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Best Paper Awards 2016

Best Research Paper

Dr. Krishna Veni Nagappan
JSS College of Pharmacy

Best Student Paper

Ms. Nisansala Bopage
The Open University of Sri lanka

Best Paper Awards 2015

Best Research Paper

Dr. Fawzy Elbarbry
Pacific University

Best Student Paper

Ms. Christine Loescher
La Trobe University

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Selected Paper Submissions for Oral Presentation at PHARMA 2017 (as at 14 June 2017)

As a continuation of our efforts to discover and develop the 1,2,4-oxadiazole derivatives as potential anticancer agents, herein we explored substitutions at the 3rd and 5th position of 1,2,4-oxadiazoles to enhance the anticancer potential of synthesized compounds. Formation of 3-aryl-5-aryl-1,2,4-oxadiazoles were accomplished by the reaction of substituted arylcarbonyl chloride with substituted N-hydroxybenzamidine or Nhydroxypyridinecarboxamidine. The in vitro cytotoxic effects of 3-aryl-5-aryl-1,2,4- oxadiazoles have been demonstrated across a wide array of tumor cell types and a few compounds (2AA, 1CC, 1AA and 1BB) exhibited highest anticancer potential against different cancer (DLD1, T47D, CaCo-2 and PC-3) cell lines respectively.
The present study aims to conduct a preliminary phytochemical analysis by the successive extraction of the bark of Annona reticulata L. using petroleum ether, chloroform, and ethanol. Investigation of the phytochemical profile on the bark of A. reticulata L. reported that presence of flavonoids, saponins, triterpenoid tannins. The n-hexane fractions of ethanolic extract was fractionated with n-hexane and acetone (15:1). The hexane fraction of ethanolic extract was forwarded to column for isolation. Bioactive directed fractionation of ethanol extract resulted in the characterization of the triterpenoid. The structure was elucidated by spectroscopic techniques included thin layer chromatography (TLC) and high performance liquid chromatography (HPLC), UV and Gas chromatography- mass spectrometric (GC-MS). One triterpenoid were isolated and characterized by chromatographic and spectroscopical analysis. The active compound taraxerol separated by isocratic mode using potassium di hydrogen orthophosphate buffer (KH2PO4), methanol (0.5:9.5%) with flow rate of 1.2 ml/min with injection volume 10 μl; UV detection was 211 nm. The present work deals with the isolation, structure elucidation and identification of the taraxerol.
With the implementation of ICH Q8, Q9, Q10, Q11 and draft Q12 guidelines, regulatory bodies mandate a data driven, science and risk based decision making process utilizing data from all three stages of the PV Lifecycle- Stage 1: Process Design, Stage 2: Process Performance Qualification (PPQ) and Stage 3: Continued Process Verification (CPV). Stage 2 PPQ can utilize practical tools to determine number of batches required for a study. This best estimate is based on statistical confidence using observed intra-batch variability and estimated inter-batch variability of similar products/processes and product label claim. Pa (Probability of Acceptance) is an innovative statistical analysis tool applicable for multi-level acceptance criteria (example Content Uniformity, Dissolution) that is fit for pharmaceuticals. Stage 3A evaluation of substantial data gathered from Stage 2 and predetermined number of batches can be used to estimate Inherent Process Variability (IPV) and PaCS index, Stage 3B trend limits and Process Capability Quality dashboard (PCQd) for a product. These novel statistical assessments can be used to gain further understanding of new product launches prior to routine monitoring. Stage 3B is an effective quality risk management tool for mitigating risks to product quality; detecting trends and implementing preventative measures prior to failures. The objective is to provide novel methodologies that can be used in Stage 2 and Stage 3 assessments to gain product understanding and confidence for future batches to meet the required specification. Product and process understanding of similar products and SPC methodologies are key components for successful PV Lifecycle Management. The 2011 FDA PV Guidance proposes process validation lifecycle approach.
Methionine enkephalin (MENK), derived from proenkephalin, plays an important role in immune regulation. The aim of this study was to investigate enhanced immune function of MENK in two mice models: cyclophosphamide (CTX)-induced immunosuppressive mice and CT26-tumor bearing mice (TBM). We found that MENK decreased percentages of MDSCs in bone marrow, spleen, blood and liver in these two models upon treatment, and those in tumor in TBM. MENK-treated mice displayed elevated ratio of CD4+T and CD8+T cells in spleen as well as increased T and B lymphocytes proliferation. Meanwhile, we noticed that MENK also ameliorated liver damage reflected by lower levels of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) in serum of model mice and reduced risks of cancer-associated index in TBM including inflammation, high lipid and high glucose. Furthermore, MENK lowered down the levels of non-esterified fatty acid (NEFA), triglycerides (TG) and total cholesterol (T-CHO) in both liver homogenate and serum. MENK treatment decreased expression of p-STAT3, increased expression of p-AKT, IRS1 and Glut4 at protein level as well as reduced lipogenesis-associated genes and elevated glycolysis-associated genes in liver of TBM. Also, abated expression of genes associated with MDSCs generation (M-CSF, GM-CSF, IL-6, IL-1β) and migration (S100A9, KC) was observed within shrunken subcutaneous tumor by MENK intervention. Our data substantiate that MENK has the ability to strength immune function against CTX-induced immunosuppression and colon cancer by reducing MDSCs and improving liver metabolism.
