Acebutolol (AC) is a chiral b-adrenergic blocking drug, which is useful clinically as the racemate in treating hypertension and is metabolized to an equipotent chiral metabolite, diacetolol (DC). In this paper we report a case of a 32 year old woman who was receiving AC during her pregnancy and lactating time for management of hypertension. The maternal plasma level and breast milk as well as cord blood collected to see whether the drug is transferred to the fetus through the mother stereoselectively. A stereospecific high-performance liquid chromatographic (HPLC) assay was used to measure the enantiomeric concentrations of AC and DC. AC and DC enantiomers are stereoselectively excreted into the milk, although the concentrations of DC enantiomers were higher than those of AC. AC concentrations were very low in both cord artery and vein samples four hours after taking the drug however, the stereoselective concentrations of metabolite, DC, was found in these samples. In conclusion, AC and DC enantiomers are excreted in human breast milk in concentrations much higher than that in maternal plasma. Furthermore, DC was found in the infant’s plasma indicating that accumulation of metabolite did occur in this infant.

A novel tandem mass spectrometry (LC-MS/MS) bio-analytical method was developed and validated for the synchronized quantitation of fingolimod (FIN) and its active metabolite, fingolimod-phosphate (FPH), in human whole blood using a unified sample preparation protocol. This method was successfully applied in a bio-equivalence study comparing a 0.5 mg test capsule to the reference product, Gilenya™, in twenty-eight healthy male subjects under fasting conditions. The study employed a randomized, single-dose, two-period, two-treatment, two-sequence crossover design with a seven-week washout period. FIN and its internal standard (IS) were extracted using liquid-liquid extraction, while FPH was isolated from the residual blood via protein precipitation. Quantitative analysis of both analytes was performed using positive electrospray ionization in multiple reaction monitoring mode (+ESI-MRM), with ion transitions of m/z 388.2 → 255.3 (IS: 392.12 → 259.2) for FIN, and m/z 308.4 → 255.3 (IS: 312.4 → 259.3) for FPH. The method was validated over dynamic calibration ranges of 10-800 pg/mL for FIN and 50-5000 pg/mL for FPH, meeting all acceptance criteria of EMEA bioanalytical method validation guidelines. Pharmacokinetic parameters including Cmax and AUC0t were determined for both FIN and FPH and compared between the test and reference formulations. The results confirmed that both products are bio-equivalent.

Background: Rhodomyrtus Tomentosa (Karamunting) is one of South Kalimantan's biodiversity. In previous research on asthma and coal dust exposure models, nebulization with an ethanol extract of R. tomentosa leaves has been shown to reduce inflammatory cells. This study aimed to investigate the anti-inflammatory activity on the stabilization of red blood cell membranes and to identify the chemical compounds present in extracts of R. tomentosa leaves. Methods: Anti-inflammatory effect of R. tomentosa leaves was evaluated by in vitro red blood cell membrane stabilization methods. Nonsteroidal anti-inflammatory sodium diclofenac was used as the reference drug. The content of chemical compounds in the ethanol extract of R. tomentosa leaves was identified using Ultra Performance Liquid Chromatography-Mass Spectrometry (UPLC-MS). Results: The results of inhibition of red blood cells membrane lysis showed the n-hexane fraction (concentration 25 ppm), ethyl acetate fraction (concentration 50 ppm), and a fraction of water (concentration 50 ppm) with an inhibition level of 54. 5%, 81. 8%, 63. 6%, respectively. The ethyl acetate fraction showed the highest inhibition of hemolysis. This result is not significantly different from the standard anti-inflammatory sodium diclofenac (90. 09%). Oleanonic acid and ursonic acid were two similar metabolites in subfractions ethyl acetate 1, 2, and 3, which may have antiinflammatory properties. Conclusions: R. Tomentosa leaves can have potency as an anti-inflammatory by increasing the red blood cell membrane stability equal to lysosome cells, depending on the concentration.

This experiment aimed to investigate the effects of liquid metabolite (LM) produced by Lactobacillus plan-tarum and dietary putrescine (PUT) on growth, blood lipids, villus height (VH), crypt depth (CD) and poly-amines (PAs) content of intestinal tissue and ileal digesta in chickens. Six treatments, replicated six time each, were factorial arrangements of two levels of LM (0 and 0. 3%) and three levels of dietary putrescine (0, 0. 03 and 0. 05%). Growth performance and PAs content of digesta and excreta (at 21 d) were measured, as well as small intestine VH and CD. Blood cholesterol, triglyceride and glucose were measured at 24, 33 and 40th d. Putrescine (0. 05%) negatively affected body weight, feed conversion ratio and protein and en-ergy efficiency ratio while increased duodenal VH significantly (P<0. 05) as compared to the 0. 03% putre-scine. Aging was effective on blood cholesterol, triglyceride and glucose. Blood triglyceride decreased by 0. 03% putrescine (P<0. 05). Faecal spermidine was increased significantly (P<0. 05) by 0. 05% putrescine. Duodenal PAs declined in the chickens fed LM, whereas dietary putrescine had no effects on intestinal tis-sue polyamine. In conclusion, luminal PAs content was not affected by treatments. LM influenced intestinal tissue PAs but had no effects on growth and ileal digesta polyamine content. However, putrescine (0. 05%) was harmful to the growth but increased duodenal VH.

An experiment was conducted to investigate the effects of supplementing Lori ewes with rumen-undegradable protein (RUP) in late pregnancy on their performance and that of their lambs. Milk yield and blood metabolite profile were measured. Forty pregnant ewes were used in a completely randomized design trial with four treatments: 1) a basal diet (control); 2) with a supplement of 5% fishmeal; 3) with a supple-ment of 5% extruded soybean and 4) with a supplement combining both sources. Supplementation started 30-days before the estimated parturition date. Dietary inclusion of fish meal significantly improved body weight at lambing compared to the other groups (P<0. 05). Lambs of ewes fed diets supplemented with ru-men undegradable protein (RUP) were heavier at birth and weaning compared to other groups (P<0. 05). Soybeans, of the combined supplement improved the colostrum concentration of IgG in postpartum ewes (P<0. 05). Diets containing extruded soybeans resulted in milk with higher milk urea nitrogen content than the control diet (P<0. 05). Serum concentration of glucose was significantly decreased in ewes fed diets containing RUP pre-partum (P<0. 05), while post-partum glucose concentration was only decreased in ewes fed diets containing fish meal without or with extruded soybeans (P<0. 05). Plasma concentration of beta-hydroxybutyric acid (BHBA) and non-esterified fatty acid (NEFA) were significantly decreased in the treated groups compared to the control group in post-partum ewes (P<0. 05).