Pharmaceutics and Drug Design Commons^™

The Fit-Hansa Demonstrates Reliability And Convergent Validity Of Functional Performance In Patients With Shoulder Disorders, Prajyot Kumta, Joy Macdermid, Saurabh Mehta, Paul Stratford

Saurabh Mehta

Study

DesignPsychometric study design.

Objectives

To assess the test-retest reliability and convergent validity of the Functional Impairment Test-Hand and Neck/Shoulder/Arm (FIT-HaNSA) in patients with shoulder disorders.

Background

Performance tests that assess functional ability of patients with shoulder disorders can provide useful information for making clinical or return-to-activity decisions. No performance-based shoulder test has yet demonstrated sufficient relevance or clinical measurement properties. The FIT-HaNSA examines upper extremity performance during repetitive tasks that emphasize shoulder reaching and static postures and, therefore, has greater relevance for assessing performance.

Methods

Thirty-six patients with shoulder disorders and 65 healthy controls were recruited for the study. …

Computer-Aided Drug Design And Discovery, Screening And Synthesis Of Small Molecule Inhibitors Of Nucleoside Transporters, Hilaire Colleen Playa

Theses and Dissertations (ETD)

Using prior biological data, pharmacophore models were made for hCNT1, hCNT3, hENT1, and hENT4. The hCNT3 and hCNT1 pharmacophore were used to select compounds for biological testing. The NBMPR analogue and dipyridamole analogue hENT1 pharmacophores were compared to each other and to a combined pharmacophore for hENT1. The dipyridamole analogue pharmacophore better predicted non-nucleoside small molecule inhibitors, and as such appears to be the better tool for aiding in the design of new small molecule inhibitors. The hCNT3 pharmacophore failed to select active compounds and as such must be redesigned. The hCNT1 pharmacophore succeeded in identifying two moderately active compounds …

Nucleoside Reverse Transcriptase Inhibitors Possess Intrinsic Anti-Inflammatory Activity, Benjamin J. Fowler, Bradley D. Gelfand, Younghee Kim, Nagaraj Kerur, Valeria Tarallo, Yoshio Hirano, Shoba Amarnath, Daniel H. Fowler, Marta Radwan, Mark T. Young, Keir Pittman, Paul Kubes, Hitesh Agarwal, Keykavous Parang, David R. Hinton, Ana Bastos-Carvalho, Shengjian Li, Testuhiro Yasuma, Takeshi Mizutani, Reo Yasuma, Charles Wright, Jayakrishna Ambati

Pharmacy Faculty Articles and Research

Nucleoside reverse transcriptase inhibitors (NRTIs) are mainstay therapeutics for HIV that block retrovirus replication. Alu (an endogenous retroelement that also requires reverse transcriptase for its life cycle)–derived RNAs activate P2X7 and the NLRP3 inflammasome to cause cell death of the retinal pigment epithelium in geographic atrophy, a type of age-related macular degeneration. We found that NRTIs inhibit P2X7-mediated NLRP3 inflammasome activation independent of reverse transcriptase inhibition. Multiple approved and clinically relevant NRTIs prevented caspase-1 activation, the effector of the NLRP3 inflammasome, induced by Alu RNA. NRTIs were efficacious in mouse models of geographic atrophy, choroidal neovascularization, graft-versus-host disease, and sterile …

Considering A New Paradigm For Alzheimer’S Disease Research, Gillian R. Langley

Gill Langley, PhD

Using Alzheimer’s disease as a case study, this review argues that it might be time to consider a new paradigm in medical research and drug discovery. The existing framework is overly dependent on often unvalidated animal models, particularly transgenic mice. Translational success remains elusive and costly late-stage drug failure is common. The conventional paradigm tends to overlook species differences and assumes that animal-based findings are generally applicable to humans. Could pathways-based research using advanced human-specific models probed with new tools, including those of systems biology, take centre stage? The current transition in chemical toxicology to a 21st-century paradigm could be …

Are Elevated Vancomycin Serum Trough Concentrations Achieved Within The First 7 Days Of Therapy Associated With Acute Kidney Injury In Children?, Chad A. Knoderer, Kristen R. Nichols, Kelsey C. Lyon, Megan M. Veverka, Amy C. Wilson

