Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 58 for “"Oral Bioavailability"”.
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Transporter-Targeted Prodrug Delivery to Improve Oral Bioavailability of Saquinavir
… and fast biotransformation lead to its poor oral bioavailability and limited therapeutic efficacy. The objective of this dissertation project is to investigate whether stereoisomerized peptide prodrugs targeting influx transporter system could improve intestinal absorption and oral …
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Improving Potency and Oral Bioavailability of Spinster Homolog 2 (Spns2) Inhibitor: A Structure-Activity Relationship Study
In healthy individuals, the autoimmune system is the body's natural defense against foreign materials and organisms. The main tools utilized for this defense mechanism are immune cells. However, in patients suffering from autoimmune diseases, the autoimmune system is overactive resulting in its …
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The Comparison of Rat and Human Intestinal and Hepatic Glucuronidation of Enterolactone Derived from Flaxseed Lignans
… disease, and inflammation. However, EL’s oral bioavailability is low and highly variable due to extensive first-pass metabolism, especially glucuronidation, which results in the large amount of glucuronide metabolites but low levels of free EL in human plasma. Hepatocytes and enterocytes …
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ASSESSMENT OF THE FEASIBILITY OF CO-ADMINISTRATION OF PHENOLIC DIETARY COMPOUNDS WITH PHENYLEPHRINE TO INCREASE ITS BIOAVAILABILITY
… (PE) is the most commonly used nonprescription oral nasal decongestant in the United States. It is a selective α1-adrenergic receptor agonist and has many years of safe usage. However, the efficacy of PE is controversial, due to its extensive pre-systemic metabolism, which leads to low and …
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A Pharmacokinetics and Pharmacodynamics (PK/PD) Guided Approach to Lead Optimization of Nitrofuranylamide Anti-Tuberculosis Agents
… clearance, short terminal half-life, and low oral bioavailability of 15.9%. These observations were further supported by the poor metabolic stability of Lee 562. Thus, two second generation follow-up compounds, Lee 878 and Lee 952 were tested that included structural modifications for …
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Exploring the utility of the pig model for predicting bioavailability in humans
… animal model is most appropriate for assessing oral bioavailability in humans. In order to streamline preclinical development, and reduce repeated testing in various animal models, it is necessary to get a better understanding which particular animal model is suitable for a specific drug …
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EVASION OF EFFLUX AND ENHANCING BIOAVAILABILITY OF AMPRENAVIR BY PRODRUG DERIVATIZATION
… substrates of efflux proteins which limit their oral bioavailability and brain permeation. Various approaches have been employed to evade the efflux and improve the bioavailability, however improving brain absorption still remains as an elusive goal. The overall objective of this dissertation …
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IN-VITRO METABOLISM AND PROTEIN BINDING OF 5-HMF, A POTENTIAL ANTISICKLING AGENT
… is expected to have low hepatic extraction, high oral bioavailability, and first-order PK for relevant blood concentrations. The IVIVE-predicted in-vivo half-lives for 5-HMF were adequate for the mouse and dog but overestimated for humans. In RBCs, 5-HMF had Clintin-vitro of 0.34(± 0.02) ml/min/ml …
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PHARMACOKINETICS AND ORAL DELIVERY OF POLYMETHOXYLATED FLAVONES
… has been identified a major barrier to their oral bioavailability. Subsequently, self-microemulsifying drug delivery system (SMEDDS) was developed and characterized. In vivo evaluation found that the oral delivery of ATE and LTE was substantially enhanced by SMEDDS. Moreover, abundant tissue …
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Physicochemical Characterization of Creatine
… made to determine solid-state properties and the oral bioavailability of creatine. Currently, creatine is available as a monohydrate or di-creatine citrate salt form. The aim of this study was to develop a simple and sensitive LC method for the determination of creatine in aqueous solution as wel) …
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Optimization of 1st-line antituberculosis dosing regimens using a population pharmacokinetic approach: food effects, drug combinations and pharmacological effects
… fat meal had the greatest effect on rifapentine oral bioavailability, increasing it by 86%; bulky low-fat, bulky-high-fat, and chicken soup resulted in 33%, 46%, and 49% increases in rifapentine oral bioavailability, respectively. Similar trends were observed for the metabolite 25-desacetyl …
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Synthesis, Physicochemical And Biopharmaceutical Characterisation Of Pro-Antibiotic Esters; Free Bases Of Ciprofloxacin
… performance in vivo, especially with respect to oral bioavailability. In the case of antibiotics, poor bioavailability can indirectly encourage antimicrobial resistance from pressure selection resulting from subtherapeutic dosing. This study was designed to synthesise esters of Ciprofloxacin, a …
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Non-traditional platinum compounds for improved cellular accumulation and tumor targeting
… Platinum Compounds for Improved Uptake, Oral Bioavailability, and Tumor Targeting The path to more potent platinum anticancer drugs with fewer side effects lies in the exploration of non-traditional platinum compounds, which do not necessarily contain the canonical ligand set of two …
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Complex Heterocycles as Mitochondrial Uncouplers
… were examined in vivo and found to have good oral bioavailability in mice with ranges in Cmax of 10-90 µM and t1/2 of 0.9 to >24 hours. We found that analogs that have F/OCF3/SO2CF3 groups on the 4-position exhibited the longest t1/2 compared to other structural isomers, suggesting that this …
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Surface Modified Solid Lipid Curcumin Nanoparticles For Oral Delivery
… well as pre-clinical trials. However, its poor oral bioavailability due to extremely low aqueous solubility, poor permeability and extensive pre-systemic metabolism has been the major limitation for its use as a chemotherapeutic agent. Solid lipid nanoparticulate formulations have been …
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Dairy ingredients-based emulsions and beta-carotene delivery
… of many bioactive nutrients greatly limit their oral bioavailability and thus their health benefits. Therefore, the delivery of these compounds requires protective mechanisms. Emulsion-based delivery systems are becoming some of the most ideal microencapsulation carriers for these lipophilic …
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Operation Hot Sandwich: Incorporating pyrones in [4 + 2] cycloaddition reactions to prepare thermorubin
… and negative bacteria but suffers from poor oral bioavailability. Difficulties in obtaining this material have led to our development of a total synthetic strategy including a new method for incorporating pyrone moieties into aromatic systems. Based off the Hauser annulation, these conditions …
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Mitochondrial Uncouplers: Development as Therapeutics for Metabolic Diseases
… of 4.3 M in L6 myoblast cells and excellent oral bioavailability and liver exposure in mice. In the preclinical stelic animal model (STAM) mouse model of NASH, administration of 2.12i at 25 mg kg-1day-1 resulted in decreased liver triglyceride levels and improved liver enzymes, NAFLD activity …
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To Investigate The Impact Of Gut Bacteria On Efflux Transporter Expression And Function In Gastrointestinal Mucosae
Gut microbiome diversity may alter oral bioavailability and contribute to individual variations in drug therapy. Therefore, understanding molecular links between the gut microbiome and oral drug disposition is critical for realizing the goals of precision medicine. The purpose of the study was to …
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Lipid & surfactant based systems for improved delivery of poorly soluble APIs
… to poor absorption and low plasma levels post oral administration. Lipids comprise of fatty acids and their derivatives and are considered a biocompatible option for drug delivery. In the studies discussed in following chapters, lipid based drug delivery systems (LBDDS) have been utilized in …
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