JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
·
2019
·Vol. 42
·期 6
·602-608
·
IF 1.175
Mei Zhang,Fang Yang,Hua-jie Yu,Tian-jing Kang,Yong-hui Ding,Meng-li Yu,Qian-kun Wang,Yuan-xin Zhu,Fan Yang
Ceftiofur, a third-generation cephalosporin antibiotic, is being extensively used by pet doctors in China. In the current study, the detection method was developed for ceftiofur and its metabolites, desfuroylceftiofur (DCE) and desfuroylceftiofur conjugates (DCEC), in feline plasma. Then, the pharmacokinetics studies were performed following one single intravenous and subcutaneous injection of ceftiofur sodium in cats both at 5 mg/kg body weight (BW) (calculated as pure ceftiofur). Ceftiofur, DCE, and DCEC were extracted from plasma samples, then derivatized and further quantified by high-performance liquid chromatography. The concentrations versus time data were subjected to noncompartmental analysis to obtain the pharmacokinetics parameters. The terminal half-life ( t 1/2λz ) was calculated as 11.29 ± 1.09 and 10.69 ± 1.31 hr following intravenous and subcutaneous injections, respectively. After intravenous treatment, the total body clearance (Cl) and volume of distribution at steady-state ( V SS ) were determined as 14.14 ± 1.09 ml hr -1 kg -1 and 241.71 ± 22.40 ml/kg, respectively. After subcutaneous injection, the peak concentration ( C max ; 14.99 ± 2.29 μg/ml) was observed at 4.17 ± 0.41 hr, and the absorption half-life ( t 1/2ka ) and absolute bioavailability (F) were calculated as 2.83 ± 0.46 hr and 82.95%±9.59%, respectively. The pharmacokinetic profiles of ceftiofur sodium and its related metabolites demonstrated their relatively slow, however, good absorption after subcutaneous administration, poor distribution, and slow elimination in cats. Based on the time of drug concentration above the minimum inhibitory concentration (MIC) (T>MIC) calculated in the current study, an intravenous or subcutaneous dose at 5 mg/kg BW of ceftiofur sodium once daily is predicted to be effective for treating feline bacteria with a MIC value of ≤4.0 μg/ml.
研究领域:
兽医学
·
药物代谢动力学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES
·
2021
·
IF 1.312
Huanhuan Li,Xuan Yu,Guoqin Zhang,Zhiying Dou,Meng Wang,Yanan Liu,Xiaoliang Ren,Chao Li
Adverse reactions that occur following the injection of traditional Chinese medicines may limit clinical use. A systematic investigation of methods to ensure the safety and stability of traditional Chinese medicine injection was performed using Shenmai Injection as an example. High-performance liquid chromatography with diode-array detection, high-performance liquid chromatography with evaporative light scattering detector, and chemical kinetics were used to study the degradation of the active ingredients (ginsenosides), pharmaceutical excipient (polysorbate 80), and carbohydrates (sucrose, glucose, and fructose) under a variety of pressure conditions (pH, temperature, light, oxidation, and starting concentrations). The main factors affecting the degradation of the ingredients in Shenmai Injection were determined by comparing the differences in the degradation rules of the ingredients in the aqueous solution and Shenmai Injection. Changes in pH of Shenmai Injection were monitored to preliminarily explore the main material factors that lead to its acidification. The results showed that with a pH of <4, the degradation of ginsenosides was accelerated with the enhancement of acidity. In acidic or neutral conditions, the degradation rate of ginsenosides increased with temperature. Alkaline environment, light, and different initial concentrations had no significant effect on the degradation of ginsenosides. For pharmaceutical excipient, increased alkalinity accelerated the degradation of polysorbate 80, which was promoted at high temperatures. The content of polysorbate 80 was almost unchanged in neutral, acidic, and light conditions. The excipient polysorbate 80 had no significant effect on the stability of ginsenosides under acidic or high-temperature conditions. Monosaccharides like glucose and fructose underwent epimerization under certain conditions, and sucrose was hydrolyzed to monosaccharides. Polysorbate 80 and carbohydrates could decrease the pH of the solution under high-temperature conditions, and the acidification of Shenmai Injection was accelerated as the temperature increased. In conclusion, we established a multi-ingredient, multi-factor stability research method. The main factors affecting the degradation of ingredients were clarified, and the stability-related factors causing acidification of Shenmai Injection were preliminarily explored.
