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兔蛛网膜下腔出血应用尼莫地平治疗的生物利用度研究 预览
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作者 杨光 李香营 +1 位作者 王雄 陈晶 《海南医学院学报》 CAS 2019年第11期826-828,833共4页
目的:观察皮下注射尼莫地平和口服尼莫地平在健康兔和蛛网膜下腔充血(SAH)兔体内的生物利用度,并探讨皮下给药是否优于口服给药并达到目标血清浓度。方法:采用随机数字表法将成年雄性NZW兔36只分为6组(n=6):口服尼莫地平组(5、15mg/kg... 目的:观察皮下注射尼莫地平和口服尼莫地平在健康兔和蛛网膜下腔充血(SAH)兔体内的生物利用度,并探讨皮下给药是否优于口服给药并达到目标血清浓度。方法:采用随机数字表法将成年雄性NZW兔36只分为6组(n=6):口服尼莫地平组(5、15mg/kg组),皮下注射尼莫地平组(2.5、5、15mg/kg组),SAH+皮下注射尼莫地平组(2.5mg/kg),测量各组尼莫地平的血浆浓度并进行统计学分析。结果:(1)口服15mg/kg的尼莫地平会产生更高的峰值血浆浓度(Tmax),并且增加峰值血浆浓度(Cmax),曲线下面积(AUC)亦大于5mg/kg。对于皮下给药后观察到达到Tmax的时间具有相反的趋势,其中15mg/kg导致较低的Tmax,并且具有比5mg/kg更低的AUC倾向。(2)相比口服给药,皮下注射组的平均尼莫地平浓度显著大于7ng/mL(P<0.01),且尼莫地平血浆浓度保持在7ng/ml以上的时间明显大于口服给药(P<0.01)。(3)健康NZW兔中2.5mg/kg皮下尼莫地平产生的Cmax、Tmax和AUC值,与5和15mg/kg皮下注射后测量值无显著性差异(P>0.05)。在24h测量的平均尼莫地平浓度高于7ng/mL的目标治疗水平条件下,健康NZW兔(12.9±10.0)ng/mL和SAH(11.8±4.6)ng/mL兔差异亦无统计学意义(P> 0.05)。结论:皮下施用尼莫地平优于口服尼莫地平,并可以将24h后尼莫地平血浆水平维持在7ng/mL以上,有助于研究尼莫地平治疗SAH后延迟血管痉挛的机制。 展开更多
关键词 尼莫地平 皮下注射 口服 蛛网膜下腔出血 生物利用度
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Editorial: Persistent endeavors for the enhancement of dissolution and oral bioavailability
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作者 Wei Wu Yi Lu Jianping Qi 《药学学报:英文版》 CSCD 2019年第1期2-3,共2页
More than 50%of marketed drugs and 90%drug candidates are believed to be poorly water-soluble, and these figures keep growing due to input of new drug entities into the pool, thanks to the fast development in drug dis... More than 50%of marketed drugs and 90%drug candidates are believed to be poorly water-soluble, and these figures keep growing due to input of new drug entities into the pool, thanks to the fast development in drug discovery. It has long been recognized that poor solubility poses problems of retarded dissolution rate and thereby poor bioavailability. 展开更多
关键词 EDITORIAL PERSISTENT endeavors for the ENHANCEMENT of DISSOLUTION and ORAL BIOAVAILABILITY
全文增补中
Adapting liposomes for oral drug delivery
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作者 Haisheng He Yi Lu +3 位作者 Jianping Qi Quangang Zhu Zhongjian Chen Wei Wu 《药学学报:英文版》 CSCD 2019年第1期36-48,共13页
Liposomes mimic natural cell membranes and have long been investigated as drug carriers due to excellent entrapment capacity, biocompatibility and safety. Despite the success of parenteral liposomes,oral delivery of l... Liposomes mimic natural cell membranes and have long been investigated as drug carriers due to excellent entrapment capacity, biocompatibility and safety. Despite the success of parenteral liposomes,oral delivery of liposomes is impeded by various barriers such as