Day 1 :
Keynote Forum
Carmen Tamayo
Heterogeneity LLC, USA
Keynote: Botanical drug development: Right and wrong on clinical studies
Time : 09:05-09:45
Biography:
Carmen Tamayo, MD directs the Canada Region of Heterogeneity, LLC. She is trained in Internal Medicine at the Central University of Venezuela. After moving to Canada with family, she completed Post-graduate studies in Public Health and Epidemiology at the University of Toronto. Since 1995, she has actively participated in policy and regulatory activities addressing traditional, complementary and alternative medicine (TCAM) research, with the Canadian National Cancer Institute. Her consulting has included government, industry, and nonprofit scientific organizations, including heterogeneity (since 2008), McMaster University Centre for Evidence Based Medicine, and the University of Western Ontario School of Medicine and Dentistry at the University of Western Ontario. For Health Canada’s Natural Health Products (NHP) Directorate, she served as Clinical Trial Project Coordinator for product review and assessment, collaborating in the agency’s development of a framework for NHP clinical trials. She has chaired and directed numerous programs and workshops as a member of the Drug Information Association (DIA), the International Pharmaceutical Federation (FIP), and the Latin American Phytomedicine Society (Sociedad Latinoamericana de Fitomedicina). She also serves as an expert reviewer for the World Health Organization and other international committees and several CAM and Phytotherapy journals, and is a past Co-editor of the Journal of Integrative and Complementary Medicine (JICM) – An international forum for evidence-based practices.
Abstract:
Medicinal plants are inexhaustible sources from which many of today’s most be useful drugs have been developed. While the majority of plant-based drugs are new (single) chemical entities (NCEs), a category of botanical drugs has recently reappeared in the US. Botanical drugs are defined as finished drugs for which the active ingredient is a complex, polymolecular drug substance. Although the criterion of adequate and well-controlled [clinical] studies remains a basis of new drug approval for the United States, botanical products pose unique challenges to clinical development due to their complex nature. This session will describe the clinical development of botanical drugs, with a focus on the US market. It will touch upon the differences between botanicals and NCEs and how these differences impact the types, designs, and even the timeline of clinical studies conducted for US drug development. Through examples, it will also relate some of the hurdles posed by complex botanical drugs which have been experienced in clinical studies of these products-both in research and in regulatory settings.
Keynote Forum
Freddie Ann Hoffman
Heterogeneity LLC, USA
Keynote: Regulatory considerations of botanicals as new drugs for the US market
Time : 09:45-10:25
Biography:
Freddie Ann Hoffman, MD founded HeteroGeneity in 2003; a Washington, DC-based consultancy focused on complex natural products, and is also its Managing Member. She has over 35 years of product development experience. She has a BS in chemistry from UCLA and received her MD and General Pediatric Residency training from the University of California at Davis. She completed a fellowship in Pediatric Hematology-Oncology at the National Cancer Institute (NCI), staying on to direct the Nutrition and Supportive Care Section of the Division of Cancer Treatment, and later, as Director of Extramural Clinical Trials of the Biological Response Modifiers Program. Leaving NCI in 1986, she served at FDA for nearly 14 years, as Chief of the Cytokines, Growth Factors and Oncologic Products Branch of the Center for Biologics Evaluation and Research, and later as Deputy Director of the Medicine Staff in the Office of the Commissioner. During her tenure, she formed and chaired an internal FDA Botanical Working Group which developed the botanical drug guidance, which the agency finalized in 2004. She also served in the Office of Dietary Supplements at the Center for Food Safety and Applied Nutrition, before moving to the private sector in 1999, joining Warner-Lambert Pfizer Consumer Healthcare, where she was Senior Medical Director for New Product Development. She continues to serve on numerous working groups, task forces, and boards of both government agencies and private companies. She has chaired and participated in numerous scientific, regulatory and policy forums addressing the development of polymolecular drugs and development of complex product. In 2014, she was an invited speaker at the 18th Presidential Commission on Bioethics (BRAIN initiative). She is a member of the American Society of Pharmacognosy and a past chair of the Drug Information Association’s Natural Health Products Track.
