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Determination of Loratadine in Human Plasma by High Performance Liquid Chromatography-Electrospray Mass Spectrometry and Studies on Its Pharmacokinetics and Relative Bioavailability 被引量:3
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作者 陈钧 高科攀 +5 位作者 史振祺 陆伟 蒋新国 荣征星 黄霞 陈红专 《Journal of Chinese Pharmaceutical Sciences》 CAS 2002年第4期137-141,共5页
A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined ... A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4~100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%~104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets. 展开更多
关键词 LORATADINE HPLC MS pharmacokinetics bioavailability
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Pharmacokinetics and Relative Bioavailability ofsustained-release Tablets of Diclofenac Sodiumin Male Volunteers
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作者 季爱民 邹恒琴 +1 位作者 张忠义 车瓯 《Journal of Chinese Pharmaceutical Sciences》 CAS 1995年第1期8-11,共4页
The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assay... The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet. 展开更多
关键词 Diclofenac sodium pharmacokinetics SUSTAINED-RELEASE ENTERIC-COATED Rela- tive bioavailability
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The chemical characteristics of different sodium iron ethylenediaminetetraacetate sources and their relative bioavailabilities for broilers fed with a conventional corn‑soybean meal diet
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作者 Shengchen Wang Bingxin Wu +8 位作者 Ling Zhu Weiyun Zhang Liyang Zhang We Wu Jiaqi Wu Yun Hu Tingting Li Xiaoyan Cui Xugang Luo 《Journal of Animal Science and Biotechnology》 SCIE CAS CSCD 2024年第2期826-843,共18页
Background Our previous studies demonstrated that divalent organic iron(Fe)proteinate sources with higher complexation or chelation strengths as expressed by the greater quotient of formation(Qf)values displayed highe... Background Our previous studies demonstrated that divalent organic iron(Fe)proteinate sources with higher complexation or chelation strengths as expressed by the greater quotient of formation(Qf)values displayed higher Fe bioavailabilities for broilers.Sodium iron ethylenediaminetetraacetate(NaFeEDTA)is a trivalent organic Fe source with the strongest chelating ligand EDTA.However,the bioavailability of Fe when administered as NaFeEDTA in broilers and other agricultural animals remains untested.Herein,the chemical characteristics of 12 NaFeEDTA products were determined.Of these,one feed grade NaFeEDTA(Qf=2.07×10^(8)),one food grade NaFeEDTA(Qf=3.31×10^(8)),and one Fe proteinate with an extremely strong chelation strength(Fe-Prot ES,Qf value=8,590)were selected.Their bioavailabilities relative to Fe sulfate(FeSO_(4)·7H_(2)O)for broilers fed with a conventional corn-soybean meal diet were evaluated during d 1 to 21 by investigating the effects of the above Fe sources and added Fe levels on the growth performance,hematological indices,Fe contents,activities and gene expressions of Fe-containing enzymes in various tissues of broilers.Results NaFeEDTA sources varied greatly in their chemical characteristics.Plasma Fe concentration(PI),transferrin saturation(TS),liver Fe content,succinate dehydrogenase(SDH)activities in liver,heart,and kidney,catalase(CAT)activity in liver,and SDH mRNA expressions in liver and kidney increased linearly(P<0.05)with increasing levels of Fe supplementation.However,differences among Fe sources were detected(P<0.05)only for PI,liver Fe content,CAT activity in liver,SDH activities in heart and kidney,and SDH mRNA expressions in liver and kidney.Based on slope ratios from multiple linear regressions of the above indices on daily dietary analyzed Fe intake,the average bioavailabilities of Fe-Prot ES,feed grade NaFeEDTA,and food grade NaFeEDTA relative to the inorganic FeSO_(4)·7H_(2)O(100%)for broilers were 139%,155%,and 166%,respectively.Conclusions The bioavailabilities of organic Fe sources relative to FeSO_(4)·7H_(2)O were closely related to their Qf values,and NaFeEDTA sources with higher Qf values showed higher Fe bioavailabilities for broilers fed with a conventional corn-soybean meal diet. 展开更多
关键词 BROILERS Chelation strengths Fe-containing enzymes NAFEEDTA relative bioavailabilities
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Enhancement in Bioavailability of CurCousin®, A Minor Metabolite from Curcuma longa by Addition of BioPerine® —A Pharmacokinetic Study