instability in the gastrointestinal tract,difficulties in crossing biomembranes, and mass production problems. By modulating the compositions of the lipid bilayers and adding polymers or ligands, both the stability and permeability of liposomes can be greatly improved for oral drug delivery. This review provides an overview of the challenges and current approaches toward the oral delivery of liposomes. 展开更多
关键词 Liposomes ORAL DRUG delivery STABILITY ABSORPTION BIOAVAILABILITY
Bioavailability study of nimodipine in rabbit subarachnoid hemorrhage
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作者 Guang Yang Xiang-Ying Li +1 位作者 Xiong Wang Jing Chen 《海南医科大学学报(英文版)》 2019年第11期25-27,共3页
Objective:To observe the bioavailability of subcutaneous injection of nimodipine and oral administration of nimodipine in healthy rabbits and rabbits with subarachnoid hemorrhage (SAH), and determine whether subcutane... Objective:To observe the bioavailability of subcutaneous injection of nimodipine and oral administration of nimodipine in healthy rabbits and rabbits with subarachnoid hemorrhage (SAH), and determine whether subcutaneous administration is superior to oral administration and to reach the target serum concentration.Methods: Thirty six adult male New Zealand white (NZW) rabbits were divided into 6 groups (n=6) by random number table method, including the oral nimodipine group (5 mg and 15 mg/kg,n=12), the subcutaneous injection of nimodipine group (2.5 mg, 5 mg and 15 mg/kg,n=18), SAH+ subcutaneous injection of nimodipine group (2.5 mg/kg,n=6), plasma concentrations of nimodipine in each group were measured and statistical analysis was performed.Results: (1) Oral administration of 15 mg/kg of nimodipine produced a higher Tmax and increased Cmax, which was also greater than 5 mg/kg. The time to peak plasma concentration (Tmax) observed after subcutaneous administration had an opposite trend, with 15 mg/kg resulting in a lower Tmax and a lower AUC tendency than 5 mg/kg. (2) Compared with oral administration, the average concentration of nimodipine in the subcutaneous group was significantly greater than 7 ng/mL (P<0.01), and the plasma concentration of nimodipine remained above 7 ng/mL for significantly longer than oral administration (P<0.01). (3) The Cmax, Tmax and AUC values of nimodipine in healthy NZW rabbits were not significantly different from those measured by subcutaneous injection of 5 and 15 mg/kg (P>0.05). There was no significant difference between healthy NZW rabbits [(12.9±10.0) ng/mL) and SAH [(11.8±4.6) ng/mL] NZW rabbits at the target level of treatment with an average nimodipine concentration of 7 ng/mL measured at 24 h (P>0.05).Conclusion: Subcutaneous administration of nimodipine is superior to oral nimodipine and can maintain the plasma level of nimodipine at 7 ng/mL after 24 h, which can help to study the mechanism of nimodipine in delaying vasospasm after SAH treatment. 展开更多
