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Propolis as a promising functional ingredient:a comprehensive review on extraction,bioactive properties,bioavailability,and industrial applications
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作者 Mengyao Liu Xiangxin Li +5 位作者 Hualei Chen Fei Pan Xing Zheng Maurizio Battino Wenli Tian Wenjun Peng 《Food Science and Human Wellness》 2025年第10期3775-3795,共21页
Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities an... Propolis is a resinous complex mixture made from plant resins collected by worker bees and mixed with their own secretions.It is rich in polyphenols and flavonoids and thus has a wide range of biological activities and is considered a functional source for promoting human health.However,propolis and its bioactive compounds have poor water solubility,rapid and intense metabolism,and low oral bioavailability,which limits their wide application.In this paper,the main bioactive substances in propolis were summarized,and the biological characteristics and therapeutic potential of propolis and its bioactive substances were discussed.In addition,this paper discussed the factors affecting the bioavailability of propolis and its functional ingredients,focusing on the research progress in improving the bioavailability and bioactivity of propolis and its functional ingredients using nanoencapsulation technology.Finally,the current situation of the global propolis market and the applications of propolis products in the pharmaceutical,food,cosmetic and other industrial fields were discussed,providing useful references for promoting the development of the propolis industry. 展开更多
关键词 PROPOLIS Chemical composition Biological activities bioavailability Industrial application
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Deep learning-based simultaneous bioavailability assessment and speciation analysis of dissolved organic copper
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作者 Zhaojing Huang Hao Li +4 位作者 Jiayi Luo Shunxing Li Ming Zhao Fengjiao Liu Haijiao Xie 《Chinese Chemical Letters》 2025年第5期645-650,共6页
Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu upt... Algal copper uptake(i.e.,Cu bioavailability)in the euphotic zone plays a vital role in algal photosynthesis and respiration,affecting the primary productivity and the source and sink of atmospheric carbon.Algal Cu uptake is controlled by natural dissolved organic Cu(DOCu)speciation(i.e.,complexed with the dissolved organic matter)that conventionally could be tested by model prediction or molecular-level characterizations in the lab,while DOCu uptake are hardly directly assessed.Thus,the new chemistrybiology insight into the mechanisms of the Cu uptake process in algae is urgent.The DOCu speciation transformation(organic DOCu to free Cu(II)ions),enzymatic reduction-induced valence change(reduction