Prediction of in vivo drug performance using in vitro dissolution coupled with STELLA: a study with selected drug products

Prediction of the in vivo performance of the drug product from the in vitro studies is the major challenging job for the pharmaceutical industries. From the current regulatory perspective, biorelevant dissolution media should now be considered as quality control media in order to avoid the risk associated. Physiological based pharmacokinetic models (PBPK) coupled with biorelevant dissolution medium is widely used in simulation and prediction of the plasma drug concentration and in vivo drug performance. The present investigation deals with the evaluation of biorelevant dissolution media as well as in vivo drug performance by PBPK modelling using STELLA® simulation software. The PBPK model was developed using STELLA® using dissolution kinetics, solubility, standard gastrointestinal parameters and post-absorptive disposition parameters. The drug product selected for the present study includes Linezolid film-coated immediate-release tablets (Zyvox), Tacrolimus prolonged-release capsules (Advagraf), Valganciclovir tablets (Valcyte) and Mesalamine controlled-release capsules (Pentasa) each belonging to different biopharmaceutics classification system (BCS). The simulated plasma drug concentration was analyzed and pharmacokinetic parameters were calculated and compared with the reported values. The result from the present investigation indicates that STELLA® when coupled with biorelevant dissolution media can predict the in vivo performance of the drug product with prediction error less than 20% irrespective of the dosage form (immediate release versus modified release) and BCS Classification. Thus, STELLA® can be used for in vivo drug prediction which will be helpful in generic drug development.     

Effect of gamma irradiation on the optical properties of CR-39 polymer

The UV-Visible absorption spectra of virgin and gamma irradiated (20–800 kGy) CR-39 polymer have been deduced by using Shimadzu Double beam Double Monochromator UV-Visible Spectrophotometer (UV-2550). The existence of the peaks, their shifting and broadening as a result of gamma irradiation has been discussed. Finally the indirect and direct band gap in virgin and gamma irradiated CR-39 has been determined. The values of indirect band gap have been found to be lower than the corresponding values of direct band gap.     

Uncertainty Assessment in Cognitive Load for Multiple Object Tracking Based on EEG

Cognitive load varies the attention level, which has serious consequences in complex dynamic situations. Assessment of uncertainty in cognitive load during multiple object tracking task is necessary, as it is used to improve the cognitive capabilities. The present research work investigates the uncertainty in cognitive load of multiple object tracking task using electroencephalograph (EEG) on 25 football players. A d2 test of neuropsychological measure of attention was employed before starting the experiment. Each player participated in four levels of the task with variation in the cognitive load, which varies in terms of the targets from 2 to 5. Percentage changes in the power spectral density were estimated for the cognitive levels. Results show that the percentage changes were much more in high cognitive load than in low cognitive load. Significant changes (p < 0.05) were observed in level 1 (− 11.07 to 1.91%), level 2 (− 3.13 to − 14.51%), level 3 (− 6.33 to − 19.46%) and level 4 (− 8.10 to − 20.88%). Variation in the EEG data in terms of the combined uncertainty corresponds very well with low to high cognitive loads. The fourth level of the task with high cognitive load has more uncertainty than the low cognitive load levels. The results are useful for assessing the cognitive state of the player, which is valuable for the design of the effective training model.     

Effect of calcination conditions of self-sintering mesocarbon microbeads on the characteristics of resulting graphite

Mesocarbon microbeads are now-a-days used as a prominent self-sintering precursor for the production of high density monolithic graphite. The quality of this graphite is highly dependent on the characteristics of these microbeads, such as the quinoline and toluene insoluble contents, -resins content and volatile matter content, which in turn, can be controlled to desired values by suitable treatments of their extraction and calcination. In the present paper, the authors give an account of the study conducted to see the effect of calcination conditions of mesocarbon microbeads on the characteristics of the resulting graphite. A calcination at a temperature in the range of 280–320 °C for 30 min. under an ambient pressure of nitrogen, or at a temperature of 245–310 °C for 10 min. under a reduced pressure (5 cm Hg) of nitrogen, results in mesocarbon microbeads having a quinoline insoluble content of 83.6–89.8%, toluene insoluble content of 94.4–99.7%, -resins content of 6.8–11.9% and a volatile matter content of 10.2–13.5%. Such microbeads have been found to lead to a monolithic graphite possessing a bulk density 1.91–2.02 g cm^–3, bending strength of 62–70 MPa, Shore hardness of 58–69, electrical resistivity of 2.1–2.6 m cm and a degree of anisotropy of 1.02–1.05.     

Highly Sensitive Pulsed Digital Holography for Built-in Defect Analysis with a Laser Excitation

A highly sensitive method is presented for noninvasive defect analysis on thin structures with a Q-switched double-pulsed ruby laser with frequency doubling (347 nm). In our research we feature an all-optical arrangement, where a focused laser pulse derived from the same ruby laser (694 nm) acts as a built-in synchronous excitation source for digital holographic interferometry. The recordings are made with a CCD camera for capturing two holograms (two states of the specimen) corresponding to the two UV laser pulses with a short time separation (10-50 mus). Subtraction of the phase distribution in two digital holograms gives a fringe phase map that shows the change in deformation of the specimen between the recordings. The advantage of the proposed method is two fold. First, the use of a shorter wavelength results in a higher sensitivity. Second, owing to the induced synchronous built-in optical excitation, the specimen is not subjected to any external physical excitation devices. Experimental results are presented on identification and evaluation of defects in thin metal sheets.     

Synthesis of nanocrystalline Ni0.5Zn0.5Fe2O4 ferrite and study of its magnetic behavior at different temperatures

Ni_0.5Zn_0.5Fe₂O₄ ferrite nanocrystals with average diameter in the range of 1–2 nm have been synthesized by reverse microemulsion. X-ray diffraction (XRD), transmission electron microscopy (TEM) and vibrating sample magnetometer (VSM) are used to characterize the structural, morphological and magnetic properties. X-ray analysis showed that the nanocrystals possess cubic spinel structure. The absence of hysteresis, negligible remanence and coercivity at 300 K indicate the superparamagnetic character and single domain in the nanocrystalline Ni_0.5Zn_0.5Fe₂O₄ ferrite materials. The nanocrystalline Ni_0.5Zn_0.5Fe₂O₄ ferrite were annealed at 600 °C. As a result of heat treatment the average particle size increases from 2 nm to 5 nm and the corresponding magnetization values have increased to 21.69 emu/g at 300 K. However, at low temperature of 100 K, the annealed samples show hysteresis loop which is the characteristic of a superparamagnetic to ferromagnetic transition. In addition, a comparative study of the magnetic properties of Ni_0.5Zn_0.5Fe₂O₄ ferrite nanocrystals obtained from reverse microemulsion has been carried out with those obtained from the general chemical co-precipitation route.     

Computer tracking of objects moving in space

A method is developed to represent movement of convex blocks in three-dimensional space from a sequence of two-dimensional camera images. The goals are to determine the objects' movement toward or away from the camera as well as left/right and up/down movement in the image plane and to build models of the blocks. The movement information is used as part of a hierarchical matching process that determines the correspondence of blocks between scenes.