Pharmacology Commons^™

Simultaneous Spectrophotometric Determination Of Difloxacin And Enrofloxacin In Urine Samples By Partial Least Squares Regression (Pls) And Direct Orthogonal Signal Correction-Partial Least Squares Regression (Disc-Ols) Methods, Kuldeep Kaur, Ashok Kumar Malik, Baldev Singh, M. Godarzi

The Thai Journal of Pharmaceutical Sciences

Simultaneous determination of difloxacin and enrofloxacin using two chemometric methods, partial least squares regression (PLS) and direct orthogonal signal correction-partial least squares regression (DOSC-PLS) is described in this paper. The simultaneous determination of these drugs is difficult due to spectral interferences. The calibration graphs were linear in the range of 1-10 μg mL-1 and 1-9 μg mL-1 with detection limits of 0.52 and 0.15 μg mL-1 for difloxacin and enrofloxacin, respectively. The experimental calibration matrix was designed with 25 mixtures of these drugs. The PLS and DOSC-PLS were used for multivariate calibration of spectrophotometric data. The root mean square error …

Facile Derivative Uv Spectroscopy Method: Simultaneous Estimation Of Tinidazole And Fluconazole In Combined Tablet Dosage Form, Saurabh Pandey, Preeti Pandey, Shaifali Dubey, Udisha Chaturvedi, Awani K. Rai

The Thai Journal of Pharmaceutical Sciences

Two derivative spectrophotometric methods have been developed for simultaneous determination of tinidazole and fluconazole in pharmaceutical formulations. The first method depends on utilization of first derivative UV spectrophotometry, with zero-crossing and peak-to-base measurement at 260.57 & 264.23 nm for fluconazole and 263.86 & 318.85 nm for tinidazole. The second method, compensation technique depends on first derivative of the ratio-spectra by measurements of the amplitudes for tinidazole and fluconazole. Calibration graphs were established for tinidazole and fluconazole in the range of 10-100 μg ml-1 and 2-20 μg ml-1, respectively. All proposed methods have been extensively validated. The results were found to …

Simultaneous Estimation Of Cefixime And Cloxacillin In Human Plasma By Reversed Phase-Hplc With Uv Detection, Sommath D. Bhinge, Sharangouda M. Malipatil, Lalit V. Sonawane

The Thai Journal of Pharmaceutical Sciences

An accurate, rapid and simple reversed-phase high performance liquid chromatography (RP-HPLC) method was developed and validated for simultaneous estimation of cefixime, cloxacillin and for chloramphenicol (internal standard) in human plasma. Chromatographic separation was accomplished using CAPCELL PAK C8 (4.6 mm Ó 250 mm, 5 μm) analytical column using phosphate buffer, methanol and acetonitrile (40:45:15) as eluent. Detection and quantification were performed by UV/Vis detection at 225 nm. The lower limit of detection and quantification were 0.01 μg†mL-1 and 0.25 μg†mL-1 for cefixime, 0.03 μg†mL-1 and 0.39 μg†mL-1 for cloxacillin. The calibration curves were linear over the concentration range 0.5 to …

Thrombolytic Activity Of Some Spices And Plants Available In Bangladesh, Md. Rakib Ai-Manun, Nabiha Amrin, Jahura Begum, Md. Abdul Mazid

The Thai Journal of Pharmaceutical Sciences

Thrombolytic activities of some plants, namely Tamarindus indica (Fabaceae), Flemingia congesta (Fabaceae), Lawsonia inermis (Lythraceae), Mesua nagassarium (Clusiaceae, and spices, namely Coriandrum sativum (Apiaceae), Curcuma longa (Zingiberaceae), Cinnamomum tamala (Lauraceae), Nigella sativa (Ranunculaceae), Eugenia aromaticum (Myrtaceae), available in Bangladesh, were evaluated using an in vitro model. The thrombolytic activity in terms of percentage of weight loss of in vitro formed clots were found as C. sativum 43.25 ± 7.18%, C. longa 53.32 ± 4.96%, C. tamala 22.10 ± 3.18%, N. sativa 28.49 ± 3.72%, E. aromaticum 32.18 ± 3.10%, T. indica 28.91 ± 2.29%, F. congesta 35.27 ± 7.35%, L. …

