No abstract

The current study evaluated the stability potential of a transdermal patch composed of eserine and pralidoxime chloride for prophylaxis against (±)-anatoxin A poisoning. The drug combinations were fabricated in an adhesive matrix system supported by a backing membrane and attached to a temporary release liner. Stability testing of the optimized formulation was established for 6 months under accelerated study conditions as per International Conference on Harmonisation guidelines. Results obtained after 6 months showed that the optimized patch formulation was stable with respect to drugs content, pH, diffusion, visual inspection, and other analytical parameters.

The present study was undertaken to investigate the food-drug interaction of carbamazepine (CBZ). Common fruit juices [grapefruit juice (GFJ), lime juice (LJ)], known to inhibit the enzyme cytochrome P450 3A4 (CYP3A4), and some widely consumed beverages [milk (M), black tea (BT)] were involved in this study in the presence of CBZ, as might happen during clinical therapy. The effects of the beverages on the pharmacokinetics and drug-induced toxicity of CBZ was observed after concomitant administration for a period of 28 days. Accordingly, the influence of altered bioavailability of CBZ on its antiepileptic activity was investigated. A significant shift in the C as well as T of CBZ was observed in the presence of LJ and GFJ. This increase in bioavailability significantly enhanced hepatotoxicity and delayed the onset of tremor and piloerection against pentylene tetrazole (PTZ)-induced seizure in experimental animals. However, increased toxicity of CBZ was found to be absent with BT. Thus, from our observation, LJ or GFJ in the presence of CBZ significantly increased the bioavailability of CBZ, which might lead to increased toxicity and antiepileptic activity of the drug.

Gymnema sylvestre is traditionally used for diabetes mellitus. A literature survey revealed very few reports, particularly on rat liver microsomal stability, caco-2 permeability and efflux concerns and its correlation with the bioavailability of gymnemagenin, an important component of G. sylvestre. Therefore, the objective of our study was to investigate the in vitro rat liver microsomal stability and caco-2 permeability along with the efflux of gymnemagenin and establish a probable correlation of these in vitro findings with pharmacokinetic parameters after oral and intravenous administration in rats. Rat liver microsomal stability studies to estimate the in vitro intrinsic half-life, clearance, and Caco-2 permeability after 21 days of culture to determine the apparent permeability from apical to basal and from basal to apical, and efflux ratio of gymnemagenin were performed using liquid chromatography-tandem mass spectrometry. A sensitive, robust bioanalytical method was validated and successfully applied to determine the plasma exposure of gymnemagenin. In vitro rat liver microsomal stability demonstrated that gymnemagenin metabolizes rapidly with a short apparent and intrinsic half-life (~?7?min) and high intrinsic clearance, i.e., 190.08??L/min/mg of microsomes. The results of the Caco-2 study indicated a poor permeability (1.31???10??6?cm/sec) with a very high efflux ratio. The pharmacokinetic study revealed poor oral bioavailability (~?14?%) of gymnemagenin and it was found to have a short half-life and a high clearance in rats. Our in vitro findings indicated low metabolic stability and poor Caco-2 permeability with high efflux, which might have a role in the observed poor oral bioavailability in rats.

Environmental and health safety of recycled slaughterhouse wastes-derived fertilizer and the produce obtained through its application is not well understood. Waste bovine blood and rumen digesta were mixed, cooked and sun-dried to obtain bovine-blood-and-rumen-digesta-mixture (BBRDM, NPK 30.36:1:5.75). 1.26 ± 0.18 log CFU mL −1 fecal coliforms were recovered in BBRDM. E. coli O157:H7, Mycobacteria, Clostridium sp., Salmonella sp., Bacillus sp. and Brucella sp. were absent. No re-growth of pathogens was observed after 60 days storage in sealed bags and in the open. However, prions and viruses were not evaluated. Heavy metals (Pb, Cr, Cd, Cu, Zn, As, Ni, Mn) concentrations in BBRDM were within internationally permissible limits. BBRDM was applied for field cultivation of tomato during 2012-2013 and 2013-2014. Lycopene and nitrate contents of BBRDM-grown tomatoes were higher than Diammonium OPEN ACCESSAgriculture 2015, 5 827 phosphate (DAP) + potash-grown tomatoes because BBRDM supplied 2.5 times more the amount of nitrogen than DAP (NPK 18:46:0) + potash (NPK 0:0:44). Heavy metals and nitrate/nitrite concentrations in tomatoes were within internationally acceptable limits. BBRDM-grown tomatoes showed no mutagenic activity in the Ames test. Sub-acute toxicity tests on Wistar rats fed with BBRDM-grown tomatoes did not show adverse clinical picture. Thus, no immediate environmental or health risks associated with BBRDM and the tomatoes produced were identified.

This study was performed to assess and correlate in vitro drug release with in vivo absorption of prednisolone (PDL) from a colon-targeted tablet prepared by compression coating of core tablet. In vivo drug absorption study was conducted using a high performance liquid chromatographic (HPLC) method, which was developed and validated for the estimation of PDL in rabbit plasma. The calibration curve showed linearity in the concentration range of 0.05 to 50 μg/mL with the correlation coefficient (r) of 0.999. The method was specific and sensitive with the limit of detection (LOD) and lower limit of quantification (LLOQ) of 31.89 ± 1.10 ng/mL and 96.63 ± 3.32 ng/mL, respectively. The extraction recovery (ER) of PDL from three different levels of quality control (QC) samples ranged from 98.18% to 103.54%. In vitro drug release study revealed that less than 10% drug was released in 6.34 h and almost complete (98.64%) drug release was achieved in the following 6 h. In vivo drug absorption study demonstrated lower values of C max, AUCtotal, and protracted T max from compression-coated tablet. The results confirmed the maximum release of drug in the colon while minimizing release in the upper gastrointestinal tract (GIT). An excellent in vitro and in vivo correlation (IVIVC) was also achieved after considering the lag time.

No abstract

No abstract