Chad A. Knoderer

Background In 2008, the empiric vancomycin dosing recommendation in children at our institution was changed from 40 to 60 mg/kg per day. Subsequently, an increased incidence of acute kidney injury (AKI) in patients receiving vancomycin was suspected. The objective of this study was to evaluate AKI in children receiving vancomycin and to determine risk factors for AKI development. Methods Medical records of patients aged 30 days through 17 years who received vancomycin for at least 72 hours between January and December 2007 (40 mg/kg per day) and January and December 2010 (60 mg/kg per day) were reviewed. Patients with cystic …

Antispasmodic And Ca++ Antagonist Potential Of Marrubiin, A Labdane Type Diterpene From Phlomis Bracteosa, Javid Hussain, Riaz Ullah, Arif-Ullah Khan, Fazal Mabood, Mohammad Raza Shah, Ahmed Al-Harrasi, Anwar Gilani

Anwar Gilani

A tricyclic labdane type diterpene was isolated for the first time from ethyl acetate soluble part of Phlomis bracteosa. Its structure was confirmed by x-ray which was found to be marrubiin. When studied in isolated rabbit jejunum, marrubiin caused concentration-dependent relaxation of spontaneous and high K+ (80 mM)-induced contractions, like that caused by verapamil, indicating that marrubiin exhibits spasmolytic activity, possibly mediated through Ca++ channel blocking action.

Canagliflozin, A New Sodium-Glucose Co-Transporter 2 Inhibitor, In The Treatment Of Diabetes, Sarah A. Nisly, Denise M. Kolanczyk, Alison M. Walton

Sarah A. Nisly

Purpose. The published evidence on the pharmacology, pharmacodynamics, pharmacokinetics, safety, and efficacy of a promising investigational agent for managing type 2 diabetes is evaluated. Summary. Canagliflozin belongs to a class of agents—the sodium–glucose cotransporter 2 (SGLT2) inhibitors—whose novel mechanism of action offers potential advantages over other antihyperglycemic agents, including a relatively low hypoglycemia risk and weight loss-promoting effects. Canagliflozin has dose-dependent pharmacokinetics, and research in laboratory animals demonstrated high oral bioavailability (85%) and rapid effects in lowering glycosylated hemoglobin (HbA1c) values. In four early-stage clinical trials involving a total of over 500 patients, the use of canagliflozin for varying periods …

Use Of A Subcutaneous Insulin Computerized Glucostabilizer™ Program On Glycemic Control In The Intensive Care Setting: A Retrospective Data Analysis., Sarah A. Nisly, Serena Harris, Laura Aykroyd, Joni Carrol, Brian Ulmer, Michael Waddell, Samuel Flanders, Rattan Juneja

Sarah A. Nisly

Background: Despite guidelines that recommend strongly against Sliding Scale Insulin (SSI) it continues to be the most commonly insulin regimen used in hospitals to treat hyperglycemia. In addition to being reactionary to a glucose that has already increased, SSI offers practical challenges in the randomness of the doses of insulin prescribed and often a disconnect with glucose testing that should be occurring in congruence to the insulin dosing. While many clinical trials have shown improved glycemic control in critical care patients receiving intravenous insulin; few studies have demonstrated the efficacy of subcutaneous (SQ) insulin in this setting. In this study, …

Inhibition Of The Thioesterase Activity Of Human Fatty Acid Synthase By 1,4- And 9,10-Diones, Herman H. Odens

Faculty Works

Fatty acid synthase (FASN) is the enzyme that synthesizes fatty acids de novo in human cells. Although FASN is generally expressed at low levels in most normal tissues, its expression is highly upregulated in many cancers. Consistent with this notion, inhibition of FASN activity has demonstrated potential to halt proliferation and induce cell death in vitro and to block tumor growth in vivo. Consequently, FASN is widely recognized as a valuable therapeutic target. In this report, we describe a variety of 1,4-quinones and 9,10- anthraquinones, including several natural compounds and some newly synthesized compounds, that potently inhibit the thioesterase (TE) …

