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1.
The polyethylene glycol (PEG) treatment of ciprofloxacin-Indion 234 complex was aimed to retard rapid ion exchange drug release
at gastric pH. Ciprofloxacin loading on Indion 234 was performed in a batch process, and the amount of K+ in Indion 234 displaced by drug with time was studied as equilibrium constant KDM. Drug-resin complex (DRC) was treated with aqueous PEG solution (0.5%–2% wt/vol) of different molecular weights (MWs) for
2 to 30 minutes. The PEG-treated ciprofloxacin-Indion 234 complex was evaluated for particle size, water absorption time,
and drug release at gastric pH. During drug loading on Indion 234, the equilibrium constant (KDM) increased rapidly up to 20 minutes with efficient drug loading. Increased time of immersion of the drug resinate in PEG
solutions significantly retained higher size particles upon dehydration. The larger DRC particles showed longer water absorption
times owing to compromised hydrating power. The untreated DRC showed insignificant drug release in deionized water; while
at gastric pH, ciprofloxacin release was complete in 90 minutes. A trend of increased residual particle size, proportionate
increase in water absorption time, and hence the retardation of release with time of immersion was evident in PEG-treated
DRC. The time of immersion of DRC in PEG-treated DRC. The time of immersion of DRC in PEG solution had predominant release
retardant effect, while the effect of molecular weight of PEG was insignificant. Thus, PEG treatment of DRC successfully retards
ciprofloxacin ion exchange release in acidic pH. 相似文献
2.
Little is known about the effect of exercise training on the expression of adiponectin receptor genes in peripheral blood mononuclear cells (PBMCs). In this study, we investigated the effects of aerobic training on the expression of AdipoR1 and AidpoR2 mRNAs in PBMCs, whole body insulin sensitivity, and circulating adiponectins in men. Thirty young men were randomly assigned to either a control (n=15) or an exercise (n=15) group. Subjects assigned to the exercise group underwent a 12-week jogging and/or running programme on a motor-driven treadmill at an intensity of 60%-75% of the age-based maximum heart rate with duration of 40 minutes per session and a frequency of 5 days per week. Two-way mixed ANOVA with repeated measures was used to test any significant time-by-group interaction effects for the measured variables at p=0.05. We found significant time-by-group interaction effects for waist circumference (p=0.001), VO2max (p<0.001), fasting insulin (p=0.016), homeostasis model assessment for insulin resistance (HOMA-IR) (p=0.010), area under the curve (AUC) for insulin response during the 75-g oral glucose tolerance test (p=0.002), high-molecular weight (HMW) adiponectin (p=0.016), and the PBMC mRNA levels of AdipoR1 (p<0.001) and AdipoR2 (p=0.001). The exercise group had significantly increased mRNA levels of AdipoR1 and AdipoR2 in PBMCs, along with increased whole body insulin sensitivity and HMW adiponectin, decreased waist circumference, and increased VO2max compared with the control group. In summary, the current findings suggest that exercise training modulates the expression of AdipoR1 and AdipoR2 mRNAs in PBMCs, implying that manipulation of the expression of these genes could be a potential surrogate for lifestyle intervention-mediated improvements of whole body insulin sensitivity and glucose homeostasis. 相似文献
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The purpose of this research was to apply vacuum foam drying (VFD) for processing of LaSota virus and to screen formulation
additives for its stability. The aqueous dispersion of harvest containing sucrose or trehalose in combination with additive
(monosaccharides, polymers, N-Z-amine) was prepared. The diluted dispersions in vials were vacuum concentrated, foamed to
form a continuous structure, and vacuum dried. The products were evaluated for foam characteristics, residual moisture, virus
titer, x-ray diffraction pattern, and stability profile. The foamability increased with solid content in solutions. The foamability
of sucrose was enhanced with incorporation of N-Z-amine (10% and 15% wt/vol) and polyvinyl pyrrolidone (PVP K30, 3% wt/vol).
The fructose- or galactose-containing mixtures were deposited irregularly on the vial surface. The virus titer increased with
disaccharides in the formulation. Sucrose provided better protection than trehalose. Unlike lyophilization, N-Z-amine with
sucrose protected the virus from Millard’s Browning. Amino acids do not have a catalytic effect on hydrolysis of sucrose during
VFD. Monosaccharides were ineffective. A synergistic effect of PVP K30 or polyethylene glycol 6000 (3% wt/vol) with N-Z-amine
provided the maximum virus titer (6.97 and 7.15, respectively). This formulation retained the desired virus potency at 5°,
25°, and 40°C. The diffraction pattern revealed that a threshold concentration of N-Z-amine was required for inhibiting crystallization
of sucrose during VFD. VFD was successfully applied to produce a solid LaSota formulation. The products were amorphous and
did not devitrify on storage.