关键词 NIMODIPINE SUBCUTANEOUS injection Oral RABBIT SUBARACHNOID hemorrhage BIOAVAILABILITY
去甲斑蝥素纳米混悬剂的制备与质量评价 预览
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作者 张淼 何瑶 《国际药学研究杂志》 CAS 北大核心 2019年第3期211-217,共7页
目的采用介质碾磨法制备去甲斑蝥素纳米混悬剂(Ncr-NS),并评价其质量。方法以羟丙基纤维素(HPC-SL浓度(X1)、碾磨速度(X2)和碾磨介质ZrO2直径(X3)作为Ncr-NS的处方和工艺参数,以碾磨120 min后Ncr-NS的平均粒径作为评价指标,使用Box-Behn... 目的采用介质碾磨法制备去甲斑蝥素纳米混悬剂(Ncr-NS),并评价其质量。方法以羟丙基纤维素(HPC-SL浓度(X1)、碾磨速度(X2)和碾磨介质ZrO2直径(X3)作为Ncr-NS的处方和工艺参数,以碾磨120 min后Ncr-NS的平均粒径作为评价指标,使用Box-Behnken实验设计优化其处方和工艺参数;采用激光粒度仪测定粒径分布和Zeta电位,扫描电镜观察其微观形态;比较微粉化Ncr原料药与Ncr-NS的体外溶出速率。结果实验优化得到的Ncr-NS最优处方和工艺参数如下:HPC-SL浓度为22%,碾磨速度为750 r/min,碾磨介质直径为0.6 mm。所制备的Ncr-NS平均粒径为(325.4±4.1)nm,多聚分散系数(PDI)为(0.184±0.009),Zeta电位为(-32.5±1.8)mV;扫描电镜下显示Ncr-NS为椭圆状球形,粒径分布较为均匀。在90 min时Ncr-NS的体外释放度是Ncr原料药的2.27倍。结论本研究采用介质碾磨法制备的Ncr-NS体外释放速率快,有望提高其口服生物利用度。 展开更多
关键词 去甲斑蝥素 纳米混悬剂 介质碾磨法 口服生物利用度
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Supersaturated polymeric micelles for oral silybin delivery: the role of the Soluplus–PVPVA complex
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作者 Chunliu Zhu Shuang Gong +4 位作者 Jinsong Ding Miaorong Yu Ejaj Ahmad Yi Feng Yong Gan 《药学学报:英文版》 CSCD 2019年第1期107-117,共11页
Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system(SDDS).... Increasing the degree of supersaturation of drugs and maintaining their proper stability are very important in improving the oral bioavailability of poorly soluble drugs by a supersaturated drug delivery system(SDDS). In this study, we reported a complex system of Soluplus–Copovidone(Soluplus–PVPVA)loaded with the model drug silybin(SLB) that could not only maintain the stability of a supersaturated solution but also effectively promote oral absorption. The antiprecipitation effect of the polymers on SLB was observed using the solvent-shift method. In addition, the effects of the polymers on absorption were detected by cellular uptake and transport experiments. The mechanisms by which the Soluplus–PVPVA complex promotes oral absorption were explored by dynamic light scattering, transmission electron microscopy, fluorescence spectra and isothermal titration calorimetry analyses. Furthermore, a pharmacokinetic study in rats was used to demonstrate the advantages of the Soluplus–PVPVA complex. The results showed that Soluplus and PVPVA spontaneously formed complexes in aqueous solution via the adsorption of PVPVA on the hydrophilichydrophobic interface of the Soluplus micelle, and the Soluplus–PVPVA complex significantly increased the absorption of SLB. In conclusion, the Soluplus–PVPVA complex is a potential SDDS for improving the bioavailability of hydrophobic drugs. 展开更多
