共查询到20条相似文献,搜索用时 78 毫秒
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水飞蓟素高生物利用度制剂的研究现状 总被引:7,自引:0,他引:7
目的:介绍近年来国内外对高生物利用度水蓟素剂型的研究现状。方法:通过查阅文献,对水飞蓟素-环糊精包合物、水飞蓟素固体分散体、水飞蓟宾—葡甲胺盐、水乙蓟宾—邻苯二甲酸甲酯钠盐、水飞蓟宾—二偏琥珀酸酯钠盐、水飞蓟宾-研究脂酰胆碱复合物等进行综述。结果:各类制剂学方法均能显著提高水飞蓟素的生物利用度,其中水冰蓟素-磷脂酰胆碱复合物,不仅能大大提高水飞蓟素的生物利用度,提高疗效,而且还具有清除自由基、抗脂质近氧化等多种作用。结论:水飞蓟素磷脂复合物是一种理想的高效水飞蓟素制剂。 相似文献
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吸收促进剂在口服制剂中增强药物生物利用度的作用 总被引:11,自引:0,他引:11
文爱东 《国外医学(药学分册)》2000,27(6):354-357
本文主要讨论口服制剂中药物的弱透过性、胃肠道的解剖学和生物化学因素,以及吸收途径,阐述了吸收促进剂的基本概念、定义、分类和毒理学作用。在分子水平上讨论了胃肠道上皮细胞膜的生物化学和生物物理特点〉肽类和蛋白质通过粘膜的生化和物理机制。 相似文献
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中药对病症进行治疗具有较高的有效性,而本文以中药的口服机制作为研究的出发点,对中药制剂的生物利用度进行相应分析,通过对中药中难容的活性成分的溶解、溶出速度进行改善,对活性成分在消化系统中的代谢进行控制,使中药组合中活性成分之间的有利影响进行充分发挥等方式,提升中药制剂口服吸收生物利用度。 相似文献
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制剂人体生物利用度试验中若干问题的讨论孙鲁远,倪慕慈(浙江省卫生厅药品审评办公室310004)根据新药审批管理的规定,对西药第四类新药中改变剂型但不改变给药途径的,如其原料药(或原制剂)属国家标准,可进行人体生物利用度研究替代临床验证(另外,对已过保... 相似文献
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口服固体制剂溶出度与人体生物利用度的相关性 总被引:1,自引:0,他引:1
口服固体制剂的溶出度是影响人体生物利用率的一个重要因素,两者有着明显的相关性。分析和研究影响制剂溶出度的各种因素,制定合理的处方和工艺设计对提高制剂的溶出速率,对保证药物的生物有效性有重要意义。 相似文献
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目的探讨提高难溶性口服药物生物利用度的方法。方法综述了影响药物吸收的因素以及改善难溶性药物吸收的方法。结果药物的吸收是影响药物生物利用度的重要因素,其吸收过程与药物因素、剂型因素、生理因素等有密切关系。结论随着药学领域中新技术、新材料的发展,难溶性药物通过口服给药也可获得较好的吸收和生物利用度。 相似文献
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如何提高眼部给药的生物利用度 总被引:3,自引:0,他引:3
钟力煌 《中国医院药学杂志》1993,13(2):77-79
眼药滴眼是眼科最常用的局部给药方法,其次是结膜下注射、眼用药膜给药及球后注射等。各种不同给药方法可用于不同疾病的治疗。为了提高眼用药物的疗效,减少毒副作用,减少药物的浪费,本文从眼药动力学角度如何提高眼部给药的生物利用度的途径作一 相似文献
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A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability 总被引:10,自引:10,他引:0
Amidon Gordon L. Lennernäs Hans Shah Vinod P. Crison John R. 《Pharmaceutical research》1995,12(3):413-420
A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption. This analysis uses a transport model and human permeability results for estimating in vivo drug absorption to illustrate the primary importance of solubility and permeability on drug absorption. The fundamental parameters which define oral drug absorption in humans resulting from this analysis are discussed and used as a basis for this classification scheme. These Biopharmaceutic Drug Classes are defined as: Case 1. High solubility-high permeability drugs, Case 2. Low solubility-high permeability drugs, Case 3. High solubility-low permeability drugs, and Case 4. Low solubility-low permeability drugs. Based on this classification scheme, suggestions are made for setting standards for in vitro drug dissolution testing methodology which will correlate with the in vivo process. This methodology must be based on the physiological and physical chemical properties controlling drug absorption. This analysis points out conditions under which no in vitro-in vivo correlation may be expected e.g. rapidly dissolving low permeability drugs. Furthermore, it is suggested for example that for very rapidly dissolving high solubility drugs, e.g. 85% dissolution in less than 15 minutes, a simple one point dissolution test, is all that may be needed to insure bioavailability. For slowly dissolving drugs a dissolution profile is required with multiple time points in systems which would include low pH, physiological pH, and surfactants and the in vitro conditions should mimic the in vivo processes. This classification scheme provides a basis for establishing in vitro-in vivo correlations and for estimating the absorption of drugs based on the fundamental dissolution and permeability properties of physiologic importance. 相似文献
