Triazine-based antiprotozoal agents are known for their lipophylic characteristics and may therefore be expected to be well absorbed following oral administration. However, although an increase in lipid solubility generally increases the absorption of chemicals, extremely lipid-soluble chemicals may dissolve poorly in gastrointestinal (GI) fluids, and their corresponding absorption and bioavail...

Etoposide, a widely used anticancer drug, exhibits low and variable oral bioavailability mainly because of being substrate for the efflux transporter, P-glycoprotein (P-gp). Therefore, the present study was aimed to investigate the effect of D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and PEG 400 as P-gp inhibitors on the intestinal absorption of etoposide. Everted sacs of rat smal...

as a supplement to the oral method has been pointed out by many workers. Moreover, the possibility of error in the result of oral method due to diminished absorption has been shown by Beeler, Bryan, Cathcart and Fitz (1922). The flat blood sugar curve obtained by Thaysen (1929) after the oral administration of glucose, as has been shown by the author, is due to the diminished absorption of gluc...

1. There are conflicting reports regarding the effect of oral contraceptives on serum and erythrocyte folate concentrations and on folate absorption. A detailed study of this problem was therefore undertaken. 2. It was first ascertained that there was no significant variation in serum folate concentrations at different stages in the normal menstrual cycle. 3. No significant difference was found...

Docetaxel is a potent anticancer drug, but development of an oral formulation has been hindered mainly due to its poor oral bioavailability. In this study, solid lipid nanoparticles (SLNs) surface-modified by Tween 80 or D-alpha-tocopheryl poly(ethylene glycol 1000) succinate (TPGS 1000) were prepared and evaluated in terms of their feasibility as oral delivery systems for docetaxel. Tween 80-e...

Lipid nanocarriers are becoming a versatile platform for oral delivery of lipophilic drugs. In this article, we aimed to explore the gastrointestinal behaviors of lipid nanoparticles and the effect of PEGylation on oral absorption of fenofibrate (FN), a Biopharmaceutics Classification System (BCS) II model drug. FN-loaded PEGylated lipid nanoparticles (FN-PLNs) were prepared by the solvent-diff...

The absorption of orally administered pivampicillin was studied in nine postoperative patients and compared with that of intravenously administered ampicillin. The absorption of pivampicillin was calculated on the basis of comparison of the areas under the serum concentration curves for both modes of administration. After an oral dose of 700 mg the absorption ranged from 40 to 95% (mean, 60%).

The anti-hepatitis C virus nucleotide prodrug GS-6620 employs a double-prodrug approach, with l-alanine-isopropyl ester and phenol moieties attached to the 5'-phosphate that release the nucleoside monophosphate in hepatocytes and a 3'-isobutyryl ester added to improve permeability and oral bioavailability. Consistent with the stability found in intestinal homogenates, following oral administrat...

BACKGROUND AND AIMS Intestinal adaptation after small bowel resection in humans is debated. We have quantified in adult short bowel (remnant small bowel length <2 m) patients oral intake and net digestive absorption and their evolution over time. PATIENTS AND METHODS Oral intake and faecal output were studied over three days in 90 patients (39 and 51 without or with parenteral nutrition, resp...

Models of systemic drug absorption after oral administration are frequently based on a direct or a delayed first-order rate process. In practice, the use of the first-order approach to predict drug concentrations in blood plasma frequently yields a considerable mismatch between predicted and measured concentration profiles. This is particularly true for the upswing of the plasma concentration a...