关键词 SILYBIN Soluplus PVPVA COMPLEX Supersaturated DRUG delivery system ORAL BIOAVAILABILITY
提高中药口服生物利用度的制剂技术研究进展 预览
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作者 刘其媛 《广州化工》 CAS 2018年第8期28-30,共3页
口服中药的生物利用度问题一直以来受到古今中外学者的关注。本文介绍了中药的生物药剂学分类,并结合具体实例对提高口服生物利用度的制剂新技术包括固体分散技术、磷脂复合技术、包合技术、白微乳技术、纳米技术等方面的研究现状进行... 口服中药的生物利用度问题一直以来受到古今中外学者的关注。本文介绍了中药的生物药剂学分类,并结合具体实例对提高口服生物利用度的制剂新技术包括固体分散技术、磷脂复合技术、包合技术、白微乳技术、纳米技术等方面的研究现状进行综合分析。探讨了制约中药高口服生物利用度制剂研究与发展中存在的问题及对策,从而为高口服生物利用度的中药制剂研究提供了参考。 展开更多
关键词 中药 口服生物利用度 制剂技术
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Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique 预览
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作者 Wenxiang Dong Xitong Su +3 位作者 Meng Xu Mingming Hu Yinghua Sun Peng Zhang 《亚洲药物制剂科学(英文)》 2018年第6期546-554,共9页
Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation... Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation method, with Poloxamer 188 as hydrophilic carriers. This formulation was then characterized by scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectroscopy. Moreover, all these studies suggested the conversion of crystalline atorvastatin calcium. In addition, the drug solubility studies as well as dissolution rates compared with bulk drug and market tablets Lipitor were also examined. Furthermore, the study investigated the pharmacokinetics after oral administration of Lipitor and solid dispersion. And the AUC 0–8 h and C max increased after taking ATC-P188 solid dispersion orally compared with that of Lipitor. All these could be demonstrated that ATC-P188 solid dispersions would be prospective means for enhancing higher oral bioavailability of ATC. 展开更多
关键词 ATORVASTATIN calcium POLOXAMER 188 Solid dispersion DISSOLUTION rate Oral BIOAVAILABILITY
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PEPT1-mediated prodrug strategy for oral delivery of peramivir 预览
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作者 Yongbing Sun Wei Gan +7 位作者 Mingdao Lei Wei Jiang Meng Cheng Junwei He Qi Sun Wan Liu Lvjiang Hu Yi Jin 《亚洲药物制剂科学(英文)》 2018年第6期555-565,共11页
