Pharmaceutics and Drug Design Commons^™

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 …

Assessment Of A Marine Polysaccharide For Use As Excipient In Pharmaceutical Hot-Melt Extrusion, Qing Ye

Theses

Pharmaceutical Hot Melt Extrusion (HME) is currently investigated by both industry and academia as a method for manufacturing solid oral dosages with improved bioavailability of poorly-water soluble active pharmaceutical ingredients (APIs) and control drug release of water-soluble APIs. Although HME is traditionally utilizing synthetic polymers to produce such dosages, biopolymers constantly gain ground by virtue of renewability, biocompatibility and in some cases biodegradability. In this work, the possibility of using Keltone, a marine polysaccharide derived from brown seaweed, as a polymeric excipient for pharmaceutical HME is explored. Keltone is insoluble in acidic pH and soluble in basic pH, therefore making …

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 …

Experimental Determination Of The Mixing Requirements For Solid Suspension In Pharmaceutical Stirred Tank Reactors, Anqi Zhou

Theses

Glass and glass-lined, stirred-tank reactors are of significant importance in the pharmaceutical and related industries. Because of fabrication issues, a retreat blade impeller (RBI) with a low impeller clearance off the tank bottom is commonly used in glass-lined reactors, typically combined with a single baffle (providing only partial baffling conditions) mounted from the top of the reactor. In addition, these reactors are often provided with a torispherical bottom. Other configurations are also used, including full baffling or no baffles at all, hemispherical bottoms, and different impeller types. Despite their common use, some of the most important mixing characteristics of this …

Dispersion And Dissolution Kinetics Of Api Particles In Pharmaceutical Hot Melt Extrusion, Wang Zhan

Theses

Pharmaceutical Hot Melt Extrusion (HME) is essentially a special case of polymer compounding. The elementary steps involved in traditional plastics melt processing are handling of particulates, melting, dispersive and distributive mixing, devolatilization and stripping, and finally pressurization and pumping. However, for pharmaceutical HME, the dissolution of the API (Active Pharmaceutical Ingredient) is an additional and very important elementary step, along with the melting of the polymeric excipient that precedes it, and mixing which accelerates the dissolution process. A major concern in pharmaceutical HME is the thermal degradation of the API. To avoid overexposure of API to heat while ensuring complete …

Design, Synthesis And Biological Evaluation Of Novel Compounds With Cns-Activity Targeting Cannabinoid And Biogenic Amine Receptors, Alexander M. Sherwood

LSU New Orleans Theses and Dissertations

This work seeks to contribute to the discipline of neuropharmacology by way of structure activity relationship from the standpoint of an organic chemist. More specifically, we sought to develop robust synthetic methodology able to efficiently produce an array of compounds for the purpose of systematic evaluation of their interaction with specific sights within the central nervous system (CNS) in order to better understand the mind and to develop drugs that may have beneficial effects on neurological function.

The focus of these studies has been toward the development of novel molecules, using a structure-activity relationship approach, that exhibit binding affinity at …

Nanotoxicity In Cells Of The Immune System, Jonathan J. Pelc

Science Scholars

Nanoparticles (NPs) provide a new medical approach to drug therapy. As with every new approach, safety precautions need to be taken, and the immediate and long-term effects for many NPs are still unclear. When administering a medical treatment into the human body, the first issue that needs to be addressed is host detection of the medicine and inflammation as a possible result of the treatment. If a new NP treatment causes inflammation before it releases its medicine, that treatment may be ineffective, even damaging to the patient. Small metallic and organic particles have been shown to elicit an inflammatory responses …

Glioma: A Tale Of Corticosteroids, Thiopurines And Proposed Novel Antiglioma Small Molecules, Amira Ahmed

Theses and Dissertations (ETD)

Glioma is a brain tumor that arises from glial cells or glial progenitor cells, and represents 80% of malignant brain tumor incidence in the United States. Glioblastoma multiforme (GBM) is the most aggressive primary brain tumor malignancy with fewer than 8% of patients with GBM surviving for 3 years. Over the past 10 years, despite improvement in diagnosis and therapies for cancer, the survival rate for high-grade glioma patients remains unchanged. The main focus of this dissertation is to investigate two therapeutic agents that are related to increase tumor resistance or increase secondary tumor incidence, which might play a role …

Development Of A Novel Vaccine Adjuvant System Utilizing An In Situ Implant System To Modified Release, Qiuye Zhang

Theses and Dissertations (ETD)

Pulsatile release formulations for single dose vaccines have been studied for many years because of the advantages that they may provide to vaccine administration with a single dose instead of prime and booster shots.

