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pharmacokinetics,distribution,and excretion of sodium oligomannate,a recently approved anti-Alzheimer's disease drug in China

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Journal of Pharmaceutical Analysis 2022年第1期12卷 145-155页

作者： Jiaojiao Lu Qiongqun Pan Jieqiang Zhou Yan Weng Kaili Chen Lv Shi Guanxiu Zhu Chunlin Chen Liang Li Meiyu Geng Zhenqing Zhang Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases College of Pharmaceutical SciencesSoochow UniversitySuzhouJiangsu215021China Shanghai Green Valley Pharma.Corp. Shanghai201203China Medicilon Preclinical Research(Shanghai)LLC Shanghai201299China State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai201203China

The National Medical Products Administration has authorized sodium oligomannate for treating mild-to-moderate Alzheimer’s disease.In this study,an LC-MS/MS method was developed and validated to quantitate sodium oligomannate in different biomatrices.The plasma pharmacokinetics,tissue distribution,and excretion of sodium oligomannate in Sprague-Dawley rats and beagle dogs were systematically investigated.Despite its complicated structural composition,the absorption,distribution,metabolism,and excretion profiles of the oligosaccharides in sodium oligomannate of different sizes and terminal derivatives were indiscriminate.Sodium oligomannate mainly crossed the gastrointestinal epithelium through paracellular transport following oral administration,with very low oral bioavailability in rats(0.6%-1.6%)and dogs(4.5%-9.3%).Absorbed sodium oligomannate mainly resided in circulating body fluids in free form with minimal distribution into erythrocytes and major tissues.Sodium oligomannate could penetrate the blood-cerebrospinal fluid(CSF)barrier of rats,showing a constant area under the concentration-time curve ratio(CSF/plasma)of approximately 5%.The cumulative urinary excretion of sodium oligomannate was commensurate with its oral bioavailability,supporting that excretion was predominantly renal,whereas no obvious biliary secretion was observed following a single oral dose to bile duct-cannulated rats.Moreover,only 33.7%(male)and 26.3%(female)of the oral dose were recovered in the rat excreta within 96 h following a single oral administration,suggesting that the intestinal flora may have ingested a portion of unabsorbed sodium oligomannate as a nutrient.

关键词： Sodium oligomannate Alzheimer’s disease pharmacokinetics LC-MS/MS Oligosaccharide

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pharmacokinetics of fucoidan and low molecular weight fucoidan from Saccharina japonica after oral administration to mice

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Journal of Oceanology and Limnology 2023年第5期41卷 1900-1909页

作者： Jiaojiao TAN Yimin SONG Jing WANG Ning WU Yang YUE Quanbin ZHANG Key Laboratory of Experimental Marine Biology Center for Ocean Mega-ScienceInstitute of OceanologyChinese Academy of SciencesQingdao 266071China Laboratory for Marine Biology and Biotechnology National Laboratory for Marine Science and Technology(Qingdao)Qingdao 266237China University of Chinese Academy of Sciences Beijing 100049China Department of Pharmaceutical Engineering Qingdao University of Science and TechnologyQingdao 266000China Laboratory for Marine Drugs and Biological Products National Laboratory for Marine Science and Technology(Qingdao)Qingdao 266237China Nantong Zhongke Marine Science and Technology Research and Development Center Nantong 226000China

The brown seaweed,Sacchairna japonica,has been used in traditional Chinese medicine for over one thousand years.Oral administration of fucoidan or low molecular weight fucoidan(LMWF)from S.japonica could ameliorate kidney dysfunction in chronic kidney diseases and inhibit diabetic vascular complications.In many studies,LMWF was found to be more potent than fucoidan with high molecular weight.However,the pharmacokinetics of LMWF still remains unclear.The purpose of the research is to compare the pharmacokinetics of fucoidan with high molecular weight(136 kDa)with that low molecular weight(9.5 kDa)after oral administration to ICR mice.Since fucose is the main and representative monosaccharide of fucoidans,we evaluate the pharmacokinetics of fucoidan and LMWF by determining the fucose concentration in mice serum.Both fucoidan and LMWF were absorbed following oral administration.Fucoidan and LMWF were provided to mice by oral administration with 60 mg/kg and the maximum Concentration(C_(max))was found at 2.5 h(0.66±0.32 mg/L)for Fucoidan and 1.5 h(1.01±0.56 mg/L)for LMWF,respectively.It seems that LMWF had a higher area under the curve(AUC_(0–t))and was absorbed more quickly than fucoidan.The estimated bioavailability of LMWF was28.3%in the mice treated with a single dose of 30 mg/kg.In addition,LMWF was found widely spreaded into different tissues following oral administration and the highest concentration was found in kidney at 19.93±7.02μg/g.In this study,we first studied the pharmacokinetics of LMWF,in order to help to understand the function of LMWF.And our results shed light on the potential of development of drugs based on LMWF.