Peramivir was a novel and highly potent neuraminidase(NA) inhibitor for the treatment of influenza A and B. However, it exhibited a very low oral bioavailability(only 3%) due to the high polarity(log P of-1.4) and the... Peramivir was a novel and highly potent neuraminidase(NA) inhibitor for the treatment of influenza A and B. However, it exhibited a very low oral bioavailability(only 3%) due to the high polarity(log P of-1.4) and the low membrane permeability across the intestine. To utilize the PEPT1-mediated prodrug strategy to improve the oral absorption and develop the oral alternative, seven amino acid ester prodrugs and seven amino acid amide prodrugs have been synthesized. The permeability of these prodrugs across Caco-2 cells were screened. Peramivr-(CH2)2-l-Val and Peramivir-l-Ile were of the highest permeability in ester prodrugs and amide prodrugs, respectively, and then they were selected for further studies. Glycylsarcosine(gly-sar) uptake by Caco-2 could be inbihited by Peramivir-(CH2)2-l-Val and Peramivir-l-Ile in a concentration-dependent manner, and the IC 50 was 1.34 ± 0.31 m M and 1.78 ± 0.48 m M, respectively. The direct uptake of Peramivir-(CH2)2-l-Val and Peramivirl-Ile in MDCK-PEPT1 cells were significantly higher than in MDCK mock cells, and could be markedly inhibited by gly-sar. The uptake of Peramivir-(CH2)2-l-Val and Peramivir-l-Ile(0.01 to 50 m M) in MDCK-hPEPT1 cells conformed to Michaelis–Menten Equation. The oral bioavailability of peramivir was 65.3% and 37.3% after the oral administration of Peramivir-(CH2)2-l-Val and Peramivir-l-Ile to rats, respectively. The oral absorption and bioactivation of Peramivir-(CH2)2-l-Val was rapid and extensive, and no Peramivir-(CH2)2-l-Val was found in plasma. Because the amide bond was relatively stable, Peramivir-l-Ile could not be totally converted to the parent drug in vivo. Peramivir-(CH2)2-l-Val with good oral profiles and rapid bioactivation might be a promising prodrug for the further clinic development. The present study also corroborated the idea that the PEPT1-mediated prodrug approach has enormous promise for improving the oral absorption of poorly absorbed drug. 展开更多
关键词 PERAMIVIR PRODRUG Peptide TRANSPORTER 1 PHARMACOKINETICS ORAL BIOAVAILABILITY
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姜黄素自微乳渗透泵控释片的制备
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作者 陈曦 周敏 《食品工业》 北大核心 2018年第10期95-98,共4页
制备姜黄素自微乳渗透泵控释片,通过微孔渗透泵制剂控释难溶性药物的释放,以期提高姜黄素的生物利用度。通过三相图考察确定影响微乳形成区域面积的3个组分的种类及用量:油相、表面活性剂、助表面活性剂;通过单因素考察确定渗透泵控释... 制备姜黄素自微乳渗透泵控释片,通过微孔渗透泵制剂控释难溶性药物的释放,以期提高姜黄素的生物利用度。通过三相图考察确定影响微乳形成区域面积的3个组分的种类及用量:油相、表面活性剂、助表面活性剂;通过单因素考察确定渗透泵控释片对药物释放影响较大的3个因素:促渗剂蔗糖的用量、包衣增重、致孔剂聚乙二醇PEG-400用量,并对优化处方进行释放拟合。结果表明,姜黄素自微乳的处方为:0.05 g姜黄素、0.40 g WL1349、0.45 g crempoher RH40、0.90 g甘油;控释片的促渗剂蔗糖用量30%,包衣增重3.5%, PEG-400 6 g。通过对制备处方的2, 4, 6, 8, 10和12 h的释放度的考察,发现该控释片12 h内的释放符合零级释放模型。自微乳渗透泵控释片可解决难溶性药物的控释制剂的设计要求。 展开更多