of free Cu(II)to Cu(I)ions),and algal Cu uptake at the algae-water interface are imitated.Herein,an intelligent system with DOCu colorimetric sensor is developed for real-time monitoring of newly generated Cu(I)ions.Deep learning with whole sample image-based characterization and powerful feature extraction capabilities facilitates colorimetric measurement.In this context,the Cu bioavailability with 7 kinds of organic ligands(e.g.,amino acids,organic acids,carbohydrates)can be predicted by the mimetic intelligent biosensor within 15.0min,i.e.,the DOCu uptake and speciation is successfully predicted and streamlined by the biomimetic approach. 展开更多
关键词 Metal bioavailability Metal speciation Primary productivity Intelligent analysis Biomimetic sensor
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Effect of Hydrothermal Coupling on Phosphorus Bioavailability in Vegetable Soil
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作者 Wenyan HE Xicheng WANG +3 位作者 Mengdie LI Aomingyang LI Tianya LIU Jifu LI 《Meteorological and Environmental Research》 2025年第1期59-63,共5页
In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and mois... In this paper,the vegetable field in the teaching base of College of Agriculture,Yangtze University was taken as the research object.The indoor simulation method was used to explore the effects of temperature and moisture on the phosphorus(P)bioavailability of vegetable soil.Three temperature gradients[T1(15℃),T2(25℃),T3(35℃)]and three humidity gradients[W1(40%),W2(70%),W3(100%)]were set in the test.The results showed that it could improve the contents of HCl-P,Enzyme-P,Citrate-P,and Olsen-P in vegetable soil by increasing soil moisture content;temperature rise was helpful to increase the contents of HCl-P and Olsen-P,but it could reduce the content of Citrate-P.The contents of Enzyme-P and CaCl 2-P were significantly affected by hydrothermal interaction.Within a certain range of soil temperature and humidity,temperature and moisture had a positive coupling effect on soil P bioavailability components,and significantly affected soil P supply capacity. 展开更多
关键词 Vegetable field Hydrothermal coupling Soil phosphorus Phosphorus bioavailability INTERACTION
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Enhancing bioavailability in traditional Chinese medicine: Exploring strategies for optimized therapeutic efficacy
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作者 John Osilama Thomas Ifeoluwa Margaret Idowu Sunitha Ganesha Rudrapatna 《Natural Therapy Advances》 2025年第1期55-69,共15页
Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug deli... Traditional Chinese medicine(TCM)offers diverse therapeutic compounds but faces challenges like poor bioavailability and instability.Recent innovations in drug delivery systems,including nanotechnology-based drug delivery systems have shown potential to enhance solubility,stability,and therapeutic efficacy.This review examines these advancements,focusing on their mechanisms and applications in improving TCM formulations.Cutting-edge techniques,such as microneedles,iontophoretic patches,and self-orienting applicators,are also discussed for their potential to revolutionize TCM delivery.By bridging traditional wisdom with modern innovations,this review emphasizes the transformative role of these strategies in advancing TCM's integration into contemporary medicine. 展开更多
关键词 traditional Chinese medicine bioavailability enhancers drug delivery NANOCARRIERS therapeutic efficacy
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Impact of Phosphate Solubilizing Bacterial Agent on Cadmium Bioavailability and Microbial Communities in Soil and Cd Accumulation in Lettuce Plants
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作者 Yue Yu Ping Li +3 位作者 Yanhong Wang Xinzhe Lu Chunlei Huang Hanqin Yin 《Journal of Earth Science》 2025年第5期2266-2278,共13页
Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.I... Cadmium(Cd)contamination in soil can lead to food chain accumulation and greatly impacts on human health.Bioremediation has gained more and more attention due to its environment-friendly,high efficiency and low-cost.In this work,we studied the impact of phosphate solubilizing bacterial agent(PSBA)on Cd bioavailability,microbial communities in soil and Cd accumulation in lettuce plants with pot experiment and field trial.Results of pot experiment showed that PSBA could decrease the bioavailability of Cd(Cd-acid extractable from 3.30 to 2.34mg/kg,Cd-reducible from 1.94 to 1.56 mg/kg),promote lettuce plants growth(increased by 33.85%height and by 33.65%fresh weight)and reduce the accumulation of Cd(from 5.85 to 3.73 mg/kg)in lettuce plants.High-throughput sequencing identified that PSBA could change the composition and structure of the soil microbial communities.The relative abundances of the three ecologically beneficial bacterial families of Pseudomonadaceae,Burkholderiaceae,and Enterobacteriaceae increased from 2.29%to 5.13%,0.56%to 5.24%,and 1.87%to 16.93%,respectively.And the former two were positively correlated with redox potential(Eh)(R^(2)=0.474,p<0.05,R^(2)=0.590,p<0.01,respectively).The bacterial networks were more complex in PSBA treatment,reflecting through more links(from 1893 to 2185)and a higher average degree(from 38.242 to 45.052)and density(from 0.390 to 0.469).Results of field trial demonstrated that PSBA could also decrease Cd content in lettuce plants and microbial composition in soil.This study indicated that PSBA could be served as an alternative material in bioremediation of Cd contamination in soil. 展开更多
关键词 Cd bioavailability microbial communities physicochemical properties PSBA BIOREMEDIATION environmental geology
