No abstract

The amine-carboxyboranes and related derivatives have been shown to be potent anti-inflammatory and anti-osteoporosis agents. Their action in part appears to be mediated by the modulation of cytokines, e.g. TNFα or IL-1. Previous studies have demonstrated that LPS induced macrophages release of TNFα maximally at 60 to 90 min. and IL-1 from 5 to 8 hr. The amine-carboxyboranes reduced significantly the release of these cytokines but also blocked TNFα high affinity binding to UMR-106 receptor at 90 min. at 10 μM, and IL-1 high affinity binding at 5 hr. at 12.5 μM. In addition, the agents suppressed IL-8 binding to CHO K1 high affinity receptor at 24 hr. at 50 μM and IL-2 binding to HuT-8 receptors at 25 μM at 90 min. and 5 hr. Correlation of metabolic events associated with osteoporosis showed that at 90 min., when TNFα receptor binding was reduced by the agents, calcium uptake into UMR-106 cells was reduced at 10 μM as well as the acid and alkaline phosphatases, and the prostaglandin cyclo-oxygenase activities and adhesion of leukocytes and macrophages to UMR-106 cell monolayers. At 5hr. when the agents reduced IL-1 binding to UMR-106 receptors, calcitonin and 1,25-dihydrovitamin D3 binding was reduced by the agents as was acid and alkaline phosphatase, and 5′-lipoxygenase activities and white blood cell adhesion. At this time calcium uptake and proline incorporation was increased significantly by the agents. At later times e.g. 18-48 hr. calcium uptake was still increased, and NAG activity was inhibited in the presence of the agents. These effects may be related more to the inhibition of other cytokine receptor binding, e.g. IL-8. Thus, many of the observed metabolic effects of amine-carboxyboranes as antiosteoporosis agents can be correlated with their inhibition of cytokine high affinity binding to target cell receptors.

Quantitative relationships between urinary cotinine excretion and environmental tobacco smoke (ETS) exposure in young children have not been determined. The objectives of this research were to: (1) determine the cotinine t(1/2) in young children up to 3 years of age using urinary cotinine excretion data and (2) establish correlations between urinary cotinine excretion and ETS exposure in young children. In 44 young children involuntarily exposed to ETS at home, urinary cotinine excretion data were collected for 6 days out of the home, and the cotinine t(1/2) was determined. The median cotinine t(1/2) was 54.7 h, and 50% of the t(1/2) values were between 38.2 and 85.6 h. Air nicotine concentrations in the home were used to measure ETS exposure. The best predictor of home air nicotine concentration was a model with sex and the zero time creatinine corrected urinary cotinine concentration (R^2 = 0.23).

Objective. To investigate the long-term (ie, 6-year) impact of a required remake vs an optional remake on student performance in a compounding laboratory course in which students' compounded preparations were analyzed. Methods. The analysis data for several preparations made by students were compared for differences in the analyzed content of the active pharmaceutical ingredient (API) and the number of students who successfully compounded the preparation on the first attempt.Results. There was a consistent statistical difference in the API amount or concentration in 4 of the preparations (diphenhydramine, ketoprofen, metoprolol, and progesterone) in each optional remake year compared to the required remake year. As the analysis requirement was continued, the outcome for each preparation approached and/or attained the expected API result. Two preparations required more than 1 year to demonstrate a statistical difference. Conclusion. The analytical assessment resulted in a consistent, long-term improvement in student performance during the 5-year period after the optional remake policy was instituted. Our assumption is that investment in such an assessment would result in a similar benefits at other colleges and schools of pharmacy.

Abstract:The metabolites of N- [(tdmethylamineboryl