关键词 姜黄素 自微乳 渗透泵控释片 生物利用度
食物影响口服药物吸收的研究进展
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作者 陈艳君 刘梅 +1 位作者 靳倩 高春生 《中国新药杂志》 CSCD 北大核心 2018年第10期1137-1143,共7页
口服给药是最常用,最方便和最安全的一种给药方式,药物经口服后首先被胃肠道吸收进入血液循环之后才能发挥治疗作用,其中药物剂型、处方中药物形态与赋形剂、胃肠道生理状况和食物成分、以及肝首过效应等代谢系统都将会对口服药物的吸... 口服给药是最常用,最方便和最安全的一种给药方式,药物经口服后首先被胃肠道吸收进入血液循环之后才能发挥治疗作用,其中药物剂型、处方中药物形态与赋形剂、胃肠道生理状况和食物成分、以及肝首过效应等代谢系统都将会对口服药物的吸收造成影响。特别是食物对口服药物吸收的影响,主要表现为直接影响和间接影响。食物与药物间的这种相互作用最终会导致药物吸收的延缓,减少或者增加,当然也有不影响药物吸收的情况。因此,探讨食物对口服药物吸收的影响非常必要。本文综述了近年来食物对于口服药物吸收和生物利用度的研究进展。 展开更多
关键词 口服给药 食物 胃肠道的生理环境 生物利用度 稳定性
基于甘草酸为载体的紫杉醇-甘草酸纳米胶束的构建和口服生物利用度的评价
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作者 杨富恒 李国锋 +4 位作者 李振东 程志宏 戴佩旻 王丽 刘旭东 《中国医院药学杂志》 北大核心 2018年第10期1040-1044,1055共6页
目的:构建紫杉醇-甘草酸纳米胶束(paclitaxel-loaded glycyrrhizic acid micelles)并对其理化性质及口服生物利用度进行考察。方法:所制备纳米胶束的包封率和载药量通过高效液相色谱法检测并计算;采用动态光散射仪测定其粒径分布;... 目的:构建紫杉醇-甘草酸纳米胶束(paclitaxel-loaded glycyrrhizic acid micelles)并对其理化性质及口服生物利用度进行考察。方法:所制备纳米胶束的包封率和载药量通过高效液相色谱法检测并计算;采用动态光散射仪测定其粒径分布;以紫杉醇溶液作为对照组,考察纳米胶束口服给药后药动学的变化;采用在体in-situ肠封闭法考察不同肠道对紫杉醇的吸收差异。结果:采用超声分散法制备载紫杉醇-甘草酸纳米胶束大小均匀,平均粒径为(245.42±5.62)nm;药物胶束的包封率为90.22%±0.27%(n=3),载药量为7.90%±0.10%(n=3);与对照组相比,纳米胶束口服生物利用度提高约6倍,很大程度上是由于紫杉醇在空肠以及结肠上吸收的增加引起。结论:该方法所制备的纳米胶束制剂能有效提高紫杉醇口服生物利用度,发挥甘草酸药物载体的特点以及药用安全性的优点,该纳米胶束可作为紫杉醇新的药物传递系统,具有临床应用前景。 展开更多
关键词 紫杉醇 甘草酸 纳米胶束 口服生物利用度
3种制剂技术对黄癸素口服生物利用度的影响 预览
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作者 李辉 刘蔓 +1 位作者 黄鸿波 丁劲松 《中成药》 CSCD 北大核心 2018年第2期309-313,共5页
目的比较3种制剂技术对黄癸素口服生物利用度的影响。方法制备固体分散体、HP-β-CD包合物、纳米混悬剂冻干粉,SD大鼠分别灌胃给予这3种制剂和原料药的混悬液。HPLC-MS/MS法测定血浆中黄癸素含有量,计算药动学参数。结果与原料药相比,3... 目的比较3种制剂技术对黄癸素口服生物利用度的影响。方法制备固体分散体、HP-β-CD包合物、纳米混悬剂冻干粉,SD大鼠分别灌胃给予这3种制剂和原料药的混悬液。HPLC-MS/MS法测定血浆中黄癸素含有量,计算药动学参数。结果与原料药相比,3种制剂技术均能显著提高该成分Cmax(P〈0.05),尤其是HP-β-CD包合物(P〈0.01);HP-β-CD包合物AUC0~6 h明显高于原料药和其他2种制剂技术(P〈0.05)。结论 HP-β-CD包合物能有效提高黄癸素口服生物利用度。 展开更多
关键词 黄癸素 固体分散体 HP-β-CD包合物 纳米混悬剂冻干粉 口服生物利用度 HPLC-MS/MS
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Improved stability and oral bioavailability of Ganneng dropping pills following transforming lignans of herpeto- spermum caudigerum into nanosuspensions
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作者 LI Juan-Juan CHENG Ling +5 位作者 SHEN Gang QIU Ling SHEN Cheng-Ying ZHENG Juan XU Rong YUAN Hai-Long 《中国天然药物:英文版》 SCIE CAS CSCD 2018年第1期70-80,共11页
口服GLP-1受体激动剂的研究进展
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作者 葛阳 赛文博 +2 位作者 田浤 唐道琪 姚文兵 《药物生物技术》 CAS 2018年第6期533-536,共4页
胰高血糖素样肽-1受体激动剂(Glucagon-like peptide-1receptor agonists,GLP-1RAs)是近年来进入2型糖尿病治疗领域的新型多肽类药物,因其具有良好的心血管收益、体重控制效果且不产生低血糖危险等特性,受到越来越多的关注。然而目前已... 胰高血糖素样肽-1受体激动剂(Glucagon-like peptide-1receptor agonists,GLP-1RAs)是近年来进入2型糖尿病治疗领域的新型多肽类药物,因其具有良好的心血管收益、体重控制效果且不产生低血糖危险等特性,受到越来越多的关注。然而目前已上市的7种GLP-1RAs类药物均为注射剂型,长期注射给药会降低患者的依从性,因此口服剂型的开发一直受到广泛关注。文章对口服递送GLP-1RAs的解决方案进行综述,重点介绍用于改善GLP-1及其类似物口服生物利用度的策略,包括研制含有吸收促进剂、细胞穿透肽、黏膜粘附剂和药物递送系统的新型制剂。 展开更多