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Innovative 3D microfluidic intestinal organoid model for assessing cadmium bioavailability in food:implications for enhanced exposure risk assessment
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作者 Yan Li Wen Sun +6 位作者 Qiao Wang Wan Shi Yu Chen Zhiyong Gong Xiao Guo Xin Liu Yongning Wu 《Food Science and Human Wellness》 2025年第5期1687-1696,共10页
Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust d... Given the severe toxicity and widespread presence of cadmium(Cd)in staple foods such as rice,accurate dietary exposure assessments are imperative for public health.In vitro bioavailability is commonly used to adjust dietary exposure levels of risk factors;however,traditional planar Transwell models have limitations,such as cell dedifferentiation and lack of key intestinal components,necessitating a more physiologically relevant in vitro platform.This study introduces an innovative three-dimensional(3D)intestinal organoid model using a microfluidic chip to evaluate Cd bioavailability in food.Caco-2 cells were cultured on the chip to mimic small intestinal villi's 3D structure,mucus production,and absorption functions.The model's physiological relevance was thoroughly characterized,demonstrating the formation of a confluent epithelial monolayer with well-developed tight junctions(ZO-1),high microvilli density(F-actin),and significant mucus secretion(Alcian blue staining),closely resembling the physiological intestinal epithelium.Fluorescent particle tracking confirmed its ability to simulate intestinal transport and diffusion.The Cd bioavailability in rice measured by the 3D intestinal organoid model((9.07±0.21)%)was comparable to the mouse model((12.82±3.42)%)but significantly lower than the Caco-2 monolayer model((26.97±1.11)%).This 3D intestinal organoid model provides a novel and reliable strategy for in vitro assessment of heavy metal bioavailability in food,with important implications for food safety and risk assessment. 展开更多
关键词 Planar Transwell model 3D intestinal organoid model Physiological relevance Cd bioavailability
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Boswellic acids: a review on its pharmacological properties, molecular mechanism and bioavailability
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作者 Na Cui Ming-Jie Li +3 位作者 Yi-Wen Wang Qian Meng Ya-Jun Shi Yi Ding 《Traditional Medicine Research》 2024年第10期64-74,共11页
Boswellic acids is a general term for a series of pentacyclic triterpenoid compounds that are isolated from the oleogin resin of the Boswellia genus and serve as the main active ingredient.It exhibits a wide range of ... Boswellic acids is a general term for a series of pentacyclic triterpenoid compounds that are isolated from the oleogin resin of the Boswellia genus and serve as the main active ingredient.It exhibits a wide range of biological