Lactobacillus Plantarum T23/3 As A Potential Probiotic Strain Isolated From Faces, Titpawan Nakpheng, Rosainee Kha, Neelam Balekar, Sanae Kaewnopparat, Teerapol Srichana

The Thai Journal of Pharmaceutical Sciences

The present study was undertaken to evaluate the properties of Lactobacillus plantarum T23/3 isolated from the feces of healthy elderly volunteer. The L. plantarum T23/3 showed better tolerance property to bile acid, simulated gastric fluid (SGF) and simulated intestinal fluid (SIF), and exhibited antimicrobial activity against tested enteropathogens. It formed macroscopic granules with surface hydrophobicity and co-aggregated with tested microbial strain. It was resistant to some antibiotics used for treatment of diarrhea so there is possibility to co-administer L. plantarum as probiotic with antidiarrheal therapy. Furthermore, adhesion and significant potential for decreasing adhesion of pathogens (E. coli 2601 and V. …

Application Of A Stability-Indicating Hptlc Method For Simultaneous Determination Of Chloramphenicol And Dexamethasone Sodium Phosphate In Eye Drop, Yimer Seid, Araya Hymete, Adnan A. Bekhit

The Thai Journal of Pharmaceutical Sciences

A high performance thin layer chromatography (HPTLC) method was developed and validated for the simultaneous quantification of dexamethasone sodium phosphate and chloramphenicol in eye drop. The HPTLC separation was achieved on an aluminum-backed layer of silica gel 60F254 using acetonitrile: water: ammonia (10:3:0.5 v/v/v), pH adjusted to 7.8 with 1M HCl, as a mobile phase. The densitometric determination of dexamethasone phosphate and chloramphenicol was carried out at 262 nm. Calibration curves for dexamethasone phosphate and chloramphenicol were linear in the range of 80-300 ng and 400-1400 ng, respectively. The method was validated according to International Conference on Harmonization (ICH) guidelines …

Enhancement Of Wttability And In Vitro Dissoution Properties Of Lercanidipine Hydrochloride By Solid Dispersion Technique, Suneel Pandey, Ekunkumar Chandekar, Amarnath Wattamwar, Sachin Pandit, Hemant Joshee, Arun Patil

The Thai Journal of Pharmaceutical Sciences

The aim of the present study was to improve lercanidipine HCl solubility and in vitro dissolution rate by preparing solid dispersion with polyethylene glycol (PEG) 6000 using the solvent evaporation technique. Solid dispersions with PEG 6000 (as carriers) were prepared in drug: carrier (1:1, 1:5 and 1:10) ratios along with the corresponding physical mixtures. Analytical techniques, FT-IR spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were used to characterize the drug in the physical mixtures and solid dispersions. The solubility and wettability studies of solid dispersions as well as physical mixtures showed greater improvement compared to the pure drug. …

Compositional Determinants Of The Pharmacological Actions Of Heparins, Angel Lee Gray-Shah

Dissertations

This dissertation primarily focuses on how differences in molecular weight (MW) and structural composition affect the pharmacological activity of heparin and its derivatives. Heparins are a mixture of glycosaminoglycans chains which are used to prevent thrombosis in a number of clinical indications. Heparins promote the inhibition of blood coagulation via their plasmatic cofactors antithrombin (AT) and heparin cofactor II (HCII).

In these studies, various heparins with molecular weights ranging from 2.6 to 16.5 kDa were investigated. Not only the molecular weight but also the oligosaccharide composition greatly varied in these agents. One of the major objectives of this research was …

Mutation In The Plasmodium Falciparum Crt Protein Determines The Stereospecific Activity Of Antimalarial Cinchona Alkaloids, Carol E. Griffin, Jonathan M. Hoke, Upeka Samarakoon, Junhui Duan, Jianbing Mu, Michael T. Ferdig, David C. Warhurst, Roland A. Cooper

