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Development and optimization of venlafaxine hydrochloride floating microspheres using response surface plots 利用响应面法开发和优化盐酸文拉法辛漂浮微球
Pub Date : 2018-01-01 DOI: 10.12991/mpj.2018.65
Sachin Kumar, R. Mazumder
The current study deals with the development of floating microspheres of venlafaxine hydrochloride. This drug is known as a serotonin-norepinephrine reuptake inhibitor and used to treat depression. Due to the short elimination half life of 4-5 h, the drug has to be administred 2-3 times in a day to maintain the plasma concentration. Thus an attempt was made to decrease the dosing frequency. The microspheres were prepared by non-aqueous solvent evaporation method. The microspheres were evaluated for particle size and morphology using a photomicroscope and scanning electron microscopy, respectively. The incorporation efficiency of microspheres of batch F2 and F6 showed entrapment of 60.6% and 57.2%, respectively. The mean diameters of particles for all batches were found in the range of 226.15 ± 24.37 to 283.37 ± 21.56 μm. The Fourier transform infrared spectroscopy revealed absence of any drug polymer interactions. The microsphers remained buoyant for more than 12 h. The drug release from developed microspheres followed Fickian diffusion with swelling. The results suggested that the developed floating microspheres containing venlafaxine hydrochloride could enhance drug entrapment efficiency, reduce the initial burst release and modulate the drug release.
本文研究了盐酸文拉法辛漂浮微球的研制。这种药物被称为血清素-去甲肾上腺素再摄取抑制剂,用于治疗抑郁症。由于消除半衰期短,4-5小时,因此必须每天给药2-3次以维持血药浓度。因此,进行了降低给药频率的尝试。采用非水溶剂蒸发法制备微球。用显微显微镜和扫描电子显微镜分别对微球的粒径和形貌进行了评价。F2和F6批次微球的混染率分别为60.6%和57.2%。各批次的平均粒径范围为226.15±24.37 ~ 283.37±21.56 μm。傅里叶变换红外光谱显示没有任何药物-聚合物相互作用。微球保持浮力12 h以上。发育后的微球以菲克氏扩散伴溶胀释放药物。结果表明,制备的盐酸文拉法辛漂浮微球能提高药物包封效率,降低初始爆发释放,调节药物释放。
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引用次数: 2
Development and in vitro evaluation of positive-charged solid lipid nanoparticles as nucleic acid delivery system in glioblastoma treatment 带正电荷的固体脂质纳米颗粒在胶质母细胞瘤治疗中作为核酸递送系统的开发和体外评价
Pub Date : 2018-01-01 DOI: 10.12991/mpj.2018.67
G. Akbaba, H. Akbaba, A. G. Kantarci
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引用次数: 9
Swelling and mucoadhesive behavior with drug release characteristics of gastoretentive drug delivery system based on a combination of natural gum and semi-synthetic polymers 天然胶与半合成聚合物复合胃保性给药系统的溶胀黏附及释药特性
Pub Date : 2018-01-01 DOI: 10.12991/mpj.2018.66
R. Bhatta, M. S. Hossain, Sujan Banik, Md Mizanur Rahman Moghal
Using ramipril as a model active pharmaceutical ingredient, the focus of the present study was to fabricate low-cost controlled release tablets using combinations of biopolymer and semi-synthetic polymers. Cellulose derivatives are more viscous where biopolymers form gels more easily. Xanthan gum can’t shape a solid gel, result in fragmentation of gel around the tablets so that depend upon high concentration. Therefore, a combination was used to formulate tablet by direct compression. This combination of polymer provides low cost product with higher potentiality. Ingredients as per formulations were mixed in small polybag through hand blending. Then tablets were compressed one by one tablet in a hydraulic press. Prepared tablets were evaluated for hardness, weight variation, content uniformity, friability, surface pH and in-vitro dissolution studies. ANOVA was used to analyze the differences between release data. Swelling index, mucoadhesive strength and in-vitro residence time was studied to show gastroretention of the tablets. Formulated products exhibit sufficient quality and strength to formulate as a mucoadhesive tablet. Significant differences were found in drug release among different formulations (p ˂0.05) in all cases. Among all of formulations, F11, F12 and F13 containing different ratio of xanthan gum and guar gum showed promising mucoadhesive strength and in-vitro residence time.
