Comparative pharmacokinetic evaluation of extended release itopride HCl pellets with once daily tablet formulation in healthy human subjects: a two treatment,four period crossover study in fasted and fed condition

Objective: In this study, pharmacokinetics (PKs) and bioavailability of newly developed extended release (ER) Itopride HCl 150?mg encapsulated ER pellets (test) and 150?mg Ganaton ER once-daily (OD) tablets (reference) were compared and evaluated under fasted and fed conditions.

Methods: Twelve healthy human subjects were enrolled in a single dose, randomized; two treatments, two sequences, four period crossover study. A modified and validated liquid chromatographic method was used for the estimation of Itopride HCl in plasma samples. The data were analyzed through non-compartmental model using PK software Phoenix Winnonlin version 7. The outcome was measured on logarithmically transformed data, where p?>?0.05 was considered as non-significant with 90% CI limit of 0.8–1.25.

Results: The C_max, AUC_0–t, and AUC_0–∞ values of Itopride HCl 150?mg ER pellets versus that of OD 150?mg tablets, in fed and fasted states, were within the limits specified by FDA to establish bioequivalence. The relative bioavailability of Itopride HCl 150?mg ER pellets were 1.019 (fed) and 1.081(fasted). The 90% CIs of AUC values for Itopride HCl 150?mg ER pellets and OD 150?mg tablets in fed versus fast were significantly greater and were not within 80–125% limit.

Conclusion: The test and reference formulations had similar pharmacokinetic parameters in each condition studied. However, an increase in the amount of drug was observed in the fed state.     

Heulandite/polyaniline hybrid composite for efficient removal of acidic dye from water; kinetic,equilibrium studies and statistical optimization

Heulandite/polyaniline (HU/PANI) composite was prepared by mechanical mixing from natural heulandite and synthesized polyaniline. HU/PANI was characterized by XRD, SEM, TEM, FT-IR, and UV–Vis spectroscopy. The product is of polycrystalline nature with an average crystallite size of 25.7?nm and optical band gap of 1.69?eV. HU/PANI shows higher efficiency in the removal of light green SF dye than natural HU or PANI in the dark and under artificial illumination. The equilibrium time was attained after 360 and 480?min in the dark and under illumination, respectively. The results fitted well with pseudo second order and Elovich kinetic models. The adsorption isotherm in the dark fitted well with Langmuir isotherm model and the calculated q_max was 44.6?mg/g. Using illumination, the data fitted better with the Freundlich and Temkin model than with the Langmuir model. Based on response surface analysis, the predicted conditions for maximum removal of light green SF dye in the dark (70.9%) were 5.5?mg/L, 24?mg, 3, and 430?min for dye concentration, HU/PANI dose, pH, and contact time, respectively. Whereas, under light illumination (97%) at operating conditions of 15?mg/L, 15?mg, 3, and 589?min, respectively. The composite also shows high efficiencies in the removal of other types of acidic and basic dyes.     

Synthesis,Characterization, and Micellization Behavior of Cationic Surfactants: n-Alkyl-3-Methylpyridinium Bromides and Their Drug Interaction Study by UV–Visible Spectroscopy and Conductometry

The synthesis of new cationic surfactants i.e., n-hexyl-3-methylpyridium bromide ( a ) and n-octyl-3-methylpyridium bromide ( b ), and their characterization using multinuclear nuclear magnetic resonance spectroscopy (NMR) (¹H, ¹³C) and Fourier-transform infrared spectroscopy (FT-IR) spectroscopic techniques were reported. The micellization behavior of the synthesized surfactants was studied using conductometry and ultraviolet–Visible spectroscopy. The critical micelle concentration (CMC) of compounds a and b was found to be 0.41 and 0.35 m mol L⁻¹, respectively. The effect of temperature on the CMC of these compounds was examined in the range of 298–318 K and thermodynamic parameters (ΔG, ΔH, and ΔS) of the micellization process were calculated. The antibacterial study of the synthesized surfactants revealed their strong activity against different bacterial strains. Moreover, the interaction of drugs i.e., flurbiprofen and ketoprofen, with the synthesized surfactants was investigated for gaining insights into the role of micelles as drug-delivery devices. Drug–surfactant interactions were also confirmed via a conductometric method.     

Aldehyde formation in frozen mackerel (Scomber scombrus) in the presence and absence of instant green tea

The effect of frozen storage on lipid peroxidation in Atlantic mackerel (Scomber scombrus) stored for up to 26 weeks at −10 or −80 °C (control), with and without green tea antioxidants, was investigated. Hydroperoxides (PV) and aldehydes (TBARS) were measured by HPLC and LC–MS and hexanal by GC. There was an increase in peroxide value which was associated with an increase in aldehydes, followed by hexanal increase with storage time and at a higher temperature of −10 °C compared with samples stored at −80 °C. Although TBARS is a common assay used to follow malondialdehyde formation, other aldehyde products can also react with thiobarbituric acid to give the red chromogen. Analysis of aldehyde–TBA adducts by LC–MS confirmed the presence of malondialdehyde and, in particular, we report the production of gluteraldehyde for the first time in stored frozen fish. Green tea (at 250 ppm) substantially slowed down the oxidation process, whereas at 500 ppm it was less effective.     

Heterologous Expression of an Unusual Ketosynthase,SxtA, Leads to Production of Saxitoxin Intermediates in Escherichia coli

Paralytic shellfish toxins (PSTs) are neurotoxic alkaloids produced by freshwater cyanobacteria and marine dinoflagellates. Due to their antagonism of voltage-gated sodium channels in excitable cells, certain analogues are of significant pharmacological interest. The biosynthesis of the parent compound, saxitoxin, is initiated with the formation of 4-amino-3-oxo-guanidinoheptane (ethyl ketone) by an unusual polyketide synthase-like enzyme, SxtA. We have heterologously expressed SxtA from Raphidiopsis raciborskii T3 in Escherichia coli and analysed its activity in vivo. Ethyl ketone and a truncated analogue, methyl ketone, were detected by HPLC-ESI-HRMS analysis, thus suggesting that SxtA has relaxed substrate specificity in vivo. The chemical structures of these products were further verified by tandem mass spectrometry and labelled-precursor feeding with [guanidino-¹⁵N₂] arginine and [1,2-¹³C₂] acetate. These results indicate that the reactions catalysed by SxtA could give rise to multiple PST variants, including analogues of ecological and pharmacological significance.     

Encoder-Decoder Based LSTM Model to Advance User <i>QoE</i> in 360-Degree Video

The development of multimedia content has resulted in a massive increase in network traffic for video streaming. It demands such types of solutions that can be addressed to obtain the user's Quality-of-Experience (QoE). 360-degree videos have already taken up the user's behavior by storm. However, the users only focus on the part of 360-degree videos, known as a viewport. Despite the immense hype, 360-degree videos convey a loathsome side effect about viewport prediction, making viewers feel uncomfortable because user viewport needs to be pre-fetched in advance. Ideally, we can minimize the bandwidth consumption if we know what the user motion in advance. Looking into the problem definition, we propose an Encoder-Decoder based Long-Short Term Memory (LSTM) model to more accurately capture the non-linear relationship between past and future viewport positions. This model takes the transforming data instead of taking the direct input to predict the future user movement. Then, this prediction model is combined with a rate adaptation approach that assigns the bitrates to various tiles for 360-degree video frames under a given network capacity. Hence, our proposed work aims to facilitate improved system performance when QoE parameters are jointly optimized. Some experiments were carried out and compared with existing work to prove the performance of the proposed model. Last but not least, the experiments implementation of our proposed work provides high user's QoE than its competitors.