activities,such as anti-inflammatory,anti-cancer,antibacterial,antiviral,hepatoprotective,neuroprotective,anti-diabetic,and anti-thrombotic properties.As a result,it has gained significant recognition among practitioners of traditional Chinese and Indian medicine.These biological effects may be associated with multiple molecular targets and signal transduction pathways.However,the poor pharmacokinetic properties of the substance lead to lower bioavailability,which affects its effectiveness.To address this issue,scientists have proposed a number of strategies,such as solid dispersions,phytosome®technologies,and novel drug delivery systems.This article aims to provide a comprehensive overview for boswellic acids on the phytochemistry,molecular mechanisms,potential therapeutic applications,and strategies to improve bioavailability. 展开更多
关键词 boswellic acids molecular mechanism pharmacological properties bioavailability
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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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Electrostatic spraying for fine-tuning particle dimensions to enhance oral bioavailability of poorly water-soluble drugs
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作者 Jung Suk Kim Seunghyun Cheon +10 位作者 Mi Ran Woo Sanghyun Woo Jee-Eun Chung Yu Seok Youn Kyung Taek Oh Soo-Jeong Lim Sae Kwang Ku Bao Loc Nguyen Jong Oh Kim Sung Giu Jin Han-Gon Choi 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2024年第5期139-151,共13页
While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs,the outcomes often exhibit suboptimal particle size distribution and large particle sizes,limiting their effecti... While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs,the outcomes often exhibit suboptimal particle size distribution and large particle sizes,limiting their effectiveness.In this study,we introduce electrostatic spraying as an advanced technology tailored for poorly water-soluble drugs,enabling the fabrication of nanoparticles with fine and uniform particle size distribution.Regorafenib(1 g),as a model drug,copovidone(5 g),and sodium dodecyl sulfate(0.1 g)were dissolved in 200 ml ethanol and subjected to conventional-spray-dryer and electrostatic spray dryer.The electrostatic spray-dried nanoparticles(ESDN)showed smaller particle sizes with better uniformity compared to conventional spray-dried nanoparticles(CSDN).ESDN demonstrated significantly enhanced solubility and rapid release in water.In vitro studies revealed that ESDN induced apoptosis in HCT-116 cells to a greater extent,exhibiting superior cytotoxicity compared to CSDN.Furthermore,ESDN substantially improved oral bioavailability and antitumor efficacy compared to CSDN.These findings suggest that ESD shows potential in developing enhanced drug delivery systems for poorly water-soluble drugs,effectively addressing the limitations associated with CSD methods. 展开更多