Abstract:
Medicinal use of plant-based products has its origins in antiquity estimated to date back at least 60,000 years. Toda approximately 80% of the world’s population continues to utilize plants and plant products to treat or prevent clinical conditions. In the United States, plant-based medicines were a major part of pharmaceutical armamentarium that is up until the passage of the US Drug amendments of 1962. The drug amendments further established requirements for new drug approval in the US, specifically requiring that the US Food and Drug Administration must affirm the safety and efficacy of a new drug prior to market approval. It was not until FDA’s dissemination of its Botanical Drug Development Guidance document, several decades later, that the US development of botanicals as drugs has experienced resurgence. At present there are two FDAapproved new botanical drugs that are sold exclusively by prescription in the US. This session will discuss how the FDA defines a botanical and the implications of the US regulatory approach on the development and approval of this renewed drug category, along with some of the lingering hurdles to this special category of new drugs.
Keynote Forum
Gus R Rosania
University of Michigan, USA
Keynote: The fine balancing act of drug formulation R&D in academia
Time : 11:00-11:40
Biography:
Gus R Rosania as Principal Investigator of the Subcellular Drug Transport Lab, is transforming the development of new drug formulations, by elucidating the micro pharmacokinetic properties of drugs in their biological, tissue microenvironments. His research group has pioneered new cheminformatic (mathematical modeling and simulation-based) approaches to the design of small molecule drugs with optimal permeability and intracellular accumulation properties, as well as application of hyperspectral Raman imaging approaches to discover new transport and disposition mechanisms acting at cellular and subcellular levels. His major contributions to pharmaceutical sciences is that his research group has discovered the most potent small molecule drug targeting mechanisms that has ever been identified to date, by studying the mechanisms of intracellular drug crystal formation. This knowledge is now being applied to the invention of new pharmaceutical formulation approaches that are poised to transform the manner in which drugs and formulations are designed, developed and regulated.
Abstract:
Statement of the Problem: In universities, pharmaceutical scientists are encouraged to dream of building marvelous creations, such as self-propelled drug delivery systems, self-assembling nanoscale devices and stimulus-responsive drug targeting mechanisms. While immense efforts are spent on accomplishing these transformative feats in chemistry, engineering and biomedicine research labs, the resulting advances are often not practical to translate into the clinical arena.
Methodology & Theoretical Orientation: In order to realign academic, drug formulation research with the more practical considerations inherent to drug product development, many challenges that precede clinical translation must be taken into account and dealt with, at the earliest, inception phase of formulation design. In this regard, my research group has grounded itself in reality, by carefully studying the nanoscale transport and distribution properties of existing drugs, prior to launching itself into a new, formulation design project.
Conclusion & Significance: By pioneering the formulation and development of biomimetic drug complexes, we have been able to balance fundamental discovery-driven research and technological innovation, with the more mundane necessities and regulatory requirements underlying successful clinical translation (from scale-up to manufacturing; and, from sterilization to commercialization).
Keynote Forum
Hai-Feng Ji
Drexel University, USA
Keynote: Diphenyl α-Aminoalkylphosphonates as prostate-specific antigen antagonists
Time : 11:40-12:20
Biography:
Hai-Feng Ji is currently working as a Professor, in Department of Chemistry, and Drexel University. His research interests focused on drug discovery, MEMS devices, nanomaterials for energy and environmental applications, nanopillars and phosphene for energy applications, and surface chemistry. He is currently a Co-author of 160 peer-viewed journal articles and book chapters. He has an H-index of 30. He is an Editorial board Member of several chemistry journals.
