Pharmacy and Pharmaceutical Sciences Commons^™

Application Of Cross-Linked Rice Starches As Drug Delivery Matrices In Monolithic Tablets, Christopher F. Peluso, Fernanda O. Onofre, Ya-Jane Wang

Discovery, The Student Journal of Dale Bumpers College of Agricultural, Food and Life Sciences

The sustained release properties of regular and waxy rice starches and their derivatives were studied in tablets. The starches were cross-linked to different levels with epichlorohydrin, and the sustained release properties, swelling power, and rheological characteristics of the matrices prepared were determined. Propranolol hydrochloride was used as a model drug. The sustained release properties of waxy rice starch improved with increasing cross-linking levels, whereas cross-linking had little impact on the functionality of regular rice starch matrices. There was an increase in swelling power for both regular and waxy rice starches as cross-linking levels increased. Both starches showed an increase in …

Antitumour And Antimalarial Activity Of Artemisinin–Acridine Hybrids, Michael Jones, Amy Mercer, Paul Stocks, Louise La Pensee, Rick Cosstick, B. Kevin Park, Miriam Kennedy, Ivo Piantanida, Stephen Ward, Jill Davies, Patrick Bray, Sarah Rawe, Jonathon Baird, Tafadzwa Charidza, Omar Janneh, Paul O'Neill

Articles

Artemisinin–acridine hybrids were prepared and evaluated for their in vitro activity against tumour cell lines and a chloroquine sensitive strain of Plasmodium falciparum. They showed a 2–4-fold increase in activity against HL60, MDA-MB-231 and MCF-7 cells in comparison with dihydroartemisinin (DHA) and moderate antimalarial activity. Strong evidence that the compounds induce apoptosis in HL60 cells was obtained by flow cytometry, which indicated accumulation of cells in the G1 phase of the cell cycle.

Association Of Antipsychotic Use With Hospital Events And Mortality Among Medicare Beneficiaries Residing In Long-Term Care Facilities, Linda Simoni-Wastila, Priscilla T. Ryder, Jingjing Qian, Ilene H. Zuckermann, Thomas Shaffer, Lirong Zhao

Scholarship and Professional Work – COPHS

Objective—Antipsychotic (AP) utilization has grown significantly in long-term care (LTC) settings. Although a growing literature associates AP use with higher mortality in elderly with dementia, the association of APs with hospital events is unclear. The authors examine prevalence and trends in AP use by Medicare beneficiaries residing in LTC and the association of APs and other drug use variables with hospital events and mortality.

Design—Retrospective analysis using sequential multivariate Cox proportional hazards models.

Setting—Medicare Current Beneficiary Survey linked to Institutional Drug Administration and Minimum Data Set files.

Participants—A total of 2,363 LTC Medicare beneficiaries, 1999–2002. Measurements—Trends in LTC AP use …

Kajian Keamanan Pemakaian Obat Anti-Hipertensi Di Poliklinik Usia Lanjut Instalasi Rawat Jalan Rs Dr Sardjito, Zullies Ikawati

Majalah Ilmu Kefarmasian

Increasing age is generally followed by increasing chronic diseases so that the elderly needs much therapy using drugs for therapy of numerous diseases they have. Hyper-tension is one of diseases of which its prevalence increases along with increasing age. Most of the elderly diagnosed as having hypertension finally take therapy using anti-hypertension drugs. Physiological changes that happen to the elderly lead to use of drugs for side effect diseases of which their consumption should be considered while having anti-hypertension drugs. Changes in biological system to the elderly will af-fect the process of drug molecular interaction, which finally affects clinical efficacy …

Incentives For Orphan Drug Research And Development In The United States, Enrique Seoane-Vazquez, Rosa Rodriguez-Monguio, Sheryl L. Szeinbach, Jay Visaria

Pharmacy Faculty Articles and Research

Background: The Orphan Drug Act (1983) established several incentives to encourage the development of orphan drugs (ODs) to treat rare diseases and conditions. This study analyzed the characteristics of OD designations, approvals, sponsors, and evaluated the effective patent and market exclusivity life of orphan new molecular entities (NMEs) approved in the US between 1983 and 2007.