研究领域:
药学
·
中药学
·
分析化学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2020
·
IF 3.209
Yanfei Chen,Zhaoliang Hu,Wenzhu Qi,Shuxiao Gao,Jing Jiang,Shixiao Wang,Lei Xu,Xin Xu,Min Song,Taijun Hang
Chinese herbal drugs are often combined with chemotherapy drugs for the treatment of cancers. However, the combination administrations often do not have scientifically sound bases established on full preclinical and clinical investigations. A commonly used anti-colon-cancer herb-drug pair, irinotecan (CPT-11) hydrochloride injection and Kang’ai (KA) injection was taken as an example to investigate the possible pharmacokinetic interactions between Chinese herbal drugs and chemotherapy injections to determine the potential adverse drug reactions (ADRs). Rats were randomly divided into three groups and received 20 mg/kg CPT-11 injection 15 min after administration of 4 mL/kg saline for the CPT-11 single administration group and 4 mL/kg KA injection for the separated co-administration group, respectively. In the pre-mixed co-administration group, rats received a mixture of 20 mg/kg CPT-11 injection and 4 mL/kg KA injection. Blood samples were collected at 10 pre-determined time points between 0 and 24 h. The tissue samples were collected at 5 and 8 min after the injections, respectively. A reliable LC–MS/MS method was established for the simultaneous determination of CPT-11 and its metabolites, SN-38, SN-38 G and APC in the rat plasma and tissue samples, after full confirmation of two injections chemical and stability compatibilities. Compared to the C 0 (5129 ± 757 ng/mL) and AUC 0-t (7858 ± 1307 ng h/mL) of CPT-11 in the CPT-11 single administration group, the C 0 (4574 ± 371 ng/mL) and AUC 0-t (8779 ± 601 ng h/mL) after the separated co-administration remained unchanged, but the pre-mixed co-administration resulted with a significant increased C 0 (29,454 ± 12,080 ng/mL) and AUC 0-t (15,539 ± 5165 ng h/mL) (p < 0.05). Since the exposures of CPT-11 in most tissues in the pre-mixed co-administration group were dramatically lower than the separated co-administration group, the increased CPT-11 plasma concentration may be produced by the delayed tissue distribution because of the encapsulation by the components contained in KA injection, such as polysaccharides. Similar differences were also found in its metabolite, SN-38 G. There are obvious herb-drug interactions between CPT-11 injection and KA injection after the pre-mixed co-administration. The resulting excessive CPT-11 in the plasma may lead to many serious ADRs. Therefore, the full evaluation of herb-drug interactions is necessary and inappropriate combinations should be avoided.
研究领域:
药理学
·
中药学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Chinese Herbal Medicines
·
2016
·
IF 0
Xiao-qian Xu,Ting Geng,She-bing Zhang,Dan-yu Kang,Yan-jing Li,Gang Ding,Wen-zhe Huang,Zhen-zhong Wang,Wei Xiao
Objective Re Du Ning Injection (RDN), a Chinese materia medica injection, is made from the extracts of Lonicerae Japonicae Flos, Gardeniae Fructus, and Artemisiae Annuae Herba. Since last decade, RDN has been widely used in China for the treatment of viral infection, fever, and inflammation. To assess the potential interacting of RDN with co-administered drugs, the inhibitory effects of RDN on the enzyme activities (CYP1A1, CYP1A2, CYP2C11, CYP2D1, and CYP3A1/2) of rat liver microsomes were investigated by a cocktail method. Methods A sensitive and specific LC-MS method capable of simultaneous quantification of five metabolites in rat liver microsomes was developed and validated. Then RDN (0.625%–1.0%) was incubated with rat liver microsomes and specific substrates. The enzyme activities were expressed as the formation rate of the specific metabolites of the substrates (pmol · mg · protein −1 · min −1 ). Results RDN competitively inhibited the activities of CYP1A2 and CYP2C11, with inhibition constant ( K i ) values determined to be 0.18% and 0.63%, respectively. RDN exhibited the mixed inhibition on the activity of CYP2D1, with a K i value of 0.15%. The activities of CYP1A1 and CYP3A1/2 were not markedly inhibited even by 1.0% RDN. Conclusion RDN could inhibit the rat enzyme activities of CYP1A2, 2C11, and 2D1 in vitro with different inhibition modes, which is worthy of promoting safety and efficacy of RDN.