The aim of this work is to develop novel formulations based on an In Situ Implant (ISI) systems to provide a modified vaccine release and altered immune response, which could act as a booster administration. This type of system was selected because ISI systems are used for long acting administration of various drugs and ease of administration. A typical ISI system is comprised of hydrophilic organic …

Uji Aktivitas Antibakteri 1-[(Kuinazolin-4-On-2-Il)Metil]Piridin-1-Ium Bromida Dan 2-Bromometilkuinazolin-4-On, Hayun Hayun, Arif Arrahman, Herman Suryadi, Arry Yanuar

Pharmaceutical Sciences and Research

Antibacterial activity tests of quinazolin-4-one derivates: 1-[(6-nitroquinazolin-4one-2-yl)methyl]piridin-1-ium bromide (1), 1-[(6-aminoquinazolin-4-on-2-yl)methyl] piridin-1-um bromide (2), 2-bromomethylquinazolin-4-one (3) and 2-bromomethyl-6nitroquinazolin-4-one(4) with trimethoprim (5) as a positive standard were conducted. The antibacterial activity tests were carried out using disc diffusion method againts E.coli, S.aureus and S.thyposa, and determination of minimum inhibitory concentration (MIC). The results showed that compounds 1 and 2 are inactive as antibacterial, whereas compounds 3 and 4 are active.The activities to E.coli were ¼ times the activity of trimethoprim (MIC : 5 x 102 µg/ml compared to 1.25 x 102 µg/ml ). The activity to S. typhosa were ½-1 times the …

Uji Toksisitas Fraksi Air Impatiens Balsamina Pada Tikus Betina Galur Sprague Dawley, Entang Nurqolbiah, Indri Kusharyanti, Siti Nani Nurbaeti

Pharmaceutical Sciences and Research

The present study was aimed to predict the level of toxicity of aqueous fraction of Impatiens balsamina by acute toxicity study using OECD guideline 425. Female Sprague Dawley 8-12 week and weight between 140-170 gram were used, the amount of experimental rats were 10 rats. Rats were sequentially administered all the fraction in single dosage (limit test) of 2000 mg/kg body weight and 5000 mg/kg of body weight. All the animals were individually studied for mortality, wellness parameters, food consumption,water consumption, body weight. Histopathological examination was done on the liver and kidney. The result of this study showed that no …

Pengaruh Natrium Hialuronat Terhadap Penetrasi Kofein Sebagai Antiselulit Dalam Sediaan Hidrogel, Hidroalkoholik Gel, Dan Emulsi Gel, Joshita Djajadisastra, Zuraida Syafara Dzuhro, Sutriyo Sutriyo

Pharmaceutical Sciences and Research

Anticellulite topical gel preparation with caffeine as active ingredient needs a penetration enhancer to reach subcutaneous layer. Sodium hyaluronate (NaHA), the sodium salt of hyaluronic acid, is a hydrophilic polysaccharide derivative polymer. It has ability to enhance percutaneous penetration by loosening the dense of the compact substance stratum corneum. The aim of this research was to observe the effects of NaHA on caffeine penetration as anticellulite active agent in three types of gel preparation: hydrogel, hydroalcoholic gel, and gel emulsion. Each gel type contained caffeine 1,5% and was varied into three formulas. Formula 1 contained HPMC 2% as gel basis; …

Respon Bioakumulator Eceng Gondok (Eichhornia Crassipes) Terhadap Logam Berat Pb Dan Cd Di Sungai Pegangsaan Dua, Sri Teguh Rahayu, Meutia Faradilla, Ester Yani Verawati, Muchrip Triana

Pharmaceutical Sciences and Research

Eichhornia crassipes is one of Indonesia’s wild plant that considered as weed. Its presence can disrupt ecosystems in the river. However, it is proven to absorb Pb and Fe. It is also believed that E.crassipes can absorb other metals such as Hg , Zn , Cu and Cd which were belong to the same group as Pb and Fe. In addition to heavy metal sequestration, Eichhornia crassipes can also absorb pesticide residues. This descriptive research was done to determine the bioaccumulator response to Pb and Cd in Pegangsaan Dua river using Inductively Coupled Plasma method. Bioaccumulator response of Eichhornia crassipes …

Formulasi Gel Pacar Air (Impatiens Balsamina Linn.) Terhadap Propionibacterium Acnes Dan Staphylococcus Epidermidis, Diah Ismarani, Liza Pratiwi, Indri Kusharyanti

Pharmaceutical Sciences and Research

Acnes vulgaris is a chronic inflammatory disease of sebaceous follicles caused by Propionibacterium acnes and Staphylococcus epidermidis. The antibacterial activity of Impatiens balsamina L. has been studied for many years. The aims of this study are to find out the antiacne effect from methanolic extract of stems and leaves of Impatiens balsamina L. that formulated in gel. Simplicia were extracted using soxhlet technique bu using methanol as solvent. Extracts were then formulated in gel in three variations of HPMC 4000 and Carbopol 934 as gel base with ratio of 70:30 (F1), 50:50 (F2) and 30:70 (F3). The determination of antiacne …

An Introduction To Drugs And The Neuroscience Of Behavior, Adam J. Prus

Books

This up-to-date text provides an introductory overview of the nervous system actions and behavioral effects of the major classes of psychoactive drugs, using pedagogy unique among pharmacology texts to make the topic approachable.