Biological Sciences Faculty Publications

The Cinchona alkaloids are quinoline aminoalcohols that occur as diastereomer pairs, typified by (-)-quinine and (+)-quinidine. The potency of (+)-isomers is greater than the (-)-isomers in vitro and in vivo against Plasmodium falciparum malaria parasites. They may act by the inhibition of heme crystallization within the parasite digestive vacuole in a manner similar to chloroquine. Earlier studies showed that a K76I mutation in the digestive vacuole-associated protein, PfCRT (P. falciparum chloroquine resistance transporter), reversed the normal potency order of quinine and quinidine toward P. falciparum. To further explore PfCRT-alkaloid interactions in the malaria parasite, we measured the in …

Maternal Immune Dysregulation In The Pathogenesis Of Neurodevelopmental Disorders: Interleukin-6 As A Central Mechanism And Therapeutic Target Of Flavonoids, Ellisa Carla Parker-Athill

USF Tampa Graduate Theses and Dissertations

Activation of the maternal immune system and resultant maternal cytokine expression due to prenatal infection has been implicated as a significant contributor to the pathology of neuropsychiatric and neurodevelopmental disorders such as schizophrenia and Autism Spectrum Disorder (ASD). Increased maternal interleukin-6 (IL-6) expression, observed clinically and in animal models of prenatal infection, and resultant activation of key signaling pathways, has been shown to be a biological indicator of pathology, and a central component of the pathological mechanism. In animal models of prenatal infection and clinically in pregnancy disorders hallmarked by immunological irregularities and increased IL-6 expression, inhibition of IL-6 has …

Modulating The Pharmacokinetics Of Bioflavonoids, Adam John Smith

USF Tampa Graduate Theses and Dissertations

One of the largest obstacles in drug development is to overcome solubility and bioavailability problems. Preformulation strategies such as nanoparticle formation are often employed but sometimes create new issues and are limited in their effectiveness and applications. Since the majority of drugs are marketed and sold as solid forms, drug delivery systems are not always desirable. This is where solid-state chemistry becomes important. Traditional solid-state chemistry approaches are often successful but are sometimes too restrictive and cannot be applied to certain compounds. Cocrystals have emerged as an alternative solid-state technique that can be applied to a broad range of compounds. …

Targeting Α4 Integrin Containing Complexes In Multiple Myeloma Using Peptidomimetics, Michael Foster Emmons

USF Tampa Graduate Theses and Dissertations

In our previous work we demonstrated that the integrin antagonist, HYD1, induced necrotic cell death in myeloma cell lines in vitro and in vivo as a single agent. In order to further delineate biomarkers of response to HYD1 we developed an isogenic drug resistant variant named H929-60. We show that the acquisition of resistance towards HYD1 correlates with reduced expression of the cleaved α4 integrin subunit and beta 1 integrin. Moreover, we demonstrate that HYD1 interacts with α4 integrin in myeloma cells. Consistent with reduced VLA-4 expression, the resistant variant showed ablated functional binding to fibronectin, VCAM-1 and the bone …

Use And Development Of Computational Tools In Drug Discovery: From Small Molecules To Cyclic Peptides, Daniel Navarrete Santiago

USF Tampa Graduate Theses and Dissertations

The scope of this work focuses on computationally modeling compounds with protein structures. While the impetus of drug discovery is the innovation of new therapeutic molecules, it also involves distinguishing molecules that would not be an effective drug. This can be achieved by inventing new tools or by refining old tools. Virtual screening (VS, also called docking), the computational modeling of a molecule in a receptor structure, is a staple in predicting a molecule's affinity for an intended target. In our Virtual Target Screening system (also called inverse-docking), VS is used to find high-affinity targets, which can potentially explain absorption, …

The Proton-Coupled Folate Transporter: Biology And Therapeutic Applications To Cancer, Sita Desmoulin

Wayne State University Dissertations

Folates are essential cofactors of tumor cell proliferation and survival required for nucleotide biosynthesis and amino acid metabolism. In cancer therapy, inhibition of folate-dependent metabolic pathways has been achieved through the use of antifolates. Unfortunately, the efficacy of many clinically approved antifolates is limited by a lack of tumor selectivity. Facilitative transport of folates into mammalian cells is achieved by the reduced folate carrier (RFC) and proton-coupled folate transporter (PCFT). As PCFT is a folate-proton symporter with an acidic pH optimum, PCFT may provide a mechanism for targeting cytotoxic antifolates to tumors, based on their acidic microenvironments. To establish the …