Purpose of the study was to synthesize and characterize twenty five oxazepine derivatives. All the synthesized compounds subjected for anti-oxidant and anti-inflammatory effects.Anti-oxidant effect screened by invitro method by hydrogen peroxide scavenging method. Anti-inflammatory effect screened by invitro as well as invivo method-carragenan induced paw oedema method.Only three compounds exhibited excellent anti-inflammatory effect. Aim/Objectives: To synthesize 25 oxazepine derivatives ,to do structural characterization spectrophotometrically and to screen newly synthesized compounds for anti-oxidant and anti-inflammatory activity.
Purpose of the study was to synthesize 25 new oxazine derivatives ,to characterize their structures by spectrophotometrically and to screen newly synthesized compounds for Amylase and Lipase inhibitory effects. All the synthesized compounds subjected to amylase and lipase inhibitory effects. Among the tested compounds only seven compounds exhibited good amylase inhibitory effect. While only three showed good lipase inhibitory effects.
Controlled release (CR) dosage forms have been extensively used to improve therapy with several important drugs. Gastro retentive drug delivery system (GRDDS) are an approach to prolong gastric residence time, there by targeting site-specific drug release in the upper GIT for local or systemic effect. The purpose of writing this review is to investigate, compile and present the recent as well as past literatures in more concise way with special focus on approaches which are currently utilized in the prolongation of gastric residence time. GRDDS has become leading methodology in site specific orally administered controlled release drug delivery system. Various drugs, which are unstable in alkaline pH, soluble in acidic pH, having narrow absorption window, site of action specific to stomach can be developed by using this technique. Various factors influence on drug retention such as density, size, shape, fed or unfed state, single or multiple unit formulation, caloric content, frequency of feed, gender, age, posture, concomitant drug administration, diseased state of the individual etc. Current approaches to GRDDS are floating drug delivery systems, swelling system, bioadhesive system and high density system.
Aripiprazole is a novel and well-known for the treatment of both negative and positive symptoms associated with schizophrenia. However, aripiprazole faces a few limitations including poor aqueous solubility along with a high first pass effect that leads to low bioavailability.
Zizyphus xylopyrus (Retz.) Willd. (Rhamnaceae) is a straggling shrub or a small tree, armed with spines, found throughout north‐western India, Pakistan and China. The root, barks, leaves and fruits of Zizyphus species used in medicine for the treatment of various diseases such as weakness, liver complaints, obesity, diabetes, skin infections, fever, diarrhoea, insomnia and digestive disorders. Ethanolic extract of leaves of Zizyphus xylopyrus (Retz.) Willd was prepared by successive solvent extraction and subjected to antimicrobial and antifungal study against Streptococcus fecallis bacteria and Aspergillus niger fungi respectively using ciprofloxacin and ketoconazole as model drugs correspondingly. Ethanolic extract of Z. xylopyrus (Retz.) Willd leaves extract was found to be significantly possessed antimicrobial and antifungal activity.
Parkinson’s disease is a chronic neurodegenerative disease which affects the body movements.
Curcumin has been reported for significant anti inflammatory effects in TNBS and DSS inflammatory models. Further, site specific curcumin delivery in inflamed colon offers increased efficacy and responsiveness.
Ferula sumbul Hook. (Syn. Ferula moschata Reinsch.) commonly called as sumbul (Hindi) or musk root (English), consists of cylindrical or tapered pieces of dried roots and rhizomes with bitter taste and slight musky odour. F. sumbul has been traditionally used for relieving anxiety, as a sedative in hysteria and other nervous disorders, and as a mild gastrointestinal stimulant.
Tricyclic antidepressants are important frontline treatments for depression worldwide but can have many serious side effects. The safety and efficacy of these drugs may be affected by both drug-drug and drug-gene interactions. The objective of the present study was to investigate the community prevalence of predicted drug and gene interactions for tricyclic anti-depressant drugs in a cohort of older Australians from the Hunter Community Study. Participants were genotyped using Affymetrix Kaiser Axiom arrays or imputation from HapMap 2 and 1000 Genome reference panels. Of 57 participants on tricyclic antidepressants, 47 (83%) were co-prescribed at least one potential interacting drug. with on average 2.5 possible interactions per participant. Genotype data were available for 32 of the 57 participants taking tricyclic antidepressant drugs. Of these 32, 22% had clinically actionable genotypes predicted to increase the likelihood of adverse effects. A change of tricyclic antidepressant dose would be recommended for patients with these genotypes under current international pharmacogenomic guidelines. The findings of this study suggest that over 1 in 5 patients on tricyclic antidepressants may be at increased risk of adverse reactions involving drug-gene interactions that may justify dose reduction and emphasise the potential value of considering the pharmacogenomics of tricyclic anti-depressants in conjunction with drug interaction analyses.

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