Abstract:
Prostate cancer (PCa) is one of the most prevalent cancers diagnosed in adult males. Chemotherapy has been widely used for PCa treatments. Although therapies targeting the androgen receptor, an upstream regulator of PSA, have been effective in treating prostate cancer, the disease state sometimes progresses and results in castrate-resistant prostate cancer. Alternative therapies should be pursued for prostate cancer treatment, especially in the scenario where androgen deprivation fails. PSA is a serine protease that has been found to control the growth of cancer metastasis and proliferation. Regulated by androgen receptor-mediated transcription pathway, the primary role of PSA biologically is the liquefaction of semen via proteolysis of coagulating proteins Fibronectin and Semenogelin within the matrix. However, with elevated PSA levels, the protease has been shown to cleave insulin-like growth factor binding protein-3 (IGFBP-3), a modulator of Mitogenic proteins insulinlike growth factors (IGF) I and II. It has been demonstrated that the involvement of PSA with the IGF molecular system leads to the progression of prostate cancer, which can in turn metastasize into the patient’s lymph nodes and bone, causing osteoblastic lesions via PSA-activation of latent transforming growth factor beta (TGFβ) and proteolysis of IGFBP-5. In this work, AutoDock 4.2 molecular docking suite was utilized to model covalent and non-covalent binding of this class of inhibitors to predict crystallographic poses and compare experimental IC50 dose-response curves and in silico potencies for providing future more specific rational drug design. The modeling study introduces novel aminoalkylphosphonates as a potential drug candidate for targeting PSA by optimizing P1 binding affinities. Several lead compounds will be reported as potent inhibitors of PSA activity.
- Drug Discovery and NCEs | Quality by Design(QbD) Approach | API: Active Pharmaceutical Ingredients | Formulations and NDDS | Analytical Strategies for Pharmaceutical Products | Pharma Market Research
Location: Philadelphia, USA
Chair
Carmen Tamayo
Heterogeneity LLC, USA
Co-Chair
Hai-Feng Ji
Drexel University, USA
Session Introduction
Maysoon A Abujarad Alhuwitat
Amman Arab University, Jordan
Title: The extent of pharmaceuticals services quality on building a superior relationship between pharmacists and their customers
Time : 13:30-14:05
Biography:
Maysoon A Abujarad Alhuwitat has completed her Bachelor's degree in Pharmacy, and a Master’s degree of MBA, major Pharmaceutical Marketing. She had worked in the private sector pharmacies (individual & chain pharmacy) as pharmacist in charge for a period of one year 2013-2014, then she opened her own pharmacy with partner.
Abstract:
Background: Pharmacy is an important profession in Jordan whereby it plays a vital role in providing the pharmaceutical services required for the health care of patients and it is an effective factor in the economy and development of the nation. Therefore, it is important to focus on the relationship between pharmacists and their customers through providing high quality pharmaceutical services.
Objectives: The current study aimed at investigating the level of pharmaceutical services quality in Jordan and its effect on building a strong relationship between pharmacists and their customers "from the pharmacist’s' perspective", through customers' perceived value, satisfaction, loyalty and CRM.
Methods: This study is a descriptive and analytical one. A self-administrated questionnaire was distributed to a convenience sample of 110 pharmacists working in public pharmacies, to measure the impact of pharmaceutical services quality on building relationship with customers.
Results: There is a statistically significant effect of pharmaceutical services quality on building a strong relationship between pharmacists and their customers at level (α=0.05) from one dimension (Responsiveness). There is a statistically significant effect of pharmaceutical services quality on customers' perceived value, satisfaction and loyalty at level (α=0.05). Also, there is no statistically significant effect of pharmaceutical services quality on CRM at level (α=0.05).
Conclusion: Pharmacies sector should focus on the quality of pharmaceutical services provided to customers as a basic standard for building a strong relationship with customers because of the direct impact of these services on customers' perceived value, satisfaction and loyalty.
