Phosphanilic acid is an antibacterial agent with a mode of action and antibacterial spectrum similar to those of sulfamethoxazole, with the exception that it has potent antipseudomonal activity. Bioavailability studies in rats (50, 300, and 600 mg/kg, oral and subcutaneous), dogs (50, 150, and 450 mg/kg, oral and intravenous infusion), and humans (400 and 800 mg, oral) showed that the extent of...

The percentage of new chemical entities synthesised with low aqueous solubility and high therapeutic efficacy is growing, this presents a major challenge for the drug delivery. To over come this challenge, different methods were developed for the improvement of oral bioavailability, but some have major disadvantages. Recently, oral lipid based formulation is developed for the improvement of ora...

This study investigates the oral bioavailability and characterizes urine metabolites of dehydroevodiamine (DeHE), one of the bioactive alkaloids isolated from the fruit of Evodia rutaecarpa . A freely moving rat model coupled with an automated blood sample system was used to evaluate the pharmacokinetics of DeHE. High-performance liquid chromatography (HPLC), mass spectrometry (MS), and nuclea...

Carvedilol is an effective nonselective alpha-1 and beta blocker discovered by Fritz Wiedemann [1] . It is an antihypertensive drug indicated for the treatment of mild to severe congestive heart failure (CHF), angina pectoris, cardiac arrhythmias and myocardial infarction [2] . Water solubility of Carvedilol is a fundamental property that affects the drug absorption after oral administration. M...

There is a possibility that even a glass of grapefruit juice (GFJ) taken several hours before oral medication may enhance the bioavailability of many drugs, exaggerate the drug action, and increase the toxic effect by exaggerating the potency of the drug. This can be explained by inhibition of CYP3A4 in the small intestine by GFJ, thus suppressing drug metabolism. This interaction with GFJ is l...

Existing experimental strategies for the in vivo evaluation of factors affecting oral bioavailability have been reviewed. Based on concepts that have evolved, an integrated set of strategies emerges that appears capable of providing estimates of the individual contributions attributable to absorption, losses in the gut lumen, and first-pass elimination in the gut wall and the liver. The only as...

In this study, a novel mesoporous silica nanoparticles drug carrier contributes to improving the solubility, dissolution, and the oral bioavailability of apigenin (AP). The apigenin of solid dispersion of mesoporous silica nanoparticles (AP-MSN) was prepared by physical absorption method and also, in-vitro drug release and in-vivo bioavailability performance were evaluated. Based on its solubil...

In this study a new soluble solid curcumin nanoemulsion powder was prepared using spray-drying technology to improve the solubility and bioavailability of curcumin. The liquid nanoemulsion consisted of curcumin, Capryol 90, Transcutol P, and Cremophor RH40. The solid nanoemulsion was prepared by spray-drying the liquid nanoemulsion in laboratory spray dryer, using lactose as solid carrier. The ...

Calcium absorption tests have rarely been validated for being representative for absolute bioavailability (true absorption) or for intraindividual variation. Therefore, we investigated the reproducibility of the absolute bioavailability of strontium chloride, a marker for intestinal calcium absorption, in healthy male volunteers (n = 8) by measuring the area under the plasma strontium concentra...