Methods: Primary data sources were the FDA Orange Book, the FDA Office of Orphan Drugs Development, and the US Patent and Trademark Office. Data included all orphan designations and approvals listed by the FDA and all NMEs approved by the FDA during …

Cytotoxic Effects Of Ruthenium Compounds On Human Cancer Cell Lines., Katie Beth Brown

Electronic Theses and Dissertations

Chemotherapy is the most common cancer treatment. Traditionally, platinum-based drugs are used in chemotherapy. More recently, researchers have focused on ruthenium based compounds as a substitute for the platinum compounds. Ruthenium-based compounds appear to be less toxic to healthy cells than traditional platinum-based compounds. In this study, 7 ruthenium-based compounds were tested on HT-29 (colon) and MCF-7 (breast) human cancer cell lines with the specific aim of determining whether or not any of the ruthenium-based compounds exhibited cytotoxic properties. In addition, levels of vascular endothelial growth factor (VEGF) production were tested in supernate from the cancer cells treated with various …

Controlled Release Of Insulin And Modified Insulin From A Novel Injectable Biodegradable Gel, Om Anand

Theses and Dissertations (ETD)

The objective of the study was to develop a controlled release dosage form of
insulin, which can provide basal concentrations of insulin in diabetic rats for 1 to 2 weeks after a single subcutaneous injection.
A biodegradable injectable drug delivery gel was prepared by dissolving a
biodegradable polymer, polylactic-co-glycolic acid (PLGA), in biocompatible
plasticizer(s), triethyl citrate (TEC) and/or acetyl triethyl citrate (ATEC). Insulin was
then loaded into the blank gel to form an insulin suspension in the polymer solution.
After the insulin-loaded gel was injected subcutaneously, the plasticizer(s) dissolved in the aqueous media and were gradually taken away from the …

Structure- And Ligand-Based Design Of Novel Antimicrobial Agents, Kirk Edward Hevener

Theses and Dissertations (ETD)

The use of computer based techniques in the design of novel therapeutic agents is a rapidly emerging field. Although the drug-design techniques utilized by Computational Medicinal Chemists vary greatly, they can roughly be classified into structure-based and ligand-based approaches. Structure-based methods utilize a solved structure of the design target, protein or DNA, usually obtained by X-ray or NMR methods to design or improve compounds with activity against the target. Ligand-based methods use active compounds with known affinity for a target that may yet be unresolved. These methods include Pharmacophore-based searching for novel active compounds or Quantitative Structure-Activity Relationship (QSAR) studies. …

Synthesis And Evaluation Of Tetramic Acids As Antimicrobial Agents, Jason B. Wilson

Theses and Dissertations (ETD)

As bacterial infectious diseases are a major cause of morbity and mortality throughout the world, and many causative organisms are resistant to currently available antibiotics, the motivation for the development of new drugs is readily apparent. A number of natural products exhibiting antimicrobial activity possess a tetramic acid (2,4-pyrrolidinedione) functional group. As their antibacterial mechanism of action is different from that of many of the currently available antibiotics, these compounds have potential to serve as a basis for a pharmacophore in synthetic compounds. However, toxicity to eukaryotic cells is frequently a problem with currently known tetramic acids. The purpose of …

Drug-Prescribing Patterns During Pregnancy In The Tertiary Care Hospitals Of Pakistan: A Cross Sectional Study., Dileep K Rohra, Nirmal Das, Syed I Azam, Nazir A Solangi, Zahida Memon, Abdul M Shaikh, Nusrat H Khan