Uji Aktivitas Antioksidan Ekstrak Metanol Bunga Dan Daun Patikala (Etlingera Elatior (Jack) R.M.Sm) Menggunakan Metode Dpph, Virsa Handayani, Aktsar Roskiana Ahmad, Miswati Sudir

Pharmaceutical Sciences and Research

Patikala (Etlingera elatior (Jack) R.M.Sm) is a plant of the Zingiberaceae family. Patikala (E. elatior (Jack) R.M.Sm) have bioactive compounds are flavonoids that act as antioxidants. The purpose of this study was to measure free radical activity in the methanol extract of the fruit and leaves Patikala (E. elatior (Jack) R.M.Sm). Extraction of flowers and leaf samples by maceration method using methanol. Qualitative analysis of chemical compounds with certain eluent using Thin Layer Chromatography (TLC) to determine the group of active compounds in the extract. Antioxidant activity assay using the immersion method of DPPH (1,1-Diphenyl-2-picryl Hidrazil) measured absorption at a …

Potensi Pemanfaatan Nigella Sativa L. Sebagaiimunomodulator Dan Antiinflamasi, Farida Sulistiawati, Maksum Radji

Pharmaceutical Sciences and Research

Nigella sativa L. has long been used as an herbal medicine in some countries, particularly in the Middle East and in other Asian countries, including in Indonesia. One component is a protein compound extracted from black cumin oil residues, known to have efficacy to enhance the immune system and as an anti-inflammatory. As the compound will be degraded when administered orally, the research on its delivery systems, is interesting to be developed. This article will review about the prospects of their utilization and strategy formulation that preparation can be delivered orally.

Efek Ekstrak Etanol Daun Premna Cordifolia Terhadap Malondialdehida Tikus Yang Dipapar Asap Rokok, Asri Adyttia, Eka Kartika Untari, Sri Wahdaningsih

Pharmaceutical Sciences and Research

Free radical from cigarrete smoke cause lipid peroxidation that could be identified by increasing levels of Malondialdehida (MDA). Premna cordifolia leaves known having antioxidant activity in in vitro study. This study aimed to know the effect of P. cordifolia leaves extract on the levels of MDA after exposure to cigarette smoke. The simplicia extracted by maseration using 70% ethanol. Twenty four male wistar rats were divided into six groups, i.e. : control normal, negative control, positive control received cigarette smoke exposure and vitamin E (18mg/kg BW) and three groups received cigarette smoke exposure and P. cordifolia leaves extract with doses …

Uji Efek Antiinflamasi Fraksi Air Daun Mahkota Dewa (Phaleria Macrocarpa (Shecff.) Boerl.) Terhadap Tikus Putih (Rattus Norvegicus L.), Aprilita Rina Yanti Eff, Ema Dewanti, Melisha Adelina H

Pharmaceutical Sciences and Research

Inflammation occurs as the attempt of body to inactivate organisms that attack the body, removing irritants and regulate tissue repair. One of the medicinal plants used empirically as antiinflammation is the leaf of Mahkota Dewa (Phaleria macrocarpa (Schecff.) Boerl). This study investigated the effect of anti-inflammatory water fraction of leaf Mahkota Dewa using oedema induction method with caragenin in rat. Water fraction of Mahkota Dewa was given at the dose 0.5 g/kg BW ,1 g/kg BW and 2 g/kg BW. Sodium diclofenac was used as a positive control and CMC as negative control. The result showed water fractions of three …

Tablet Effervescent Ekstrak Belimbing Wuluh (Averrhoa Bilimbi L.) Dengan Variasi Kadar Pemanis Aspartam, Rosmala Dewi, Iskandarsyah Iskandarsyah, Devi Octarina

Pharmaceutical Sciences and Research

Averrhoa bilimbi is fruit that has many benefits but the usage is not optimal. That is why the aim of the research is to get formulation of effervescent granule and tablet containing dry Averrhoa bilimbi extract with modified concentration of aspartame as sweetening agent for commercial healthy drink. Granules and tablets were produced with dry method granulation with 40% of relative humidity (RH) and 25ºC of temperature. The three of formulation were qualified as effervescent granules and tablets. Favorite tests showed that no significant differences of appearances, tastes for three of effervescent granules and tablets.