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作者 Muhammed Majeed Kalyanam Nagabhushanam +2 位作者 Sarang Bani Anjali Pandey Smitha Thazhathidath 《Journal of Biosciences and Medicines》 2024年第2期282-293,共12页
In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary m... In recent years, metabolic syndrome has been a growing health concern across the world. The role of nutraceuticals and functional foods in this area has a significant place due to the adverse effects of contemporary modes of treatment. CurCousin<sup>®</sup> is a nutritional ingredient containing bioactive Calebin A, (analog of Curcumin) with self-affirmed GRAS status. CurCousin<sup>®</sup> has been a clinically studied dietary supplement ingredient with a positive impact on body weight, lipid levels and metabolic health. Bioenhancers play an important role in increasing the bioavailability of the active in turn enhancing efficacy as well as reducing the dosage required to achieve the therapeutic effect. This study investigated the possible pharmacokinetic interaction between CurCousin<sup>®</sup> at two different doses (2.25 and 4.5 mg/kg) in the presence and absence of BioPerine<sup>®</sup> (0.27 mg/kg), a natural bioenhancer in Sprague-Dawley rats. The results revealed that the addition of BioPerine<sup>®</sup> into CurCousin<sup>®</sup> (2.25 mg/kg) half the dose when administered enhances the bioavailability and was equipotent to CurCousin<sup>®</sup> (4.5 mg/kg) double the dose without BioPerine<sup>®</sup>. Thus, leading to future clinical studies to evaluate its improved pharmacological efficacy as well as reduced therapeutic dosage. 展开更多
关键词 Metabolic Health bioavailability pharmacokinetics CurCousin® BioPerine® Calebin A
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Study on the Pharmacokinetics and Relative Bioavailability of Irbesartan Capsules in Healthy Volunteers 被引量:2
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作者 顾世芬 陈汇 +2 位作者 邱应海 师少军 曾繁典 《Journal of Huazhong University of Science and Technology(Medical Sciences)》 SCIE CAS 2002年第1期14-16,共3页
The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomiz... The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomized 2 way crossover study. The concentrations in plasma were determined by HPLC UV method. The main parameters of irbesartan capsules were: C max : 1.502±0.295 μg/ml, t max : 1.44±0.34 h, t 1/2 : 20.21±14.71 h, AUC 0 t : 11.087±3.443 μg/ml -1 ·h. The relative bioavailability of capsule to tablet was (101.4±28.9) %. The results of statistical analysis showed that two formulations were bioequivalent. 展开更多
关键词 IRBESARTAN pharmacokinetics bioavailability HPLC
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HPLC Determination of Captopril in Human Plasma with Pre-column Derivation and Solid-phase Extraction and Studies on Its Pharmacokinetic and Relative Bioavailability
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作者 丁劲松 张毕奎 +2 位作者 李焕德 刘义钊 邓航 《Journal of Chinese Pharmaceutical Sciences》 CAS 2001年第3期152-156,共5页
A new pre-column derivation HPLC method with solid-phase extraction to determine captopril in human plasma was established. Derivation products were extracted by a solid-phase extraction method after the reagent, p-a-... A new pre-column derivation HPLC method with solid-phase extraction to determine captopril in human plasma was established. Derivation products were extracted by a solid-phase extraction method after the reagent, p-a-dibromoacetophenone(p-BPB), was added in the plasma samples. The samples were analyzed in a VP-ODS column with UV-detector. The calibration curve of captopril was linear within the range of 5~1000 ngmL-1 with r=0.9987, the recovery of this method was 98.652.04%, within day and between day RSD were no more than 3.4% and 8.4% respectively. To study the pharmacokinetics and the relative bioavailability of captopril tablets, two formulations of captopril tablets were given to 18 healthy male volunteers according to a randomized 2-way cross-over design with a 1-week washout period. The respective AUC0~6 , Cmax and Tmax values of the two formulations were 424.5125.7 and 439.4113.3 mghL-1; 505.9244.6 and 504.8172.2 mgL-1; 0.6620.181 and 0.5280.176 h. Results from statistics analysis showed that there were no significant difference between the AUC0~6 , Cmax and Tmax values of the two formulations, The relative bioavailability of tablets I with respect to II was 96.114.6% from AUC0~6 measurement. Bioequivalance was observed between the two tablets. 展开更多
