MATERIALS AND METHODS: A randomized, 2-treatment, 2-period, 2-sequence, single dose, crossover with a washout period of 2 weeks, was conducted in 24 healthy Thai male volunteers. Blood samples were collected at 0, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72 and 96 h following drug administration. Plasma concentrations of risperidone and 9-hydroxyrisperidone were determined using a validated LC-MS-MS method. The pharmacokinetic parameters of risperidone and 9-hydroxyrisperidone were determined using a non-compartmental model.
RESULTS: The geometric means ratios (%) and 90% confidence interval (CI) of the test and reference products for the log-transformed pharmacokinetic parameters, Cmax, AUC0-t and AUC0-inf of risperidone were 104.49 % (92.79% - 117.66%), 100.96 % (92.15% - 110.61 %) and 97.99 % (90.72% - 105.85%). The 90% CI of geometric means ratios of the test and reference products for the log-transformed pharmacokinetic parameters, Cmax, AUC0-t and AUC0-inf of 9-hydroxyrisperidone were 97.00%, 96.97% and 97.49%.
CONCLUSIONS: The 90% CI for the geometric means ratios (test/reference) of the log-trasformed Cmax, AUC0-t and AUC0-inf of risperidone and its major active metabolite were within the bioequivalence acceptance criteria of 80% - 125% of the US-FDA.
PATIENTS AND METHODS: With concern over its rising microbial resistance, we explored the association of empiric antibiotics choices with the hospital outcomes of patients treated for microbial proven K. pneumoniae pneumonia in an urban-based teaching hospital.
RESULTS: In 313 eligible cases reviewed retrospectively, hospital mortality and requirement for ventilation were 14.3% and 10.8% respectively. Empiric regimes that had in vitro resistance to at least one empiric antibiotic (n = 90) were associated with higher hospital mortality (23.3% vs. 10.8%, P = 0.004) with risk increased by about two-fold [Odds ratio (OR), 2.5; 95% confidence interval (CI), 1.3 to 4.8]. Regimes (n = 84) other than the commonly recommended "standard" regimes (a beta-lactam stable antibiotic with or without a acrolide) were associated with higher ventilation rates (16.7% vs. 8.8%, P = 0.047) with similar increased risk [OR, 2.0; 95% CI, 1.0 to 4.3].
CONCLUSIONS: Our findings reiterate the clinical relevance of in vitro microbial resistance in adult K. pneumoniae pneumonia and support empiric regimes that contain beta-lactam stable antibiotics.
Aim: Compositional modification of conventional glass ionomer luting cements by incorporating two types of all-ceramic powders in varying concentrations and evaluation of their film thickness, setting time, and strength. Material & Methods. Experimental GICs were prepared by adding different concentrations of two all-ceramic powders (5%, 10, and 15% by weight) to the powder of the glass ionomer luting cements, and their setting time, film thickness, and compressive strength were determined. The Differential Scanning Calorimetry analysis was done to evaluate the kinetics of the setting reaction of the samples. The average particle size of the all-ceramic and glass ionomer powders was determined with the help of a particle size analyzer.
Results: A significant increase in strength was observed in experimental GICs containing 10% all-ceramic powders. The experimental GICs with 5% all-ceramic powders showed no improvement in strength, whereas those containing 15% all-ceramic powders exhibited a marked decrease in strength. Setting time of all experimental GICs progressively increased with increasing concentration of all-ceramic powders. Film thickness of all experimental GICs was much higher than the recommended value for clinical application.
Conclusion: 10% concentration of the two all-ceramic powders can be regarded as the optimal concentration for enhancing the glass ionomer luting cements' strength. There was a significant increase in the setting time at this concentration, but it was within the limit specified by ISO 9917-1:2007 specifications for powder/liquid acid-base dental cements. Reducing the particle size of the all-ceramic powders may help in decreasing the film thickness, which is an essential parameter for the clinical performance of any luting cement.
MATERIALS AND METHODS: The ethanolic extract was used to synthesise copper nanoparticles. The copper nanoparticles were successfully synthesised from copper sulphate solution which was identified by the colour change from dark green colour of the extract. Thus the B.oleracea var acephala is a good source to synthesis copper nanoparticles. The synthesised copper nanoparticles were characterised using Scanning Electron Microscope (SEM) analysis. The SEM image displayed the high-density nanoparticles synthesised by leaf extracts and that the nanoparticles were crystals in shape.
RESULTS: The copper nanoparticles (CNP) bind to the leaf extract. B.oleracea var acephala also has shown the antimicrobial and antioxidant activity. A comparative study was done between ethanolic its crude extract and nanoparticles. Both extracts exhibited zone of inhibition and better antioxidant potential but the CuNPs shows major zone of inhibition and showed more antioxidant activity. Anticancer activity of B.oleracea var acephala against Cervical HeLa cell line was confirmed using ethanolic crude extract and CNP. The results showed that HeLa cells proliferation was inhibited with increasing concentration of ethanolic crude extract and copper nanoparticles. From the results, it was seen that percentage viability of the cancer cells decreased with increased concentration of the samples whereas cytotoxicity against HeLa cell lines increased with the increased concentration of the samples.
CONCLUSION: Thus B.oleracea var acephala possesses anticancer activity against HeLa cell lines.
RESULTS AND DISCUSSION: The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug.
CONCLUSION: Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC50 values were more potent than 5-fluorouracil.
CONCLUSION: Anticancer screening of the synthesized compounds using Sulforhodamine B (SRB) assay demonstrated that compounds 2y (IC50 = 0.01 µmol/mL) and 4y (IC50= 0.02 µmol/mL) have high antiproliferative potential against human colorectal carcinoma cancer cell line than the reference drug (5- fluorouracil) and these compounds also showed best dock score with better potency within the ATP binding pocket and may also be used lead for rational drug designing.