Ultrasound-assisted preparation of novel ibuprofen-loaded excipient with improved compression and dissolution properties

Context: Most of the active pharmaceutical ingredients (APIs) suffer from a drawback of poor aqueous solubility. In addition to the same, some APIs show poor tabletting behavior creating problems in formulation development. Crystal engineering can be an efficient tool in rectification of such problems associated with the APIs. Thus present work deals with crystallization of ibuprofen (a model drug) onto the surface of dicalcium phosphate (DCP) particles using different techniques.

Objective: The objective of the present work was to prepare ibuprofen-loaded DCP particles and further to analyze them for compressibility and dissolution behavior.

Materials and methods: Various crystallization techniques such as solvent evaporation (SE), melt crystallization (MC), melt sonocrystallization (MSC), antisolvent crystallization (AC), and antisolvent sonocrystallization (ASC) were screened for the preparation of ibuprofen-loaded DCP. Products obtained from different techniques were analyzed for physicochemical, micromeritic and compression properties.

Results and discussion: ASC technique was found to be suitable for preparing directly compressible ibuprofen-loaded DCP particles. The change in the crystal habit (needle to plate shape) of ibuprofen and its crystallization in miniscular form onto the surface of DCP particles showed significant improvement in the dissolution rate and compression properties of ibuprofen due to an increase in specific surface area when compared with ibuprofen crystallized by other techniques. Additionally, the tablets prepared from ASC powder did not require binder since ibuprofen acted as melt binder during compression.

Conclusion: Directly compressible ibuprofen-loaded DCP particles can serve as an alternative for conventional ibuprofen tablets prepared by wet granulation technique.     

Extrusion of Hulled Barley Affecting β-Glucan and Properties of Extrudates

Grits from eight different hulled barley cultivars were subjected to extrusion cooking on a twin screw extruder, and the effect of extrusion variables (temperature and moisture) on β-glucan and physicochemical properties was evaluated. The highest bulk density was observed for extrudates extruded at 150 °C and 20% moisture (low temperature high moisture, LTHM) while the highest expansion was observed for the extrudates extruded at 150 °C and 15% moisture (low temperature low moisture). Extrusion reduced the lightness (L*) of the extrudates and the highest decrease observed for LTHM extrudates. Increasing the feed moisture decreased water solubility index (WSI) significantly while increasing the extrusion temperature significantly increased WSI. The high temperature high moisture (HTHM) extrudates exhibited the highest water absorption capacity. The total β-glucan content was not affected by extrusion cooking, but a significant increase in soluble β-glucan was observed with the highest in high temperature low moisture extrudates. The ratio of soluble to insoluble β-glucan varied from 0.7 to 1.5 in the control barley, but after extrusion cooking, the ratio was changed from 1.2 to 3.1. The β-glucan extractability increased by up to 8% after extrusion with extrudates from HTHM showing the highest extractability. The extent of starch gelatinization varied from 80% to 100% upon extrusion, and the highest was observed in HTHM extrudates. A significant decrease in the peak and final viscosity of the extrudates at all the extrusion conditions was observed.     

Phenolic Content and Antioxidant Activity of Germinated and Cooked Pulses

Five commonly consumed pulses, Mah (Vigna mungo), Green mung (Vigna radiata), Arhar (Cajanas cajan), Masur (Lens esculantus), and Moth (Vigna aconitifolia), were studied for their total phenolic content and antioxidant activity after germination (12 and 24 h) and pressure cooking. Arhar had the highest total phenolic content (6.71 mg ferulic acid/g flour) whereas Moth had the least (1.54 mg/g). All pulses, except Moth, showed a significant decrease in total phenolic content after germination. The antioxidant activity of the pulses varied from 10.61 to 36.38% (DPPH radical scavenging activity), which significantly decreased with germination in all pulses except Moth. The total phenolic content highly correlated with the antioxidant activity in the pulses. Cooking lowered the total phenolic content by 10–45% and antioxidant activity by 27–68% in the control and germinated pulses.     

Spark Plasma Sintering of Nanostructured Aluminum: Influence of Tooling Material on Microstructure

The influence of tooling material, i.e., graphite and WC-Co, on the microstructure of a spark plasma sintering (SPS) consolidated, nanostructured aluminum alloy is studied in this paper. The results show that tooling selection influences microstructure evolution, independent of process parameters. The influence of tooling on microstructure is rationalized on the basis of the following factors: heating rate, electrical current density, localized heating, and imposed pressure. A theoretic framework, based on the physical properties of graphite and WC-Co, is formulated to explain the observed behavior.     

Enhancing the isolation between the strips of dipoles antenna at terahertz frequency with cuboid-shaped graphene layer

Wireless Networks - In this paper, the concept of mantle cloaking method uses to enhance the isolation between the two electrically close dipole antenna at low-terahertz (THz) frequencies, two...     

