Transporters play important roles in tissue distribution and urinary- and biliary-excretion of drugs and transporter molecules involved in those processes have been elucidated well. Furthermore, an involvement of efflux transporters such as P-glycoproteins, multidrug resistance associated protein 2, and breast cancer resistance protein as the intestinal absorption barrier and/or intestinal lumi...

Low oral bioavailability and a negative meal effect on drug plasma levels motivated studies on formulation and meal composition effects on the absorption of LY303366, a poorly water-soluble, semisynthetic, cyclic peptide antifungal drug. Solid drug particle size and meal composition studies were evaluated in beagle dogs. Canine regional absorption studies were also carried out utilizing surgica...

The influence of oral sodium bicarbonate and aluminium hydroxide on the absorption of indomethacin has been studied in normal volunteers. While sodium bicarbonate appeared to increase indomethacin absorption, aluminium hydroxide markedly reduced both the rate and extent of absorption. The buccal absorption of indomethacin over the pH range 5-9 was also studied in normal volunteers, and showed t...

BACKGROUND 20(S)-protopanaxadiol (PPD), similar to several other anticancer agents, has low oral absorption and is extensively metabolized. These factors limit the use of PPD for treatment of human diseases. METHODS In this study, we used cubic nanoparticles containing piperine to improve the oral bioavailability of PPD and to enhance its absorption and inhibit its metabolism. Cubic nanoparti...

By FREDERICK A. Kuis nn I HE ABSORPTION of folic acid occurs primarily in the proximal small intestine and is thought to be mediated, in part at least, by an active transport 2 l)iminished absorption of folic acid commonly occurs in disease characterized by diffuse atrophy of the jejunal mucosal villi, such as idiopathic steatorrhea ( non-tropical sprue, gluten enteropathy ) and tropical sprue ...

Liquid crystal (LC)-forming lipids represent an important class of biocompatible amphiphiles and their application extends to cosmeceutical, dietary, and pharmaceutical technologies. In the present study, we aimed to develop strategies for designing and optimizing oral and topical LC formulations by evaluating their in vitro and in vivo drug absorption performances. C17-Monoglycerol ester (MGE)...

The rate of paracetamol absorption following oral administration has been used as a model of drug absorption and as an indirect estimate of the rate of gastric emptying before and after elective or emergency surgery in 13 adult patients. The rates of paracetamol absorption before and after surgery were not significantly different and compared well with results obtained previously in normal volu...

Patients undergoing carotid endarterectomy were pretreated with low-dose, oral beta carotene to determine whether the carotenoid content of plaque could be increased in vivo. Beta carotene-treated patients had a 50-fold increase in their plaque beta carotene level from 0.066 to 3.3 micrograms beta carotene/g plaque. Microscopy and microspectrophotometry demonstrated that plaque from beta carote...

The synthesis, antibacterial activity and oral absorption in rats of new 7/?-[(Z)-2-(2-aminothiazol4-yl)-2-(carboxymethoxyimino)acetamido]cephalosporins (1) having various substituted-alkylthio groups at the C-3 position of the cephemnucleus are described. Of these, the cephalosporins with a cyanomethylthio group (Id) and fluoroethylthio group (lp) at the C-3 position showed a potent in vitro a...

A series of new 7j5-[(Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]cephalosporins (1) having various substituted-vinylthio groups at the C-3 position of the cephem nucleus was synthesized and evaluated for antibacterial activity and oral absorption in rats in comparison with cefixime. Of these, the cephalosporins (la and lc) with a lower alkoxycarbonylvinylthio group (Z-form) at ...