食物对两种桂利嗪胶囊人体生物利用度的影响(英文)

目的比较食物对两种桂利嗪胶囊(A和B)人体生物利用度的影响。方法用HPLC紫外检测法测定健康受试者分别在禁食及餐后一次口服50mg桂利嗪胶囊A或B后血清药物浓度。结果胶囊A的Cmax 及AUC不受食物影响 ,胶囊B的吸收受食物影响 ,禁食后的Cmax 和AUC显著低于餐后的Cmax 和AUC。结论胶囊A的制剂优于胶囊B的制剂 ,其人体生物利用度不受食物影响     

食物对两种桂利嗪胶囊人体生物利用度的影响

目的 比较食物对两种桂利嗪胶囊（A和B）人体生物利用度的影响。方法 用HPLC紫外检测法测定健康受试分别在禁食及餐后一次口服50mg桂利嗪胶囊A或B后血清药物浓度。结果 胶囊A的Cmax及AUC不受食物影响，胶囊B的吸收受食物影响，禁食后的Cmax和AUC显低于餐后的Cmax和AUC。结果 胶囊A的制剂优于胶囊B的制剂，其人体生物利用度不受食物影响。     

药品说明书中“服药时间”项的调查分析

口服给药的时间有空腹服用、餐前服用、餐时服用、餐后服用、清 (早 )晨服用、睡前 (晚间)服用等几种类型 ,它是根据药物在体内的吸收、药物的生物利用度、药物与食物的关系以及药物不良反应等多种因素来决定的。掌握正确的服药时间是保证药物治疗效果的要素之一 ,而指导患者正确服药的最重要的依据是药品说明书。为了规范调剂工作中的发药交待环节 ,笔者对口服药物药品说明书中的“服药时间”项进行了调查、分析。1资料与方法随机查阅重庆长航医院和成都市第三人民医院2002年12月以前正在使用的口服药物药品说明书349份 ,分别按药理作用及…     

掌握用药常识 合理有效用药

一、服药时间概念1．清晨空腹服药。因空腹时,胃和小肠已基本没有食物,胃排空快。此时服用药物迅速到达小肠,吸收充分,作用迅速有效。如抗结核药利福平胶囊,空腹服药,没有食物影响药物吸收,血药浓度可达高峰,并很快吸收分布到全身。其它如容积性     

空腹或餐后服用国产伊曲康唑胶囊的人体生物等效性研究

目的:评价健康男性志愿者空腹或餐后单次口服国产伊曲康唑胶囊与进口伊曲康唑胶囊(商品名为斯皮仁诺胶囊)的生物等效性.方法:本研究包括两个随机、开放、双周期、单次口服给药试验,各入组24名健康中国男性受试者,分别在空腹和餐后服用200 mg试验制剂和200 mg参比制剂后,采用HPLC-MS/MS方法测定给药后伊曲康唑的血药浓度.计算主要药动学参数,分别对两种制剂的空腹或餐后给药进行生物等效性评价.结果:空腹给药试验制剂与参比制剂的主要药动学参数为.Cmax为(124±79)和(124±86) μg/L;tmax为(2.9±0.8)和(2.5±0.9)h;AUC0-t为 (1320±826) 和(1348±1095) μg·h·L-1; AUC0-∞为(1420±902)和(1444±1148) μg·h·L-1;AUC0-t/AUC0∞为(93.0±4.9)和(92.3±5.1)％;t1/2为(17.7±4.7)和(18.1±2.8)h.空腹给药试验制剂的相对生物利用度F为(106.5±35.4)％.餐后给药试验制剂和参比制剂的主要药动学参数为:Cmax为(202±107)和(218±109) μg/L;tmax为(4.2±0.8)和(3.9±0.8) h;AUC0-t为(2494±1163)和(2657±1424) μg·h·L-1;AUC0-∞为(2705±1290)和(2870±1578) μg·h·L-1;AUC0-t/AUC0∞为(92.3±5.2)和(93.6±4.1)％;t1/2为(19.3±5.5)和(18.0±5.1)h.餐后给药试验制剂的相对生物利用度F为(100.5±33.1)％.结论:两种制剂在空腹给药和餐后给药时都具有生物等效性.餐后给药组Cmax和AUC均明显高于空腹给药组,建议临床使用餐后服用药物,以提高药物的生物利用度,增强疗效.     