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无定形药物在提高难溶性药物溶解度、改善其溶出及生物利用度方面具有显著优势,故而广泛应用于药物制剂领域。但无定形药物处于能量较高的非稳态,易发生结晶,从而失去其在溶解度和溶出速率等方面的优势。因此,在无定形药物制剂的制备和储存过程中,为控制质量需要对其进行相应表征。目前,已有包括光学技术、热分析技术、光谱学技术等在内的多种技术被广泛用于无定形药物制剂的研究领域。本文简述无定形药物制剂的多种新发展的表征技术,包括偏光显微镜-控温热台联用、表面光栅衰减、X射线粉末衍射-同步辐射光源技术联用、热分析技术、宽频介电谱、纳米红外光谱分析、拉曼光谱成像、固态核磁共振、荧光分析、X射线光电子能谱等技术,并重点介绍近几年该领域的研究进展及其应用,以期为无定形药物制剂研究和开发提供借鉴。 相似文献
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PURPOSE: The aim of this study was to investigate the effects of different doses of polyethylene glycol 400 (PEG 400) on the bioavailability of ranitidine in male and female subjects. METHOD: Ranitidine (150 mg) was dissolved in 150 ml water with 0 (control), 0.5, 0.75, 1, 1.25 or 1.5 g PEG 400 and administered to 12 healthy human volunteers (six males and six females) in a randomized order. The cumulative amount of ranitidine and its metabolites excreted in urine over 24 h was determined for each treatment using a validated HPLC method. RESULTS: In the male volunteers, the mean cumulative amount of ranitidine excreted in the presence of 0, 0.5, 0.75, 1, 1.25 and 1.5 g PEG 400 were 35, 47, 57, 52, 50 and 37 mg respectively. These correspond to increases in bioavailability of 34%, 63%, 49%, 43% and 6% over the control treatment. In the female subjects, the mean cumulative quantity of ranitidine excretion in the absence and presence of increasing amounts of PEG 400 were 38, 29, 35, 33, 33 and 33 mg, corresponding to decreases in bioavailability of 24%, 8%, 13%, 13% and 13% compared to the control. The metabolite excretion profiles followed a similar trend to the parent drug at all concentrations of PEG 400. CONCLUSIONS: All doses of PEG 400 enhanced the bioavailability of ranitidine in male subjects but not females, with the most pronounced effect in males noted with the 0.75 g dose of PEG 400 (63% increase in bioavailability compared to control, p < 0.05). These findings have significant implications for the use of PEG 400 in drug development and also highlight the importance of gender studies in pharmacokinetics. 相似文献
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Alberti Ingo Kalia Yogeshvar N. Naik Aarti Guy Richard H. 《Pharmaceutical research》2001,18(10):1472-1475
Pharmaceutical Research - 相似文献
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《Journal of pharmaceutical sciences》2019,108(9):3020-3028
At present, coamorphous systems have attracted increasing interest in the pharmaceutical field owing to their enhanced stabilities, increased solubilities, and improved bioavailabilities compared with those of their pure amorphous and crystalline counterparts. In this study, a novel coamorphous solid form of ibrutinib (IBT) and saccharin (SAC) (1:1 molar ratio) was prepared through rotary vacuum evaporation and then characterized. Differential scanning calorimetry and X-ray powder diffraction indicated the formation of the coamorphous IBT-SAC after rotary vacuum evaporation. Compared with amorphous IBT, coamorphous IBT-SAC exhibited enhanced stability owing to the intermolecular interaction between IBT and SAC. Moreover, the solubility and dissolution of the coamorphous IBT-SAC were increased up to 4.0-7.7 times and 4.3 times, respectively, compared with those of its crystalline Form A. In addition to the superior behaviors of coamorphous IBT-SAC in vitro, the in vivo bioavailability study revealed notable increases in the Cmax and area under the curve0-t of the coamorphous form compared with those of its crystalline Form A. The current study demonstrates that the coamorphization of IBT and SAC presents a promising technology to overcome the limitations of solubility and stability that arise from IBT and can therefore contribute to a major improvement in the bioavailability of IBT. 相似文献
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