Imeda Rubashvili
Tbilisi State University, Georgia
Title: Development and validation of extraction procedures and quantitative determination methods of natural colorants obtained from agro-industrial waste materials using stepwise extraction techniques and high-performance liquid chromatography
Time : 14:05-14:40
Biography:
Imeda Rubashvili is an Assistant Professor, a Scientific Researcher at Ivane Javakhishvili Tbilisi State University and the Head of Validation Department of Pharmaceutical Company “Aversi-Rational” Ltd. He has published more than 30 scientific papers and participated in more than 30 international scientific conferences. He is the Member of the Council of Young Scientists of the Georgian National Academy of Sciences.
Abstract:
The manufacture of food products and dietary supplements using natural food colorants has been attracted attention in modern food industry. Carotenoids and anthocyanins as natural colorants show strong antioxidant and immunomodulation activities and may prevent degenerative diseases as well. The present research concerns the development of stepwise extraction procedures and HPLC analysis of carotenoids and anthocyanins containing agro-industrial waste materials (tangerine, orange peel and grape skin). Extractions were carried out in a dynamic supercritical fluid-carbon dioxide (SC-CO2) and ultrasound assisted extraction systems. The effects of operating pressure and temperature, extraction time, pH, flow rate of the SC-CO2, sample size and solvent nature used were investigated. The optimal conditions for extraction were found. The drying process of samples obtained from agro-industrial waste materials was studied as well. The main carotenoids-beta-carotene, lycopene and total anthocyanins obtained in organic extracts were quantified using new, rapid, effective and selective developed and validated HPLC methods. The HPLC methods were validated with respect to system suitability test, specificity, linearityrange, accuracy, precision, limit of detection (LOD) and quantitation (LOQ). The stability of solutions was studied as well. The calibration curves of developed HPLC methods are linear over a concentration range 0.08-6.50 μg/mL for beta-carotene (r2=0.9992), 0.34-200.20 μg/mL for lycopene (r2=0.9999); 0.04-80.50 μg/mL and 0.12-80.50 μg/mL for total anthocyanins expressed as cyanidine chloride (r2=0.9999) and kuromanine chloride (r2=0.9999); The average recovery equals to 106.8% for beta-carotene, 101.4% for lycopene, 95.62% for cyanidine chloride and 94.9% for kuromanine chloride.
Maysoon A Abujarad Alhuwitat
Amman Arab University, Jordan
Title: The extent of Jordanian pharmacists satisfaction on their labor right
Time : 14:40-15:15
Biography:
Maysoon A Abujarad Alhuwitat has completed her Bachelor's degree in Pharmacy, and a Master’s degree of MBA, major Pharmaceutical Marketing. She had worked in the private sector pharmacies (individual & chain pharmacy) as pharmacist in charge for a period of one year 2013-2014, then she opened her own pharmacy with partner.
Abstract:
Background: Pharmacists’ jobs in Jordan are important and contribute to the welfare of patients and citizens. Through interviews of a number of pharmacists it was felt that there is need to study their feelings about their rights and satisfaction.
Objectives: The aim of this study is to measure the perceptions of Jordanian pharmacists on attaining their rights, and the impact of these rights on their satisfaction.
Methods: The study is an observational one. A random sample of 49 pharmacists was chosen to fill a self- administered questionnaire covering the dimensions of pharmacists and their satisfaction. The study tested the following hypothesis: there is no significant impact (at level α=0.05) of Pharmacists’ rights on their satisfaction.
Results: The null hypothesis was rejected indicating a significant impact of pharmacists’ rights on their satisfaction. The results also showed that pharmacists were not highly satisfied, whereby they reported satisfaction mean of 2.8 out of 5. Pharmacists’ perception on salary was also low, (mean=2.71). Means and standard deviations of all questionnaire items are reported.
Conclusion: Based on the results of this research, there should be effort from the employers and the Jordan Pharmacists’ Association to develop higher understanding and regard toward Pharmacists’ rights, especially salary and working conditions which showed effect on satisfaction.