研究领域:
药理学
·
生物化学
✓ 已验证
产品关联
DOI
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY
·
2018
·Vol. 29
·期 7
·1455-1463
·
IF 1.444
Yang Aihong,Zhang Shun,Zhang Lei,Zhong Jingjing,Kou Xiaodi
Both Shuang-Huang-Lian and Xue-Bi-Jing injections are clinically proven efficient and low cost medicines. However, the studies of their chromatographic separation are limited. In this study, a column based on ionic liquid stationary phase was applied for the first time for the analysis of these two injections. For Shuang-Huang-Lian injection, U-shaped plots of retention factors vs. mobile phase constitutions were obtained. This unique kind of separation behavior allowed a flexible adjustment of retention by tuning the mobile phase constituents. Then acids group was analyzed with hydrophilic chromatography mode, while glycosides group was analyzed with reversed phase chromatography mode. Similarly, constituents in Xue-Bi-Jing injection were analyzed with mixed mode high performance liquid chromatography (HPLC). Higher, medium and lower polarity groups were analyzed with hydrophilic interaction, reversed phase and normal phase liquid chromatography modes, respectively. Results from this work provided valuable information for the separation of complicated systems such as traditional Chinese medicine injections.
研究领域:
药学
·
分析化学
✓ 已验证
DOI
高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2024
·Vol. 47
·期 1
·2300545
·
IF 2.8
Chen Yang,Jing-Wen Zhang,Jin Qi,Bo-Yang Yu
Pseudoallergy is a typical and common adverse drug reaction to injections, especially in traditional Chinese medicine injections (TCMIs). At present, the evaluation methods for pseudoallergy include cell methods in vitro and animal methods in vivo. The mast cell evaluation method based on the β-hexosaminidase (β-Hex)-catalyzed substrate, 4-nitrophenyl-β-N-acetyl-D-glucosaminide (4-NPG), is an important method for the evaluation of drug-induced pseudoallergy, but it is prone to false positive results and has insufficient sensitivity. In this study, a novel β-Hex evaluation system with rat basophilic leukemia-2H3 cells based on high-performance liquid chromatography-fluorescence detection (HPLC-FLD) was established, which effectively increased the sensitivity and avoided false positive results. Cell viabilities were measured by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl tetrazolium bromide assay. In addition, a method for the determination of histamine, which is another indicator in the development of pseudoallergy, was established to validate the above method. The results of this novel method indicated that two TCMIs (Shuxuening injection and Shenqi Fuzheng injection), which were considered to be pseudoallergenic using 4-NPG, were not pseudoallergenic. Overall, the novel β-Hex/HPLC-FLD evaluation system using Rat basophilic leukemia-2H3 cells established was effective and precise. It could be used for the evaluation of pseudoallergic reactions caused by TCMIs and other injections.