Department of Biological & Biomedical Sciences

Background: The rationale for use of drugs during pregnancy requires a careful assessment as in addition to the mother, the health and life of her unborn child is also at stake. Information on the use of drugs during pregnancy is not available in Pakistan. The aim of this study was to evaluate the patterns of drug prescriptions to pregnant women in tertiary care hospitals of Pakistan. Methods: This was a cross-sectional study conducted at five tertiary care hospitals of Pakistan. Copies of outPatient medicinal prescriptions given to pregnant Patients attending the antenatal clinics were collected. The drugs were classified according …

Oxidative Stress-Mediated Anticancer Activity Of Novel Ahr Modulators Af & 5f203, Lancelot S. Mclean

Loma Linda University Electronic Theses, Dissertations & Projects

Estrogen receptor positive (ER+) breast cancer tends to respond to anti-estrogen agents such as Tamoxifen. Approximately 40% of ER+ breast cancer is resistant to these agents and those that initially respond often acquire resistance. Estrogen receptor negative (ER-) breast cancer remains largely unresponsive to these agents. It is therefore vital to discover drugs that are potent in both forms of breast cancer. Aminoflavone, (5-amino-2, 3-fluorophenyl)-6,8-difluoro-7-methyl-4H-l-benzopyran-4-one; AF; NSC 686288) and 5F203, (2-[-Amino-3-methy phenyl]-5-flurobenzothiazole) are novel anticancer candidate agents that display potent in vitro and in vivo anti-proliferative activity against select human tumor cells with a unique anticancer activity profile in the …

Experimental Investigation Of The Fluid Velocity Distribution In Stirred Tank Reactors Equipped With Retreat-Blade Impellers Using Laser Doppler Velocimetry, Deepak Rajesh Madhrani

Theses

Stirred tank reactors are commonly used in the pharmaceutical industry for synthesis of Active Pharmaceutical Ingredients (API's) and their intermediates. Typically, these vessels are glass-lined and are provided with a single retreat-blade glass-lined impeller and a single baffle. Despite their ubiquitous utilization in the pharmaceutical industry for at least the past 40 years, the mixing characteristics of these systems have not been studied to any great extent, making it difficult to predict mixing performance in any given operation.

In this work, the velocity distribution inside the typical glass-lined vessel/impeller system was experimentally quantified using Laser Doppler Velocimetry (LDV), which is …

Design, Synthesis, And Evaluation Of Small Molecules In The Discovery Of Novel Antimicrobial Agents, Kimberly D. Grimes

Theses and Dissertations (ETD)

The increasing prevalence of antibiotic-resistant bacteria, including Mycobacterium tuberculosis, Streptococcus pneumoniae, Staphylococcus aureus, and Enterococcus faecalis, pushes us to discover new antibacterial agents to maintain adequate patient coverage. This body of work highlights the use of medicinal chemistry methodologies that encompass cross-disciplinary fields of study. Chapter 1 gives an introduction to the antibacterial drug targets, resistance, and how scientists are working to overcome obstacles encountered with drug-resistant bacteria. It also details modern medicinal chemistry applications in antimicrobial drug discovery. Chapter 2 details the use of a structure-guided library approach to drug design, in which large virtual libraries against the target …

Flavonoids And Related Compounds As Nucleoside Transporter Inhibitors, Surekha Ravaji Pimple

Theses and Dissertations (ETD)

Mammalian nucleoside transporters can be classified into two main categories, namely, equilibrative nucleoside transporters (ENTs) and concentrative nucleoside transporters (CNTs). ENTs are ubiquitous, and mediate sodium-independent bi-directional facilitated diffusion nucleoside transport processes. CNTs on the other hand, are secondary active unidirectional transporters that are sodium-dependent. Both the equilibrative and the concentrative nucleoside transporters have several family members which are ENT1 to ENT4 and CNT1 to CNT6. Over the past two decades, important advances in the understanding of nucleoside transporter functions have been made. Identification and molecular cloning of the ENT and CNT families from mammals and protozoan parasites have provided …