关键词 CAPTOPRIL Solid-Phase Extraction HPLC pharmacokinetics bioavailability
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Pharmacokinetic Study of Ipriflavone in Healthy Volunteers by HPLC and Determination of the Relative Bioavailability of Its Tablet Preparation
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作者 马晓红 刘天培 《The Journal of Biomedical Research》 CAS 1997年第1期34-37,共4页
Two kinds of Ipriflavone tablets (IP) were orally cross administered to 8 healthy volunteers. The serum level of IP at different time was determined by HPLC, 3P87 pharmacokinetic package was used in the analysis of ... Two kinds of Ipriflavone tablets (IP) were orally cross administered to 8 healthy volunteers. The serum level of IP at different time was determined by HPLC, 3P87 pharmacokinetic package was used in the analysis of the time course of serum concentration and it had shown that the data well fitted a 2 compartment model. Pharmacokinetic parameters and area under curve (AUC) were calculated. The relative bioavailability of Tabellae IP made in China vs that made in Japan (as a reference) was 1.003( P >0.05). The values of AUC T max and C max of the two preparations were also comparable by the statistical analysis, so they were bioequivalent. 展开更多
关键词 tabellae ipriflavone HPLC BIOEQUIVALENCE pharmacokinetics relative bioavailability
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Pharmacokinetics and Bioavailability of 2-Amino-6-Cyclopropylamino-9-(2,3 -Dideoxy-β-D-glyceropent-2-enofuranosyl) Purine (Cyclo-D4G) in Rats
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作者 刘薏 杨振军 +2 位作者 BOUDINOT F.Douglas CHU Chung Kuang 张礼和 《Journal of Chinese Pharmaceutical Sciences》 CAS 2004年第1期37-41,共5页
AimTo characterize the pharmacokinetics of 2 -amino-6-cyclopropylamino-9-(2,3-dideoxy-β-D-glyceropent-2-enofuran osyl) purine (Cyclo-D4G) following intravenous administration and oral administ ration to rats. Methods... AimTo characterize the pharmacokinetics of 2 -amino-6-cyclopropylamino-9-(2,3-dideoxy-β-D-glyceropent-2-enofuran osyl) purine (Cyclo-D4G) following intravenous administration and oral administ ration to rats. MethodsThe concentrations of Cyclo-D4G in rat (Sprague-Dawley male rats) plasma and urine were analyzed by high performance liquid chromatography (HPLC). ResultsFollowing intravenous adm inistration to rats, concentrations of Cyclo-D4G in plasma declined with a term inal phase half-life of 0 78±0 14 h (±s). Total clearance was 0 90±0 21 L·h -1 ·kg -1 . Renal excretion of unchanged Cyclo-D4G accounted for approximately 20% of total clearance. Steady state volume of distr ibution was 0 91±0 07 L·kg -1 . After oral administration to rats, conce ntrations of Cyclo-D4G in plasma declined with a terminal phase half-life of 0 83±0 13 h (±s). Total clearance was 3 81±2 03 L·h -1 ·kg -1 . Renal excretion of unchanged Cyclo-D4G accounted for approximat ely 9% of total clearance. Oral bioavailability of Cyclo-D4G in rat was 26 9%. ConclusionThe favorable pharmacokinetic profiles and lower to xicity provide support for further development of Cyclo-D4G clinical trials. 展开更多
关键词 pharmacokinetics bioavailability HPLC analysi s D4G prodrug
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Quantitative determination of D_(4)-cystine in mice using LC-MS/MS and its application to the assessment of pharmacokinetics and bioavailability 被引量:1
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作者 Shuning Li Zhenyao Lu +4 位作者 Li Jiao Ran Zhang Yu Hong Jiye Aa Guangji Wang 《Journal of Pharmaceutical Analysis》 SCIE CAS CSCD 2021年第5期580-587,共8页
