Biography:

Dong-Kwon Rhee has completed his PhD at University of Illinois at Chicago in 1988 and Postdoctoral studies from Yale University School of Medicine. He was the Director of World Class University at Sungkyunkwan University, which is ranked 47th in Pharmacy and Pharmacology World rankings 2014. He has published 154 papers in reputed journals and is serving as a President of Korean Society of Ginseng.

Abstract:

Panax ginseng C A Meyer is one of the most popular herbal medicines in Korea, and has long been used in Asian countries for stimulating immunity and inhibiting various cancers. Although the role of ginseng in regulating the development of cancer is well defined, the mechanism by which it protects brain cells from oxidative stress is not well understood. Since brain myelin sheaths contain relatively large amounts of iron and lipids and have high rates of oxidative metabolism with limited antioxidant capacity, brain is highly susceptible to oxidative damage. In this study, Korean Red Ginseng (KRG) extract was shown to inhibit oxidative stress-induced apoptosis in neuro-blastoma cells. This apoptosis inhibition was mediated by ER-β up-regulation via the PI3K/AKT signaling pathway. The up-regulation of PI3K/AKT signaling inhibited apoptotic signals by decreasing p-p53 and caspase-3 expression, but increasing BCL2 expression. Therefore, KRG protected brain cells from oxidative stress-induced cell death. Collectively, these data suggest that activation of ER-β by KRG inhibits apoptosis in oxidatively stressed

Biography:

Mehmet Bilgehan Pektas has completed his PhD at the age of 28 years from Gazi University and postdoctoral studies from Afyon Kocatepe University School of Medicine. He has published more than 7 papers in reputed journals and has been serving as an editorial board member of repute

Abstract:

Visfatin is a recently discovered hormone known to be synthesized in adipocyte, hepatocyte and granulocytes and its production or suppression is modulated with diabetes mellitus. It has many cellular functions such as cell proliferation, biosynthesis of nicotinamide mono- and dinucleotide and posesses insulin-like hypoglycemic effect. This study aims to investigate the effects of diabetes on the hepatic visfatin, Asymmetric Dimethylarginine (ADMA), Erythropoietin (EPO) levels and histo-pathological features in streptozotocin-induced diabetes. In addition, the effects of resveratrol known as strong protective molecule were explored. Recruited Wistar male rats randomly divided into four groups; (1) control/vehicle; (2) control/20 mg/kg resveratrol; (3) diabetic/vehicle; (4) diabetic/20 mg/kg resveratrol. Hepatic visfatin, ADMA, EPO and insulin levels were measured with ELISA kits. Histo-pathological examinations were carried out to reveal hepatic tissue damage and inflammation. Body weight, hepatic insulin and ADMA levels reduced significantly but hepatic glucose, visfatin and EPO levels increased in the diabetic group. Furthermore, diabetes amplified damage, nuclear atypia and density of Kuppfer cells observed in the liver. Resveratrol treatment normalized these complications in the diabetic group. Oxidative damage triggered by diabetes enhanced ADMA levels but decreased visfatin and resveratrol improved this situation. This may be due to the protective activity of resveratrol on relationship between inflammation-visfatin pathways.

Biography:

Novotny L was born on October 5, 1955 in Svitavy, Czechoslovakia. He had obtained his Bachelor’s Degree in Pharmaceutical Science from Kharkov Pharmaceutical Institute, Ukraine in 1980; Doctor of Pharmaceutical degree from Charles University in 1981; Doctor of Philosophy degree from Czechoslovak Academy of Sciences in Prague in 1984; Doctor of Science degree from Slovak Academy of Sciences, Bratislava in 1997. He is working as a Professor of Pharmaceutical Chemistry in Kuwait University, since 1998. He is the acting dean of Faculty Pharmacy, since 2003. He is the member of Kuwait Pharmaceutical Association, European Association Cancer Research, American Association Cancer Research, Slovak Pharmacol. Society, Slovak Pharmaceutical Society. He contributed more than 140 articles to reputed Science journals.