关键词 胰高血糖素样肽-1 吸收促进剂 细胞穿透肽 黏膜粘附剂 口服递送 生物利用度 2型糖尿病
栀子苷磷脂复合物的制备及评价 预览 被引量:1
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作者 唐岚 吴兰 +5 位作者 孙伯璇 沈丽婷 余小兰 徐兴 单伟光 欧志敏 《浙江工业大学学报》 北大核心 2018年第1期110-113,118共5页
采用溶剂挥发法制备栀子苷磷脂复合物(GE-PLC),以提高栀子苷的口服生物利用度,并利用单因素试验优化制备工艺.采用UV,IR和DSC对GE-PLC进行表征,并测定了大鼠口服给药的药动学参数.结果表明:优化的制备工艺为以无水乙醇为反应溶剂,栀... 采用溶剂挥发法制备栀子苷磷脂复合物(GE-PLC),以提高栀子苷的口服生物利用度,并利用单因素试验优化制备工艺.采用UV,IR和DSC对GE-PLC进行表征,并测定了大鼠口服给药的药动学参数.结果表明:优化的制备工艺为以无水乙醇为反应溶剂,栀子苷与磷脂的质量比m(栀子苷)∶m(磷脂)=1∶4,栀子苷质量浓度16.7 mg/m L,40℃条件下反应1.5 h.物性表征显示栀子苷与磷脂未形成新的化合物,GE-PLC的脂溶性约为栀子苷的15倍.药动学结果显示GE-PLC的药时曲线下面积为栀子苷的1.63倍.GE-PLC制备工艺稳定且复合率较高,脂溶性得到明显改善,促进了栀子苷的吸收,可见磷脂复合物对水溶性好、膜渗透性差的药物提高生物利用度有较好的作用. 展开更多
关键词 栀子苷 磷脂复合物 制备 口服生物利用度
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基于网络药理学的黄芪建中汤治疗慢性萎缩性胃炎作用机制研究
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作者 许文倩 秦雪梅 刘月涛 《中草药》 CSCD 北大核心 2018年第15期3550-3561,共12页
目的筛选黄芪建中汤中治疗慢性萎缩性胃炎的主要活性成分,预测活性成分的作用靶点,建立单味药-活性成分-作用靶点网络,进一步探讨黄芪建中汤治疗慢性萎缩性胃炎的潜在作用机制。方法采用中药系统药理学技术平台(TCMSP)中的药动学参数... 目的筛选黄芪建中汤中治疗慢性萎缩性胃炎的主要活性成分,预测活性成分的作用靶点,建立单味药-活性成分-作用靶点网络,进一步探讨黄芪建中汤治疗慢性萎缩性胃炎的潜在作用机制。方法采用中药系统药理学技术平台(TCMSP)中的药动学参数[口服利用度(OB)和药物相似性(DL)]筛选黄芪建中汤的潜在活性成分,整合靶点预测网站服务器(STPD)与人类基因数据库(Genecard)、人类孟德尔遗传数据库(OMIM)预测和筛选其治疗慢性萎缩性胃炎的作用靶点,借助Cytoscape构建"单味药-活性成分-作用靶点"网络。通过Systems Dock Web Site对4个主要活性成分与作用靶点进行分子对接验证。采用String数据库与Cytoscape软件绘制蛋白质相互作用网络,并利用Dis Ge NET数据库对作用靶点类型进行归属。采用DAVID数据库对黄芪建中汤作用靶点进行生物功能及代谢通路分析。结果通过OB和DL参数筛选得到118个潜在活性成分,共涉及16个作用靶点,与疾病靶点有关的活性成分为52个,主要通过调控癌症通路、病灶黏连、精氨酸和脯氨酸代谢、血管内皮生长因子(VEGF)信号转导与神经营养因子信号通路等发挥对慢性萎缩性胃炎的治疗作用。结论黄芪建中汤对慢性萎缩性胃炎的治疗作用体现了中药多成分-多靶点-多途径的特点,为阐释其治疗慢性萎缩性胃炎的作用机制与物质基础提供了科学依据。 展开更多
关键词 黄芪建中汤 慢性萎缩性胃炎 口服利用度 药物相似性 癌症通路 病灶黏连
Soluplus micelles for improving the oral bioavailability of scopoletin and their hypouricemic effect in vivo
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作者 Ying-chun ZENG Sha LI +4 位作者 Chang LIU Tao GONG Xun SUN Yao FU Zhi-rong ZHANG 《中国药理学报:英文版》 SCIE CAS CSCD 2017年第3期424-433,共10页
Scopoletin 是拥有许多药理学活动的活跃香豆素,包括 anti-hyperuricemic 效果,但是与差的溶解度。改进它的口头的 bioavailability,我们试图包含 scopoletin 进 Soluplus 微粒(基于 Soluplus 的 scopoletin 微粒, Sco 女士) 并且... Scopoletin 是拥有许多药理学活动的活跃香豆素,包括 anti-hyperuricemic 效果,但是与差的溶解度。改进它的口头的 bioavailability,我们试图包含 scopoletin 进 Soluplus 微粒(基于 Soluplus 的 scopoletin 微粒, Sco 女士) 并且评估了 Sco-Ms.Sco 女士的 hypouricemic 行动用一个薄电影的水和方法被准备。Sco 女士与 59.4 灭敬整祬戠潬正摥 ? 噓木椭摮 ' 讚?的一种平均尺寸显示了近球形的形状 ?? 桰獯桰牯汹瑡潩 ? 猠杵敧瑳湩 ? 桴瑡 ??? ‵捡楴杮甠獰牴慥? 景 ?? 愠摮瀠??偁欠湩獡 e 展开更多
关键词 SCOPOLETIN Soluplus 微粒 口头的 bioavailability PHARMACOKINETICS 织物分发 hyperuricemic 老鼠