进食时机对口服抗肿瘤药物生物利用度影响的研究进展

目的探索食物对口服抗肿瘤药物生物利用度的影响。方法检索SCI、GeenMedical、PubMed、中国知网、万方数据库,查询食物对口服抗肿瘤药物生物利用度影响的相关文献并进行汇总整理。结果食物可影响一部分口服抗肿瘤药物的生物利用度,需要空腹服用的药物有依托泊苷、替莫唑胺、索拉非尼、塞瑞替尼,需要与食物一起服用的药物有长春瑞滨、伊马替尼、维莫非尼、阿来替尼,需要避免与食物一起服用的药物有尿嘧啶替加氟、替吉奥、卡培他滨、拉帕替尼、厄洛替尼、帕唑帕尼、阿法替尼、阿帕替尼、曲美替尼、达拉非尼、依西美坦、阿比特龙。结论临床需要注意食物对口服抗肿瘤药物生物利用度的影响,指导患者合理用药,保证抗肿瘤药物的有效性和安全性。     

植物药-化学药间基于有机阴离子转运多肽介导的相互作用研究进展

有机阴离子转运多肽(OATPs)是人及动物体内最重要的细胞膜吸收转运蛋白,在肝脏中有大量分布,介导多种内源性物质及临床常用药物的吸收转运,影响着药物在体内的吸收、分布和清除过程.许多植物药及其有效成分是OATPs的底物,它们对OATPs活性表现出抑制或者诱导作用,从而对OATPs介导的其他药物转运产生影响,改变药物生物利用度或产生不良反应.本文概述了基于OATPs介导的植物药-化学药物之间可能发生的相互作用研究进展.     

磷酸奥司他韦胶囊在健康中国受试者的生物等效性研究

目的:评价磷酸奥司他韦胶囊受试制剂与参比制剂(达菲?)在健康受试者空腹和餐后状态下的生物等效性和安全性.方法:采用单中心、随机、开放、两周期、自身交叉、单次给药试验设计,健康受试者分别空腹(36例)和餐后(36例)服用75 mg磷酸奥司他韦胶囊受试制剂或参比制剂,采用高效液相色谱-串联质谱(UPLC-MS/MS)检测奥...     

406种口服药品说明书用药时间与方法的统计分析

目的调查某院2018年度口服药品说明书服药时间和服药方法的标注情况,为提高患者用药安全提供参考依据。方法调查某院精配软件系统中2018年度有使用过的406种口服药品电子版说明书。根据药品说明书中的用法用量和注意事项下的内容,对药品的用药时间和用药方法标注情况进行统计分析。结果406份口服药品说明书中,标注服药时间的共186份(占45.81%),未标注的220份(占54.19%)。其中餐前服用28份(占6.90%),餐中服用23份(占5.67%),餐后服用33份(占8.13%),空腹服用31份(占7.64%),晚上(或睡前)服用16份(占3.94%),服药不受进食影响55份(占13.55%)。标注具体服用方法的有67份(占16.50%),未标注的339份(占83.50%)。结论406份口服药品说明书不管是服用时间还是服用方法标注率都偏低,这样的药品说明书标注现状对于患者用药是存在安全隐患的。所以药品说明书的修订和完善还需要相关部门加强管理,不断改进,确保临床用药安全有效。     

头孢氨苄缓释胶囊的开发及人体生物利用度研究

通过制剂学手段延长头孢氨苄的释放,制成一日服2次代替原需分4次服用的口服制剂,以提高病人的顺应性和临床治疗效果。用微生物法测定头孢氨苄缓缓释胶囊在10例健康志愿者体内的药物动力学和生物利用度,并与进口复粒胶囊和普通胶囊进行了比较研究。生物利用度结果表明,缓释胶囊的有关药动学参数与进口复粒胶囊相比,均无显著性差异(P>0.05),与普通胶囊相比,T_(max)和T_(1/2)有显著的差异(P<0.05),而C_(max)和AUC均无显著性差异。缓释胶囊对进口复粒胶囊的相对生物利用度为98.70％,对普通胶囊为97.28％。     

Effect of food intake on the bioavailability of boswellic acids from a herbal preparation in healthy volunteers