Abstract:

In search for new therapies, traditional medicines of plant origin are investigated using modern scientific techniques. One of such products is produced under the name Natural Diabetea. It is a mixture of powders of several medicinal plants. It is prescribed as a drink for diabetes and other diseases in some Asian countries. The active constituents of this mixture of medicinal plants were investigated by Gas Chromatography-Mass Spectrometry (GC-MS) for identification and quantification of active natural compounds present for possible elucidation of the therapeutic action. GC-MS analysis of the methanol extract of the tea product indicated the major biologically active constituents, i.e. caffeine, β-sitosterol, β-amyrin, lupeol, linoleic acid and vitamin E. The identification of the substances was performed based on retention times and molecular ion masses by matching the MS spectra of GC chromatographic peaks with spectra of reference compounds in the NIST library. Furthermore, GC/MS analyses of available individual herbal constituents of this tea mixture, e.g., Nuga (Ficus bengalensis) and Attikka (Ficus racemosa) extracts were also conducted for comparison. The analysis indicated the presence of lupeol and β-amyrin in Nuga extract and β-sitosterol in Attikka extract. Quantification of the major active constituents, β-sitosterol, β-amyrin and lupeol, was based on measurement of the peak areas of these components in herbal extracts of tea product in comparison to β-sitosterol, β-amyrin and lupeol reference solutions of known concentrations. Using the above formula, approximate concentrations of lupeol, β-amyrin and β-sitosterol at 10 mg, 3.0 mg and 7.0 mg per 1 gm of the tea mixture were calculated. Conclusion: The beneficial properties of Natural Diabetea are likely, at least partially, due to the presence of phytosterols, namely β-amyrin, lupeol and β-sitosterol. Several of these substances were detected, confirmed and quantified using GC/MS analysis.

Biography:

Dr. Ahmed Mohamed Kabel had the Ph.D. degree in Pharmacology in 2013 from Faculty of Medicine, Tanta University, Egypt. He is involved in teaching undergraduate and postgraduate students as well as supervised one master student and one Ph.D. student in Egypt. He has published more than 21 research articles in reputable international peer reviewed journals. His areas of research interests are pharmacy practice, oncology and pediatric pharmacology.

Abstract:

Solid Ehrlich carcinoma is a transplantable tumor model used in tumor studies. Adriamycin is a cytotoxic anthracycline antibiotic used in treatment of many types of cancer. Metformin is anti-diabetic drug and is under investigation for treatment of cancer. The aim of this work was to study the effect of each of adriamycin and metformin alone and in combination on solid Ehrlich tumor in mice. One hundred albino mice were divided into five equal groups: Control untreated group, SEC, SEC+adriamycin, SEC+metformin, SEC+adriamycin+metformin. Tumor volume, survival rate, tissue catalase, tissue reduced glutathione, tissue malondialdehyde, tissue sphingosine kinase 1 activity, tissue caspase 3 activity and tissue tumor necrosis factor alpha were determined. A part of the tumor was examined for histo-pathological and immune-histochemical study. Adriamycin or metformin alone or in combination induced significant increase in the survival rate, tissue catalase, reduced glutathione and tissue caspase 3 activity with significant decrease in tumor volume, tissue malondialdehyde, tissue sphingosine kinase 1 activity and tumor necrosis factor alpha and alleviated the histopathological changes with significant increase in p53 expression and apoptotic index compared to SEC group. The combination of adriamycin and metformin has a better effect than each of adriamycin or metformin alone against transplantable tumor model in mice.

Biography:

V Ravi Chandran is a distinguished alumnus of the University of Florida, USA where he graduated with a PhD in Pharmaceutical Sciences in 1986. Since then, as an independent scientist and business leader, he has been engaged in pharmaceutical manufacturing, research and development of new drug molecules, hitech drug manufacturing and distribution in USA, and has more than 25 patents for excess of 9000 new molecules in various countries including USA, Japan, Australia and others. With his breakthrough research in anti-platelet drugs, he demonstrated that to develop a new drug, it is not necessary to start with thousands of molecules. Instead, by combining ideas from a multidisciplinary approach, few drugs can be zeroed in on at a very early stage and carry them to final regulatory approval.

Abstract:

While guerilla marketing and guerilla warfare are well known, guerilla innovation is a new concept. Guerilla tactics used by a pharmaceutical drug discovery innovator are not only effective, but also force one to think outside the box. The techniques used to bring the drugs to market without compromising safety and efficacy is of paramount importance to a guerilla innovator. How does guerilla innovator different from a drug discovery scientist? A guerilla innovator does not spend huge amount of other people’s money to design and develop a new drug. Instead, the guerilla innovator uses bridging two apparently disjointed concepts, brings them together to postulate a mechanism of action, and then reverse engineers to the right molecule with extreme precision. This means a guerilla innovator does not synthesize thousands of chemicals and go through an expensive screening process. Instead, based upon reverse engineered process, zeros in on either two to four molecules right for the treatment of any underlying disease. Yes, one or all of the three or four molecules are the ultimate drugs, and they all should work, if the guerilla innovators thinking process is correct. Key requirement for the guerilla innovation is that the safety of a drug is critical, the precise molecules must be almost devoid of toxicity, and thus therapeutic efficacy is multifold compared to existing drugs.

