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1.
Drug Des Devel Ther ; 14: 715-730, 2020.
Article in English | MEDLINE | ID: mdl-32158191

ABSTRACT

INTRODUCTION: Enrofloxacin is used in the treatment of a wide variety of bacterial infections in mammals. However, its poor solubility limits the clinical use. METHODS: In order to improve the solubility of enrofloxacin, the enrofloxacin mesylate (EM) were obtained by a chemical synthesis method. The characterization of EM was carried out using ultraviolet scan (UV), synchronous thermal analysis (SDT), fourier transform infrared spectrometer (FTIR) and mass spectrometry (MS), nuclear magnetic resonance (NMR) and X-ray powder diffraction analysis (XRPD). Acute toxicity of EM in Kunming mice was studied. Besides, pharmacokinetic studies were performed in New Zealand rabbits at a single oral dose of 10 mg/kg, and the antibacterial activity of EM was also evaluated. RESULTS: EM was successfully synthesized and purified. The stoichiometric ratio of mesylate to enrofloxacin was 1:1 and the aqueous solubility of EM was 483.01±4.06 mg/mL, the solubility of EM was about 2000 times higher than enrofloxacin. The oral lethal dose (LD50) of EM was 1168.364 mg/kg, and the pharmacokinetics indicated that the oral relative bioavailability of EM was about 1.79 times and 1.48 times higher than that of enrofloxacin and enrofloxacin hydrochloride, respectively. In addition, the in vitro antibacterial activity of EM was not significantly changed compared with enrofloxacin and enrofloxacin hydrochloride. CONCLUSION: EM has higher solubility, low toxicity for oral use, and increases the oral bioavailability in rabbit. This study may be of benefit for the development of new enrofloxacin drugs.


Subject(s)
Anti-Bacterial Agents/pharmacokinetics , Enrofloxacin/pharmacokinetics , Staphylococcus aureus/drug effects , Animals , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Dose-Response Relationship, Drug , Enrofloxacin/chemical synthesis , Enrofloxacin/chemistry , Mice , Mice, Inbred Strains , Microbial Sensitivity Tests , Molecular Structure , Rabbits , Solubility
2.
Guang Pu Xue Yu Guang Pu Fen Xi ; 36(1): 268-72, 2016 Jan.
Article in Chinese | MEDLINE | ID: mdl-27228780

ABSTRACT

The technology of computational spectral imaging changes the traditional imaging modalities by introducing a coded aperture in the optical path to achieve transformation of the targets spectral imformation, then we can get the spectral data cube by reverse transform. This paper introduces the principle of a push-broom imaging coded aperture computational spectral imager. In practical applications, the matching error between the push speed and the frame rate can affect the accuracy of the spectral data reconstruction. The error terms are deduced based on the model of pushroom, the influences of matching errors to the spectral data reconstruction are anlyzed. And the second spectra derivative and strehl ratio are introduced as the evaluation parameters to, respectively, evaluate the reconstructed spectral and spatial image in the data simulation analysis. It showed that, when the accumulated error of a complete set of data is more than one pixel, the shading dramaticly area's reconstructed results are relatively poor, but the relatively homogeneous regions are affected small; when cumulative error does not exceed half pixel, strehlretio of each channel were above 0.9, and the lower of the spectral energy, the channels strehl ratio smaller, so the more the ranks of the coding template, the higher the platform's stability required.

3.
Guang Pu Xue Yu Guang Pu Fen Xi ; 36(12): 4105-12, 2016 Dec.
Article in Chinese | MEDLINE | ID: mdl-30256586

ABSTRACT

In this paper, a kind of snapshot imaging spectrometer is designed by using image replication based on Wollaston prism. The system includes telephoto lens, collimator lens, Wollaston prism, the imaging lens and compensation filters. With this optical system, we can obtain two-dimensional information at different wavelengths of the same target through one time exposure. When Light beam is passing Wollaston prisms, in order to make sure that the different wavelengths will not overlap, the Wollaston prism needs to be designed with relatively large beam splitting angle. Then the incidence angle of the imaging lens is relatively large. It will increase the difficulty of the imaging lens design. We design, analyze the principle and the characteristics of the snapshot imaging spectrometer using image replication based on Wollaston prism, and design a complete set of imaging spectrometer system. The structure is complex; the aperture of the optical system must be well matched. In order to make sure that we can obtain good image quality through the single lens, but also the whole system, we design the telephoto lens which is imaging telecentric structure, the collimator lens which is objective telecentric structure. We use the multiple structures in ZEMAX to optimize the 16 spectral bands. At 56 lp·mm(-1), the MTF is close to the diffraction limit, the RMS of the SPT is in the Airy disk, proving good image quality.

4.
Guang Pu Xue Yu Guang Pu Fen Xi ; 34(11): 3157-61, 2014 Nov.
Article in Chinese | MEDLINE | ID: mdl-25752078

ABSTRACT

In the present paper, we simulated the system optical magnification error's influence on the quality of reconstructed image, analyzed the variant of the coded aperture with different optical magnification, then proposed an accurate curve of image quality and optical magnification in 128 x 128 code template, which provide important references for the design and development of push-broom coded aperture spectrometer.

5.
Guang Pu Xue Yu Guang Pu Fen Xi ; 33(5): 1401-5, 2013 May.
Article in Chinese | MEDLINE | ID: mdl-23905361

ABSTRACT

In order to get a high compression ratio, according to the spatial dimension correlation and the interference spectral dimension correlation of interference hyperspectral image data, the present article provides a new compression algorithm that combines spectral classification with local DPCM. This algorithm requires spectral classification for the whole interference hyperspectral image to get a classification number matrix corresponding to the two-dimensional space and a spectral classification library corresponding to the interference spectra first, then local DPCM is performed for the spectral classification library to get a further compression. As the first step of the compression, the spectral classification is very important to the compression effect. This article analyzes the differences of compression effect with different standard and different accuracy of classification, the relative Euclidean distance standard is better than the angle standard and the interference RQE standard. Finally, this article chooses an appropriate standard of compression and achieves the combined compression algorithm with programming. Compared to JPEG2000, the compression effect of combined compression algorithm is better.

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