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

Scholarship and Professional Work – COPHS

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 …

Cinacalcet Administration By Gastrostomy Tube In A Child Receiving Peritoneal Dialysis, Kristen R. Nichols, Chad A. Knoderer, Bethanne Johnston, Amy C. Wilson

Scholarship and Professional Work – COPHS

A 2-year-old male with chronic kidney disease with secondary hyperparathyroidism developed hypercalcemia while receiving calcitriol, without achieving a serum parathyroid hormone concentration within the goal range. Cinacalcet 15 mg (1.2 mg/kg), crushed and administered via gastrostomy tube, was added to the patient’s therapy. This therapy was effective in achieving targeted laboratory parameters in our patient despite instructions in the prescribing information that cinacalcet should always be taken whole.

Electrostatic Charge Effects On Pharmaceutical Aerosol Deposition In Human Nasal-Laryngeal Airways, Jinxiang Xi, Xiuhua Si, Worth Longest

University Faculty Publications and Creative Works

Electrostatic charging occurs in most aerosol generation processes and can significantly influence subsequent particle deposition rates and patterns in the respiratory tract through the image and space forces. The behavior of inhaled aerosols with charge is expected to be most affected in the upper airways, where particles come in close proximity to the narrow turbinate surface, and before charge dissipation occurs as a result of high humidity. The objective of this study was to quantitatively evaluate the deposition of charged aerosols in an MRI-based nasal-laryngeal airway model. Particle sizes of 5 nm-30 μm and charge levels ranging from neutralized to …

Facile, Regio-And Diastereoselective Synthesis Of Spiro-Pyrrolidine And Pyrrolizine Derivatives And Evaluation Of Their Antiproliferative Activities, Abdulrahman I. Almansour, Raju Suresh Kumar, Farzana Beevi, Amir Nasrolahi Shirazi, Hasnah Osman, Rusli Ismail, Tan Soo Chen, Brian Sullivan, Kellen Mccaffrey, Alaa Nahhas, Keykavous Parang, Mohamed Ashraf Ali

Pharmacy Faculty Articles and Research

A number of novel spiro-pyrrolidines/pyrrolizines derivatives were synthesized through [3+2]-cycloaddition of azomethine ylides with 3,5-bis[(E)-arylmethylidene] tetrahydro-4(1H)-pyridinones 2a-n. Azomethine ylides were generated in situ from the reaction of 1H-indole-2,3-dione (isatin, 3) with N-methylglycine (sarcosine), phenylglycine, or proline. All compounds (50 M) were evaluated for their antiproliferative activity against human breast carcinoma (MDA-MB-231), leukemia lymphoblastic (CCRF-CEM), and ovarian carcinoma (SK-OV-3) cells. N-alpha-Phenyl substituted spiro-pyrrolidine derivatives (5a-n) showed higher antiproliferative activity in MDA-MB-231 than other cancer cell lines. Among spiro-pyrrolizines 6a-n, a number of derivatives including 6a-c and 6i-m showed a comparable activity with doxorubicin in all three cell lines. Among all compounds …

Effects Of Hepatic Ischemia-Reperfusion Injury On The P-Glycoprotein Activity At The Liver Canalicular Membrane And Blood-Brain Barrier Determined By In Vivo Administration Of Rhodamine 123 In Rats, M. K. Miah, Imam H. Shaik, Ulrich Bickel, Reza Mehvar

Pharmacy Faculty Articles and Research

Purpose To investigate the effects of normothermic hepatic ischemia-reperfusion (IR) injury on the activity of P-glycoprotein (P-gp) in the liver and at the blood-brain barrier (BBB) of rats using rhodamine 123 (RH-123) as an in vivo marker.

Methods Rats were subjected to 90 min of partial ischemia or sham surgery, followed by 12 or 24 h of reperfusion. Following intravenous injection, the concentrations of RH-123 in blood, bile, brain, and liver were used for pharmacokinetic calculations. The protein levels of P-gp and some other transporters in the liver and brain were also determined by Western blot analysis.

Results P-gp protein …