Biography:

Mohamed Zakaria Gad is Professor and Head of Biochemistry Department at German University in Cairo. He graduated 1st of 500 from Pharmacy, Cairo University and completed PhD from Medical College of Pennsylvania, USA. He worked as Professor/Head of Biochemistry at Cairo, October 6 and Helwan Universities, Vice-Dean for Research and Graduate Studies at Ain Shams University, Chief Coordinator of TEMPUS Curriculum Development Project in Pharmacy (5 European and 3 Egyptian Universities). He received Fellowship from American Heart Association and National Promotional Prize in Biomedical Sciences (2002) and also received STDF grant from National Academy of Science (2011-2014). He is a Board Member of Egyptian National Committee of Biochemistry and Molecular Biology and a Reviewer to several scientific journals. He has 56 publications and 65 conference abstracts, published selected articles in “Biology of Nitric Oxide” book, Portland Press, 2000, was the Principal Author and Editor of book: A Model Pharmacy Curriculum: An Egyptian-European Experience, Higher Education Academy, UK.

Abstract:

Cardio-vascular disease (CVD) remains the leading cause of death worldwide. Coronary artery disease (CAD) represents the major CVD among several populations. Despite huge efforts and great advances in studying the genetic component of CAD, there is still a great need for exploring the genetic and environmental factors contributing in the development of this disease. Among these factors emerge modulation of Nitric Oxide (NO) homeostasis and oxidative stress as central players according to recent reports. A range of biochemical disturbances including reduced availability of NO and oxidative stress has been shown to be associated with Endothelial Dysfunction (ED). Many studies described the contribution of ED in the predisposition of CAD; in particular Myocardial Infarction (MI). Recent evidence indicates that ED may be genetically determined. This presentation points out to the key players that influence vascular NO levels and their role in the protection and/or predisposition to CAD.

Biography:

Mohamed Salah Omar has completed his PhD from Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wrocław, Poland. He is currently an Assistant Professor of Biochemistry in the College of Clinical Pharmacy, Taif University, KSA. He has three patents, one is US, one is European and the third is Polish. He has published more than 11 papers in reputed journals.

Abstract:

One of the means to improve therapeutic activity of drugs is their conjugation with biological or synthetic macromolecular carriers. The idea of the carrier is to provide selectivity to the system. Past reports described synthesis, chemical and anti-tumour assays of Methotrexate (MTX) conjugates, but high selectivity was spoiled by toxicity. We developed a new method of coupling MTX with carriers (US 8,623,998 B2): MTX was transformed into its anhydride by treatment with dicyclohexyl carbodiimide. Then, MTX anhydride was coupled to native and glycated fibrinogen in aqueous solution at room temperature. At these conditions, only one of the two carboxylic groups could be acylated, thus chemical cross-linking was avoided. The obtained conjugates were characterized by reasonable uniformity, high purity, lower hydrophobicity and lack of cross-linked fractions as compared to those obtained without control of the reactivity of dicarboxylic functionality of MTX. These effects together reduced the non-specific interactions with hydrophobic components of tissues and thus emphasized the selectivity of the carrier. Native and glycated fibrinogen-MTX conjugates were a prospective way for new anti-cancer drug development due to their high anti-tumor activity. Moreover, their anti-arthritic activity was significantly more effective in suppression of the onset of arthritis in a mouse model than was free MTX. In conclusion, a correct selection of the drug and carrier as well as the type of chemical modification is important. The conditions of modification reaction should allow retention of biological activities of both the drug and the carrier. Native and glycated fibrinogen appear to be a suitable carrier in leukemia and RA.

Biography:

Medani A B has completed her PhD from University of Khartoum and Postdoctoral studies from University of Medical Sciences & Technology. She is an Assistant Professor of Pharmacology & Toxicology, Faculty of Pharmacy, UMST. She has published more than 5 papers in reputed journals and has been serving as an Editorial Board Member of repute.