关键词 Electrostatic spray drying Poorly water-soluble drug Regorafenib Particle size distribution Oral bioavailability Oral antitumor efficacy
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NONMEM法分析静滴异丙酚在中国人体的群体药代动力学 被引量:34
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作者 张兴安 芮建中 +2 位作者 吴群林 施冲 王若松 《中国临床药理学杂志》 CAS CSCD 北大核心 2004年第6期444-448,共5页
目的 考察中国人静脉匀速滴注异丙酚的群体药代动力学。方法 51例腰麻-硬膜外联合麻醉病人匀速输注异丙酚直至暴发脑电抑制,以HPLC法测定异丙酚血浆浓度,用NONMEM程序分析中国人异丙酚群体药代动力学。结果 异丙酚药代动力学符合三... 目的 考察中国人静脉匀速滴注异丙酚的群体药代动力学。方法 51例腰麻-硬膜外联合麻醉病人匀速输注异丙酚直至暴发脑电抑制,以HPLC法测定异丙酚血浆浓度,用NONMEM程序分析中国人异丙酚群体药代动力学。结果 异丙酚药代动力学符合三室线性开放模型,群体参数CL(L.min-1)、Vc(L)、Q2(L.min-1)、V2(L)、Q3(L.min-1)和V3(L)的标准值分别为1.10,7.63,1.54,15.0,0.76和175;体重对CL的校正为体重除以60的0.70次方,CL和Q2年龄≥60的病人较年龄<60的分别低18.1%和32.1%;年龄对V2和Q3的校正分别为年龄除以50的-0.66次方和-0.71次方。结论 NONMEM法对以三室模型群体参数估算的血药浓度值与实测值有良好相关性,体重、年龄对参数影响较大。 展开更多
关键词 异丙酚 群体药代动力学 nonmem
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NONMEM法估算地高辛相对生物利用度和药动学参数 被引量:7
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作者 周燕 芮建中 +2 位作者 谈恒山 蔡明虹 凌树森 《中国医院药学杂志》 CAS CSCD 北大核心 2000年第7期393-396,共4页
目的 :一步法分析地高辛相对生物利用度和药物动力学参数。方法 :用NONMEM程序包及其新的POSTHOC子模块功能 ,估算地高辛相对生物利用度和药动学参数 ,并与经典的 3P87方法比较。结果 :两者的相对生物利用度一致 ;青年健康受试者口服地... 目的 :一步法分析地高辛相对生物利用度和药物动力学参数。方法 :用NONMEM程序包及其新的POSTHOC子模块功能 ,估算地高辛相对生物利用度和药动学参数 ,并与经典的 3P87方法比较。结果 :两者的相对生物利用度一致 ;青年健康受试者口服地高辛的主要药动学参数典型值K10 (h-1)、Vc/F(L)和 β(h-1)分别为 0 .115 ,12 8和 0 .0 18,而老年病人的典型值K10 (h-1)、Vc/F(L)和 β(h-1)分别为 0 .0 40 3,76 .0和 0 .0 148。结论 :老年病人的主要药动学参数明显低于青年健康受试者 ,差异存在显著性。用NONMEM法在取样点数较少时可获得与经典法一致的个体药动学参数。 展开更多
关键词 地高辛 nonmem 相对生物利用度 药物动力学
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用NONMEM法建立中国癫痫儿童丙戊酸钠的群体药动学模型 被引量:25
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作者 姜德春 王丽 卢炜 《中国药学杂志》 CAS CSCD 北大核心 2007年第4期291-294,317,共5页
目的建立中国癫痫儿童丙戊酸钠(VPA)的群体药动学(PPK)模型,促进个体化用药。方法回顾性地收集246例癫痫患儿应用VPA的临床数据,血药浓度都是常规监测的稳态浓度。将患儿分为两组,PPK模型组(n=146):用NONMEM软件求算PPK参数值,建立基本... 目的建立中国癫痫儿童丙戊酸钠(VPA)的群体药动学(PPK)模型,促进个体化用药。方法回顾性地收集246例癫痫患儿应用VPA的临床数据,血药浓度都是常规监测的稳态浓度。将患儿分为两组,PPK模型组(n=146):用NONMEM软件求算PPK参数值,建立基本模型和最终模型;PPK验证组(n=100):分别用基本模型和最终模型预测PPK验证组患儿的血药浓度,比较两模型的平均预测误差(MPE)、预测误差均方(MSPE)、平均预测误差平方根(RMSPE)和权重残差(WRES),进行模型验证。结果用NONMEM法拟合为一室一级吸收模型,PPK基本模型的参数为:Ka2.38 h-1,Vd 6.54 L,CL0.232 L.h-1;最终模型参数为:Ka2.38 h-1,Vd(2.03+0.189).体重(L),CL(0.097 8+0.010 4).年龄(L.h-1)。基本模型经PPK验证组检验的结果,MPE,MSPE,RMSPE,WRES及其95%C I分别为:-25.03(-32.74,-17.32),4 105.71(2 803.93,5 407.49),44.34(38.29,50.39),-0.03(-0.11,0.05);最终模型经PPK验证组检验的结果,MSE,MSPE,RMSPE,WRES及其95%C I分别为:-1.29(-6,3.4),1 268.38(1 050.64,1 486.12),28.46(25.66,31.26),0.12(-0.04,0.28)。最终模型比基本模型更优化、预测更准确。结论用NONMEM软件成功地建立了中国癫痫儿童VPA的PPK模型。 展开更多
关键词 群体药动学 nonmem 癫痫 儿童 丙戊酸钠
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群体药动学原理及NONMEM法数据分析 被引量:15
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作者 胡敏 张静华 +2 位作者 孙鹤 施孝金 钟明康 《药学服务与研究》 CAS CSCD 2002年第4期227-230,共4页
