Light-emitting-diode Fourier-transform spectroscopy of HD16O between 11200 and 12400 cm-1

The absorption spectrum of monodeuterated water, HDO has been investigated between 11200 and 12400 cm-1. The spectrum has been recorded using IFS-125M interferometer with spectral resolution of 0.05 cm-1. For measurements White’s-type cell were used. The bright light emitting diode (LED) EDEI-1LS3-R was applied as a source of radiation. Signal to noise ratio was about 104. The spectral line parameters - line positions, intensities and half-widths were obtained by least square fitting. As a result of the spectrum analysis the line list containing more than 1500 lines was created. The spectral line parameters have been compared with the previous measured and calculated data. © (2015) COPYRIGHT Society of Photo-Optical Instrumentation Engineers (SPIE). Downloading of the abstract is permitted for personal use only

Verification of H2O lines from the HITRAN database for remote sensing of the water vapour isotopic composition

The quality of the spectroscopic line parameters from the HITRAN Database for remote sensing of the water vapour isotopic composition of the atmosphere is widely discussed. In this research we show that the HITRAN-2008 data for H2O isotopologues in the near infrared spectral range (4000-6400 cm-1) is reasonably good. The HITRAN data was tested with independent calculation (ab initio et al.). For the evaluation we've used two following criteria: a quality of the fitting of atmospheric spectra measured at the Ural Atmospheric Station (UAS, Kourovka) with the high-resolution Fourier-transform infrared spectrometer and an agreement between the retrieved HDO/H2O relative concentration ratios in the atmospheric column and the results of the simulation of the isotopic general circulation model ECHAM5-wiso (validated for Kourovka region). © (2015) COPYRIGHT Society of Photo-Optical Instrumentation Engineers (SPIE). Downloading of the abstract is permitted for personal use only

Is rat a good model for assessment of particulate-based taste-masked formulations?

Recently there has been an increased interest to develop specialised dosage forms that are better suited to specific patient populations, such as paediatrics and geriatrics. In these patient populations the acceptability of the oral dosage form can be paramount to the products success. However, many active pharmaceutical Ingredients (APIs) are known to cause an aversive taste response. One way to increase the acceptability and to enhance the palatability of the formulation is to design coated taste-masked particulate-based dosage forms. The masking of poorly tasting drugs with physical barriers such as polymer coatings can be utilised to prevent the release of drug within the oral cavity, thus preventing a taste response. However, currently, there are few assessment tools and models available to test the efficiency of these particulate-based taste-masked formulations. The rat brief access taste aversion model has been shown to be useful in assessment of taste for liquid dosage forms. However, the applicability of the rat model for particulate-based taste masked formulations is yet to be assessed. It is not understood whether dissolution, solubility and thus exposure of the drug to taste receptors would be the same in rat and human. Therefore, rat saliva must be compared to human saliva to determine the likelihood that drug release would be similar within the oral cavity for both species. In this study rat saliva was characterised for parameters known to be important for drug dissolution, such as pH, buffer capacity, surface tension, and viscosity. Subsequently dissolution of model bitter tasting compounds, sildenafil citrate and efavirenz, in rat saliva was compared to dissolution in human saliva. For all parameters characterised and for the dissolution of both drugs in rat saliva, a substantial difference was observed when compared to human saliva. This discrepancy in saliva parameters and dissolution of model drugs suggests that preclinical taste evaluation of particulate-based taste-masked formulations suggests rat is not a good model for predicting taste of solid dosage forms or undissolved drug where dissolution is required. Alternative preclinical in vivo models in other species, or improved biorelevant in vitro models should be considered instead

Postprandial administration but not controlled release in the colon increases oral bioavailability of DF030263, a promising drug candidate for chronic lymphocytic leukemia

For treatment of chronic cancers, the oral administration route is preferred as it provides numerous advantages over other delivery routes. However, these benefits of oral chemotherapy can be limited due to unfavorable pharmacokinetics. Accordingly, pharmacokinetic development of chemotherapeutic agents is crucial to the improvement of cancer treatment. In this study, assessment and optimization of biopharmaceutical properties of a promising drug candidate for cyclin-dependent kinase 9 (CDK9) inhibitor (DF030263) was performed to promote oral delivery. Oral bioavailability of DF030263 in fasted rats was 23.8%, and a distinct double-peak phenomenon was observed. A two-site absorption windows mechanism was proposed as a possible explanation to the phenomenon. The two-site absorption window hypothesis was supported by in vitro solubility assays in biorelevant fluids with different pH levels, as well as by in silico simulation by GastroPlusTM. Controlled release to the colon was conducted in rats in order to exploit the colonic absorption window but did not improve the oral bioavailability. On the other hand, oral administration at postprandial conditions in rats (performed based on the high in vitro solubility in fed state simulated fluid and reduced pH-dependency) resulted in an almost 3-fold increase in bioavailability to 63.6%. In conclusion, this study demonstrates an efficient in vitro-in vivo-in silico drug development approach for improving the oral bioavailability of DF030263, a promising candidate for the treatment of chronic lymphocytic leukemia

Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system

The intestinal lymphatic system plays an important role in the pathophysiology of multiple diseases including lymphomas, cancer metastasis, autoimmune diseases, and human immunodeficiency virus (HIV) infection. It is thus an important compartment for delivery of drugs in order to treat diseases associated with the lymphatic system. Lipophilic prodrug approaches have been used in the past to take advantage of the intestinal lymphatic transport processes to deliver drugs to the intestinal lymphatics. Most of the approaches previously adopted were based on very bulky prodrug moieties such as those mimicking triglycerides (TG). We now report a study in which a lipophilic prodrug approach was used to efficiently deliver bexarotene (BEX) and retinoic acid (RA) to the intestinal lymphatic system using activated ester prodrugs. A range of carboxylic ester prodrugs of BEX were designed and synthesised and all of the esters showed improved association with chylomicrons, which indicated an improved potential for delivery to the intestinal lymphatic system. The conversion rate of the prodrugs to BEX was the main determinant in delivery of BEX to the intestinal lymphatics, and activated ester prodrugs were prepared to enhance the conversion rate. As a result, an 4-(hydroxymethyl)-1,3-dioxol-2-one ester prodrug of BEX was able to increase the exposure of the mesenteric lymph nodes (MLNs) to BEX 17-fold compared to when BEX itself was administered. The activated ester prodrug approach was also applied to another drug, RA, where the exposure of the MLNs was increased 2.4-fold through the application of a similar cyclic activated prodrug. Synergism between BEX and RA was also demonstrated in vitro by cell growth inhibition assays using lymphoma cell lines. In conclusion, the activated ester prodrug approach results in efficient delivery of drugs to the intestinal lymphatic system, which could benefit patients affected by a large number of pathological conditions

Light-emitting-diode Fourier-transform spectroscopy of HD16O between 11200 and 12400 cm-1

The absorption spectrum of monodeuterated water, HDO has been investigated between 11200 and 12400 cm-1. The spectrum has been recorded using IFS-125M interferometer with spectral resolution of 0.05 cm-1. For measurements White’s-type cell were used. The bright light emitting diode (LED) EDEI-1LS3-R was applied as a source of radiation. Signal to noise ratio was about 104. The spectral line parameters - line positions, intensities and half-widths were obtained by least square fitting. As a result of the spectrum analysis the line list containing more than 1500 lines was created. The spectral line parameters have been compared with the previous measured and calculated data. © (2015) COPYRIGHT Society of Photo-Optical Instrumentation Engineers (SPIE). Downloading of the abstract is permitted for personal use only

Study of HDO absorption in the 11,200-12,400 cm-1 range using LED-based Fourier transform spectroscopy

A high resolution Fourier transform spectrum of mono-deuterated water vapor was studied between 11,200 and 12,400 cm−1 using a Fourier transform spectrometer with the spectral resolution of 0.05 cm−1, coupled to a multi-pass White-type cell that provided an optical path length of 24 m. A light-emitting diode was used as the radiation source to obtain a measurement signal-to-noise ratio of about 104. The rotational-vibrational assignment of more than 1560 lines was carried out using the VTT variational line list. The parameters of the spectral lines (line centers, intensities and half-widths) were determined by least-squares fitting of the Voigt contour parameters to the experimental data. A total of 584 rotational–vibrational energy levels with maximum rotational quantum numbers of J = 16 and Ka = 9 were determined. For the first time, 64 new energy levels belonging to the nine vibrational states: (032), (112), (301), (141), (410), (221), (330), (061) and (170) were derived from the experiment

Methods Improving Energy Efficiency of Photovoltaic Systems Operating under Partial Shading

This article is devoted to the relevant problem of increasing the efficiency of PV systems. The presented analysis discusses the available methods for improving the power generation of PV modules under partial shading. Mathematical models for power loss calculation were compiled based on the results of this analysis. The proposed approach minimizes the negative impact of partial shading on the energy production of PV modules. It is based on the equalization of voltages of parallel-connected arrays of modules by installing additional power elements in them. The proposed solution is promising for various areas; it allows for the minimization of the unfavorable influence of existing urban objects (buildings, trees, communications, etc.) on the energy efficiency of PV modules. The obtained results are useful for the sustainable development of the urban environment in the context of digital transformation. They are the basis for the promising methodology of the parametric optimization of power plants using renewable energy sources

Study of HDO absorption in the 11,200-12,400 cm-1 range using LED-based Fourier transform spectroscopy

A high resolution Fourier transform spectrum of mono-deuterated water vapor was studied between 11,200 and 12,400 cm−1 using a Fourier transform spectrometer with the spectral resolution of 0.05 cm−1, coupled to a multi-pass White-type cell that provided an optical path length of 24 m. A light-emitting diode was used as the radiation source to obtain a measurement signal-to-noise ratio of about 104. The rotational-vibrational assignment of more than 1560 lines was carried out using the VTT variational line list. The parameters of the spectral lines (line centers, intensities and half-widths) were determined by least-squares fitting of the Voigt contour parameters to the experimental data. A total of 584 rotational–vibrational energy levels with maximum rotational quantum numbers of J = 16 and Ka = 9 were determined. For the first time, 64 new energy levels belonging to the nine vibrational states: (032), (112), (301), (141), (410), (221), (330), (061) and (170) were derived from the experiment

Verification of H2O lines from the HITRAN database for remote sensing of the water vapour isotopic composition

The quality of the spectroscopic line parameters from the HITRAN Database for remote sensing of the water vapour isotopic composition of the atmosphere is widely discussed. In this research we show that the HITRAN-2008 data for H2O isotopologues in the near infrared spectral range (4000-6400 cm-1) is reasonably good. The HITRAN data was tested with independent calculation (ab initio et al.). For the evaluation we've used two following criteria: a quality of the fitting of atmospheric spectra measured at the Ural Atmospheric Station (UAS, Kourovka) with the high-resolution Fourier-transform infrared spectrometer and an agreement between the retrieved HDO/H2O relative concentration ratios in the atmospheric column and the results of the simulation of the isotopic general circulation model ECHAM5-wiso (validated for Kourovka region). © (2015) COPYRIGHT Society of Photo-Optical Instrumentation Engineers (SPIE). Downloading of the abstract is permitted for personal use only