研究领域:
药理学
·
免疫学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Nanomaterials
·
2022
·Vol. 12
·期 21
·3742
·
IF 5.719
Qiao Li,Xiaosong Zheng,Xiaoyu Shen,Shuai Ding,Hongjian Feng,Guohua Wu,Yaohong Zhang
Colloidal AgBiS2nanocrystals (NCs) have attracted increasing attention as a near–infrared absorbent materials with non–toxic elements and a high absorption coefficient. In recent years, colloidal AgBiS2NCs have typically been synthesized via the hot injection method using hexamethyldisilathiane (TMS) as the sulfur source. However, the cost of TMS is one of the biggest obstacles to large–scale synthesis of colloidal AgBiS2NCs. Herein, we synthesized colloidal AgBiS2NCs using oleylamine@sulfur (OLA–S) solution as the sulfur source instead of TMS and optimized the synthesis conditions of colloidal AgBiS2NCs. By controlling the reaction injection temperature and the dosage of OLA–S, colloidal AgBiS2NCs with adjustable size can be synthesized. Compared with TMS–based colloidal AgBiS2NCs, the colloidal AgBiS2NCs based on OLA–S has good crystallinity and fewer defects.Keywords:AgBiS2;colloidal nanocrystals;hot injection;sulfur source
研究领域:
材料科学
·
化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
·
2024
·
IF 1.5
Fang Yang,Long-Ji Sun,Fan Yang,Shi-Hao Li,Yu-Xin Chen,Wen-Rui Wang
The objective of this study was to determine the pharmacokinetics of enrofloxacin and its metabolite, ciprofloxacin, in Nanyang cattle after a single intravenous (IV), and intramuscular (IM) administration of enrofloxacin at 2.5 mg/kg body weight (BW). Blood samples were collected at predetermined time points. Enrofloxacin and ciprofloxacin concentrations in plasma were simultaneously determined using a high-performance liquid chromatography (HPLC) assay method and subjected to a non-compartmental analysis. After IV administration, enrofloxacin had a mean (±SD) volume of distribution at steady state ( V SS ) of 1.394 ± 0.349 L/kg, a terminal half-life ( t 1/2 λz ) of 3.592 ± 1.205 h, and a total body clearance (Cl) of 0.675 ± 0.16 L/h/kg. After IM administration, enrofloxacin was absorbed relatively slowly but completely, with a mean absorption time (MAT) of 6.051 ± 1.107 h and a bioavailability of 99.225 ± 7.389%. Both compounds were detected simultaneously in most plasma samples following both routes of administration, indicating efficient biotransformation of enrofloxacin to ciprofloxacin. After IV injection, the peak concentration ( C max ) of ciprofloxacin was 0.315 ± 0.017 μg/mL, observed at 0.958 ± 0.102 h. Following IM injection, the corresponding values were 0.071 ± 0.006 μg/mL and 3 ± 1.095 h, respectively. Following IV and IM administration, the conversion ratio of enrofloxacin to ciprofloxacin was calculated as 59.2 ± 9.6% and 31.2 ± 7.7%, respectively. The present results demonstrated favorable pharmacokinetic profiles for enrofloxacin, characterized by complete absorption with relatively slow kinetics, extensive distribution, efficient biotransformation to ciprofloxacin, and prolonged elimination in Nanyang cattle.
研究领域:
兽医药理学
·
动物科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Artificial Cells Nanomedicine and Biotechnology
·
2018
·
IF 3.026
Guotao Li,Yan Liang,Changzhen Sun,Xinyu Peng,Na Hao,Miaochang Liu,Wenxia Gao,Huayue Wu,Bin He
Percutaneous ethanol injection (PEI) therapy was used in liver cancer treatment, however, the therapeutic ethanol in PEI easily flew away from injected solid tumours and hinder the treatment effect. In this paper, injectable supramolecular gels formed by self-assembly of low molecular weight gelators (LMWGs) based on glycylglycine modified phenylboronic acid were prepared to localize ethanol and load chemotherapeutic drug for in situ synergistic therapy. The mechanism, morphology and rheological property of supramolecular gels were characterized by NMR, UV, SEM, etc. The rheological study revealed that the gels were formed in situ rapidly and recovered promptly once damaged. The gels were non-toxicity to both normal 3T3 fibroblasts cells and 4T1 breast cancer cells. Doxorubicin (DOX) hydrochloride and ethanol were encapsulated in the gels for the combination of chemotherapy and PEI therapy. The in vivo anticancer activity of the DOX-loaded gels was carried out in tumour bearing mice. The injected gels were coated around tumour tissues to lock ethanol, and DOX was released sustainingly from the gels to maintain effective concentration to induce the apoptosis of tumour cells. DOX-loaded gels and the ethanol exhibited excellent therapeutic efficacy and low side effects in local cancer therapy.