治疗药物监测 (TDM)的核心是个体化给药 ,即充分考虑病人的生理、病理及环境因素 ,根据病人的具体情况制定更加合理、安全、有效的用药方案 [1 ] ,其关键是获得理想的个体参数。群体药动学 (population pharm acokinetics,PPK)即是将经... 治疗药物监测 (TDM)的核心是个体化给药 ,即充分考虑病人的生理、病理及环境因素 ,根据病人的具体情况制定更加合理、安全、有效的用药方案 [1 ] ,其关键是获得理想的个体参数。群体药动学 (population pharm acokinetics,PPK)即是将经典药动学与统计学原理相结合 ,使用零散的血药浓度测定结果 ,估算群体参数值 ,结合 Bayes反馈法 ,较准确地估算出个体参数 ,优化给药方案 ,使 TDM更切合临床实际需要。本文将对 PPK的基本原理及其 NONMEM法数据分析作一简介。 展开更多
关键词 群体药代动力学 nonmem 模型验证
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NONMEM法优化苯妥英个体用药方案 被引量:8
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作者 芮建中 王莉 +2 位作者 蔡明虹 谈恒山 凌树森 《中国临床药理学杂志》 CAS CSCD 北大核心 2000年第4期277-279,共3页
用NONMEM-POSTHOC法优化苯妥英(PHT)个体用药方案。方法:一步法分析临床常规监测的219例门诊癫痫病人PHT的每日剂量-稳态血药浓度数据361对(其中回顾性收集161例258对,前瞻性收集58例103对... 用NONMEM-POSTHOC法优化苯妥英(PHT)个体用药方案。方法:一步法分析临床常规监测的219例门诊癫痫病人PHT的每日剂量-稳态血药浓度数据361对(其中回顾性收集161例258对,前瞻性收集58例103对)的群体药代动力学参数。结果:群体典型病人(体重60kg,年龄>15a,未合并用苯巴比妥、安定或氯硝安定)的Vm为433 mg·d-1, Km为5.84(mg·L-1)。体重对Vm的调整值为WT/60的0.56次方,合并用药时Vm增加7.7 mg·d-1,年龄<15a时Km下降6%。以POSTHOC子模块进行Bayesian反馈, 219例回顾性检验结果为:剂量估算误差为13.54 ± 4,17mg·d-1和5.31±1.62%,浓度估算误差为1.46 ± 0.82mg· L-1和 10.22 ± 5.46%。 54例因浓度未达到治疗窗或疗效不佳而调整剂量的前瞻性检验结果为:测定浓度与预测浓度的误差为0.97±0.31mg·L-1和6.82±2.12%。结论:NONMEM法能较好地应用于PHT的个体化给药。 展开更多
关键词 nonmem 用药方案 苯妥英 群体药代动力学 个体化给药 癫痫
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NONMEM法分析临床病人静脉输注阿米卡星的群体药代动力学 被引量:4
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作者 储小曼 芮建中 +3 位作者 周永刚 戴永健 蔡卫民 凌树森 《药学学报》 CAS CSCD 北大核心 1996年第12期881-885,共5页
收集52例呼吸科感染病人静脉输注阿米卡星(amikacin,AMK)的临床数据,用荧光偏振兔疫法(FPIA)测定临床病人AMK的血清浓度275点,按二房室开放模型,用NONMEM程序一步估算出AMK的群体药代动力学参... 收集52例呼吸科感染病人静脉输注阿米卡星(amikacin,AMK)的临床数据,用荧光偏振兔疫法(FPIA)测定临床病人AMK的血清浓度275点,按二房室开放模型,用NONMEM程序一步估算出AMK的群体药代动力学参数,并定量地分析病人的体重、肌酥清除率、长期用药和病理状况(馒性阻塞性肺病,COPD)等固定效应对药代动力学参数的影响。经统计分析病人的肌酥清除率和COPD对AMK的药代动力学参数的影响有显著意义,而体重对表现分布容积Vc的影响无显著意义。由最终回归模型估算出AMK的群体药代动力学参数。 展开更多
关键词 阿米卡星 药物动力学 nonmem程序 抗菌素
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用NONMEM法建立西酞普兰群体药代动力学模型 被引量:4
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作者 孙丽丽 司天梅 +3 位作者 刘薏 杨琴 翟所迪 卢炜 《中国临床药理学杂志》 CAS CSCD 北大核心 2008年第2期151-155,共5页
目的建立中国人西酞普兰(抗抑郁药)的群体药代动力学(PPK)模型,为临床个体化给药提供参考。方法用群体药代动力学方法,对西酞普兰生物等效性研究中23例受试者的血药浓度和临床资料进行分析,用NON-MEM软件求算西酞普兰的PPK参数值,建立... 目的建立中国人西酞普兰(抗抑郁药)的群体药代动力学(PPK)模型,为临床个体化给药提供参考。方法用群体药代动力学方法,对西酞普兰生物等效性研究中23例受试者的血药浓度和临床资料进行分析,用NON-MEM软件求算西酞普兰的PPK参数值,建立西酞普兰的PPK模型,并进行模型验证。结果经NONMEM法处理,所有因素中,年龄、体重以及CYP2C19基因型对中央隔室清除率有显著性的影响;体重对分布容积有显著性的影响。年龄和体重的增加对清除率影响分别为-0.39L·h-1.a-1和0.18L.h-1·kg-1。结论用NONMEM软件拟合获得的西酞普兰群体药代动力学最终模型,经验证稳定可靠。 展开更多
关键词 西酞普兰 群体药代动力学 nonmem
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NONMEM法估算中国癫痫患者卡马西平的清除率 被引量:11
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作者 焦正 钟明康 +6 位作者 施孝金 胡敏 李中东 王大猷 张莉莉 张静华 王宏图 《中国药理学通报》 CAS CSCD 北大核心 2003年第3期314-318,共5页