Rayhana Begum
Primeasia University, Bangladesh
Title: Coumaroyl Lupendioic acid attenuates oxidative stress in adjuvant induced arthritis
Time : 15:50:16:25
Biography:
Dr. Rayhana is a recognized expert in Extraction techniques (Column Chromatography, Flash Chromatography) use of ELISA, Immunohistochemistry, the measurement of pro-inflammatory cytokines, acute phase protiens and oxidative biomarkers for the determination of anti inflammatory and anti-arthritic activities of drugs and quantitative determination of drugs by spectrophotometer, HPTLC and HPLC. Study of Bioavailability and bioequivalence profile of drugs. After obtaining B.Pharm. Degree and M. Pharm Degree in Clinical Pharmacy and Pharmacology from the University of Dhaka in 2005 and 2006, respectively, she has been awarded the Ph.D Degree in Pharmacology by Hamdard University, NewDelhi, India in 2016.
Abstract:
The present study was intended to elucidate the effect of coumaroyl lupendioic acid, a new lupane-type triterpene isolated from Careya arborea (Lecythidaceae) stem bark, on the biomarkers of oxidative stress in Complete Freund's Adjuvant (CFA)- induced arthritic rats. Arthritis was induced by injecting 0.1 ml of CFA (5 mg/ml of heat killed Mycobacterium tuberculosis) into the sub plantar region of the left hind paw. Treatment with coumaroyl lupendioic acid (10 and 20 mg/kg, p.o.) and reference drugs (indomethacin and dexamethasone at the dose of 5 mg/kg, p.o.) were started on the day of induction and continued up to 28 days. The effect of coumaroyl lupendioic acid on oxidative indicators (e.g. nitric oxide, myeloperoxidase, malondialdehyde) and antioxidant enzymes (e.g. superoxide dismutase and glutathione peroxidase) was measured at the end of the study. Furthermore, ankle joints and spleen were collected and prepared for histological examination. The present study showed that the oxidative indicators such as nitric oxide, myeloperoxidase, malondialdehyde were downregulated by coumaroyl lupendioic acid. A significant upsurge in the level of superoxide dismutase and glutathione peroxidase was observed. Moreover, histopathological examination showed that the inflammatory cells infiltration, synovial hyperplasia and cartilage erosion had considerably improved on administration of coumaroyl lupendioic acid. In conclusion, our study strongly demonstrated that coumaroyl lupendioic acid has efficient scavenger and protective effect against oxidative stress elevated after CFA injection.
- Pharmaceutical Packaging and Logistics | Regulatory Authority Compliance | Clinical Trials and Pharmacovigilance | Pharmacoeconomics | Pharmaceutical Manufacturing, Scale Up and Tech Transfer | QC & QA: Quality Control and Quality Assurance
Location: Philadelphia, USA
Chair
Freddie Ann Hoffman
Heterogeneity LLC, USA
Co-Chair
Michael Chorny
University of Pennsylvania, USA
Session Introduction
Hongbin Wang
California Northstate University, USA
Title: Complement peptide C4a mitigates LPS-induced endothelium disruption, cytokine production, ERK activation, and [Ca2+] influx from human moncytes- A new therapeutic intervention for endotoxin shock
Time : 10:55:11:30
Biography:
Hongbin Wang received his PhD in 2010 from the University of Pennsylvania and Post-doctoral training from University of Pennsylvania Perelman School of Medicine. Now, he is an Assistant Professor of Pharmacology in the Department of Pharmaceutical and Biomedical Sciences at the California Nothstate University College of Pharmacy. He has published more than 40 papers in peer reviewed journals.
