) are expected to be biocompatible and are needed to prevent leakage caused by the invasion of peripheral epithelium and connective tissue at the onset of bone formation. In this report, a thermosensitive in situ gelling system was preferred to prevent soft tissue migration to the defect site during bone formation and prolong the residence time of the nanoparticles in this region. It is aimed to promote osteoblast cell activity with minimized dose by providing controlled release of alendronate sodium (AS) loaded in the PLGA nanoparticles. ASloaded PLGA nanoparticles having a particle size of about 100 nm were prepared by nanoprecipitation method. AS was effectively encapsulated in PLGA nanoparticles and TEM images revealed the spherical shape of nanoparticles. Optimized AS nanoparticles were then dispersed in a thermosensitive Pluronic F127 gelling system. Thermosensitive hydrogel formulation containing nanoparticles significantly prolonged the release of AS over 24 hours. Efficacy of in-situ gel system in combination with PLGA nanoparticles for enhanced bone regeneration was investigated by implanting in 0.5x0.5 cm critical size defect in tibia and femur of New Zealand female rabbits. According to the histopathological results, fibroblast formations were found at defect area after 2 and 8 weeks of post implantation and any healing was observed in the untreated control defect. In contrast, treatment with the in-situ gelling formulation including AS loaded PLGA nanoparticles provided woven-bone formation was observed after 4 weeks of post implantation and mature-bone structures were found after 8 weeks of post implantation.