阿奇霉素口服混悬液在比格犬体内的药动学研究
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作者 茹仁萍 李松龙 +2 位作者 王琦 蔡汉萍 赵亚 《抗感染药学》 2017年第8期1463-1466,共4页
目的:建立比格犬血浆中阿奇霉素的超高效液相色谱.串联质谱(LC-MS/MS)测定方法,研究比格犬体内阿奇霉素口服混悬液中阿奇霉素的药动学参数。方法:血浆样品中加入内标罗红霉素后,加入乙腈提取,采用LC-MS/MS法正离子方式定量检... 目的:建立比格犬血浆中阿奇霉素的超高效液相色谱.串联质谱(LC-MS/MS)测定方法,研究比格犬体内阿奇霉素口服混悬液中阿奇霉素的药动学参数。方法:血浆样品中加入内标罗红霉素后,加入乙腈提取,采用LC-MS/MS法正离子方式定量检测;药动学实验采用双周期随机交叉实验设计,取6只健康比格犬将其随机分为2组(每组3只),按犬体质量10mg/kg阿奇霉素给予内服单次药物,两周期之间间隔2周为洗脱期。结果:阿奇霉素血浆浓度在0.2~50.0ng/mL范围内呈良好的线性关系(r=0.9963),其在血浆中的定量限为0.2ng/mL;回收率介于92.8%~103.8%之间,精密度小于10.9%;单次给予阿奇霉素口服混悬液或干混悬剂后的药动学参数AUC0-120、Cmax、tmax、t1/2分别为(9111.91±2072.13)和(6260.12±2006.02)ng/(h·mL)、(570.39±192.16)和(663.73±213.69)ng/mL、(1,42±0.92)和(0.67±0.26)h、(52.85±22.48)和(38.15±7.62)h。结论:该方法灵敏度高,无杂质干扰,结果准确;阿奇霉素口服混悬液或干混悬剂生物利度不等效,其口服混悬液AUC明显高于干混悬剂,其他药动学参数之间经比较其差异无统计学意义。 展开更多
关键词 阿奇霉素 口服混悬液 LC-MS/MS 药动学 生物利用度
Application of hot melt extrusion to enhance the dissolution and oral bioavailability of oleanolic acid 预览
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作者 Nannan Gao Mengran Guo +1 位作者 Qiang Fu Zhonggui He 《亚洲药物制剂科学(英文)》 2017年第1期66-72,共7页
The aim of this study was to improve the in vitro dissolution rate and oral bioavailability of oleanolic acid(OA), a water insoluble drug belonging to BCS class IV. Hot melt extrusion(HME) was applied to develop OA am... The aim of this study was to improve the in vitro dissolution rate and oral bioavailability of oleanolic acid(OA), a water insoluble drug belonging to BCS class IV. Hot melt extrusion(HME) was applied to develop OA amorphous solid dispersions. The characterizations of the optimal formulation were performed by differential scanning calorimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy and in vitro dissolution test.The in vivo pharmacokinetic study was conducted in rats. As a result, OA solid dispersion based on PVP VA 64(OA-PVP) was successfully prepared. In the dissolution medium containing 0.3% SDS, OA-PVP dramatically increased the releasing rate of OA compared with the physical mixture(PM-PVP) and commercial tablet. Furthermore, OA-PVP exhibited higher AUC(P < 0.05) and Cmax(P < 0.05) than PM-PVP and commercial tablet. The superior dissolution property and bioavailability of OA-PVP mainly attributed to the amorphous state of OA in PVP VA64 and the well dispersion caused by thermal melting and shearing. Overall, hot melt extrusion was an efficient strategy to enhance the dissolution rate and oral bioavailability of OA. 展开更多
关键词 Hot MELT EXTRUSION Solid dispersion Oleanolic acid DISSOLUTION rate ORAL BIOAVAILABILITY
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