Abstract:

New Zealand rabbits were purchased, weighed and divided into 3 groups, each of three. Group 1 animals were the undosed controls. Test groups were given alum at dose rates of 1% and 20% for groups 2 and 3, respectively for acute toxicity under ideal experimental conditions. Clinical signs, post-mortem and histo-pathological changes were observed. Serum investigations included enzymatic concentrations, metabolic changes, fluctuations in electrolyte levels and hematological changes. Mortalities occurred to variable degrees irrespective of the dose level. The tested rabbits showed uncontrolled diarrhoea, uncontrolled salivation, dullness, shivering, inappetance and finally recumbency depending in severity on the dose. On atomic absorption, only the lungs kept residual alum, while the livers washed it out. Oral dosing with alum caused congestion of livers with white spots, stiff-greenish lungs and inflammed empty intestines. The un-dosed group 1 rabbits showed a normal picture. On histopathology, alum-dosed group of rabbits showed nephro-necrosis in the cortex and medulla, emphysema in the lungs and congestion and necrosis of the hepatocytes. Alum was considered toxic to New Zealand rabbits at all dose rates tried.

Biography:

Abstract:

Objectives: To assess the overall safety of high-dose intravenous immunoglobulin (IG) products used to treat patients with neuro immunological disorders in a supervised home-based setting. Methods: The incidence of adverse reactions was assessed in a retrospective chart review of 420 patients who consecutively received 4076, home-based, individual, intravenous immunoglobulin (IVIG) infusions between January 2009 and December 2009. Results: A total of 90 patients (21.4%) developed adverse reactions related to IVIG administration (2.6% per individual infusion). A total of 95.5% of adverse reactions were mild, and no serious side effects were observed. The incidence of adverse reactions was significantly lower in the subgroup of patients with neuro immunological disorders who received premedication (18.2% compared with 29.3%, P = 0.02). There was no significant statistical difference in the incidence of side effects among the different brands of IVIG used in this study. Conclusions: The combination of premedication and well defined clinical, IVIG infusion policies may reduce the incidence of high-dose IVIG adverse reactions administered in a home-based setting in patients with neuroimmunological disorders.

Biography:

Camilia Michel has completed her Ph.D. at the age of 34 years benefiting from a channel system between Cairo University and Institute of Pharmaceutical Biology, Bonn, Germany. She is working as Deputy Manager at the Quality Assurance Unit of the Faculty of Pharmacy, Cairo University and as External Evaluator at the National Authority for Quality Assurance and Accreditation for Education (NAQAAE) in Egypt, the only responsible authority for accrediting Higher Educational Institution in Egypt. She has published more than 20 papers in reputed journals and serving as an editorial board member of repute.

Abstract:

Citrus maxima (Burm.) Merr., commonly known as Shaddock or Pomelo, is an original citrus plant belonging to family Rutaceae. Essential oils of peels of four different cultivars (Giza, Jordan, Syria, and Alexandria) obtained by hydro-distillation and by Solid Phase Micro Extraction (SPME) were analyzed by Gas Chromatography coupled with Mass Spectrometer (GC/MS). Limonene was found to be the major constituent reaching a percentage of 97.4% (Giza), 93.2% (Jordan), 90.8% (Syria) and 87.2% (Alexandria). The hydro-distilled essential oils of leaves at four different seasons were similarly analyzed by GC/MS and showed that the percentage of hydrocarbons (α–pinene, Β-pinene, α–phellandrene, camphene, sabinene, myrcene, cymene, limonene, careen, terpinine) were higher than that of oxygenated compounds (1-terpinen-4-ol, terpineol, santalol, eucalyptol, linalool, fenchone, citronellol, citral, eugenol methyl ether, bergamol) with no major constituent. Anti-inflammatory, antioxidant and antimicrobial activities of oils obtained from the peel were investigated.

Biography:

Salwa Elmeligie has completed her PhD from Cairo University and Postdoctoral studies from Faculty of Pharmacy, Iowa University, USA. She is Head of Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University. She is also Reviewer for Higher Education Institutions (HEIs), conducted by the National Authority of Quality Assurance and Accreditation of Education (NAQAAE), and credited trainer in Egypt. She has published more than 36 papers in reputed journals and has been serving as an Editorial Board Member of repute in addition to attending more than 20 training courses in Quality Assurance systems.

