نتایج جستجو برای: low bioavailable drug
تعداد نتایج: 1728796 فیلتر نتایج به سال:
Atmospheric inputs of iron to the open ocean are hypothesized to modulate ocean biogeochemistry. This review presents an integration of available observations of atmospheric iron and iron deposition, and also covers bioavailable iron distributions. Methods for estimating temporal variability in ocean deposition over the recent past are reviewed. Desert dust iron is estimated to represent 95% of...
The role of endogenous sex hormones in many diseases makes understanding factors that influence levels of these hormones increasingly important. This study examined age-associated variations in total and bioavailable testosterone and estradiol levels among community-dwelling Caucasian men in Rancho Bernardo, California. Plasma samples obtained from 810 men aged 24-90 years in 1984-1987 were ana...
Hepatocellular carcinoma (HCC) is one of the most common lethal human malignancies worldwide and its advanced status is frequently resistant to conventional chemotherapeutic agents and radiation. We evaluated the cytotoxic effect of the orally bioavailable dual PI3K/mTOR inhibitor, NVP-BGT226, on a panel of HCC cell lines, since hyperactivated PI3K/Akt/mTOR signaling pathway could represent a b...
Of all the pharmaceutical compounds, about 40% are considered poorly water soluble and hence, the development of efficacious formulation is being halted. It has been shown that a drug should have a minimum aqueous solubility of 1% to avoid bioavailability problems. During preformulation study, sufficient time should be invested in order to improve the solubility of these kinds of drug. At the v...
Maximizing oral bioavailability is therapeutically important because the extent of bioavailability directly influences plasma concentrations and therapeutic efficacy after oral drug administration. Bioavailability of poor bioavailable drugs can be increased from the many available approaches in the literature and the most recent approach is the use of bioavailability enhancers. The use of bioen...
While natural products or their derivatives and mimics have contributed around 50% of current drugs, there has been no approach allowing front-loading of chemical space compliant with lead- and drug-like properties. The importance of physicochemical properties of molecules in the development of orally bioavailable drugs has been recognized. Classical natural product drug discovery has only been...
A series of alpha-alkyl-alpha-amino-beta-sulphone hydroxamates was prepared and evaluated for potency versus MMP-2 and MMP-13, and for selectivity versus MMP-1. Low nanomolar potency was obtained with selectivity versus MMP-1 ranging from >10 to >1000. Selected compounds were orally bioavailable.
Prior studies showed conflicting results regarding the association between 25-hydroxyvitamin D (25(OH)D) levels and mineral metabolism in end-stage renal disease. In order to determine whether the bioavailable vitamin D (that fraction not bound to vitamin D-binding protein) associates more strongly with measures of mineral metabolism than total levels, we identified 94 patients with previously ...
The effect of the dosing vehicle (e.g., dough) on the ability of an in vitro gastrointestinal (IVG) method to predict relative bioavailable Pb associated with soil ingestion was evaluated. Bioaccessible Pb determined by the IVG method was compared with relative bioavailable Pb measured from dosing trials using juvenile swine for 18 contaminated soils ranging from 1270 to 14200 mg Pb kg(-1). Bio...
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