In this study we investigated the effects of concomitant food intake on the bioavailability of distinct boswellic acids (BAs) from the test preparation BSE-018, a dry extract from Boswellia serrata gum resin. In a randomised, open, single-dose, two-way crossover study, healthy male subjects received three capsules of BSE-018 equivalent to 786 mg dry extract of Boswellia serrata gum resin either in the fasted state or together with a standardised high-fat meal. BA plasma concentrations were analysed for up to 60 h after oral dosing by reversed phase HPLC. As compared to the fasted state (treatment A), the administration of BSE-018 concomitantly with a high-fat meal (treatment B) led to several-fold increased areas under the plasma concentration-time curves as well as peak concentrations of beta-boswellic acid (betaBA), 11-keto-beta-boswellic acid (KbetaBA) and acetyl-11-keto-beta-boswellic acid (AKbetaBA). Plasma levels of both acetyl-alpha-boswellic acid (AalphaBA) and alphaBA became only detectable when administered with treatment B, i.e., the high-fat meal. Accordingly, pharmacokinetic data could be calculated for betaBA, KbetaBA and AKbetaBA (treatment A) and for betaBA, KbetaBA, AKbetaBA, alphaBA, and AalphaBA (treatment B). For the first time these data reveal detailed kinetics of BAs after oral dosing of an extract and demonstrate a profound effect of food intake on the pharmacokinetic profile of the BAs. This finding should be very important whenever BAs would be considered for therapeutic use.     

Effect of food on the pharmacokinetics and bioavailability of oral imiquimod relative to a subcutaneous dose

OBJECTIVES: The present study, the first clinical pharmacokinetic report of the immune response modifier imiquimod, was conducted to assess the effect of food on the oral absorption of imiquimod, to characterize its pharmacokinetics, and to estimate its oral bioavailability. SUBJECTS AND METHODS: Sixteen healthy male volunteers completed this open-label, randomized, three-period crossover study. Subjects received a 100 mg oral dose of imiquimod after fasting in one period, after a standarized, high fat meal in another, and a 30 mg subcutaneous dose in the third period. RESULTS: The oral bioavailability of imiquimod was on average 47%, and independent of whether imiquimod was administered with or without food. Oral imiquimod was absorbed in both fasted and non-fasted states with an absorption half-life of approximately 1 hour. However, there seemed to be a delay in the initiation of the absorption process when food was administered, which translated in to a Tmax of approximately 2.6 hours while fasting and one hour later in the non-fasted state. Imiquimod was rapidly eliminated with a half-life of approximately 2.5 hours and a total body clearance of approximately 970 ml/hxkg. Although equivalence could not be established due to the large intersubject variability, no significant differences in rate (Cmax) and extent (AUC) of oral absorption were observed between the fasted and non-fasted states. In addition, the Cmax, AUC and bioavailability values for individual subjects were consistent between both oral treatments. CONCLUSION: This study suggests that food does not have a major effect on the rate, extent of absorption or bioavailability of oral imiquimod, and thus, it is suitable to administer imiquimod orally in either the fasted or non-fasted states.     

Drug administration and control in a large mental retardation facility

Better control and more accurate drug dosing in the large institution has long been needed. This project focused on the proven unit dose concept with variations for the long-term care institution. The system described serves a client population of 875 mentally retarded persons. Operation and maintenance of the system requires a staff of three FTE pharmacists and three FTE pharmacy technicians. The concept is based on a 72-hour exchange cycle and features the use of a 3-day carrier package for each oral solid medication dispensed. Single dose identification provides pharmacy personnel with the capability to closely monitor drug administration activities. For example, omitted doses can be readily linked to a specific date and time of occurrence. Single doses are dispensed into separate dosing sections, even though several tablets or capsules may be required for one dose. The package design additionally permits first-dose administration times to be programmed by the pharmacist in order to minimize delays in starting newly prescribed medications, such as antibiotics. Use of the package eliminates the need to purchase tablets and capsules in commercial unit dose form. It is also unnecessary to buy automatic packaging equipment. The entire process is adaptable to both manual and computerized pharmacy systems.     