Aktivitas Penghentian Pendarahan Luar Ekstrak Etanol Daun Berenuk (Crescentia Cujete L) Secara In-Vivo, Anjar Mahardian Kusuma, Adri Nurrakhmat Sulistyo, Susanti Susanti, Sabikis Sabikis

Pharmaceutical Sciences and Research

Crescenti cujete L. or better known as calabash is a plant that thrives in Indonesia. Calabash has a great potential as an herbal remedy, but there is only some scientific research conducted on this plant, one of which is antibacterial against Bacillus subtilis and Escerichia coli on 2006 by Susanti. The method in this research was an experimental activities of the cessation external bleeding with 3 dose variation of calabash leaf extract 80%, 60%, and 40% by counting the bleeding time at base of the tail in mice. As a result, all groups of external bleeding cessation activities have better …

Ligand-Receptor Interactions For Supramolecular Disassembly With Applications In Screening And Drug Delivery, Diego Amado Torres

Doctoral Dissertations

Proteins have the capacity to bind specific sets of compounds known as ligands, these are small molecules with a recurrent theme in their molecular design that is a characteristic exploited here to (i) identify particular affinities of small molecules for proteins with the aim of using them as ligands, inhibitors, or targeting moieties in more complex systems by means of a methodology that screens small molecules based on protein affinity; (ii) decorate a self-assembling supramolecular system at different positions, making it responsive to a complementary protein with the aim of exploring differences in disassembly and sensitivity of the release of …

Effect Of Twin Screw Granulator Process Parameters On Granule Attributes, Haosheng Xu, Ridade Sayin, James Litster

The Summer Undergraduate Research Fellowship (SURF) Symposium

Twin screw wet granulation has been considered as an efficient and effective technique of manufacturing granules (agglomerates made up of small particles) and has been widely applied in pharmaceutical industry. However, narrow granule size distributions are difficult to achieve. This study aims to elucidate the effect of process parameters such as liquid feed rate and screw configuration on the granule attributes through granule characterization. The methods used are sieve analysis (for size distribution), liquid distribution (determining the dye concentration in the granules) and density and porosity (percentage gas volume in the granule) analyses. A sieve shaker is used to divide …

Electrochemical Investigations Of Benzanthrone, Antonio Trevino, Kefa Karimu Onchoke

Undergraduate Research Conference

No abstract provided.

In Vitro Metabolic Stability Study Of New Cyclen Based Antimalarial Drug Leads Using Rp-Hplc And Lc-Ms/Ms, Apoorva V. Rudraraju, Mohammad F. Hossain, Anjuli Shrestha, Prince N.A. Amoyaw, Babu L. Tekwani, M. O. Faruk Khan

Pharmaceutical Science and Research

Metabolic stability of the new antimalarial drug leads is determined using Human Liver Microsome (HLM) and specific cytochrome P450 enzyme (CYP2C8) taking the clinically used antimalarial drug chloroquine as a positive control. Experiment is done using standard methods. All the assays were conducted in 0.5 M phosphate buffer at pH 7.4. In general the metabolic reaction was initiated by adding 1 mM NADPH and 0.5 mg of enzyme. Incubations were done with time frequency of 0 hr, 1 hr, and 2 hrs at 37°C and the reactions were terminated by adding acetonitrile in the equal amounts of the assay mixture …

Hydrodynamic Cfd Modeling Of A Pharmaceutical Reactor Vessel Provided With A Retreat-Blade Impeller Under Different Baffling Conditions, Christopher G. Foehner

Theses

In the pharmaceutical industry, glass-lined reactors and vessels are often utilized to carry out a variety of different unit operations. Within these systems, both the vessel and impellers are typically glass-lined in order to provide superior corrosion resistance, prevent product contamination, and enhance cleanability. This approach, in turn, often requires the use of different, and sometimes sub-optimal, baffling conditions, which affect the hydrodynamics of the vessels and the reactor performance.

Computational Fluid Dynamics (CFD) is a computational tool that employs numerical methods and algorithms to discretize and numerically solve partial differential equations (PDEs) representing mass, energy, and momentum conservation equations …