Design and Evaluation of Ginkgolides Gastric Floating Controlled Release Tablets Based on Solid Supersaturated Self-nanoemulsifying.

Ginkgolides are receptor antagonist of platelet activating factor with great clinical prospect, but its application is limited by its low solubility, short half-life and poor alkaline environment stability. It is difficult to solve these problems with a single drug delivery system. In this study, supersaturated self-nanoemulsifying gastric floating tablets of ginkgolides were developed through the combination of solid supersaturated self-nanoemulsifying drug delivery system (solid S-SNEDDS) and gastric retentive floating drug delivery system (GFDDS) to solve these problems of ginkgolides. Solid S-SNEDDS was prepared by D-optimal mixture design, normalization method and single factor experiment. The properties of solid-S-SNEDDS were studied by TEM, PXRD, FT-IR, SEM and in vitro drug release profile. Then, the optimal formulation of stomach floating tablet was obtained through single factor experiment and center composite design, followed by the study of in vitro release, model and mechanism of release, in vitro buoyancy and kinetics of erosion and swelling. PXRD and FT-IR showed that the drug in solid S-SNEDDS existed in an amorphous manner and formed hydrogen bond with excipients. The results showed that the cumulative release of GA and GB in the optimal tablets was 96.12% and 92.57% higher than the simple tablets within 12 h. The release mechanism of the tablet was skeleton erosion and drug diffusion. In 12 h, the optimal tablets can float stably in vitro and release the drug at a constant rate, with a cumulative release of more than 80%. In summary, the combination of SNEDDS and GFDDS is a promising means to solve the problems of ginkgolides.

On the Stability of Nano-formulations Prepared by Direct Synthesis: Simulated Ostwald Ripening of a Typical Nanocrystal Distribution Post-nucleation.

Compared to more traditional top-down processing, the less common route to preparing drug nanocrystals through direct synthesis, e.g., starting with the nucleation of dissolved drug molecules (bottom-up processing), can offer both speed and cost advantages that makes it worthy of investigation. The current, theoretical work puts forth a technical basis and simulated results that could provide additional impetus for conducting further experimental work in this area. Specifically, an asymmetrical particle size distribution generated through the nucleation of a typical small-molecule drug, mirrored after carbamazepine hydrate based on a recent work [Skrdla PJ. J Phys Chem C 116:214-25, 2012], is subject to growth over time by a particle-coarsening mechanism using simulations of Ostwald ripening. Compared to a symmetrical, Gaussian distribution under the same conditions (fixed, relatively low concentration of free drug molecules in solution), it is found that, at longer times, the asymmetrical distribution formed through nucleation broadens more slowly. This finding could represent an additional benefit of synthetic strategies for the preparation of nano-formulations, previously unreported.

High-Efficiency and Ultra-Stable Cesium-Bismuth-Based Lead-free Perovskite Solar Cells without Modification.

Perovskite solar cells (PSCs) have become a new photovoltaic technology with great commercial potential because of their excellent photovoltaic performance. However, the toxicity and poor environmental stability of Pb in Pb-based perovskites limit its large-scale application. Exploring alternatives to Pb is an available approach to develop environmentally friendly PSCs. As an adjacent element of Pb, Bi shows many similar physical and chemical properties; therefore, it is commonly applied for B site substitution in Pb-based PSCs. CsBiSCl2, a new Pb-free perovskite system, was synthesized for the first time as a light absorber. By preparing DMABiS2 as an intermediate, Cs-Bi-based CsBiSCl2 perovskite films with a band gap over 2.012 eV were prepared by introducing CsCl, and the optimal annealing temperature, time, and stoichiometric ratio of the film were explored in this work. The conventional structure of CsBiSCl2 PSCs achieved a power conversion efficiency (PCE) of 10.38%, and the efficiency declined by only 3% after aging in air for 150 days, showing excellent stability, which is one of the most stable devices in inorganic PSCs. This work opens up a new road for the future development of environmentally friendly and commercially stable lead-free PSCs.

Characteristics of a Cavitating Spoiler Mixing Device and Its Performance in a Foam Dust Suppression System.

The unsteady foaming-agent mixing ratio in traditional foam-dust-suppression technology limited the dust suppression efficiency. Recent studies proved that the steady mixing ratio could be guaranteed by keeping the jet pumps or Venturis working under cavitation conditions, but the pressure loss of the current devices was over 50%. To decrease the pressure loss under cavitation conditions, we proposed a new mixing device by introducing a spoiler in the Venturi structure. Through computational fluid dynamics (CFD) simulation, the spoiler structure influence on the downstream flow field and the cavitation cloud structure, which affected the total pressure loss of the device, were revealed. For structure optimization, the effect of the other geometric parameters, including the throat length and divergent angle, on the pressure loss was also studied. The proposed device enhanced the cavitation on the suction tube side of the throat; meanwhile, the cavitation in other parts of the device was avoided. Therefore, the cavitation zone in the proposed device was much smaller than that in current devices, and the pressure loss was reduced significantly. When the flow ratio was 0.5-1%, the critical pressure ratio of the proposed mixing device was 0.71-0.68, which indicated that the pressure loss was only 29%-32%. The laboratory experiment verified that when the proposed device worked under cavitation conditions, the accurate and steady mixing ratio was guaranteed. The field experiment indicated that due to the reduced pressure loss of the proposed device, the required water inlet pressure decreased to 0.29 MPa, and the dust suppression rate increased dramatically. This study was of important value in manipulating cavitation cloud structure using a spoiler, clarifying the influence of the cavitation cloud structure on the liquid mixing performance and expanding the application field of the cavitating mixing method.

