Scintigraphic evaluation of a novel colon-targeted delivery system (CODES) in healthy volunteers.

The purposes of this study are to investigate the gastrointestinal transit and release properties of a novel, colon-targeted delivery system (CODES) administered to healthy volunteers using gamma scintigraphy and to confirm that lactulose functions to promote disintegration in the colon. Two placebo formulations were studied: one was CODES, which consisted of a lactulose containing core overcoated with both Eudragit E and Eudragit L designed to rapidly disintegrate in the colon, the other was lactulose-free reference formulation (LFRF) that consisted of lactulose-free tablet core overcoated with the same materials. Transit and disintegration of the radiolabeled formulations were followed by gamma scintigraphy.

Plasma carnitine concentrations in patients undergoing open heart surgery.

Carnitine is an essential cofactor for fatty acid (FA) metabolism, the predominant source of ATP in the normal aerobic heart. During myocardial ischemia, FA metabolism is impaired and tissue carnitine levels are depleted. Since the heart cannot synthesize carnitine, plasma carnitine could play an important role in maintaining myocardial carnitine levels during reperfusion.

Potential use of cyclodextrins to enhance the solubility of YM466 in aqueous solution.

Various solubilizing agents for YM466, a new Factor Xa inhibitor, were investigated to begin designing the aqueous formulation for subcutaneous administration. The tentative target concentration was 5 mg/mL. First, three kinds of buffer solutions (glycine-HCl, citrate, and lactate) were examined for their solubilizing effects.

Timed-release formulation to avoid drug-drug interaction between diltiazem and midazolam.

The purpose of this study was to investigate whether the use of a timed-release (TR) drug formulation can avoid unfavorable pharmacokinetic drug-drug interactions in vivo. First, the effects of the time interval between administration of midazolam and diltiazem on the known drug-drug interaction between these drugs were investigated in dogs. When dogs were given midazolam orally at the same time they were orally given an aqueous diltiazem solution, the area under the plasma concentration-time curves of midazolam increased significantly compared with that of midazolam given orally in the absence of diltiazem.

A new stressed test to predict the foreign matter formation of minodronic acid in solution.

A formulation containing 0.5 mg/ml minodronic acid, 40 mM citrate, pH 4.5, and sodium chloride, stored in regular flint glass ampoules, was stable without particulate increase under high temperature conditions, such as 40 degrees C for 6 months, or 50 or 60 degrees C for 3 months.

Failure of stability prediction for minodronic acid injectable by accelerated stability testing.

A liquid formulation containing 0.5 mg/ml minodronic acid, 40 mM, pH 4.5, citrate, and sodium chloride added to adjust the osmolarity of the final formulation was stored in flint glass ampoules at 25, 40, 50, and 60 degrees C.