Cystine is the primary source material for the synthesis of glutathione.However,the pharmacokinetics and tissue distribution of cystine are largely unknown.A surrogate analyte D_(4)-cystine was employed to generate ca... Cystine is the primary source material for the synthesis of glutathione.However,the pharmacokinetics and tissue distribution of cystine are largely unknown.A surrogate analyte D_(4)-cystine was employed to generate calibration curves for the determination of levels of D_(4)-cystine and endogenous cystine in mice by liquid chromatography-tandem mass spectrometry(LC-MS/MS).Validation assessments proved the sensitivity,specificity and reproducibility of the method with a lower limit of quantification(LLOQ)of 5 ng/mL over 5e5000 ng/mL in plasma.The pharmacokinetics of D_(4)-cystine were evaluated after administering injections and oral solutions,both of which minimally impacted endogenous cystine levels.The absolute bioavailability of cystine was 18.6%,15.1%and 25.6%at doses of 25,50 and 100 mg/kg,respectively.Intravenously injected D_(4)-cystine resulted in dramatically high plasma levels with reduced levels in the brain and liver.Intragastrically administered D_(4)-cystine resulted in high levels in the plasma and stomach with relatively low levels in the lung,kidney,heart and brain. 展开更多
关键词 CYSTINE LC-MS/MS pharmacokinetics DISTRIBUTION Absolute bioavailability
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Pharmacokinetics of fucoidan and low molecular weight fucoidan from Saccharina japonica after oral administration to mice
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作者 Jiaojiao TAN Yimin SONG +3 位作者 Jing WANG Ning WU Yang YUE Quanbin ZHANG 《Journal of Oceanology and Limnology》 SCIE CAS CSCD 2023年第5期1900-1909,共10页
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 ki... 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. 展开更多
关键词 FUCOIDAN low molecular weight fucoidan pharmacokinetics bioavailability tissue distribution
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Pharmacokinetic Study of Nanoparticulate Curcumin: Oral Formulation for Enhanced Bioavailability
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作者 R. Ravichandran 《Journal of Biomaterials and Nanobiotechnology》 2013年第3期291-299,共9页
Curcumin, a bioactive component of turmeric, which is a commonly used spice and nutritional supplement, is isolated from the rhizomes of Curcuma longa Linn. (Zingiberaceae). In recent years, the potential pharmacologi... Curcumin, a bioactive component of turmeric, which is a commonly used spice and nutritional supplement, is isolated from the rhizomes of Curcuma longa Linn. (Zingiberaceae). In recent years, the potential pharmacological actions of Curcumin in inflammatory disorders, cardiovascular disease, cancer, Alzheimer’s disease and neurological disorders have been shown. However, the clinical application of Curcumin is severely limited by its main drawbacks such as instability, low solubility, poor bioavailability and rapid metabolism. Multifarious nanotechnology-based drug delivery systems for Curcumin including liposomes, polymeric nanoparticles, solid lipid nanoparticles, micelles, nanogels, nanoemulsions, complexes and dendrimer/dimer, have been attempted to enhance the oral bioavailability, biological activity or tissue-targeting ability of Curcumin. We attempted the nanosuspensions based delivery of curcumin. Nanonisation renders curcumin completely dispersible in aqueous media. To enhance the curcumin absorption by oral administration, nanoparticulate solid oral formulation of curcumin was prepared by us and the resulting capsule was then examined for its efficiency on bioavailability in Male Wistar rats at a dose of 100 mg curcumin/kg body weight and the pharmacokinetic parameters were compared to those of normal curcumin powder and a commercial curcumin capsule CUR-500. The bio-distribution of curcumin in organs of rat was also studied. Nanoparticulation significantly raised the curcumin concentration in selective organs in the body. The results obtained provide promising results for nanoparticulate Curcumin to improve its biological activities. Enhanced bioavailability of curcumin in the form of nanoparticle is likely to bring this promising natural product to the forefront of therapeutic agents for treatment of human disease. The available information also strongly suggests that nano-formulation of ingredients such as curcumin may be used as a novel nutrient delivery system too. 展开更多
关键词 CURCUMIN NANOPARTICLES pharmacokinetics bioavailability
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Determination of Lovastatin Level in Human Plasma and Lovastatin Capsules Bioavailability in Healthy Volunteers Using HPLC-MS
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作者 肖红 沈鸿 +1 位作者 陈建芳 肖大伟 《Journal of Chinese Pharmaceutical Sciences》 CAS 2006年第4期233-237,共5页
Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was ... Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was extracted with acetoacetate. Simvastatin was added as internal standard (IS). Samples were separated on a C_ 18 column with a mobile phase consisting of methanol and 50 mmol·L~ -1 sodium acetate (88 ∶ 12). The flow rate was 1 mL·min~ -1 . Sample was detected using an electrospray ionization (ES... 展开更多
关键词 LOVASTATIN pharmacokinetics bioavailability HPLC-MS
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Pharmacokinetics of recombinant human parathyroid hormone after subcutaneous administration in Rhesus monkeys by immunoradiometric assay
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作者 宋雪伟 陈知航 +4 位作者 车津晶 单成启 侯禹男 郑仁玖 程远国 《Journal of Chinese Pharmaceutical Sciences》 CAS 2008年第2期118-121,共4页
The purpose of this research was to study the pharmacokinetics and the bioavailability of recombinant human parathyroid hormone [rhPTH (1-34)] in Rhesus monkeys after single and multiple subcutaneous administration.... The purpose of this research was to study the pharmacokinetics and the bioavailability of recombinant human parathyroid hormone [rhPTH (1-34)] in Rhesus monkeys after single and multiple subcutaneous administration. An immunoradiometric assay (IRMA) was used to determine the plasma drug concentration of rhFFH (1-34) after giving single dose of 10, 20 and 40 ug/kg and daily dose of 40 ug/kg for 7 d by subcutaneous administration, and intravenous injection of 20 ug/kg in Rhesus monkeys. The pharmacokinetic parameters were calculated by noncompartmental analysis. The drug plasma level quantitation range was from 0.027 to 2.22 ng/mL. The intra- and inter-assay precision (CV) of analysis were less than 15%, and the average recovery was about 93.0% ± 8.6% - 116.5% ± 14.0%. After subcutaneous administration of rhPTH(1-34) at dose of 10, 20 and 40 ug/kg, the average Tmax was 0.67, 0.5 and 0.83 h, Cmax were 1.85 ± 0.05, 3.23 ± 0.25 and 7.15 ± 1.19 ng/mL, the AUC(0-∞) were 3.4 ± 0.6, 10.7 ± 1.3 and 12.6 ± 1.5 ng/h/mL, and terminal-phase elimination T1/2 were 0.72 ± 0.10, 1.15 ± 0.10 and 1.03 ± 0.06 h, respectively. The absolute bioavailability of rhPTH (1-34) was 46.96% after subcutaneous administration of 20 ug/kg. There was no evidence of accumulation during systemic exposure of rhPTH (1-34) upon multiple dosing in Rhesus monkeys. The IRMA assay method provide reasonable sensitivity and specificity for the pharrnacokinetic study of rhPTH (1-34) after subcutaneous or intravenous administration in Rhesus monkeys. The pharmacokinetic characteristic of rhPTH (1-34) in monkeys shows linear relationship with the dose administered subcutaneously. 展开更多
关键词 RhPTH (1-34) pharmacokinetIC IRMA bioavailability Rhesus monkey
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Advance in Pre-Clinical Pharmacokinetics of Paeoniflorin, a Major Monoterpene Glucoside from the Root of <i>Paeonia lactiflora</i> 被引量:4
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作者 Orleans N. K. Martey Xiaoyan Shi Xin He 《Pharmacology & Pharmacy》 2013年第7期4-14,共11页
Paeoniflorin (PF) is one of the main bioactive components of total glucosides of paeony (TGP) extracted from the root of Paeonia lactiflora Pall. TGP exhibit various biological activities such as improvement in memory... Paeoniflorin (PF) is one of the main bioactive components of total glucosides of paeony (TGP) extracted from the root of Paeonia lactiflora Pall. TGP exhibit various biological activities such as improvement in memory, hepatoprotection, antimutagenic properties and platelet aggregation inhibition. The aim of this paper is to review the pharmacokinetics (PK) of PF as a pure compound and in single or multiple herb(s) of traditional Chinese medicine (TCM) prescriptions. The distribution of PF or PF in TCM fitted one or two compartmental model after oral administration or intravenous injection, respectively. However, PF has a low bioavailability (BA) in rabbit (7.24%) and rat (3.24%) after oral administration. The PK profiles and BA of PF were remarkably improved when co-administered with sinomenine or glycyrrhizin acid. The PK profiles and BA of PF in Radix Paeonia Rubra (RP-R) and Jing-zhi guan-xin were improved, but in co-administration of RP-R with Radix Angelicae Sinensis, the BA was significantly reduced. PK profiles and BA of PF in Shan yao gan-cao tang or Danggui-Shaoyao-San was either remarkably improved or not. However, neither the PK profiles nor the BA of PF in Radix paeonia alba, Huangqin-tang Si ni san or Tang-Min-Ling-Wan was improved. Metabolism in the liver did not play any role in the low oral BA of PF. The low BA was thus attributed to poor permeation due to low lipophilicity, P-glycoprotein mediated efflux, intestinal bacteria and hydrolytic degradation in the intestine by the intestinal brush border lactase phlorizin hydrolase (LPH) and certain esterases. These findings show the in vivo course of PF and provide information on the maximum biological actions of PF that may help traditional Chinese herbal medicinal practitioners. 展开更多
