Pharmaceutical Preparations Commons^™

Itraconazole Nanocomposites Prepared Via Rotary Evaporator Drying Of Nanomilled Suspensions, Alexander Santos Coelho

Theses

The aim of this study is to explore the feasibility of rotary evaporation for drying wetmilled drug suspensions as a novel approach to produce drug nanocomposites that exhibit fast redispersion and immediate drug release. To this end, the physical stability of the nanomilled itraconazole (drug) suspensions, a.k.a., nanosuspensions, during the milling and storage; the drying of the itraconazole nanosuspensions via the rotary evaporator; and the type/loading of various polymers/surfactants (dispersants) on aqueous redispersion and drug release from the nanocomposites were examined. Our results suggest that smaller drug particle size, owing to nanomilling, and smaller nanocomposite particle size, owing to optimized …

Sglt2 Inhibitors In The Management Of Heart Failure With Reduced Ejection Fraction, Susannah Jackson, Meghan Mathis

Physician Assistant Capstones, 2020-current

Objective: to assess whether SGLT2 inhibitors significantly reduce the risk of hospitalization for heart failure (HAHF) and cardiovascular death in patients with heart failure with reduced ejection fraction (HFrEF). Design: systematic literature review. Methods: searches were conducted in PubMed with the terms "SGLT2 Inhibitors,” “heart failure with reduced ejection fraction (HFrEF),” and "hospitalization” and the following limits: publication within the last 5 years, clinical trials, meta-analyses, randomized control trials, humans, and English. These criteria determined the selected literature: randomized control trial (RCT), use of an SGLT2i compared to placebo, and outcomes including HAHF and/or cardiovascular related death. Results: DAPA-HF: 27% …

Ketamine As A Treatment Modality For Treatment-Resistant Depression, Tracy Wulff, Shen Cao

Physician Assistant Capstones, 2020-current

Many recent studies have demonstrated the ability of ketamine, an NMDA receptor antagonist, to produce antidepressant effects that may be effective in helping reduce treatment-resistant major depression. In particular, three double-blinded randomized control trials have been conducted to assess the viability and effectiveness of this medication for treatment. This systematic literature review will analyze these studies and determine if the overall research indicates that ketamine is useful in improving depression as measured by the Montgomery–Asberg Depression Rating Scale (MADRS)¹.

Objective: Assess the effectiveness of IV Ketamine in reducing treatment-resistant major depressive disorder as measured by the Montgomery–Asberg …

Design And Synthesis Of Small Molecular Probes For Cns And Kidney Disorders, Swagat H. Sharma

Theses & Dissertations

The G protein regulated inwardly rectifying potassium channels (GIRK) are a family of inwardly rectifying potassium channels and are key effectors in signaling pathways. GIRK 1/2 channel subunit, predominantly found in the brain, is involved pathophysiology of various neurological disorders including, but not limited to, epilepsy, anxiety, Parkinson's, pain, reward, and addiction. Previously, our laboratory had identified a series of urea containing molecules as GIRK1/2 preferring activators. Unfortunately, the urea series suffers from significant PK liabilities (solubility, brain penetration and high clearance). The chapter 1 of the dissertation describes our efforts in developing three new series of activators with improved …

Evaluation Of Cost Savings Opportunity With The Use Of An Alternative Factor Vii Product Within A Tertiary Academic Medical Center And Health System, Kevin Rivera Jr., Pharmd, Anthony Renzoni Pharmd, Bcps, Bcemp, Evan Zahn Pharmd, Bcccp, Bcemp

Posters

• Eptacog alpha is the factor VII product on formulary
• It is approved by the FDA to treat bleeding in adults or children with hemophilia A or B with inhibitors •
• Additional approved uses include Glanzmann’s Disease, and factor VII deficiency and off label uses include cardiac surgery, and trauma salvage therapy
• Eptacog beta is an alternative recombinant factor VII product approved by the Food and Drug Administration in 2020 to treat bleeding in patients 12 years old or greater with hemophilia A or B with inhibitors
• In evaluating contracting pricing for each of these factor agents eptacog beta is potentially …

November / December 2021, Cindy Brooks, Randy Curry

RURAL ROCKS

Rural Rocks, the Rural Health Network newsletter by the SWOSU College of Pharmacy.

Computational Design Of Β-Fluorinated Morphine Derivatives For Ph-Specific Binding, Makena Augenstein, Nayiri Alexander, Matthew Gartner

Student Scholar Symposium Abstracts and Posters

Molecular extension and dissection techniques are used to design a morphine derivative that promotes selective binding in inflamed tissue due to its lower pH while avoiding dangerous activation in the brain. Morphine is used to treat pain associated with inflammation. While being effective analgesics, opioids carry the risk of central side effects, including addiction, respiratory depression, and sedation. Opioids are agonists that bind to the μ-opioid peptide receptor (MOR) within central and peripheral nerves and act via a G-protein coupled receptor pathway.