Abstract:
Activation of the complement cascade is a major effector of the inflammatory response. Cleavage of complement components in the course of activation produces low-molecular-weight peptides, including C3a, C4a, and C5a. Both C3a and C5a have potent anaphylatoxin properties. Our recent study idnetified that C4a mediates effector functions through binding to proteaseactivated receptors (PAR) 1 and PAR4. Early study demonstrated that animals with complement C4 deficiency were reported to be more susceptable to endotoxic shock, suggesting that C4 protects animals from endotoxic effects. However, the molecular mechanism for C4 protective effect on endotoxin shock in animals is poorly understood. We propose that C4 activation peptide, C4a, possiblly through binding to PAR1/4 on platelets, monocytes, and endothelial cells, inhibits LPS-induced platelet aggregation, IL-1β and TNFα cytokine production from monocytes, and endothelium permeability to achieve C4 protective effects in endotoxin shock animal models. In the present study, we found that pretreatment with C4a to human primary monocytes can significantly inhibit LPS-induced IL-1β and TNFα production. Moreover, LPS-induced ERK phosphorylation and [Ca2+] influx were significantly inhibited by the pretreatment of C4a. Our experiments also revealed that C4a significantly decreased endothelium permeability when human endothelial cells were cultured in the presence of LPS, indicating under endotoxemia condition, C4a prevents endothelium disruption. Our data provide deeper insight into the mechanism of C4’s protective effect on endotoxic shock and would provide a valuable resource for the wider scientific community to generate future therapeutic interventions for the treatment of clinical endotoxemia.
Aysu Yurdasiper Erdem
Ege University, Turkey
Title: Characterization and aerolization properties of Carrageenan dry powder inhalers containing ibuprofen
Time : 11:30:12:05
Biography:
Aysu Yurdasiper Erdem obtained her BSc and MSc degrees from Faculty of Pharmacy at Ege University, Izmir, Turkey respectively, followed by a PhD Degree from Department of Pharmaceutical Technology, Ege University. She has studied as a PhD Student with TUBITAK Scholarship in Cardiff University, Welsh School of Pharmacy, Cardiff, UK. Her work is focused on dry powder inhalers, dermal delivery (topical, transdermal drug systems), controlled release formulations (nanoparticles, microparticles) for drug delivery. She is Editor in Chief of American Journal of Drug Delivery and Therapeutics, also Editor on the Editorial Board of several international journals. She has filed a national patent on dry powder inhaler formulation. She has been working as a Researcher in Department of Pharmaceutical Technology, Ege University. Her current research interests focus on development of novel nanomedicine including polymers and in vitro-in vivo evaluation for treatment of asthma.
Abstract:
Statement of the Problem: Delivery via the lung represents a unique opportunity to circumvent the prostaglandin independent mucosal injury associated with the oral administration of NSAIDs, as it eliminates the direct GI exposures to these drugs. Furthermore, the pulmonary drug delivery route usually decreases the dose requirements by 10 to 20 folds. Additionally, a slower rate of respiratory decline is shown in cystic fibrosis patients on high, oral doses of IBU in comparison to placebo. Dry powder inhalation is the most versatile way of pulmonary administration of API. It allows numerous formulation variations and many different dry powder inhaler (DPI) devices to design a drug product matching therapeutic needs. The purpose of the present research was to formulate IBU dry powder inhalers (DPI) containing Carrageenan as a natural polymer and to indicate appropriate excipient and polymer to improve the aerodynamic properties of the DPI formulations.
Materials & Methods: Trehalose and leucine were dissolved in Carrageenan solution. IBU was added into the solution. The mixture was then sprays and dried with constant stirring using a Büchi Nanospray dryer B-90. The formulations were analyzed by thermogravimetry (Perkin Elmer 4000). The in vitro aerosolization performance was investigated using next generation impactor (Copley). In vitro dissolution studies were done with paddle over disc method USP apparatus 2.
Results & Discussion: Encapsulation efficiency and the Carr’s Index increased with increasing Carrageenan. The highest encapsulation efficiency value was 78.6±2.9. On the other hand, the process yield decreased with increasing carrageenan. The lowest process yield value was 71.16±1.7%. The fine particle fractions of the formulations were over 37.8±3.2% thanks to the nanospray dryer. The release of IBU was nearly complete within 8 hours with 1:1 drug: polymer.
Conclusions: In this study, IBU DPI containing carrageenan was obtaining with good process yield, aerolization properties and low cohesively.