Application Of Prodrugs To Inflammatory Diseases Of The Gut, Helieh S. Oz, Jeffrey L. Ebersole

Center for Oral Health Research Faculty Publications

Oral delivery is the most common and preferred route of drug administration although the digestive tract exhibits several obstacles to drug delivery including motility and intraluminal pH profiles. The gut milieu represents the largest mucosal surface exposed to microorganisms with 10^10-12 colony forming bacteria/g of colonic content. Approximately, one third of fecal dry matter is made of bacteria/ bacterial components. Indeed, the normal gut microbiota is responsible for healthy digestion of dietary fibers (polysaccharides) and fermentation of short chain fatty acids such as acetate and butyrate that provide carbon sources (fuel) for these bacteria. Inflammatory bowel disease (IBD) results …

Ultra-Fine Particle Formation Using Principle Of Rapid Expansion Of Supercritical Solutions`, Miraj Minesh Sheth

Theses

There are indications in the chemical and pharmaceutical industries that the reduction in size of a crystalline particle can lead to better performance of the drug compound, particularly for water insoluble drugs, in the final dosage form. Many particle formation techniques have been investigated in recent years by researchers to obtain desired particulate sizes and size distributions. Supercritical fluid technologies have been successfully investigated for particle formation due to its unique gas/liquid properties in the supereritical state. In this report, results of particle formation using the principles of Rapid Expansion of Supercritical Solutions (RESS) have been documented.

In the RESS …

Development And Evaluation Of Brain Tumor Targeted Liposome Delivery System For Paclitaxel, Murali Krishna Divi

Theses and Dissertations (ETD)

Primary brain tumors are a relatively common cause of cancer-related deaths. High-grade gliomas are the most common type of primary brain cancer, and the affected patients have a median survival of less than 1 year. Almost all malignant gliomas are incurable with the present standards of healthcare. Currently accepted therapeutic adjuvants to surgery, such as radiotherapy and chemotherapy, provide only a minor improvement in the disease course and life expectancy for patients diagnosed with malignant gliomas. Often, chemotherapy has failed to make any significant impact on the prognosis of disease because of significant local and systemic toxicity, problems with transport …

The Role Of Multi-Drug Resistance Associated Protein 4 And P-Glycoprotein In Resistance Of Neuroblastoma To Topotecan And Irinotecan, Patricia Kellie Turner

Theses and Dissertations (ETD)

High-risk neuroblastoma presents a significant therapeutic challenge because the 5-year survival rate remains less than 30% despite the use of surgery, multi-agent chemotherapy, radiation, and autologous bone marrow transplant. Novel therapeutic modalities are under development. The camptothecin analogs topotecan and irinotecan have been identified as successful cytotoxic agents. For topotecan, pharmacokinetically guided dosing to achieve a systemic exposure associated with preclinical anti-tumor activity in neuroblastoma xenograft models is feasible and has elicited favorable responses in children with high-risk neuroblastoma. However, some children with high-risk disease did not respond to the putatively effective topotecan systemic exposure. These children represent a subset …

Synthesis Of Novel Sulfonamide-Based Calpain Inhibitors And Their Potential As Anti-Tumor Agents, Jin Xu

Theses and Dissertations (ETD)

Calpain is a class of intracellular cytoplasmic cysteine proteases.1 The enzyme participates in different intracellular signaling pathways that are mediated by Ca2+.2 The two major isoforms of calpain universally distributed in most mammalian tissues are calpain 1 (µ-calpain) and calpain 2 (m-calpain). The exact in vivo function of the enzyme is not clear, but calpain has been implicated in a variety of physiological and pathological conditions,3 such as cancer, stroke, cardiac ischaemia, muscular dystrophy, cataract and Alzheimer’s disease. Calpain inhibitors are therefore of interest as therapeutic agents and as biomedical tools.

Several potent calpain inhibitors isolated from natural sources as …