Behaviour of ejaculated spermatozoa from bull, boar and ram during thin-layer countercurrent partition in aqueous two-phase systems.
(41/353)
Ejaculated spermatozoa from bulls, boars and rams were subjected to thin-layer countercurrent partition in aqueous two-phase systems composed of dextran T500 and polyethylene glycol 6000 (PEG) in sucrose-based Hepes-buffered media. In the basal system, the great majority of spermatozoa tended to partition with the dextran-rich bottom phase; however, by including very low levels of phosphate, they could be made to partition increasingly with the PEG-rich top phase (complete at 10 mM phosphate). A procedure was developed for carrying out four separations simultaneously under identical conditions, whereby it could be shown that distribution varied with the number of spermatozoa in the sample. In the case of bull, the effect of cell number could be reduced considerably by inclusion of small quantities of seminal plasma in the phase system, but no such effect was found for ram or boar. Considerable variation in distribution pattern was seen between samples, which did not appear to be due to technical inconsistency. Livability in the phase systems was also variable, and we believe that PEG may exert a detergent-like effect on the sperm surface that is exacerbated in highly defined media free of protective proteins. (+info)
Effects of oxidation on changes of compressibility of bovine serum albumin.
(42/353)
The methods of ultrasound velocity and density measurements were used to study the adiabatic compressibility of bovine serum albumin (BSA) during its oxidation by the prooxidants Cu2+ and 2,2'-azobis(2-amidinopropane) hydrochloride (AAPH). We did not find changes of compressibility of BSA in the presence of copper ions at rather high molar ratio Cu2+/BSA = 0.66 mol/mol. This can be explained by binding of the Cu2+ to the binding site of BSA and thus protecting the prooxidant action of the copper. However, AAPH-mediated oxidation of BSA resulted in an increase of its apparent specific compressibility (psik/beta0). These changes could be caused by the fragmentation of the protein. (+info)
Stability of sulfadiazine oral liquids prepared from tablets and powder.
(43/353)
PURPOSE: To assess the stability of sulfadiazine (SDZ) oral liquids prepared from tablets and powder at two temperatures. METHODS: Solutions of SDZ 200 mg/mL were prepared from commercially available 500 mg tablets and powder in sterile water for irrigation. They were stored in amber glass bottles at 4 degrees C and 23 degrees C. The concentrations of SDZ were determined in duplicate by high-performance liquid chromatography at 0, 1, 3, 7 and 14 days. The initial and final pH of solutions was compared. The recovery of SDZ from tablets was determined. A loss exceeding 10% of the initial concentration of SDZ was considered excessive degradation. RESULTS: The recovery of SDZ from tablets was 100 +/- 3%. The initial pH values were significantly different between solutions prepared from tablets and powder, 6.9 and 9.8 respectively. No significant difference was found between initial and final pH values for the two all formulations. Detectable change in odor was observed for the solutions stored at 23 degrees C. The solution prepared from powder was stable 3 days stored at 4 degrees C. Other formulations lost over 10% of the initial SDZ concentration within 2 days. CONCLUSIONS: SDZ 200 mg/mL oral solution prepared from powder could be used to facilitate drug administration to very young children by nurses but by taking account of its fast degradation. (+info)
Effect of high-pressure-induced ice I-to-ice III phase transitions on inactivation of Listeria innocua in frozen suspension.
(44/353)
The inactivation of Listeria innocua BGA 3532 at subzero temperatures and pressures up to 400 MPa in buffer solution was studied to examine the impact of high-pressure treatments on bacteria in frozen matrices. The state of aggregation of water was taken into account. The inactivation was progressing rapidly during pressure holding under liquid conditions, whereas in the ice phases, extended pressure holding times had comparatively little effect. The transient phase change of ice I to other ice polymorphs (ice II or ice III) during pressure cycles above 200 MPa resulted in an inactivation of about 3 log cycles, probably due to the mechanical stress associated with the phase transition. This effect was independent of the applied pressure holding time. Flow cytometric analyses supported the assumption of different mechanisms of inactivation of L. innocua in the liquid phase and ice I (large fraction of sublethally damaged cells due to pressure inactivation) in contrast to cells subjected to ice I-to-ice III phase transitions (complete inactivation due to cell rupture). Possible applications of high-pressure-induced phase transitions include cell disintegration for the recovery of intracellular components and inactivation of microorganisms in frozen food. (+info)
Particle deposition in industrial duct bends.
(45/353)
A study of particle deposition in industrial duct bends is presented. Particle deposition by size was measured by comparing particle size distributions upstream and downstream of bends that had geometries and flow conditions similar to those used in industrial ventilation. As the interior surface of the duct bend was greased to prevent particle bounce, the results are applicable to liquid drops and solid particles where duct walls are sticky. Factors investigated were: (i) flow Reynolds number (Re = 203 000, 36 000); (ii) particle Reynolds number (10 < Repinfinity < 200); (iii) particle Stokes number (0.08 < Stk < 16); (iv) bend angle (theta = 45 degrees, 90 degrees, 180 degrees ); (v) bend curvature ratio (1.7 < R0 < 12); (vi) orientation (horizontal-to-horizontal and horizontal-to-vertical); and (vii) construction technique (smooth, gored, segmented). Measured deposition was compared with models developed for bends in small diameter sampling lines (Re < 20 000; Repinfinity < 13). Whereas deposition measured in this work generally agreed with that estimated with models for particles <30 microm (Stk < 0.7), it was significantly lower than that estimated for larger particles. As the flow around larger particles became increasingly turbulent, the models progressively under-represented drag forces and over-estimated deposition. For particles >20 microm, deposition was slightly greater in the horizontal-to-horizontal orientation than in the horizontal-to-vertical orientation due to gravitational settling. Penetration was not a multiplicative function of bend angle as theory predicts, due to the developing nature of turbulent flow in bends. Deposition in a smooth bend was similar to that in a gored bend; however, a tight radius segmented bend (R0 = 1.7) exhibited much lower deposition. For more gradual bends (3 < R0 < 12), curvature ratio had negligible effect on deposition. (+info)
Physiological capacity of the reticuloendothelial system for the degradation of hemoglobin vesicles (artificial oxygen carriers) after massive intravenous doses by daily repeated infusions for 14 days.