Deprotonation of the tertiary amine induces a negative charge on the nitrogen, discouraging binding at physiological pH (pH=7.4). …

Characterizing And Overcoming Resistance To Aminomethylspectinomycins In Gram-Negative Bacteria, Nisha Das

Theses and Dissertations (ETD)

Spectinomycin (SPC) is a broad-spectrum aminocyclitol antibiotic. Its use in agriculture has led to widespread resistance in enteric bacteria, necessitating the development of more effective analogs. Aminomethyl spectinomycins (amSPC) are modified spectinomycins with increased potency against many bacterial species. These species include Legionella pneumophila, which harbors a chromosomally encoded aminoglycoside modifying enzyme (AME). In this study, we follow up on this observation and examine the extent to which the amSPCs are substrates for AMEs through adenylation (ANTs) and phosphorylation (APH). APH(9)-Ia and ANT(3")(9) were expressed in E. coli BL21(DE3) and purified using the Ni-affinity chromatography. The ability of AMEs to …

Pharmacist-Directed Vancomycin Therapeutic Drug Monitoring In Pediatric Patients: A Collaborative-Practice Model, Kashif Hussain, Rahila Ikram, Gul Ambreen, Muhammad Sohail Salat

Department of Biological & Biomedical Sciences

Background: Therapeutic drug monitoring (TDM) of Vancomycin (VCM) is required to prevent inappropriate dosage-associated bacterial resistance, therapeutic failure, and toxicities in pediatrics. Anecdotal experience and studies show that many healthcare institutions confront barriers while implementing TDM services, this study aimed to assess a pharmacist-directed VCM-TDM service for optimizing patient care in our institution.
Materials and methods: Patients aged 1 month-18 years who received intravenous VCM were included in this quasi-experimental study. The pre-implementation phase (March-June 2018) consisted of retrospective assessment of pediatric patients, the interventional phase (July 2018 to February 2020) included educational programs and the post-implementation phase (March-June 2020) …

Dz-Bau2021-14n As Novel Pyrazolopyridine Nanocrystals: Appraisal Of Anticancer Activity Against Hct-116 And Ht-29 Colorectal Cancer Cell Lines, Zahra Kassem, Soumaiah Abou Staiteieh, Jamal Nasr, Amina Mneimneh, Ali Youssef, Nadine Darwiche, Doaa Issa, Raghida Bou Merhi, Mohammed Mehanna

BAU Journal - Health and Wellbeing

Mentioning DZ-BAU2021-14 (C₁₉H₁₇N₅O₂,347.370 g/mol) developed in BAU Labs, its promising preliminary antitumor effect nominated it to be selected as a lead antiproliferative compound against colorectal cancer cell lines owing to its proved Cyclin Dependent Kinase 2 (CDK2) inhibition (Kassem et al., 2021). Solving many problems restricting traditional cancer therapy, nanotechnology is offering safety margins and targeted delivery of poorly soluble drug. The potential effect of this compound was combined with the advantages of nanotechnology, precisely nanocrystals to achieve better antiproliferative and hopeful less cytotoxic patterns. The nanocrystals DZ-BAU2021-14N were …

Continuous Liquid-Liquid Extraction Of Lomustine Synthesis, Devna Grover

The Journal of Purdue Undergraduate Research

No abstract provided.

September / October 2021, Randy Curry, Cindy Brooks

RURAL ROCKS

Rural Rocks, the Rural Health Network newsletter by the SWOSU College of Pharmacy.

Preliminary Findings Of A Study On The Practice Of Self-Medication Of Antibiotics Among The Practicing Nurses Of A Tertiary Care Hospital, Akbar Shoukat Ali, Rahim Jandani, Arwa A. Al-Qahtani, Abdulkarem A S. Alenzi

Department of Medicine

Objectives: Antibiotic resistance is indeed a global concern. It is of significant concern especially in the low-middle income countries because of the ease of accessibility, affordability, and absence of regulations pertaining to the dispensing of non-prescription antibiotics. This study aims to estimate the frequency and factors associated with the self-medication of antibiotics found among the practicing nurses.
Methods: We conducted a descriptive cross-sectional study at a tertiary care hospital in Karachi, Pakistan from July 2016 to August 2016.
Results: Of the 48 recruited nurses, 60.4% (29/48) were practicing self-medication of antibiotics. There were slightly more male nurses (17/29) than their …

Decreasing Unintentional Pregnancies For Tennesseans, Paula M. Todd

Electronic Theses and Dissertations

In 2018, 49% of all pregnancies in the United States were unintended, with women with a lower- income status being five times more likely to experience an unplanned pregnancy. Tennessee has a high rate of unintended pregnancies, particularly among the uninsured, low-income, and rural teen populations; some 22% of these unintended pregnancies end in abortion. Oral or transdermal contraceptives that are affordable and accessible for women of childbearing age can reduce unintentional pregnancies. The addressed gap in clinical practice was that contraceptives are not currently available over the counter in Tennessee pharmacies without a prescription, which necessitates a costly medical …

The Costs Of Developing Treatments For Alzheimer’S Disease: A Retrospective Exploration, Jeffrey L. Cummings, Dana P. Goldman, Nicholas R. Simmons-Stern, Eric Ponton

