Objective: Solubility is a key parameter as it is one of the main causes for poor bioavailability. The objective was to improve the solubility and dissolution profile of poorly-soluble silymarin with a water-soluble carrier fulvic acid. Materials and methods: Phase solubility studies were carried out for the determination of stoichiometric ratio between silymarin and fulvic acid by Higuchi and ...

Bupropion, an efficacious antidepressant and smoking cessation agent, inhibits dopamine and norepinephrine transporters (DAT and NET, respectively). Recently, bupropion has been reported to noncompetitively inhibit 3 2, 3 4, and 4 2 nicotinic acetylcholine receptors (nAChRs) expressed in Xenopus oocytes or established cell lines. The present study evaluated bupropion-induced inhibition of nativ...

Recently, it was shown that both Bcr and Bcr-Abl can interact with xeroderma pigmentosum group B (XPB/ ERCC3), a protein implicated in DNA repair after UVinduced damage. To further analyze the effect of Bcr-Abl on the DNA damage response, we used cell lines stably transfected with the BCR-ABL gene and their parental counterparts (MBA-1 versus MO7E and Bcr-AblT1 versus 4A2 pZAP) and several assa...

Chondrocytes isolated from bovine articular cartilage were plated at high density and grown in the presence or absence of ascorbate. Collagen and proteoglycans, the major matrix macromolecules synthesized by these cells, were isolated at times during the course of the culture period and characterized. In both control and ascorbate-treated cultures, type II collagen and cartilage proteoglycans a...

The objective of this research was the identification of the metabolic profile of fluasterone, a synthetic derivative of dehydroepiandrosterone, in dogs treated orally or subcutaneously with [4-C]fluasterone. Separation and characterization techniques used to identify the principal metabolites of fluasterone in urine and feces included high-performance liquid chromatography (HPLC), liquid scint...

-During CC14 intoxication in rats, a disruption of hepatic mitochondrial structure and function occurs, which is characterized by a loss of respiratory activity, loss of phosphorylation coupled to respiration, and mitochondrial swelling, attended by loss of cristae structure. Within 15-25 hr, after full development of the mitochondrial lesion, the function and structure of the mitochondria are ...

The absorption, metabolism, and excretion of (1-[[3-hydroxy-1adamantyl) amino] acetyl]-2-cyano-(S)-pyrrolidine (vildagliptin), an orally active and highly selective dipeptidyl peptidase 4 inhibitor developed for the treatment of type 2 diabetes, were evaluated in four healthy male subjects after a single p.o. 100-mg dose of [C]vildagliptin. Serial blood and complete urine and feces were collect...

Cotinine, a major peripheral metabolite of nicotine, has recently been shown to be the most abundant metabolite in rat brain after peripheral nicotine administration. However, little attention has been focused on the contribution of cotinine to the pharmacological effects of nicotine exposure in either animals or humans. The present study determined the concentration-response relationship for (...