Abstract:

Stereochemistry is a unique science concerned with the study of how molecules are affected by the way their atoms are arranged in space. It is also known as 3D chemistry. Stereochemistry has become a significant issue for both of the pharmaceutical industry and the regulatory authorities. There are different types of stereoisomers especially enantiomers. Accordingly, this workshop reviews the concepts of stereochemistry and enantiomers, emphasizes the potential biological and pharmacological differences between the 2 enantiomers of a drug, and highlights the clinical experience with single enantiomers of the selective. Most natural products, the essential products of life, are asymmetric and this established the only well marked line of demarcation between chemistry of dead matter and the chemistry of living matter. So, the importance of stereochemistry in drug action is gaining greater attention in medical practice, and a basic knowledge of the subject will be necessary for clinicians to make informed decisions regarding the use of single-enantiomer drugs. For some therapeutics, single-enantiomer formulations can provide greater selectivity for their biological targets, improved therapeutic indices, and/ or better pharmacokinetics than a mixture of enantiomers. Indeed, more stereochemically pure drug agents will become clinically available and pharmacists will be relied upon for their knowledge and expertise in this area.

Biography:

Prof. Dr. Mohamed Taky El-Din Khayyal, emeritus Professor of Pharmacology, Faculty of Pharmacy, Cairo University, Egypt, was born on 26th October 1937. He obtained his B.Pharm Degree in 1958 from Alexandria University and his PhD from London University (UK) in 1964. He is presently President of the Egyptian Society of Pharmacology and is a member of many scientific societies, including the German Pharmacological and Pharmaceutical Societies, the American Gastroenterology Association, the German Society of Neurogastroenterology, and served as Councillor to the International Union of Pharmacology (2002 – 2010).He obtained Fellowships from Alexander von Humboldt Foundation, (1978), and Fulbright Foundation (1987).He has nearly 100 scientific publications in national and international Journals. His main interests lie in the field of inflammatory and gastrointestinal disorders, herbal medicine and the effects of radiation exposure. He is fluent in both spoken and written English, German, and French apart from his native tongue, Arabic.

Abstract:

Intestinal mucositis is a common adverse effect in patients undergoing radiotherapy and constitutes a treatment-limiting condition. Since no agents are yet known that can adequately guard against its development, the search continues to find safe and effective measures that could prevent this serious side-effect of radiation without affecting its anti-tumor activity. The present study was intended to investigate whether the herbal preparation, STW 5, could offer a potentially effective agent in this respect. STW5 is a multi-target herbal preparation consisting of standardized extracts of bitter candytuft (Iberis amara), lemon balm (Melissa officinalis), chamomile (Matricaria recutita), caraway fruit (Carum carvi), peppermint leaf (Mentha piperita), Angelica root (Angelica archangelica), milk thistle (Silybum marianum), celandine herb (Chelidonium majus), and liquorice root (Glycyrrhiza glabra). The preparation is of proven clinical efficacy in functional dyspepsia and irritable bowel syndrome. Intestinal mucositis was induced in rats by exposing them to different exposure levels of whole body gamma-irradiation. According to these results, a level of 6 Gy was used in later experiments. Rats were treated orally with STW 5 (5 or 10 ml/kg) for five days before and two days after irradiation. One day later, rats were sacrificed and segments of small intestine were examined histologically to assess mucosal integrity. Intestinal homogenates and serum samples were used to assess relevant parameters for mucosal functional activity, such as the brush border enzymes sucrase and alkaline phosphatase, citrulline and cholecystokinin, as well as different markers for inflammation, oxidative stress and apoptotic changes. Exposure to radiation produced dose-dependent extents of intestinal injury associated with changes in functional activity and apoptotic parameters with high radiation levels. Apoptosis was associated with an increase in cytosolic calcium, depletion of mitochondrial cytochrome c, B-cell lymphoma-2 and complex I. Oxidative stress parameters (reduced glutathione, thiobarbituric acid reactive substance and total nitrate/nitrite) were deranged. Inflammation markers (tumor necrosis factor and myeloperoxidase) and indices of intestinal damage (serum diamine oxidase) were increased. STW 5 protected to a large extent against histological changes and counteracted the deranged parameters indicative of apoptosis and of functional integrity. The findings provide strong experimental evidence for the potential therapeutic usefulness of STW5 in protecting against the development of radiation-induced intestinal mucositis and in preserving the functional activity of the small intestine in the face of radiation exposure.

Biography:

Kadriye Benkli has completed her PhD from Anadolu University. She is a Professor and works at Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University. She has published more than 40 papers in reputed journals and has been serving as an Editorial Board Member of repute.