Accurate wavelength measurements of a putative standard for near-infrared diffuse reflection spectrometry.

The diffuse reflection (DR) spectrum of a sample consisting of a mixture of rare earth oxides and talc was measured at 2 cm-1 resolution, using five different accessories installed on five different Fourier transform near-infrared (FT-NIR) spectrometers from four manufacturers. Peak positions for 37 peaks were determined using two peak-picking algorithms: center-of-mass and polynomial fitting. The wavenumber of the band center reported by either of these techniques was sensitive to the slope of the baseline, and so the baseline of the spectra was corrected using either a polynomial fit or conversion to the second derivative. Significantly different results were obtained with one combination of spectrometer and accessory than the others. Apparently, the beam path through the interferometer and DR accessory was different for this accessory than for any of the other measurements, causing a severe degradation of the resolution. Spectra measured on this instrument were removed as outliers. For measurements made on FT-NIR spectrometers, it is shown that it is important to check the resolution at which the spectrum has been measured using lines in the vibration-rotation spectrum of atmospheric water vapor and to specify the peak-picking and baseline-correction algorithms that are used to process the measured spectra. The variance between the results given by the four different methods of peak-picking and baseline correction was substantially larger than the variance between the remaining five measurements. Certain bands were found to be more suitable than others for use as wavelength standards. A band at 5943.13 cm-1 (1682.62 nm) was found to be the most stable band between the four methods and the six measurements. A band at 5177.04 cm-1 (1931.61 nm) has the highest precision between different measurements when polynomial baseline correction and polynomial peak-picking algorithms are used.

Discrimination of normal and malignant gastric tissues with FTIR spectroscopy and principal component analysis.

In this paper, the identification of normal and malignant gastric tissues, including 11 cases of cancerous tissues and 10 cases of normal tissues, was investigated using mid-IR spectroscopy and principal componentanalysis (PCA). The results indicated that the difference between cancerous and normal tissues was found in the first principal component. The IR detection and PCA results are in agreement with the biopsy results. The combination of these two methods might provide a new opportunity for clinical application.

Preparation of magnetic microspheres from water-in-oil emulsion stabilized by block copolymer dispersant.

A new method for the preparation of magnetic microspheres is reported. The preparation involved first the dispersion of an aqueous phase, containing magnetite nanoparticles and a water-soluble homopolymer, into droplets in an organic medium using an amphiphilic block copolymer as the dispersant. This was followed by water distillation at a raised temperature from the aqueous droplets to yield polymer/magnetite particles. The structure of the particles was then locked in by a reagent being added to cross-link the water-soluble copolymer block and homopolymer. Since the hydrophobic block of the copolymer consisted of a protected polyester, the removal of the protective moieties from the coronal chains yielded poly(acrylic acid) or other functional polymers to render water dispersibility to the spheres and to enable biomolecule immobilization.

Kinetic modeling of the adsorption rate of a gaseous adsorbate on a granular adsorbent by ultra-rapid-scanning Fourier transform infrared spectrometry.

A novel method for determining the rates of adsorption of gaseous adsorbates on granular adsorbents in the millisecond time regime is described. Mixtures of the adsorbate and nitrogen are passed through a solenoid valve and 100 mg of the adsorbent for periods of (typically) 100 ms. The concentration of the adsorbate passing into a low-volume, long path length gas cell is measured with an ultra-rapid-scanning Fourier transform infrared spectrometer capable of gathering 200 mid-infrared spectra per second with 6-cm(-1) resolution. The pressure of the gas entering the cell is measured simultaneously with a capacitance manometer. A dynamic mathematical model was developed to analyze and describe the results in terms of a Langmuir isotherm. The success of this approach is demonstrated by the estimation of the rate of adsorption of vapor-phase acetaldehyde on aminopropylsilylated granular silica gel.

Kinetic modeling of aldehyde adsorption rates on bare and aminopropylsilyl-modified silica gels by ultra-rapid-scanning fourier transform infrared spectrometry.

Enhancements of a model capable of precisely defining rates of adsorption in terms of a Langmuir isotherm and determined from infrared and pressure data collected in the millisecond time regime are described in detail. Rates of adsorption are determined for formaldehyde and acetaldehyde exposed to bare and aminopropylsilyl-derivatized silica gel. The model fits the collected data by varying the number of adsorption sites and the adsorption and desorption rate constants and determines the best fit based on the measured IR absorbance, partial pressure, exposure backpressure, number of adsorption sites, and time. The rate of adsorption onto irregular-shaped silica gel was faster than the rate onto the corresponding spherical silica gel. Formaldehyde was adsorbed more efficiently than acetaldehyde on APS silica gel than on bare silica gel, whereas acetaldehyde was adsorbed more efficiently than formaldehyde on underivatized silica, indicating the possibility that formaldehyde is adsorbed through the formation of a Schiff base.