关键词 bioavailability Intestinal Bacteria pharmacokinetics PAEONIFLORIN (PF) P-glycoprotein (P-gp)
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Determination of Mirtazapine in Human Plasma by HPLC-MS and Bioavailability of Newly Developed Mirtazapine Tablets in Healthy Volunteers 被引量:3
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作者 LIRong-shan DINGLi +1 位作者 JIANLong-hai XIAOHong 《Journal of Chinese Pharmaceutical Sciences》 CAS 2004年第3期171-175,共5页
Aim To establish a sensitive and specific liquid chromatography-mass spectrometry method for determination of mirtazapine in human plasma and evaluation of its relative bioavailability. Methods After being alkalized... Aim To establish a sensitive and specific liquid chromatography-mass spectrometry method for determination of mirtazapine in human plasma and evaluation of its relative bioavailability. Methods After being alkalized by 25% ammonia, mirtazapine in the plasma was extracted with n-hexane. Desloratadine was used as internal standard (IS). Solu-tes were separated on a C_(18) column with a mobile phase of methanol-ammonium acetate buffer (pH 3.5) (75∶25). The flow rate of the mobile phase was 1 mL·min^(-1). Detection was performed on an electrospray ionization (ESI) mass spectrometer and operated in selected ion monitoring (SIM) and positive-ionization mode using target ionsat m/z 266.2 for mirtazapine and m/z 311.2 for the IS. The fragmentor voltage was 90 V. A randomized cross-over study was performed in 20 healthy volunteers. In the two study periods, twenty healthy Chinese male subjects received a single oral dose of mirtazapine 30 mg. Results The calibration curve was linear over the range of 0.3-200 ng·mL^(-1). The limit of quantitation was 0.1 ng·mL^(-1). The parameters for mirtazapine test tablet and reference tablet were as follows: T_(1/2)(24.7±4.1) and (23.6±4.3) h, T_(max)(1.6±0.8) and (1.5±0.8) h, C_(max)(95.9±29.8) and (91.9±26.7) ng·mL^(-1), respectively. Conclusion The established HPLC-MS method is rapid, sensitive and specific for the determination of mirtazapine in human plasma. The relative bioavailability was 100.0%±10.8%. 展开更多
关键词 mirtazapine pharmacokinetics bioavailability HPLC-MS
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Absolute bioavailability,dose proportionality,and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method 被引量:1
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作者 Haihua Shang Xiaohan Dai +7 位作者 Mi Li Yueyi Kai Zerong Liu Min Wang Quansheng Li Yuan Gu Changxiao Liu Duanyun Si 《Journal of Pharmaceutical Analysis》 SCIE CAS CSCD 2022年第2期278-286,共9页
Rotundic acid(RA),an ursane-type pentacyclic triterpene acid isolated from the dried barks of Ilex rotunda Thunb.(Aquifoliaceae),possesses diverse bioactivities.To further study its pharmacokinetics,a simple and sensi... Rotundic acid(RA),an ursane-type pentacyclic triterpene acid isolated from the dried barks of Ilex rotunda Thunb.(Aquifoliaceae),possesses diverse bioactivities.To further study its pharmacokinetics,a simple and sensitive liquid chromatography with triple quadrupole mass spectrometry(LC-QqQ-MS/MS)method was developed and validated to quantify RA concentration in rat plasma and tissue using etofesalamide as an internal standard(IS).Plasma and tissue samples were subjected to one-step protein precipitation.Chromatographic separation was achieved on a ZORBAX Eclipse XDB-C_(18) column(4.6mm×50mm,5μm)under gradient conditions with eluents of methanol:acetonitrile(1:1,V/V)and 5mM ammonium formate:methanol(9:1,V/V)at 0.5mL/min.Multiple reaction monitoring transitions were performed at m/z 487.30→437.30 for RA and m/z 256.10→227.10 for IS in the negative mode.The developed LC-QqQ-MS/MS method exhibited good linearity(2-500 ng/mL)and was fully validated in accordance with U.S.Food and Drug