Abstract:

The use of fosfomycin is in the treatment of multidrug-resistant bacterial infections and in the treatment of pediatric cancer patients. The continued chemotherapeutic application of cisplatin cis-diammine dichloroplatinum [II] necessitates reduction of its dose-limiting toxicity without decreasing its tumoricidal effect. Fosfomycin is considered a potential antidote for the doselimiting ototoxicity and nephrotoxicity of cisplatin chemotherapy. In this research, some metal complexes of the fosfomycin have been synthesized. The characterization of the intermediate and final compounds arising from this work was carried out by means of a variety of spectroscopic methods, which include 1H NMR, IR, MS, and elemental analysis.

Biography:

Dalia Hussein Soliman has completed her PhD from AL-Azhar University and Postdoctoral studies from the same University in addition to Ain-Shams University. She is currently working as an Associate Professor of pharmaceutical chemistry, pharmaceutical chemistry department at the Egyptian Russian University. She has published more than 12 papers in reputed journals

Abstract:

Prostate cancer is one of the most commonly diagnosed cancers in men, and the second leading cause of cancer deaths in the European Union and United States of America. The high mortality rate is mainly attributed to the invasiveness and metastasis of advanced prostate cancer. Cathepsin B is a cysteine protease found mainly in the lysosomes. The increased expression and secretion of cathepsin B have been shown to be involved in migration and invasion of numerous human and experimental tumors. Therefore, the use of cathepsin B inhibitors reduces both tumor cell motility and invasiveness in vitro. In the present study a series of novel chalcones were prepared and studied for both their anti-prostate and cathepsin B inhibition. Furthermore, a QSAR study was carried out where models were successfully built from which the physicochemical parameters were correlated to the activity.

Biography:

Suad Yousif Abdalla Alkarib has completed her PhD from University of Khartoum. She is the Founder of College of Pharmacy in Karary University. Before that, she was a Director General Manager for the Wafrapharma Laboratories Ltd. She is a Member of the Sudanese Medical Council, the Scientific Researches Committee in Gum Arabic Board (Sudan), and the Arab Administrative Development Organization (League of Arab States). She is the Rapporteur of the Industrial Pharmacy Committee in the Pan Arab Colleges of Pharmacy (October-2012). She is the Member of the proposed Fellowship in Technology of Industrial Pharmacy (Council of pharmaceutical specialties, Sudan). She has got a Certificate of Honor as a Leader in the field of pharmacy, and the first female Major-General (Jan-2011) of Sudan. She has got major awards and decorations in Competency - Duty - The National Rescue - Golden Defense. She has published more than ten papers in different journals and conferences.

Abstract:

Introduction: Gum arabic is a complex, loose aggregate of sugars and hemicelluloses composed of arabic acid nucleus connected with calcium, magnesium, potassium and sugars arabinose, galactose, and rhamnose. In this study, the use of gum arabic acacia in the manufacturing of tablet coating material, using water and plasticizer to add elasticity and flexibility is detailed. Methodology: The study was performed using a solution of gum arabic acacia in a concentration (10%), using a pilot small coating machine with an inlet temperature 400C, and spraying rate 10ml every 5 minutes on the top of placebo tablet bed while continuous drying. The ratio of gum: water and plasticizer plays good roles in final coat characteristic. Physical tests were done for the tablets before and after the process. Results: The final placebo products after coating, should be inspected and tested for appearance and performance inspection should include checks for color, size, appearance, and any physical deficits in the coating, which could affect the performance or/and stability of the product. Conclusion: However, the effect of such variables water: plasticizer ratio gives different profiles with different physical characteristics. This study concludes optimized and stable coating formula from gum arabic. The use of colors and anti-transparency additives is highly required for both film and enteric coat, for technological identification, and according to customers reeds.

Biography:

Kal Ramnarayan, Ph.D. is Founder, President and Chief Scientific Officer of Sapient Discovery and co-founder of Focus Synthesis, LLC. He was formerly the co-founder, Vice President and Chief Scientific Officer of Cengent Therapeutics, Inc. Dr. Ramnarayan (Dr. Ram) was also the co-founder and Chief Scientific Officer of Structural Bioinformatics, Inc. He was part of the management team that raised over US$50M from venture capitalists. In addition he has lead several projects with big-pharma and biotech companies resulting in over $US50M in revenues to the company making his division very profitable. He was the former Head of Computational Chemistry at ImmunoPharmaceutics Inc., where he contributed to the design of a highly active endothelin receptor antagonists (which has resulted in one approved drug in EU, Thelin and one in Phase III clinical trials, Sitaxsenten), TNF antagonists, and FGF antagonists. Previously, Dr. Ram was a Senior NIH Research Associate at the Scripps Research Institute, La Jolla. He has authored numerous scientific papers on computational protein and peptide structure determination and protein structure-based drug design. He is also a co-inventor on U.S. Patent No. 5,571,821 and 6,541,498 covering small molecule endothelin receptor antagonists which entered the clinic in Oct. 1996 and U.S. Patent No. 6, 436, 933 covering the discovery of inhibitors of anthrax lethal factor activity. He has several patent applications pending. He is on the Advisory Board of IBM’s BlueGene program, Keck Graduate Institute and Strand Genomics. He is on the editorial board of Current Proteomics. Dr. Ram holds a Ph.D. degree in Molecular Biophysics from the Indian Institute of Science, Bangalore, India.