目的 考察中国癫痫患者卡马西平的群体药动学参数。方法 癫痫病例来自上海、北京两地 4所医院 ,采集服用卡马西平的 5 92例患者的稳态血药浓度 (n =70 3)。NONMEM程序估算分析时 ,采用一级吸收和消除的药动学模型并固定吸收速率、生... 目的 考察中国癫痫患者卡马西平的群体药动学参数。方法 癫痫病例来自上海、北京两地 4所医院 ,采集服用卡马西平的 5 92例患者的稳态血药浓度 (n =70 3)。NONMEM程序估算分析时 ,采用一级吸收和消除的药动学模型并固定吸收速率、生物利用度和表观分布体积参数。结果 体重 (TBW )、剂量 (Dose)、合用丙戊酸钠 (VPA)且其日剂量大于 2 0mg·kg-1·d-1、苯妥英 (PHT)、苯巴比妥 (PB)和年龄大于 6 5岁的老年人 (ELDER)均为卡马西平清除率(CL)的影响因素。性别、合用氯硝西泮、妥吡酯不改变卡马西平的清除率。最终模型为 :CL(CL/F) (L/h) =1 32·Dose(g·kg-1·d-1) 0 42 1·TBW (kg) 0 .691·1 2 0 VPA·1 4 3PHT·1 14 PB·0 836 ELDER。讨论 根据中国癫痫患者的群体药动学模型 ,结合患者服用的剂量、体重和合并用药可估算其清除率 。 展开更多
关键词 卡马西平 群体药动学 非线性混合效应模型 nonmem 中国 癫痫患者 清除率
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用NONMEM法建立中国成年患者服用地高辛群体药动学模型 被引量:3
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作者 白玉国 张爱琴 +2 位作者 刘翎 赵强 赵秀丽 《中国药学杂志》 CAS CSCD 北大核心 2009年第18期1404-1408,共5页
目的建立中国成年人中服用地高辛患者的群体药动学(PPK)模型,促进个体化给药。方法收集155名长期规律服用地高辛患者的262例次稳态地高辛的测定结果以及相关临床数据。应用NONMEM软件求算PPK参数值,建立基本模型和最终模型。运用内部验... 目的建立中国成年人中服用地高辛患者的群体药动学(PPK)模型,促进个体化给药。方法收集155名长期规律服用地高辛患者的262例次稳态地高辛的测定结果以及相关临床数据。应用NONMEM软件求算PPK参数值,建立基本模型和最终模型。运用内部验证法,验证模型的可靠性。结果地高辛达到稳态时,其PPK模型符合口服吸收一室模型。地高辛体内清除和患者血清肌酐浓度、体重、是否有合并用钙离子拮抗剂(CCB)、螺内酯(SPR)有关。最终模型可表达为:CL/F=9.33×0.512(SCR/119.1)×[1+0.017×(Weight-61.2)]×(1-0.21×CCB)×(1-0.19×SPR)L·kg-1·h-1。Ka=1.54h-1;Vd/F=187L。经内部验证法验证,本模型稳定、可靠。新取5个地高辛数据应用本模型进行预测,预测结果与临床实际监测结果相符较好。结论用NONMEM软件成功建立中国成年人服用地高辛的PPK模型。 展开更多
关键词 地高辛 群体药动学 治疗药物监测 nonmem软件
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NONMEM法考察中国癫痫患者丙戊酸和卡马西平的药动学相互作用 被引量:19
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作者 焦正 钟明康 +6 位作者 施孝金 胡敏 李中东 王大猷 张莉莉 张静华 王宏图 《中国药学杂志》 EI CAS CSCD 北大核心 2004年第2期130-132,共3页
目的 考察中国癫痫患者中丙戊酸(VPA)和卡马西平(CBZ)的药物相互作用。方法 采用非线性混合效应模型,通过估算722例服用VPA和(或)CBZ的中国癫痫患者的清除率来定量考察两药的药动学相互作用。结果 VPA的清除率为CL=0.007 26×TBW0。... 目的 考察中国癫痫患者中丙戊酸(VPA)和卡马西平(CBZ)的药物相互作用。方法 采用非线性混合效应模型,通过估算722例服用VPA和(或)CBZ的中国癫痫患者的清除率来定量考察两药的药动学相互作用。结果 VPA的清除率为CL=0.007 26×TBW0。890×(1+18.1DOSE)×1.36CBZ×1.22CHILD,CBZ的清除率为:CL=1.21×DOSE0.409×TBW0.292×1.16VPA×0.845ELDER,其中CL为清除率(L·h-1);TBW为体重(kg);DOSE为日剂量(g·kg-1·d-1);当服用CBZ时,CBZ=1,反之CBZ=0;当服用VPA且VPA日剂量大于19 mg·kg-1时,VPA=1,反之VPA=0;当小于6岁的儿童时CHILD=1,反之CHILD=0;当大于65岁的老人,ELDER=1,反之ELDER=0。结论 卡马西平和丙戊酸合用时,丙戊酸的清除率增加36%,当丙戊酸的日剂量大于19 mg·kg-1 时,卡马西平的清除率增加16%。 展开更多
关键词 nonmem 中国 癫痫 丙戊酸 VPA 卡马西平 CBZ 药动学 血药浓度
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NONMEM法分析肾移植患者环孢素A的群体药动学 被引量:8
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作者 芮建中 卓海通 +1 位作者 姜国华 陈刚 《药学学报》 CAS CSCD 北大核心 1995年第4期241-247,共7页
用HPLC和FPIA法(单克隆抗体)测定全血中环孢素A(CsA)浓度,收集临床60例肾移植患者牛奶送服CsA后浓度数据281点,应用NONMEM程序一步法估算其群体药动学参数,并定量地分析体重、年龄、性别,长期用药对... 用HPLC和FPIA法(单克隆抗体)测定全血中环孢素A(CsA)浓度,收集临床60例肾移植患者牛奶送服CsA后浓度数据281点,应用NONMEM程序一步法估算其群体药动学参数,并定量地分析体重、年龄、性别,长期用药对清除率的影响。按口服吸收一室开放模型估算的群体药动学参数为:清除率CL(L·h-1)、表现分布容积Vd(L)和口服吸收速率常数Ka(h-1)分别等于59.8,227及1.28,其个体间变异QCL(%),QVL(%)及QKa(%)分别为30.27,29.02和75.10,浓度观察值与模型预测值的残差变异QE(%)等于31.19固定效应与CL的定量关系为:以体重的0.03倍加法调整,男性较女性患者增加4.31,长期用药患者下降12.7。 展开更多
关键词 环孢素A 肾移植 群体药动学 nonmem
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