(46/353)
A hemoglobin vesicle (HbV; diameter 252 +/- 53 nm) or liposome-encapsulated Hb is an artificial oxygen carrier developed for use as a transfusion alternative, and its oxygen-transporting capacity has been well characterized, although critical physiological compartments for the Hb degradation after a massive infusion of HbV and the safety outcome remain unknown. In this study, we aimed to examine the compartments for its degradation by daily repeated infusions (DRI) of HbV, focusing on its influence on the reticuloendothelial system (RES). Male Wistar rats intravenously received the HbV suspension at 10 ml/kg/day for 14 consecutive days. The cumulative infusion volume (140 ml/kg) was equal to 2.5 times the whole blood volume (56 ml/kg). The animals tolerated the DRI well and survived, and body weights continuously increased. One day after DRI, hepatosplenomegaly occurred significantly through the accumulation of large amounts of HbV. Plasma clinical chemistry was overall normal, except for a transient elevation of lipid components derived from HbV. These symptoms subsided 14 days after DRI. Hemosiderin deposition and up-regulation of heme oxygenase-1 coincided in the liver and spleen but were not evident in the parenchyma of these organs. Furthermore, the plasma iron and bilirubin levels remained unchanged, suggesting that the heme-degrading capacity of the RES did not surpass the ability to eliminate bilirubin. In conclusion, phospholipid vesicles for the encapsulation of Hb would be beneficial for heme detoxification through their preferential delivery to the RES, a physiological compartment for degradation of senescent RBCs, even at doses greater than putative clinical doses. (+info)
Bitterness evaluation of medicines for pediatric use by a taste sensor.
(47/353)
The purpose of this study was to evaluate the bitterness of 18 different antibiotic and antiviral drug formulations, widely used to treat infectious diseases in children and infants, in human gustatory sensation tests and using an artificial taste sensor. Seven of the formulations were found to have a bitterness intensity exceeding 1.0 in gustatory sensation tests (evaluated against quinine as a standard) and were therefore assumed to have an unpleasant taste to children. The bitterness intensity scores of the medicines were examined using suspensions in water or an acidic sports drink. In the case of three macrolide antibiotic formulations containing erythromycin (ERYTHROCIN dry syrup), clarithromycin (CLARITH dry syrup for pediatric), and azithromycin (ZITHROMAC fine granules for pediatric use), the bitterness intensities of suspensions in acidic sports drinks were dramatically enhanced compared with the corresponding scores of suspensions in water. This enhancement could be predicted using the taste sensor. On the other hand, a reduction of bitterness intensity was observed for an acidic sports drink suspension of an amantadine product (SYMMETREL fine granules) compared with an aqueous suspension. This reduction in bitterness could also be predicted using the taste sensor output value. Thus, the taste sensor could predict whether or not suspension in an acidic sports drink would enhance or reduce the bitterness intensity of pediatric drug formulations, compared with suspensions in water. (+info)
Disposition of posaconazole following single-dose oral administration in healthy subjects.
(48/353)
Posaconazole is a potent, broad-spectrum triazole antifungal agent currently in clinical development for the treatment of refractory invasive fungal infections. Eight healthy male subjects received a single 399-mg (81.7 microCi) oral dose of [(14)C]posaconazole after consuming a high-fat breakfast. Urine, feces, and blood samples were collected for up to 336 h postdose and assayed for total radioactivity; plasma and urine samples were also assayed for parent drug. Posaconazole was orally bioavailable, with a median maximum posaconazole concentration in plasma achieved by 10 h postdose. Thereafter, posaconazole was slowly eliminated, with a mean half-life of 20 h. The greatest peak in the radioactivity profile of pooled plasma extracts was due to posaconazole, with smaller peaks due to a monoglucuronide, a diglucuronide, and a smaller fragment of the molecule. The mean total amount of radioactivity recovered was 91.1%; the cumulative excretion of radioactivity in feces and in urine was 76.9 and 14.0% of the dose, respectively. Most of the fecal radioactivity was associated with posaconazole, which accounted for 66.3% of the administered dose; however, urine contained only trace amounts of unchanged posaconazole. The radioactivity profile of pooled urine extracts included two monoglucuronide conjugates and a diglucuronide conjugate of posaconazole. These observations suggest that oxidative (phase 1) metabolism by cytochrome P450 isoforms represents only a minor route of elimination for posaconazole, and therefore cytochrome P450-mediated drug interactions should have a limited potential to impact posaconazole pharmacokinetics. (+info)