Effect of a high-fat meal on thalidomide pharmacokinetics and the relative bioavailability of oral formulations in healthy men and women

The effect of food on the oral pharmacokinetics of thalidomide and the relative bioavailability of two oral thalidomide formulations were determined in an open label, single dose, randomized, three-way crossover study. Five male and eight female healthy volunteers received a single oral dose of 200 mg Celgene thalidomide capsules under fasted and non-fasted conditions, and a single dose of 200 mg tablets of Serral thalidomide under fasted conditions. The high-fat meal resulted in a 0.5-1.5 h absorption lag time, an increased mean C(max), a decreased mean AUC and a delay in mean T(max). The Serral tablet formulation resulted in a lower mean C(max), and slower terminal decline in plasma thalidomide concentrations compared with both Celgene treatments. Mean C(max) concentrations were 1.99+/-0.41 microg/mL (range 1.28-2.76) within 4.00+/-1.13 h (2-5) for the Celgene formulation fasted, 2.17+/-0.51 microg/mL (1.43-3.01) within 6.08+/-2.33 h (3-12) for the Celgene formulation with food, and 1. 05+/-0.31 microg/mL (0.62-1.65) within 6.23+/-1.88 h (5-10) for the Serral formulation fasted. Mean terminal half-lives were 13.50+/-6. 77 h for the Serral product, compared with 5.80+/-1.72 h and 5. 09+/-1.03 h for Celgene fasted and fed, respectively. Celgene's formulation exhibited slightly greater bioavailability than Serral's formulation, with mean ratios of 122% and 110% for Ln-transformed AUC(0-t) and AUC(0-infinity), respectively. The mean C(max) for the Celgene formulation was approximately two times greater than Serral's. Food delayed the onset of absorption of by 0.5-1.5 h, but had little effect on the extent of absorption from the Celgene capsule. Under fasted conditions, the Celgene thalidomide resulted in a two-fold greater C(max) and 10% greater AUC(0-infinity) than the Serral formulation.     

501种口服药品说明书用药时间和方法的统计分析

目的：调查口服药品说明书中关于服药时间和方法的标注情况,为提高患者用药安全和医院药学信息化建设提供参考。方法：统计某院口服药物共501种药品说明书中服用时间和方法的标注情况并进行整理、归纳和分析。结果：501份药品说明书中,标注服用时间的共计128份,占比25.55%,其中餐前服用占12.18%,餐中服用占2.20%,餐后服用占6.99%,晚上服用占4.19%,标注特殊服用方法共计50份,占比为9.98%,未标注共335份,占66.87%。结论：口服药品说明书对服药时间和方法的标注率偏低,同成分不同厂家的口服药品说明书标注存在差异,使临床用药存在一定风险,药品说明书信息仍需进一步规范和完善。     

An evaluation of the effect of food on the oral bioavailability of sustained-release morphine sulfate tablets (ORAMORPH SR) after multiple doses.

The effect of food on the oral bioavailability of sustained-release morphine sulfate tablets (ORAMORPH SR; Roxane Laboratories, Inc., Columbus, OH; OSR) was examined in an open-label, randomized, two-period crossover study. Healthy male volunteers received a 30-mg OSR tablet orally every 12 hours for seven doses during both the fasted and fed states. Dosing periods were separated by a 14-day washout. Volunteers in the fasted group received all doses either 2 hours before or after meals. Volunteers in the fed group received all doses immediately after meals. All meals were standardized. Serial blood samples were collected for analysis of plasma morphine concentration by radioimmunoassay. Pharmacokinetic parameters were calculated using plasma concentration data collected after the last dose at 72 hours of each dosing period. The two one-sided t analysis indicated confidence intervals between 80% and 120% for maximum peak plasma concentration (Cmax), AUC72-84hr, Cavg, and Cmin. The relative bioavailability of OSR administered after meals was 90.2% of that administered in the fasted state. As compared with the fasted condition, morphine bioavailability was essentially unchanged when multiple oral doses of 30-mg OSR tablets were given after meals.     

Absorption of vitamin K2 by dogs after oral administration of a soft gelatin capsule formulation containing a new emulsion-type vehicle