Abstract:

Drug discovery has evolved from serendipity to rational design to high throughput screening to focused screening. Success and failures in each of these approaches could be extracted from literature as well as from the number of drugs in the “pipeline” of Pharma companies. It is hard to pinpoint any single reason as the root cause of failure of compounds at the safety studies stage or at clinical studies stage. Each of these methods have their merits and in this era of tight research budgets as well as the lack of venture/angel funding for “Discovery” projects one has to adapt the best practices to enhance success and prove druggability very early on. At Sapient Discovery we use computer derived methods to design molecules that have lower attrition rate by adapting “Target class” approach in combination with focused screening and enhanced drug-like filtering of “hits” prior to actual biological assays. Our technology “Genes to Leads” has been applied to over 30 targets and has resulted in compounds making to clinic and preclinical stage. We will outline our methodology and show our successes.

Biography:

Abstract:

The Androgen Receptor (AR) is one of the most validated therapeutic targets in Prostate Cancer (PCa). Conventional anti-androgens lose effectiveness as cancer therapeutics because anti-androgen resistance usually develops after long term treatment. The challenge is that the current therapeutics should bind to the same site of the AR (hormone binding pocket) and act via the same mode, to which the receptor has already developed effective resistance mechanisms. Hence, there is a pressing need for novel therapeutics that inhibit the AR through novel, alternative modes of action. Recent studies have identified a novel binding pocket on the surface of AR called Binding Function 3 (BF3) that is important for the AR transcriptional activity. In order to identify compounds that specifically bind to BF3 site and inhibit the AR, we conducted a systematic in silico screen (that included large-scale docking, in-site rescoring, and consensus voting procedures) followed by experimental validation of the identified hit molecules. As a result, we have discovered a novel chemical series of indoles as lead BF3 inhibitors. One of the most potent inhibitors identified, VPC-13566, demonstrated an IC50 of 0.20 uM in AR eGFP transcriptional assay. Confirming it as a true BF3 binder, VPC-13566 neither displaced the co-activator from an alternative co-activator binding site, activation function 2 site, nor androgen from the hormone binding pocket. Additionally, the Biolayer Interferometry assay detected direct reversible interactions between the AR ligand binding domain and the inhibitor. VPC-13163 demonstrated strong anti-proliferative activity against LNCaP and Enzalutamide-resistant prostate cancer cell lines (MR49F) whereas it did not affect the growth of AR independent PC3 cell line. It also inhibits Prostate Specific Antigen (PSA) in both LNCaP and MR49F and reduces expression of AR target genes, PSA and TMPRSS2. These findings suggest that VPC-13566 exhibits AR BF3 specific mechanism of action. Furthermore, VPC-13566 reduces AR-dependent growth of xenograft tumors in vivo. Based on these outcomes, it can be anticipated that such drug prototypes will lay a foundation for the development of alternative or supplementary small-molecule therapies capable of combating PCa even in its drug resistant forms. Because the emergence of castration resistance is the lethal end stage of the disease, we anticipate that the proposed research will eventually have a substantial impact on patient survival.

Biography:

Hesham Haffez has completed his Master’s degree in 2011 from Pharmacy College, Helwan University, Cairo, Egypt. Now, he is pursuing his PhD degree in Medicinal Chemistry from Durham University, United Kingdom.

