JOURNAL OF VETERINARY MEDICAL SCIENCE
·
2018
·
IF 0.803
Xinrui DONG,Xueye SHU,Yingnan WANG,Zhaohuan NIU,Shixia XU,Yue ZHANG,Shuchun ZHAO
Valnemulin, successfully developed by Sandoz in 1984, is a new generation derivative of pleuromutilin related to tiamulin. Valnemulin has low water-solubility, a short half-life period, low bioavailability, and instability. The application of valnemulin was restricted. Therefore, finding a more moderate delivery system is necessary to improve the shortcomings of valnemulin. The purpose of the study was to improve the strong stability and the irritation caused by of valnemulin hydrochloride power through pegylated-valnemulin prodrug mode. The prepared pegylated-valnemulin prodrug was characterized and evaluated by in vitro release performance under buffer solutions with pH levels of 7.4 and 3.6. The loading rate of valnemulin in PEG-succinic-valnemulin prodrug was determined by ultraviolet spectrophotometer and high performance liquid chromatography (HPLC). HPLC with evaporative light scattering detector was applied to determine the amount of PEG-succinic acid. The loading rate of valnemulin in PEG-succinic-valnemulin prodrug was 6.46%. PEG-succinic-valnemulin prodrug demonstrated a satisfactory solubility of valnemulin with 523 mg·ml−1 and excellent stability verified by the stability experiment. The result of the in vitro release test showed that the prepared PEG-valnemulin prodrug has controlled release ability and the release rate of valnemulin from PEG-valnemulin prodrug with a pH of 7.4 was 64.98%, which was higher than that of pH3.6 with release rate of 31.90%. Therefore, the prepared PEG-succinic-valnemulin prodrug has great application potential.
研究领域:
药学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Current Drug Delivery
·
2022
·Vol. 19
·期 3
·337-346
·
IF 3.758
Liang Yongjie,Hu Danlei,Yan Yuanyuan,Chen Dongmei,Xie Shuyu
Background: The bitter taste and strong irritation of valnemulin hydrochloride limit its wide clinical application in pigs by oral. Method: In order to improve its palatability and residence time in the body, the valnemulin hydrochloride taste-masking granules with sustained-release
were prepared by combining solid dispersion based on fatty acid with wet granulation. The formulation was screened by orthogonal test with content, yield, grain size and angle of repose as evaluation indexes. Result: The results showed that the optimal granules were composed of corn starch,
sucrose, citric acid, valnemulin hydrochloride and myristic acid at a ratio of 40: 20: 20: 11: 19. The daily feed intake of pigs in the optimum taste-masking granule groups was similar to that of its self-control, and significantly higher than that in the valnemulin hydrochloride active ingredient
group, suggesting that the optimum granules have satisfactory palatability. The prepared granules improved the oral bioavailability of valnemulin hydrochloride by 3.04 folds and extended its mean residence time (MRT) by 2.33 folds. Conclusion: The granules developed in this study could
obviously improve the palatability and sustained release of valnemulin hydrochloride. The producing method of granules by combining solid dispersion powder with wet granulation can provide ideas for other drugs with poor palatability and a short half-life.
研究领域:
药学
·
兽医学
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
Crystals
·
2019
·Vol. 9
·期 12
·675
·
IF 2.061
Jinbo Ouyang,Jian Chen,Limin Zhou,Fangze Han,Xin Huang
To improve the physicochemical properties of valnemulin (VLM), different solid forms formed by VLM and organic acids, including tartaric acid (TAR), fumaric acid (FUM), and oxalic acid (OXA), were successfully prepared and characterized by using differential scanning calorimetry (DSC), scanning electron microscope (SEM), X-ray powder diffraction (XRPD), and Fourier-transform infrared spectroscopy (FT-IR). The excess enthalpyHexbetween VLM and other organic acids was calculated by COSMOthermXsoftware and was used to evaluate the probability of forming multi-component solids between VLM and organic acids. By thermal analysis, it was confirmed that multi-component solid forms of VLM were thermodynamically more stable than VLM itself. Through dynamic vapor sorption (DVS) experiments, it was found that three multi-component solid forms of VLM had lower hygroscopicity than VLM itself. Furthermore, the intrinsic dissolution rate of VLM and its multi-component forms was determined in one kind of acidic aqueous medium by using UV-vis spectrometry. It was found that the three multi-component solid forms of VLM dissolved faster than VLM itself.Keywords:valnemulin;solid forms;dissolution rate;hygroscopicity
研究领域:
药学
·
物理化学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF FOOD SCIENCE
·
2020
·Vol. 85
·期 6
·1681-1688
·
IF 2.479
Guanqiong Na,Xiaofei Hu,Yaning Sun,Sharon Kwee,Guangxu Xing,Yunrui Xing,Gaiping Zhang
Valnemulin (VAL) and tiamulin (TIA) are pleuromutilin antibiotics used primarily for treating bacterial infections in swine or other food animals. Furthermore, VAL and TIA are also employed as feed additives to promote animal growth. However, the illegal use of VAL and TIA could cause a series of hazards to consumers. Here, VAL was designed to be conjugated with bovine serum protein to prepare immunogen. A highly sensitive monoclonal antibody that recognized both VAL and TIA has been successfully produced. Moreover, an immunochromatographic strip assay for rapidly screening VAL and TIA in porcine liver was established with visual detection limits (cutoff values) of 50 and 25 ng/g, respectively. The IC 50 values calculated from the equation of the standard curve were 6.06 and 3.45 ng/g and the limits of detection were 0.96 and 0.29 ng/g for VAL and TIA. According to the recovery experiment results, the test strip exhibited acceptable accuracy and precision. Generally, the proposed strip provided a practical tool for the detection of VAL and TIA. Practical Application We produced a highly sensitive monoclonal antibody and developed an immunoassay strip for simultaneously monitoring TIA and VAL. Additionally it was preliminarily confirmed that the rapid detection tool was suitable for screening TIA and VAL in porcine liver.
研究领域:
兽医学
·
分析化学
·
食品安全
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）