关键词： fucoidan low molecular weight fucoidan pharmacokinetics bioavailability tissue distribution

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pharmacokinetics of Enrofloxacin and Its Metabolite in Carp (Cyprinus carpio) After a Single Oral Administration in Medicated Feed

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Journal of Ocean University of China 2023年第1期22卷 171-180页

作者： LIU Ying LI Zhaoxin ZHANG Dahai XING Lihong SUN Weihong SUN Xiaojie PENG Jixing ZHANG Yonggang LI Xianguo College of Chemistry and Chemical Engineering Ocean University of ChinaQingdao 266100China Qingdao Fishery Technology Service Station Qingdao 266071China Qingdao Marine Management Support Center Qingdao 266071China Key Laboratory of Testing and Evaluation for Aquatic Product Safety and Quality Laboratory of Quality&Safety Risk Assessment for Aquatic ProductsMinistry of Agriculture and Rural AffairsYellow Sea Fisheries Research InstituteChinese Academy of Fishery SciencesQingdao 266071China

A precise and reliable analytical method of high performance liquid chromatography-tandem mass spectrometry(HPLCMS/MS)was developed to measure trace levels of enrofloxacin(ENR)and its major metabolite ciprofloxacin(CIP)in carp tissues.Optimized chromatographic separation was obtained on a Waters Xterra MS C_(18) reversed-phase column using gradient elution with methanol and 0.1%formic acid aqueous solution including 5mmolL^(-1) of ammonium acetate.The established method was applied to study the pharmacokinetics and distribution of ENR and CIP in tissues of carp following a single oral administration in feed at a dosage of 40mgkg^(-1) bw(body weight).Data were analyzed using DAS 2.0 dynamics software,and the experimental results suggest that ENR was rapidly absorbed and extensively distributed in carp tissues through systemic circulation,and the pharmacokinetic characteristics can be described with a two-compartment model.The elimination half-lives(t_(1/2β))from muscle,liver,gill,plasma and skin were 131,160,104,132 and 310 h,respectively.The areas under the drug concentration-time curves(AUC)for these tissues were 491,972,750,249 and 706hmgkg^(-1),respectively.The maximum concentration(C_(max))values were 13,29,37,9 and 5mgkg^(-1) with peak times(t_(max))of 8,4,4,2 and 4 h,respectively.Ciprofloxacin,the active metabolite of ENR,was also detected in carp tissues,indicating that only 1.54%of de-ethylation of ENR occurs in carp.At a water temperature of 18℃,the drug withdrawal time was determined to be no less than 24 d while the carp was fed at a single dosage of 40mgkg^(-1).

关键词： Cyprinus carpio enrofloxacin ciprofloxacin pharmacokinetics liquid chromatography-tandem mass spectrometry

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pharmacokinetics and enterohepatic circulation of jervine,an antitumor steroidal alkaloid from Veratrum nigrum in rats

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Journal of Pharmaceutical Analysis 2019年第5期9卷 367-372页

作者： Bingjing Zheng Caihong Wang Wenwen Song Xiaoxia Ye Zheng Xiang School of Pharmaceutical Sciences Wenzhou Medical University

Jervine,a novel steroidal alkaloid from Veratrum nigrum L.,exhibits both antitumor effect and potential toxicity.The aim of study was to characterize the pharmacokinetic behaviors and enterohepatic circulation of jervine in rats.A rapid and simple ultra-high performance liquid chromatography-tandem mass spectrometric method was developed and validated for quantification of jervine and alpinetin (internal standard) in rat plasma.After extraction from rat plasma by a simple protein-precipitation method,the analyte was separated on a C18 column (2.1 mm×50 mm,1.7μm) using water with 0.1%formic acid and acetonitrile as the mobile phase delivered at a flow rate of 0.4mL/min.Jervine and alpinetin were determined in the positive mode with multiple reaction monitoring (MRM) of the ion transitions at m/z426.3→108.8 and m/z 271.0 166.9,respectively.Molecular docking method was used to investigate the binding of jervine to p-glycoprotein and dehydroepiandrosterone sulfotransferase.The method was well validated within acceptance limits including specificity,matrix effect,recovery,precision,accuracy,and stability,and was successfully applied to the pharmacokinetic study of jervine after oral and intravenous administration to rats.Jervine presented a small volume of distribution,fast absorption,high oral bioavailability,and enterohepatic circulation.The enterohepatic circulation was first observed in veratrum alkaloids,and was further investigated by molecular docking studies,which was related to the binding of jervine to p-glycoprotein and dehydroepiandrosterone sulfotransferase.The pharmacokinetic properties and enterohepatic circulation of jervine in rats provided a significant basis for the drug-drug interaction and toxicity study in the future.