Abstract:

All-Trans Retinoic Acid (ATRA) is widely used to direct differentiation of cultured stem cells and pluripotent Embryonal Carcinoma (ECs) stem cell lines into neuronal cells. EC23 and EC19 are synthetic analogues of Retinoic Acid (RA) differing from each other with respect to the position of the carboxylic acid group. EC23 has been shown to be a more potent inducer of neuronal differentiation than either EC19 or ATRA. In order to investigate the molecular basis of the functional difference, binding assays to RA Receptors (RAR α, β and γ, respectively) and molecular modeling studies were performed. EC50 values for EC23 are generally lower than for EC19 or ATRA on RAR-α and-β, indicating a higher binding affinity and co-activator recruitment. In silico molecular docking studies confirmed these differences in binding interactions, and showed that the carboxylic acid group of EC23 in the para-substitution creates the best fit to the ligand binding site with minimal steric hindrance, favoring the downstream binding of transcriptional co-activators. For EC19, the meta-substitution of the carboxylic acid group points away from a favorable interaction with Arg278 (RAR-γ) or create steric clashes with RAR-α/-β, resulting in interference with downstream co-activator binding activity. In comparison, ATRA shows similar protein-ligand interactions to EC23, supporting the notion that ATRA and EC23 possess similar molecular activation mechanisms. This study was able to combine chemical structures, receptor binding assay and molecular docking tools to shed light on the reported biological activity of these synthetic retinoids.

Biography:

Rashid Mahmood has 13 years diversified work endurance of Laboratory Management, Quality Assurance, Registration Affairs, NDA, ANDA, BLA, GMP Requirements, Drugs Laws, Statistical Methodology, Method Validation, Process & Cleaning Validation, Equipment Validation, etc. He has done Certificate Courses on cGMP, cGLP, Process Validation, ISO/IEC 17025:2005, 14001:2004, OHSAS 18001:2007, SA 8000 and 9001:2008. With strong scientific, analytical, statistical, planning, managerial and training skills, he has written several articles and attended many international conferences as a Speaker and presented various speeches in USA & China on Cleaning Validation, cGMP Guidelines, Quality Risk Management, etc. Currently, he is working as a Senior Manager Quality Assurance & Quality Management Representative for Surge Labs. (Manufacturer of Microencapsulated APIs, Liquid & Dry Powder Parentrals) which is the best export oriented company in Pakistan and we are the only manufacturer of microencapsulated APIs in Pakistan using European Technology and it has taken over lot of Business of Ranbaxy & Ind. Swift India worldwide. We are participating as Exhibiter in all the CPhIs taking place worldwide round the year. Stancos Private Limited (Cosmetic Plant), it is the only cosmetic plant in Pakistan which is ISO 22716:2007 GMP & ISO 9001:2008 QMS Certified by BVC and we are also exporting our cosmetic products to European countries. We are the Contract Manufacturer of L'oreal Paris Products and Sanofi famous brand (Selsun Blue Shampoo) in Pakistan.

Abstract:

Cleaning Validation can be defined as “The process of providing documented evidence that the cleaning methods employed within a facility consistently controls potential carry-over of product (including intermediates and impurities), cleaning agents and extraneous material into subsequent product to a level which is below predetermined levels”. The cleaning validation program shall primarily address the cross contamination of active ingredients of previous product into next product by means of sharing common equipment contact surfaces. In accordance with this, all equipments that have product contact surfaces shall be brought into the purview of cleaning validation. Special emphasis shall be given to cleaning procedure requirements as part of design requirement. Cleaning is one of the critical processes in pharmaceutical manufacturing. It is critical to avoid carryover of trace amounts of either active or other materials from one batch to another in order to avoid cross-contamination of the subsequent product. For that reason, equipment used in pharmaceutical manufacturing must be cleaned meticulously, and the cleaning procedure used must be validated. In the pharmaceutical industry, Good Manufacturing Practices (GMP) requires that the cleaning of drug manufacturing equipment be validated. Many different validation techniques can demonstrate that the manufacturing equipment is cleaned and essentially free from residual active drug substances and all cleaning agents. Common analytical techniques in the validation process include HPLC, Spectrophotometry (UV/Vis) and TOC. Cleaning validation must be performed using a pre-approved protocol. Selection of appropriate sampling to demonstrate that residues are removed to an acceptable level is vital for the success of cleaning validation. In addition, use of sampling techniques such as recovery study for swab and rinse and thorough visual inspection can reduce the number of samples required for cleaning validation. This article provides background on cleaning validation and the associated regulations, cleaning methods, validation strategy, and new product introduction. It also covers validation samples, acceptance criteria, clean hold time, training, change control, and revalidation. The intention of this article will be to define a comprehensive approach to the validation of cleaning procedures in pharmaceutical manufacturing facilities. It defines the basic concepts and terms associated with cleaning validation in the pharmaceutical industry. It also serves as a guide from which master plans, protocols and reports may be compiled