Imeda Rubashvili
Tbilisi State University, Georgia
Title: Validation of sampling procedures and quantitative determination HPLC method of Alprazolam residues for cleaning validation
Time : 12:05:12:40
Biography:
Imeda Rubashvili is an Assistant Professor, a Scientific Researcher at Ivane Javakhishvili Tbilisi State University and the Head of Validation Department of Pharmaceutical Company “Aversi-Rational” Ltd. He has published more than 30 scientific papers and participated in more than 30 international scientific conferences. He is the Member of the Council of Young Scientists of the Georgian National Academy of Sciences.
Abstract:
Cleaning validation is a critical analytical responsibility of quality assurance system in pharmaceutical industry and ensures the efficiency of the cleaning routine procedure used in production which means that it is capable and effective in removing active pharmaceutical ingredient residues from the manufacturing equipment surfaces below a predetermined level and to prevent cross-contamination of next product. The aim of this study was to validate swab and rinse sampling procedures and demonstrate the applicability of developed HPLC method for quantitative estimation of alprazolam residues in cleaning control samples collected from pharmaceutical equpment surfaces after manufacturing of alprzolam 1 mg uncoated tablets.The swab and rinse sampling procedures were developed in order to obtain a suitable recovery (>90 %). The known amounts of alprazolam are spiked onto representative surfaces, which are dried, sampled and analyzed using the validated HPLC method. Additionally, the robustness of sampling procedures was assessed. For swab sampling the surface (sampling area - 5 × 5 cm2) was successively wiped with one micro polyester swab (3×2.5×10 mm) moistened with diluent – methanol. The method was developed using LC system “Ag 1260 Infinity” and Prodigy C8(2) 250 × 4.0 mm, 5 μm column with a mobile phase - a mixture of methanol, phosphate buffer pH 3.0 and acetonitrile (10 : 45 : 45 v/v); The flow rate – 1.4 ml/min; The detector wavelength - 220 nm; The injection volume – 20 μL; The column temperature – 300C. The method was validated with respect to robustness, system suitability test, specificity, linearity-range, accuracy, precision (intra-day and inter day), limit of detection (LOD) and quantitation (LOQ). The stability of alprazolam solutions was also studied. These studies were performed in accordance with established ICH Q2 guideline. The calibration curve is linear r2=1.00000 over a concentration range 0.025 – 10 μg/mL; LOD - 0.005 μg/mL and LOQ - 0.025 μg/mL.
Adella Aparna
Vaagdevi College of Pharmacy, India
Title: Enhancement of solubility and bioavailability of Clopidogrel by selfnanoemulsifying drug delivery system
Time : 13:50-14:25
Biography:
Abstract:
A self-nanoemulsifying drug-delivery system (SNEDDS) has been explored to improve the solubility and dissolution profile of poorly soluble drug clopidogrel. Different formulations were prepared using different oils, surfactants and cosurfactants. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, drug content, % transmittance, globule size, freeze-thaw, in vitro dissolution studies, particle size analysis and zeta potential. On the basis of particle size, zeta potential and dissolution profile and other studies, F6 was found to be the best formulation of clopidogrel SNEDDS. The particle size of the emulsion is a crucial factor in self-emulsification performance because it determines the rate and extent of drug release as well as absorption. The average particle size of clopidogrel SNEDDS for transparent micro-emulsions should be less than 50nm. The particle size of the optimized SNEDDS formulation was found to be 5.2 nm and zeta potential was found to be -29 mV which comply with the requirement of the zeta potential for stability. The faster dissolution from SNEDDS may be attributed to the fact that in this formulation, the drug is a solubilized form and upon exposure to dissolution medium results in small droplet that can dissolve rapidly. The % release from optimized SNEDDS formulation F6 was highest (98.93%) and faster than other SNEDDS formulations and pure drug substance indicating influence of droplet size on the rate of drug dissolution. FTIR data revealed no physicochemical interaction between drug and excipients. Thus clopidogrel with SNEDDS formulation may be used for the improvement of solubility and dissolution rate in the effective management of heart disease.