This study has evaluated the performance of a newly developed vehicle for administration of a drug in a soft gelatin capsule. The absorption of vitamin K2 in dogs after oral administration of the vitamin in a soft gelatin capsule containing the newly developed vehicle was compared with absorption after administration of a control formulation prepared by encapsulating the contents of a commercially available vitamin K2 capsule (Glakay capsules 15 mg) in the same type of soft gelatin. Under non-fasted conditions the profile of the plasma concentration of vitamin K2 against time for the test formulation was comparable with that for the control formulation in non-fasted dogs. Under fasted conditions, however, both the maximum concentration (Cmax) and the area under the plot of concentration against time (AUC) were significantly smaller for the test formulation than for the control formulation. The Cmax and AUC for the test formulation were about 10 times larger for non-fasted dogs than for fasted dogs whereas values for the control formulation were about twice as large. These results suggest that both formulations might require the presence of food or digestive fluid components, or both, for better absorption of vitamin K2. It seems that although the performances of the test and control formulations were comparable in the presence of these components, the control formulation works better in their absence. It should be also noted that, in contrast with the results from the absorption tests, the dispersibility of the test vehicle in water was much better than that of the control vehicle. This suggests that dispersibility does not significantly affect vitamin K2 absorption. In conclusion, although the new vehicle did not perform better than the control vehicle in terms of vitamin K2 absorption, the performance of the control formulation was comparable for non-fasted dogs. Because the new vehicle contains considerably less surfactant than the vehicles currently used in soft gelatin capsules, it could be a safer alternative for use under non-fasted conditions.     

Reduced food-effect and enhanced bioavailability of a self-microemulsifying formulation of itraconazole in healthy volunteers.

Self-microemulsifying drug delivery systems (SMEDDS) represent a possible alternative to traditional oral formulations of lipophilic compounds. This study was designed to compare the oral bioavailability and food-effect of SMEDDS of itraconazole (ITRA-GSMP capsule containing 50mg itraconazole) to that of the currently marketed formulation (Sporanox capsule containing 100mg itraconazole). Eight healthy volunteers received Sporanox or ITRA-GSMP capsule in the fasted state or after a high-fat diet on four separate dosing occasions with a 2-week washout period. Blood samples were collected and analyzed. After administration of the ITRA-GSMP capsule, AUC0-24 and Cmax were 1.9- and 2.5-fold higher in the fasted state and 1.5- and 1.3-fold higher in the fed state, respectively, than those of the Sporanox capsule. Moreover, ITRA-GSMP capsules yielded more reproducible blood-time profiles than Sporanox capsules. Food had a marked effect on itraconazole absorption from the Sporanox capsule, whereas the influence was less pronounced for the ITRA-GSMP capsule. Collectively, our data suggest that a new self-microemulsifying formulation may provide an alternative oral formulation for itraconazole with improved oral bioavailability and reduced food-effect.     

Effect of food on absorption of indoprofen administered orally to man in two dosage forms.

The influence of food on the bioavailability of two oral dosage forms (100-mg capsules and 200-mg tablets) of indoprofen, a new propionic acid derivative with marked anti-inflammatory and analgesic properties, has been investigated. Plasma levels and urinary excretion of indoprofen were determined both in the fasting state and after a standard meal in healthy volunteers after administration of two 100-mg capsules (4 subjects) and of one 200-mg tablet (6 subjects). Indoprofen in biological fluids was determined by gas-liquid chromatography. The extent of absorption from tablets was not affected by food as indicated from the values of the total area under plasma level curves and urinary excretion of the drug. The rate of absorption was faster after meal than in the fasting state. The opposite was found for capsules, which showed a slightly delayed absorption after food. The results suggest that food may differently influence the absorption pattern of different pharmaceutical forms of the same drug.     

Development of self-microemulsifying drug delivery systems for oral bioavailability enhancement of alpha-Asarone in beagle dogs

A self-microemulsifying drug delivery system (SMEDDS) for enhancement of oral absorption of a poor water-soluble drug, alpha-Asarone (ARE), is reported. Solubility of ARE was determined in various vehicles. SMEDDS consisted of a mixture of oils, surfactants, and cosurfactants that were emulsified in an aqueous medium under the gentle agitation and digestive motility. Pseudo-ternary phase diagrams were used to identify the efficient self-emulsification regions. The particle size distribution of the resulting microemulsions was determined using a laser scatter particle size analyzer (LSPSA). The optimized SMEDDS formulations containing Ethyl oleate (20%), Tween 80 (60%), and PEG 400 (20%) were tested for in vitro dissolution. The percentage of ARE released from the SMEDDS was significantly higher than that from the conventional tablets. Oral bioavailability of ARE in the SMEDDS via the hard capsules and the conventional tablets was evaluated in fasted beagle dogs. The bioavailability of ARE formulated in SMEDDS showed approximately 4.8-fold higher bioavailability than that in the conventional tablets. The results indicated that SMEDDS is potentially a good drug delivery system for oral delivery of the hydrophobic compound ARE.