Administration bioanalytical guidelines.Dose proportionality and bioavailability in rats were determined by comparing pharmacokinetic data after single oral(10,20,and 40mg/kg)and intravenous(10mg/kg)administration of RA.Tissue distribution was studied following oral administration at 20mg/kg.The results showed that the absolute bioavailability of RA after administration at different doses ranged from 16.1%to 19.4%.RA showed good dose proportionality over a dose range of 10-40 mg/kg.RA was rapidly absorbed in a dose-dependent manner and highly distributed in the liver.In conclusion,this study is the first to systematically elucidate the absorption and distribution characteristics of RA in rats,which can provide additional information for further development and evaluation of RA in drug metabolism and pharmacokinetic studies. 展开更多
关键词 Rotundic acid LC-QqQ-MS/MS bioavailability Tissue distribution pharmacokinetics Dose proportionality
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A Comparative Study on Pharmacokinetics of Tricin, a Flavone from Gramineous Plants with Antiviral Activity 被引量:1
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作者 Galina I. Solyanik Oleg S. Zulphigarov +3 位作者 Iryna V. Prokhorova Olga N. Pyaskovskaya Denis L. Kolesnik Viktor P. Atamanyuk 《Journal of Biosciences and Medicines》 2021年第2期76-91,共16页
Tricin (and tricin containing plant extracts) has been shown to exert a pronounced antiviral activity, high radical scavenging activity and is favored for its safety profile. In the present study we have analyzed the ... Tricin (and tricin containing plant extracts) has been shown to exert a pronounced antiviral activity, high radical scavenging activity and is favored for its safety profile. In the present study we have analyzed the pharmacokinetics of tricin after a single intravenous and oral administration to Wistar rats of an ethanol extract of <em>Calamagrostis Adans</em> and <em>Deschampsia Beauv</em> plants (test agent) at different doses. Tricin concentrations in blood plasma and blood cells were measured at different time points. Two-compartment (for intravenous injection) and one compartment (for oral administration) models were used for the analysis of tricin pharmacokinetics. The results showed that the pharmacokinetics of tricin after intravenous injection of test agent has a pronounced biphasic character, is well described by a two-compartment pharmacokinetic model, and is characterized by non-linear dose-dependence. The pharmacokinetics of tricin administered orally is characterized by a high rate of absorption from the gastrointestinal tract into the blood and rather slow elimination, which leads to a large volume of distribution in the body and a fairly high bioavailability. The obtained results indicate the advantages of the oral route of administration over the intravenous route. 展开更多
关键词 Polyphenolic Compounds TRICIN pharmacokinetics bioavailability
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Microdialysis in awake macaque monkeys for central nervous system pharmacokinetics 被引量:2
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作者 Thibaud Thiollier Caisheng Wu +4 位作者 Gregory Porras Erwan Bezard Qin Li Jinlan Zhang Hugues Contamin 《Animal Models and Experimental Medicine》 2018年第4期314-321,共8页
Background: The brain bioavailability of novel small molecules developed to address central nervous system disease is classically documented through ex vivo or in vivo analyses conducted in rodent models. Data acquire... Background: The brain bioavailability of novel small molecules developed to address central nervous system disease is classically documented through ex vivo or in vivo analyses conducted in rodent models. Data acquired in rodent models are, however,not easily transferrable to human as the pharmacokinetic and pharmacodynamics profiles of the species are quite different.Methods: Using drugs selected for their differential transport across the blood-brain barrier, we here demonstrate the feasibility of brain microdialysis in normal vigil macaque monkey by measuring brain extracellular fluid bioavailability of carbamazepine, digoxin, oxycodone, and quinidine.Results: All drugs, but digoxin, were found in dialysate samples. Drugs that are substrate of P-glycoprotein show a difference of bioavailability or brain pharmacokinetic parameters between rodents and primates.Conclusion: Data suggest that brain microdialysis in vigil macaque monkey, the species of choice for classic pharmacokinetic/pharmacodynamics studies could help predicting human brain bioavailability of a small molecule depending on the protein involved in the efflux transport from the brain. 展开更多