关键词： Jervine UPLC-MS/MS pharmacokinetics Enterohepatic circulation

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pharmacokinetics,bioavailability,metabolism and excretion of δ-viniferin in rats

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Acta Pharmaceutica Sinica B 2016年第3期6卷 243-252页

作者： Ping Mao Yinping Lei Tingting Zhang Chen Ma Bo Jin Tong Li Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College

A highly rapid and sensitive liquid chromatographic–electrospray ionization tandem mass spectrometric(LC–ESI-MS/MS) method was developed and validated for the determination of trans-δ-viniferin(Rs-1) in rat plasma, urine and feces. All biological samples were prepared by liquid–liquid extraction and hesperetin was included as an internal standard(IS). Chromatographic separation was achieved on a shim-pack XR-ODS column using a gradient mobile phase. MS/MS detection was performed by negative ion electrospray ionization. The method was sensitive with a lower limit of quantification of 1.42 ng/m L and linear over the range of 1.42–2172 ng/m L in all matrices. The method was applied to study the pharmacokinetics, bioavailability, metabolism, and excretion of Rs-1 in rats following a single oral or intravenous dose. Two metabolites, Rs-1 glucuronide and Rs-1 sulfate, were detected in plasma and in urine after administration of Rs-1. The absolute oral bioavailability of Rs-1 was2.3%, and the total absorption rose to 31.5% with addition of its glucuronide and sulfate metabolites. Only0.09% of the gavaged dose, including Rs-1 and metabolites, was excreted in the urine, while 60.3% was found in the feces in unchanged form. The results indicate that both poor absorption and extensive metabolism were the important factors that led to the poor bioavailability of Rs-1, which can provide a basis for further studies on structural modification and dosage form design.

关键词： Viniferin pharmacokinetics Excretion Metabolism Bioavailability LC–MS/MS

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pharmacokinetics of the prototype and hydrolyzed carboxylic forms of ginkgolides A, B, and K administered as a ginkgo diterpene lactones meglumine injection in beagle dogs

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Chinese Journal of Natural Medicines 2017年第10期15卷 775-784页

作者： WANG Shu-Yao A Ji-Ye FEI Fei GENG Jian-Liang PENG Ying OUYANG Bing-Chen WANG Pei JIN Xiao-Liang ZHAO Yu-Qing WANG Jian-Kun GENG Ting LI Yan-Jing HUA NG Wen-Zhe WANG Zhen-Zhong XIAO Wei WANG Guang-Ji School of Chinese Pharmacy Beijing University of Chinese Medicine Beijing 100102 China Jiangsu Kanion Modern Chinese Medicine Institute Nanjing 210017 China State Key Labonatory of Pharmaceutical New-Techfor Chinese Medicine Jiangsu Kanion Pharmaceutical Co. Ltd. Lianyungang222001 China Key Lab of Drug Metabolism and pharmacokinetics State Key Laboratory of Natural Medicines China Pharmaceutical UniversityNanjing 210009 China