Published: July 21, 2006 相似文献
5.
Genetic and environmental heterogeneity of residual variance of weight traits in Nellore beef cattle
Background
Many studies have provided evidence of the existence of genetic heterogeneity of environmental variance, suggesting that it could be exploited to improve robustness and uniformity of livestock by selection. However, little is known about the perspectives of such a selection strategy in beef cattle.Methods
A two-step approach was applied to study the genetic heterogeneity of residual variance of weight gain from birth to weaning and long-yearling weight in a Nellore beef cattle population. First, an animal model was fitted to the data and second, the influence of additive and environmental effects on the residual variance of these traits was investigated with different models, in which the log squared estimated residuals for each phenotypic record were analyzed using the restricted maximum likelihood method. Monte Carlo simulation was performed to assess the reliability of variance component estimates from the second step and the accuracy of estimated breeding values for residual variation.Results
The results suggest that both genetic and environmental factors have an effect on the residual variance of weight gain from birth to weaning and long-yearling in Nellore beef cattle and that uniformity of these traits could be improved by selecting for lower residual variance, when considering a large amount of information to predict genetic merit for this criterion. Simulations suggested that using the two-step approach would lead to biased estimates of variance components, such that more adequate methods are needed to study the genetic heterogeneity of residual variance in beef cattle. 相似文献6.
Nagarajan Muthukaman Macchindra Tambe Mahamadhanif Shaikh Dnyandeo Pisal Sanjay Deshmukh Shital Tondlekar Neelam Sarode Lakshminarayana Narayana Jitendra M. Gajera Vidya G. Kattige Srinivasa Honnegowda Vikas Karande Abhay Kulkarni Dayanidhi Behera Satyawan B. Jadhav Girish S. Gudi Neelima Khairatkar-Joshi Laxmikant A. Gharat 《Bioorganic & medicinal chemistry letters》2017,27(11):2594-2601
A series of substituted tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives have been synthesized and their mPGES-1 biological activity has been disclosed in detail. Structure-activity relationship (SAR) optimization provided inhibitors with excellent mPGES-1 potency and low to moderate PGE2 release A549 cell potency. Among the mPGES-1 inhibitors studied, 7, 9 and 11l provided excellent selectivity over COX-2 (>200-fold) and >70-fold selectivity for COX-1 except 11l, which exhibited dual mPGES-1/COX-1 activity. Furthermore, the above tested mPGES-1 inhibitors demonstrated good metabolic stability in liver microsomes, high plasma protein binding (PPB) and no significant inhibition observed in clinically relevant CYP isoforms. Besides, selected mPGES-1 tool compounds 9 and 11l provided good in vivo pharmacokinetic profile and oral bioavailability (%F = 33 and 85). Additionally, the representative mPGES-1 tool compounds 9 and 11l revealed moderate in vivo efficacy in the LPS-induced thermal hyperalgesia guinea pig pain model. 相似文献
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Lipid composition of whole roots of wheat (Triticum vulgare Vill. cv. Svenno Spring Wheat) and oat (Avena sativa L. cv. Brighton) and of cell wall fractions, mitochondrial fractions and microsomal fractions of these roots were studied. Lipid composition depended upon the level of mineral nutrition. In wheat total phospholipids, phosphatidyl choline and sulfolipid content was highest in the roots grown at the higher salt concentration, while the reverse was true for oat roots. In both species glycolipid and sterol content was lower in the high salt roots, at the same time as higher proportions of them were built into the microsomal fraction. Phosphatidyl choline content of the wheat root membrane fractions increased with the salt level, while the opposite occurred in the oat roots. The phosphatidyl choline content may be correlated with the (Ca2+, Mg2+)-stimulated ATPase activity. 相似文献
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Activation by Ca2+, Mg2+, Zn2+, or Mn2+ of adenosine triphosphatases in a microsomal fraction from wheat roots depends upon the growth temperature when the plants are grown under low salt conditions, but not when the plants get a full-strength culture medium. At low ionic strength, cultivation at 25°C gives only half as high activation as cultivation at 18°C or at high ionic strength at both temperatures. Corresponding data for activation of ATPases from oats also show that low ionic strength during growth gives the highest temperature dependence. Low temperature together with low salt conditions during growth gives the highest ATPase activity after stimulation with divalent cations. High growth temperature and full-strength medium decrease the ATPase activity. Activation energies (Ea) were calculated for the two temperature intervals 35–20°C and 20–5°C. The dominating ATPase stimulation (Ca2+ in wheat, Mg2+ in oats) is characterized by high specific activity combined with a low Ea value. The differences in ATPase activity between oats and wheat can be correlated with different cultivation requirements known from agriculture. 相似文献