关键词 AWAKE bioavailability blood BRAIN barrier BRAIN central nervous system crossing methods MICRODIALYSIS non-human PRIMATE pharmacokinetIC
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Pharmacokinetics and Tissue Residues of Tylosin in Broiler Chickens 被引量:1
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作者 Ahmed M. Soliman Mahmoud Sedeik 《Pharmacology & Pharmacy》 2016年第1期36-42,共7页
The pharmacokinetics and tissue residue of tylosin in broiler chickens were studied after I.V. and oral administrations in a dose of 50 mg tylosin/kg.b.wt. Tylosin was obeyed a two-compartment open model following I.V... The pharmacokinetics and tissue residue of tylosin in broiler chickens were studied after I.V. and oral administrations in a dose of 50 mg tylosin/kg.b.wt. Tylosin was obeyed a two-compartment open model following I.V. administration at a dose of 50 mg/kg.b.wt. The disposition kinetics of tylosin following I.V. administration revealed that tylosin was highly distributed with V<sub>d(area)</sub> of 6 L/kg and eliminated with half-life (t<sub>1/2β</sub>) equal to 7.29 hours. The disposition kinetics of tylosin following oral administration revealed that the maximum blood concentration (C<sub>max</sub>) was 3.40 μg/ml attained at (t<sub>max</sub>) of 1.08 hour. Tylosin was eliminated with half-life (t<sub>1/2β</sub>) equal to 5.78 hours. The mean systemic bioavailability of tylosin after oral administration was 90.29%. Following repeated oral administration of 50 mg tylosin base/kg.b.wt once daily for 5 consecutive days, the blood (μg/ml) and tissue (μg/g) residues of tylosin showed that liver, kidney and lung contained the highest tylosin residues and completely disappeared from those tissues at 6 days after the last oral dose. Chickens should not be slaughtered for human consumption within the treatment and 6 days after the last oral administrations of tylosin. 展开更多
关键词 pharmacokinetics TYLOSIN Broiler Chickens bioavailability Tissue Residue
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Quantification of neomangiferin in rat plasma by liquid chromatography–tandem mass spectrometry and its application to bioavailability study
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作者 Bo Yang Zhirui Liu +2 位作者 Shenglan Shang Xiaojian Qin Peiyuan Xia 《Journal of Pharmaceutical Analysis》 SCIE CAS 2016年第5期335-340,共6页
Neomangiferin, a natural C-glucosyl xanthone, has recently received a great deal of attention due to its multiple biological activities. In this study, a rapid and sensitive ultra-high performance liquid chromatograph... Neomangiferin, a natural C-glucosyl xanthone, has recently received a great deal of attention due to its multiple biological activities. In this study, a rapid and sensitive ultra-high performance liquid chromatography tandem mass spectrometry(UHPLC–MS/MS) method for the quantification of neomangiferin in rat plasma was developed. Using chloramphenicol as an internal standard(IS), plasma samples were subjected to a direct protein precipitation process using methanol(containing 0.05% formic acid). Quantification was performed by multiple reactions monitoring(MRM) method, with the transitions of the parent ions to the product ions of m/z 583.1-330.9 for NG and m/z 321.1-151.9 for IS. The assay was shown to be linear over the range of 0.2–400 ng/m L, with a lower limit of quantification of 0.2 ng/m L. Mean recovery of neomangiferin in plasma was in the range of 97.76%–101.94%. Relative standard deviations(RSDs) of intra-day and inter-day precision were both o 10%. The accuracy of the method ranged from94.20% to 108.72%. This method was successfully applied to pharmacokinetic study of neomangiferin after intravenous(2 mg/kg) and intragastric(10 mg/kg) administration for the first time. The oral absolute bioavailability of neomangiferin was estimated to be 0.53% 7 0.08% with an elimination half-life(t_(1/2)) value of 2.747 0.92 h, indicating its poor absorption and/or strong metabolism in vivo. 展开更多
关键词 Neomangiferin UHPLC–MS/MS RAT PLASMA pharmacokinetics bioavailability
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