Ginkgo diterpene lactones meglumine injection(GDLI)is a commercially available product used for neuroprotection.However,the pharmacokinetic properties of the prototypes and hydrolyzed carboxylic forms of the primary components in GDLI,i.e.,ginkgolide A(GA),ginkgolide B(GB),and ginkgolide K(GK),have never been fully evaluated in beagle dogs.In this work,a simple,sensitive,and reliable method based on ultra-fast liquid chromatography-tandem mass spectrometry(UFLC-MS/MS)was developed,and the prototypes and total amounts of GA,GB,and GK were determined in beagle dog plasma.The plasma concentrations of the hydrolyzed carboxylic forms were calculated by subtracting the prototype concentrations from the total lactone concentrations.For the first time,the pharmacokinetics of GA,GB,and GK were fully assessed in three forms,i.e.,the prototypes,the hydrolyzed carboxylic forms,and the total amounts,after intravenous administration of GDLI in beagle dogs.It was shown that ginkgolides primarily existed in the hydrolyzed form in plasma,and the ratio of hydrolysates to prototype forms of GA and GB decreased gradually to a homeostatic ratio.All of the three forms of the three ginkgolides showed linear exposure of AUC to the dosages.GA,GB,and GK showed a constant half-life approximately 2.7,3.4,and 1.2 h,respectively,which were consistent for the forms at three dose levels(0.3,1.0,and 3.0 mg·kg^(-1))and after a consecutive injection of GDLI for 7 days(1.0 mg·kg^(-1)).

关键词： Hydrolysates of ginkgolides LC-MS/MS pharmacokinetics Ginkgo diterpene lactones Beagle dog

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pharmacokinetics of H002, a novel S1PR_1 modulator, and its metabolites in rat blood using liquid chromatography–tandem mass spectrometry

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Acta Pharmaceutica Sinica B 2016年第6期6卷 576-583页

作者： Jiaqi Mi Manman Zhao Shu Yang Shuang Yang Jing Jin Xiaojian Wang Qiong Xiao Jinping Hu Yan Li Department of Drug Metabolism Beijing Key Laboratory of Non-Clinical Drug Metabolism and PK/PD StudyKey Laboratory of Active Substances Discovery and Drug Ability Evaluation State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College

A rapid and sensitive liquid chromatography–tandem mass spectrometry(LC–MS/MS) method was developed and validated for the simultaneous determination of H002 and its phosphorylated metabolite, H002-P and hydroxylated metabolite H002-M, in rat blood. H001, an analogue of H002, was used as the internal standard.Blood samples were prepared by simple protein precipitation. The analytes and internal standard were separated on a Zorbax SB-C18 column with a gradient mobile phase consisting of methanol and water containing 0.1% formic acid at a flow rate of 0.2 mL /min with an operating temperature of 20 1C. The detection was performed on a triple quadrupole tandem mass spectrometer with positive electrospray ionization in multiple-reaction monitoring mode.Linear detection responses were obtained from 0.2–100 ng/mL for H002 and H002-M, while 0.5–100 ng/mL for H002-P. The intra- and inter-day precision(RSD%) was within 11.76%, with the accuracy(RE%) ranging from –9.84% to 9.12%. The analytes were shown to be stable during sample storage, preparation and analytic procedures.The method was applied to determine the pharmacokinetics of H002 in rats, and a preliminary study showed that the pharmacokinetics of H002 correlated with its biological effect on peripheral blood lymphocytes.

关键词： S1P receptor S1PR1 modulator Sphingosine-1-phosphate S1P analogue Metabolite LC–MS/MS pharmacokinetics Periphery blood lymphocyte

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pharmacokinetics and correlation between in vitro release and in vivo absorption of bio-adhesive pellets of panax notoginseng saponins

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Chinese Journal of Natural Medicines 2017年第2期15卷 142-151页

作者： LI Ying ZHANG Yun ZHU Chun-Yan Institute of Medicinal Plant Development Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100193China

The present study was designed to prepare and compare bio-adhesive pellets of panax notoginseng saponins(PNS) with hydroxy propyl methyl cellulose(HPMC), chitosan, and chitosan : carbomer, explore the influence of different bio-adhesive materials on pharmacokinetics behaviors of PNSbio-adhesive pellets, and evaluate the correlation between in vivo absorption and in vitro release(IVIVC). In order to predict the in vivo concentration-time profile by the in vitro release data of bio-adhesive pellets, the release experiment was performed using the rotating basket method in p H 6.8 phosphate buffer. The PNS concentrations in rat plasma were analyzed by HPLC-MS-MS method and the relative bioavailability and other pharmacokinetic parameters were estimated using Kinetica4.4 pharmacokinetic software. Numerical deconvolution method was used to evaluate IVIVC. Our results indicated that, compared with ordinary pellets, PNS bio-adhesive pellets showed increased oral bioavailability by 1.45 to 3.20 times, increased Cmax, and extended MRT. What's more, the release behavior of drug in HPMC pellets was shown to follow a Fickian diffusion mechanism, a synergetic function of diffusion and skeleton corrosion. The in vitro release and the in vivo biological activity had a good correlation, demonstrating that the PNS bio-adhesive pellets had a better sustained release. Numerical deconvolution technique showed the advantage in evaluation of IVIVC for self-designed bio-adhesive pellets with HPMC. In conclusion, the in vitro release data of bio-adhesive pellets with HPMC can predict its concentration-time profile in vivo.