研究领域:
肿瘤学
·
药剂学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF POLYMER SCIENCE
·
2025
·
IF 3.6
Haihua Wang,Mengfan Yang,Ke Li,Na Li,Ling Song,Mengxi Wang,Meng Wei,Xin Yang,Yushan Liu
At present, the development trend of dressing materials is being multifunctional for convenient and long-term nursing care processes of some complicated and infectious wounds. Here, based on the theory of wound moist healing, we offer a series of injectable and self-healing hydrogels with antibacterial activity (CD/C x G y ). Compared with pure hydrogels, the introduction of CDs significantly shortened the gelation time of CD/C x G y from 1036.3 to 301.6 s and lowered the gelation temperature from 40.1°C to 31.9°C. The excellent syringeability and self-healing behaviors endowed the CD/C x G y hydrogels with personalized repair ability. Moreover, the CD/C x G y hydrogels had an 85% antibacterial rate and made the wound basically completely healed on the 14th day, and compared to the initial, the fluorescence intensity also decreased by 44.49%, which had good application potential in visible monitoring of the wound repair process. This study explored the mechanism by which CDs affect the formation of injectable hydrogels. And establishing the application of CD-functionalized injectable hydrogels in wound repair, providing opportunities for wound visualization monitoring and antibacterial treatment. Graphical We have successfully developed a CD-functionalized hydrogel that possesses remarkable antibacterial properties, outstanding optical characteristics, and excellent biocompatibility. Compared to pure hydrogels, the addition of CDs led to a notable reduction in the gelation time and gelation temperature of the CD-functionalized hydrogel. At the same time, the carbon spot functionalized hydrogel also shows excellent antibacterial and visual repair functions, which provid opportunities for wound visualization monitoring and antibacterial treatment.
研究领域:
生物材料
·
纳米技术
·
生物医学工程
·
伤口愈合
·
抗菌治疗
✓ 已验证
产品关联
DOI
高影响因子
COMPOSITES PART A-APPLIED SCIENCE AND MANUFACTURING
·
2024
·
IF 8.1
Yiwei Zhang,Jiewei Hu,Wenbo Song,Fasheng Zou,Jie Zhang
Polypropylene/elastomer/filler composites are one of the most commonly used materials for spray-free automotive parts to meet the requirements of lightweight. However, its application is serious affected by the flow marks on the surface. Therefore, the reduction or elimination of flow marks defect is important to improve surface quality. In this work, polyolefin elastomer was slightly crosslinked to study its effect on flow marks. The results show that the slightly crosslinking significantly increases the elasticity of elastomer, which makes the melt flow more stable. Meanwhile, the enhanced elasticity is beneficial not only to resist shear deformation of elastomer, but also to recover from deformation during injection molding. As a result, the difference of dispersed phase morphology and surface gloss is reduced, and the flow marks defect is improved. The slightly crosslinked elastomer has little effect on the processability and tensile properties of composites, while the impact properties increase marginally.
研究领域:
材料科学
·
高分子科学
✓ 已验证
产品关联
DOI
高影响因子
EUROPEAN POLYMER JOURNAL
·
2022
·
IF 5.546
Peng An,Hua Wei,Yansheng Zhang,Yang Zhou,Hua Zhang,Wenfeng Li,Baolong Niu,Jing Chen
Injectable hydrogels possess strict requirements of network structure and biocompatibility for cell therapy. It is highly required to load and deliver cells with no damage during the injection operation and accelerate their proliferation after injection at the lesions. Herein, naturally derived chitosan (CS) and hyaluronic acid (HA) were chemically modified to synthesize methylacrylylated chitosan (CSMA) and aldehyde-containing hyaluronic acid (OHA). The imine cross-linkage can be rapidly constructed and reversibly broken between amino and aldehyde groups, endowing the resulting hydrogel with highly efficient mechanical adaptivity, including shearing-thinning and fast self-healing. Besides, the methacrylate groups of CSMA can be cross-linked by photoinitiation, making the dynamic hydrogel with adjustable elasticity and modulus to match the cell culture. The dynamic crosslinked hydrogel demonstrated good compatibility with a wide variety of body cells and bone marrow mesenchymal stem cells (BMSCs). Benefiting from the excellent mechanical adaptivity and cytocompatibility, BMSCs were in situ encapsulated in the dynamic hydrogel and then extruded through a clinically used syringe. Remarkably, the percentage of living cells still reached 87.6% after injection, with no significant cell damage compared with their original state before injection. Moreover, the osteogenic and chondrogenic differentiation abilities of stem cells were not affected by the extrusion injection due to the mechanically adaptive three-dimensional network of the dynamic hydrogel. Taken together, the proposed mechanically adaptive “all-sugar” hydrogels intensify the cell-laden injectability and enhance the long-term viability of cell culture, which shows great potential in the field of cell therapy and tissue engineering.
研究领域:
材料科学
·
生物医学工程
·
细胞治疗
·
组织工程
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）