Metabolites and Genes behind Cardiac Metabolic Remodeling in Mice with Type 1 Diabetes Mellitus

Metabolic remodeling is at the heart of diabetic cardiomyopathy. High glycemic fluctuations increase metabolic stress in the type 1 diabetes mellitus (T1DM) heart. There is a lack of understanding on how metabolites and genes affect metabolic remodeling in the T1DM heart. We hypothesize that differential expression of metabolic genes and metabolites synergistically influence metabolic remodeling preceding T1DM cardiomyopathy. To test our hypothesis, we conducted high throughput analysis of hearts from adult male hyperglycemic Ins2^+/− (Akita) and littermate normoglycemic Ins2^+/+ (WT) mice. The Akita mouse is a spontaneous, genetic model of T1DM that develops increased levels of consistent glycemic variability without the off-target cardiotoxic effects present in chemically- induced models of T1DM. After validating the presence of a T1DM phenotype, we conducted metabolomics via LC-MS analysis and genomics via next-generation sequencing in left ventricle tissue from the Akita heart. Ingenuity Pathway Analyses revealed that 108 and 30 metabolic pathways were disrupted within the metabolomics and genomics datasets, respectively. Notably, a comparison between the two analyses showed 15 commonly disrupted pathways, including ketogenesis, ketolysis, cholesterol biosynthesis, acetyl CoA hydrolysis, and fatty acid biosynthesis and beta-oxidation. These identified metabolic pathways predicted by the differential expression of metabolites and genes provide the foundation for understanding metabolic remodeling in the T1DM heart. By limited experiment, we revealed a predicted disruption in the metabolites and genes behind T1DM cardiac metabolic derangement. Future studies targeting these genes and metabolites will unravel novel therapies to prevent/improve metabolic remodeling in the T1DM heart.     

Lead sorption onto ferrihydrite. 3. Multistage contacting

Few studies have demonstrated the practical application of surface complexation models, calibrated with fundamental macroscopic and spectroscopic metal sorption data, in helping to solve industrial trace metal emissions problems. In this work, multistage ferrihydrite sorption systems are evaluated for their effectiveness in reducing single-solute lead(II) [Pb(II)] concentrations in contaminated water streams to very low levels. Experimental data and modeling results indicate that a multistage sorption system can significantly reduce Pb(II) effluent concentrations for the same total amount of sorbent or, alternatively, dramatically lower total sorbent consumption for the same effluent Pb(II) concentration. Model predictions were generated using a steady-state, multistage, equilibrium adsorber model that was specifically developed for and integrated into 0LI Systems' Environmental Simulation Program. The modified triple-layer model was used to simulate Pb(II) surface-liquid equilibria within the adsorber model. Engineering screening evaluations indicate that a 2-3-stage sorption process can provide significant economic savings when compared to a 1-stage process operating with the same target effluent Pb(II) concentration. Additional equilibrium stages beyond 2 or 3 provide diminishing economic returns. The major economic driver for multiple contacting stages is reduced capital investment and operating costs for sludge handling, dewatering, and disposal.     

利用基于扫描相机的荧光寿命成像显微技术研究细胞周期

利用基于扫描相机的荧光寿命成像显微系统,以细胞周期为模型,研究转染绿色荧光蛋白的HeLa细胞的荧光寿命。结果表明,处于周期内不同进程的细胞的荧光寿命为2.50~3.00 ns。处于分裂期的细胞的荧光寿命在1 h内从2.86 ns下降到2.82 ns;在DNA合成前期的8 h内,荧光寿命从2.82 ns下降到2.78 ns。荧光寿命的差异反映了细胞周期中核浆内大分子浓度的变化,对了解细胞周期的分子机制有一定的意义。     

Identifying and predicting adolescent smokers' developmental trajectories.

Very few studies have defined trajectories of smoking. In the present study, we modeled growth in adolescent smoking and empirically identified prototypical trajectories. We conceptualized escalation of smoking as a growth process and modeled rates of change and heterogeneity of these patterns using latent growth mixture modeling. The analysis identified six trajectories with low ambiguity about group membership (early rapid escalators, late rapid escalators, late moderate escalators, late slow escalators-smokers, stable puffers, and late slow escalators-puffers). A trajectory of quitters was not identified. We also examined predictors of the smoking trajectories. The predictors were assessed across the adolescent years and included variables related to smoking and other substance use, as well as a range of variables related to sociodemographic factors and mental health. Observed change in the pattern of predictors across age has implications for the mechanism of effect of these variables in relation to smoking trajectories, including predictors that differentiated among daily smokers, variables that may determine the trajectory (e.g., friends smoking), and variables that may result from the trajectory (e.g., marijuana use, less attachment to friends).