关键词： Panax notoginseng saponins Bio-adhesive pellets pharmacokinetics In vivo and in vitro correlation

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pharmacokinetics and pharmacodynamics of Shengjiang decoction in rats with acute pancreatitis for protecting against multiple organ injury

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World Journal of Gastroenterology 2017年第46期23卷 8169-8181页

作者： Lv Zhu Jun-Yi Li Yu-Mei Zhang Hong-Xin Kang Huan Chen Hang Su Juan Li Wen-Fu Tang Sichuan Provincial Pancreatitis Center Department of Integrative MedicineWest China HospitalSichuan University Department of Traditional Chinese Medicine Wuhan Union Hospital

AIM To explore the pharmacokinetics and pharmacodynamics of Shengjiang decoction(SJD) in rats with acute pancreatitis(AP) for protecting against multiple organ injury.METHODS An AP model was established by retrograde perfusion of 3.5% sodium taurocholate into the biliopancreatic duct, and a control group(CG) received 0.9% sodium chloride instead. Twelve male Sprague-Dawley rats were randomly divided into a CG treated with SJD(CG + SJD) and a model group treated with SJD(MG + SJD), both of which were orally administered with SJD(5 g/kg) 2 h after surgery. Blood samples were collected via the tail vein at 10, 20, and 40 min and 1, 2, 3, 4, 6, 8, and 12 h after a single dose of SJD to detect its main components using high-performance liquid chromatography-tandem mass spectrometry. The pharmacokinetic parameters were compared. In the pharmacodynamic experiment, 18 male SpragueDawley rats were randomly divided into a CG, an AP model group(MG), and an SJD treated AP group(SJDG). Serum amylase, lipase, and inflammatory cytokines were measured, and heart, lung, liver, spleen, pancreas, kidney, and intestine tissues were collected for pathological examination.RESULTS The MG + SJD displayed significantly shorter mean residence time(MRT) and higher clearance(CL) for emodin and aloe-emodin; significantly shorter time of maximum concentration and T1/2 and a lower area under curve(AUC) for aloe-emodin; a significantly higher AUC and lower CL for rhein; and longer MRT and lower CL for chrysophanol than the CG + SJD. In the pharmacodynamic experiment, the amylase, interleukin(IL)-6, IL-10, and tumor necrosis factor(TNF)-α levels in the MG were higher than those in the CG(P < 0.05). After the herbal decoction treatment, the SJDG had higher IL-10 and lower TNF-α levels than the MG(P < 0.05). The MG had the highest pathological scores, and the pathological scores of the lung, pancreas, kidney, and intestine in the SJDG were significantly lower than those in the MG(P < 0.05).CONCLUSION AP may have varying effects on the pharmacokine

关键词： Pancreatic distribution Pharmacodynamics Shengjiang decoction pharmacokinetics Acute pancreatitis

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pharmacokinetics of propafenone hydrochloride sustained-release capsules in male beagle dogs

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Acta Pharmaceutica Sinica B 2015年第1期5卷 74-78页

作者： Liping Pan Yafang Qian Minlu Cheng Pan Gu Yanna He Xiaowen Xu Li Ding Department of Pharmaceutical Analysis China Pharmaceutical University

This paper describes the development and validation of a liquid chromatography–mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hydrochloride sustained-release capsule(SR-test), as an instant-release tablet(IR-reference) and as the market leader sustained-release capsule(Rythmol, SR-reference) in male beagle dogs(n ? 8). In Study A comparing SR-test with IR-reference in a crossover design T_(max) and t_(1/2) of propafenone for SR-test were significantly higher than those for IR-reference while C_(max) and AUC were lower demonstrating the sustained release properties of the new formulation. In Study B comparing SRtest with SR-reference the observed C_(max) and AUC of propafenone for SR-test(124.57140.0 ng/m L and612.07699.2 ng·h/m L, respectively) were higher than for SR-reference(78.52772.92 ng/m L and423.67431.6 ng·h/m L, respectively) although the differences were not significant. Overall, the new formulation has as good if not better sustained release characteristics to the market leader formulation.

关键词： Propafenone pharmacokinetics Sustained-release Beagle dog Plasma

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