Classification Of Plants According To Their Heavy Metal Content Around North Mara Gold Mine, Tanzania: Implication For Phytoremediation, N. Mganga, Mlk Manoko, Z. K. Rulangaranga

Tanzania Journal of Science

Plants like other living organisms respond differently under different environmental conditions. An elevated level of heavy metals is one of the stresses which results into three classes of plants depending on their heavy metal content. The classes of plant species according to their accumulated heavy metals around North Mara Gold Mine were not known. To study such classes, a line transect of 700m long was established opposite the gold mine wastes. A total of eight sampling points were systematically established each after every 100m in that transect. Fifteen plant species were sampled; at least one species per sampling point. Approximately …

Modelling Β2ar Regulation, Sharat J. Vayttaden

Dissertations and Theses (Open Access)

The β2 adrenergic receptor (β2AR) regulates smooth muscle relaxation in the vasculature and airways. Long- and Short-acting β-agonists (LABAs/SABAs) are widely used in treatment of chronic obstructive pulmonary disorder (COPD) and asthma. Despite their widespread clinical use we do not understand well the dominant β2AR regulatory pathways that are stimulated during therapy and bring about tachyphylaxis, which is the loss of drug effects. Thus, an understanding of how the β2AR responds to various β-agonists is crucial to their rational use. Towards that end we have developed deterministic models that explore the mechanism of drug- induced β2AR regulation. These mathematical models …

Store-Operated Calcium Channels In The Function Of Intracardiac Neurons, Timetria Bonds

USF Tampa Graduate Theses and Dissertations

Proper autonomic regulation of mammalian cardiac function is dependent upon very complex and precise communication among the intracardiac ganglia and individual neurons within the ganglia. An array of neuromodulators is found within the ganglia that direct neuronal activity by modulating the movement of calcium. The current study determines that opioidergic agonists, which have been found to contribute to severe cardiac disease states and intracellular calcium mobilization, are also responsible for changes in the function of the intracardiac neuron via their effects on store-operated calcium channels (SOCs).

Previous studies suggest that phosphorylation plays a role in SOC regulation. Using Fura-2 calcium …

Minimal Structural Requirements Of Alkyl Γ-Lactones Capable Of Antagonizing The Cocaine-Induced Motility Decrease In Planarians, Debra Baker, Sean Deats, Peter Boor, James Pruitt, Oné R. Pagán

Biology Faculty Publications

We recently reported that the natural cyclic lactone, parthenolide, and related analogs prevent the expression of behavioral effects induced by cocaine in planarians and that parthenolide’s γ-lactone ring is required for this effect. In the present work, we tested a series of alkyl γ-lactones with varying chain length (1–8 carbons) to determine their ability to antagonize the planarian motility decrease induced by 200 μM cocaine. Alkyl lactones with up to a 4-carbon alkyl chain did not affect planarian motility or antagonized the cocaine-induced motility decrease; only the compound γ-nonalactone (a γ-lactone with a 5-carbon chain) was able to prevent the …

Physiologically-Based Pharmacokinetic Modeling For Predicting Drug-Drug Interactions, David M. Ng, Ali Navid

STAR Program Research Presentations

Dynamics of interactions between the drugs caffeine and ciprofloxacin are predicted using physiologically-based pharmacokinetic (PBPK) modeling. Pharmacokinetic means the model determines where the drugs are distributed in the body over time. Physiologically-based means the anatomy and physiology of the human body is reflected in the structure and functioning of the model. Multiple drugs can interact to increase or decrease their beneficial and/or undesired effects. This is important because some common substances, such as caffeine in coffee and soft drinks, are actually drugs that affect the body. By implementing the model as a computer program, it is relatively straightforward to perform …

Role Of Dopamine In Impulse Control, Paul Rafael Sabandal ^, Young-Cho Kim, Kyung-An Han *

COURI Symposium Abstracts, Summer 2011

No abstract provided.