School of Medicine Faculty Research

Introduction: With the exception of the recent accelerated approval of aducanumab, in over 26 years of research and development (R&D) investment in Alzheimer's disease (AD), only five novel drugs—all for symptomatic treatment only—have reached FDA approval. Here, we estimate the costs of AD drug development during this period in the private sector. Methods: To estimate private R&D funding, we collected information on AD clinical trials (n = 1099; phases 1–4) conducted between January 1, 1995 and June 21, 2021 from various databases. Costs were derived using previously published methodologies and adjusted for inflation. Results: Since 1995, cumulative private expenditures on …

No Ordinary Proteins: Adsorption And Molecular Orientation Of Monoclonal Antibodies, Ankit D. Kanthe, Andrew Ilott, Mary Krause, Songyan Zheng, Jinjiang Li, Wei Bu, Mrinal K. Bera, Binhua Lin, Charles Maldarelli, Raymond S. Tu

Publications and Research

The interaction of monoclonal antibodies (mAbs) with air/water interfaces plays a crucial role in their overall stability in solution. We aim to understand this behavior using pendant bubble measurements to track the dynamic tension reduction and x-ray reflectivity to obtain the electron density profiles (EDPs) at the surface. Native immunoglobulin G mAb is a rigid molecule with a flat, “Y” shape, and simulated EDPs are obtained by rotating a homology construct at the surface. Comparing simulations with experimental EDPs, we obtain surface orientation probability maps showing mAbs transition from flat-on Y-shape configurations to side-on or end-on configurations with increasing concentration. …

Development Of Once-A-Year Injectable Formulation Of Cabotegravir For Prevention And Treatment Of Hiv Infection, Tanmay Abhay Kulkarni

Theses & Dissertations

Long-acting cabotegravir (CAB) extends antiretroviral drug (ARV) dosing to monthly for maintenance of human immunodeficiency virus type one (HIV-1) suppression and to every other month for prevention of viral transmission. However, injection dose volumes, site reactions, and clinical oversights that are required remain obstacles towards broad usage. To meet these needs, surfactant coated hydrophobic and lipophilic CAB prodrugs were created with controlled prodrug dissolution, hydrolysis and drug tissue penetration. To such ends, fatty acid ester CAB nanocrystal prodrugs with 14, 18, and 22 added carbon chains were synthesized then nanoformulated as NMCAB, NM2CAB, and NM3CAB. These nanocrystal formulations were tested …

Uplc-Ms/Ms Analysis Of The Michaelis-Menten Kinetics Of Cyp3a-Mediated Midazolam 1′- And 4-Hydroxylation In Rat Brain Microsomes, Devaraj Venkatapura Chandrashekar, Barent Dubois, Reza Mehvar

Pharmacy Faculty Articles and Research

Midazolam (MDZ) is a short-acting benzodiazepine with rapid onset of action, which is metabolized by CYP3A isoenzymes to two hydroxylated metabolites, 1′-hydroxymidazolam and 4-hydroxymidazolam. The drug is also commonly used as a marker of CYP3A activity in the liver microsomes. However, the kinetics of CYP3A-mediated hydroxylation of MDZ in the brain, which contains much lower CYP content than the liver, have not been reported. In this study, UPLC-MS/MS and metabolic incubation methods were developed and validated for simultaneous measurement of low concentrations of both hydroxylated metabolites of MDZ in brain microsomes. Different concentrations of MDZ (1–500 µM) were incubated with …

Insights Into The Mechanisms Of Brain Endothelial Erythrophagocytosis, Jiahong Sun, Prema Vyas, Samar Mann, Annlia Paganini-Hill, Ane C. F. Nunes, Wei Ling Lau, David H. Cribbs, Mark J. Fisher, Rachita K. Sumbria

Pharmacy Faculty Articles and Research

The endothelial cells which form the inner cellular lining of the vasculature can act as non-professional phagocytes to ingest and remove emboli and aged/injured red blood cells (RBCs) from circulation. We previously demonstrated an erythrophagocytic phenotype of the brain endothelium for oxidatively stressed RBCs with subsequent migration of iron-rich RBCs and RBC degradation products across the brain endothelium in vivo and in vitro, in the absence of brain endothelium disruption. However, the mechanisms contributing to brain endothelial erythrophagocytosis are not well defined, and herein we elucidate the cellular mechanisms underlying brain endothelial erythrophagocytosis. Murine brain microvascular endothelial cells (bEnd.3 …

Characterization Of Lamellar Liquid Crystal Emulsifiers In Topical Creams Containing A Novel Solvent, Melinda Joanna Sutton

Graduate Theses/Dissertations

Diethylene glycol monoethyl ether (DEGEE) is a promising solvent component in topical cream formulations due to its superior solubilizing abilities with certain active pharmaceutical ingredients. One of the goals of this study is to characterize the effects of pH on the physical and chemical stabilities of topical cream formulations containing particularly high concentrations of DEGEE by characterizing a full topical pH profile of 3.5 – 9.0. The second goal is to evaluate the presence, amount, and characteristics of lyotropic liquid crystals (LLCs), molecularly structured in a lamellar phase, in a model cream emulsion utilizing polarized light microscopy (PLM). The presence …