本研究以雷米普利为模型活性药物成分,采用生物聚合物和半合成聚合物组合制备低成本控释片。纤维素衍生物黏性更强,生物聚合物更容易形成凝胶。黄原胶不能形成固体凝胶,导致片剂周围的凝胶碎裂,因此依赖于高浓度。因此,采用一种组合方式直接加压制片。这种聚合物的组合提供了低成本和高潜力的产品。根据配方的成分通过手工混合在小塑料袋中。然后在液压机中一片一片地压缩药片。对制备的片剂进行硬度、重量变化、含量均匀性、脆性、表面pH和体外溶出度的评价。采用方差分析(ANOVA)分析各发布数据之间的差异。以肿胀指数、黏附强度和体外停留时间为指标考察其胃潴留效果。配方产品具有足够的质量和强度,可配制成黏合剂片剂。在所有病例中,不同剂型的药物释放有显著差异(p小于0.05)。其中,黄原胶和瓜尔胶配比不同的配方F11、F12和F13均表现出较好的粘接强度和体外停留时间。
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引用次数: 6
A novel hydrogel-thickened microemulsion of dapsone for acne treatment: Development, characterization, physicochemical stability and ex vivo permeation studies 一种用于痤疮治疗的新型水凝胶增稠氨苯砜微乳:开发、表征、理化稳定性和体外渗透研究
Pub Date : 2018-01-01 DOI: 10.12991/mpj.2018.64
Lida Beheshti-Mall, H. Shafaroodi, Zahra Jafariazar, M. Afshar
Acne vulgaris is a common inflammatory skin condition, which has been reclassified as a chronic disease. The spectrum of topical acne treatments has expanded substantially in recent years and various topical medications including topical dapsone are available. Dapsone has special physicochemical properties that make its topical formulation challenging. The aim of this study was preparing a hydrogelthickened microemulsion as a topical delivery system for dapsone. The microemulsions composed of dapsone (5%), isopropyl myristate, tween 80, diethylene glycol monoethyl ether, ethanol and water were prepared. The optimum microemulsion was modified with carbomer 940. Droplet size, pH, refractive index, conductivity, rheology of the optimized formulation, and skin permeation of dapsone through rat skin were evaluated. The optimized formulation significantly increased the skin permeation of dapsone in comparison to that of control gel. Although incorporation of menthol increased the particle size, the flux of microemulgel consisting of menthol (5%) was 2.51 times higher than that of the control. However, the skin absorption of the drug was less than 3%. Six month accelerated studies proved the physicochemical stability of microemulgels. The results of this research indicate that menthol based hydrogelthickened microemulsion system could be a promising vehicle for topical delivery of dapsone.
寻常痤疮是一种常见的炎症性皮肤状况,已被重新归类为慢性疾病。近年来,局部痤疮治疗的范围大大扩大,各种局部药物包括局部氨苯砜都是可用的。氨苯砜具有特殊的物理化学性质,使其局部配方具有挑战性。本研究的目的是制备一种水凝胶增稠微乳剂作为氨苯砜的局部给药系统。制备了以氨苯砜(5%)、肉豆酸异丙酯、吐温80、二甘醇单乙醚、乙醇和水为主要原料的微乳。用卡波姆940对最佳微乳液进行改性。考察了优化制剂的滴度、pH、折射率、电导率、流变性以及对大鼠皮肤的透皮性。与对照凝胶相比,优化后的配方显著提高了氨苯砜的透皮性。虽然薄荷醇的加入增加了粒径,但薄荷醇(5%)微乳的通量是对照的2.51倍。然而,该药物的皮肤吸收率低于3%。六个月的加速研究证明了微凝胶的物理化学稳定性。本研究结果表明,基于薄荷醇的水凝胶增稠微乳液体系可能是一种很有前途的局部给药载体。
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引用次数: 5
Feedback for a simulation practice on communication skills in pharmacy education: A pilot study 药学教育中沟通技巧模拟实践的反馈:初步研究
Pub Date : 2018-01-01 DOI: 10.12991/mpj.2018.69
Elif Deniz, B. Sahne, S. Yeğenoğlu, M. Elcin
Although simulation practice with standard patients became popular in curriculums since years of various countries, it hasn’t been used in the education of pharmacists and pharmacy technicians in Turkey yet. In this study, it is aimed to conduct a pilot study with standard patients on students in the simulation laboratory for the first time and get feedback of them. This study was conducted with 22 pharmacy technicians, four pharmacy students and four standard patients in 15-16 December 2015. Six scenarios were used. After the study, video recordings of the "student-standard patient interaction" were watched with the students to improve the simulation laboratory and the practices planned to be. The physical properties of the place, the use of body language, issues related to the needs and feelings during practice for the development of training programs has come to fore during the feedback of the students. It is useful to generalize this pilot study in terms of both student groups for starting their profession with communication skills and achieving the golden standards in education.
虽然标准病人模拟实习多年来在各国的课程中都很流行,但在土耳其,还没有在药剂师和药学技术人员的教育中使用。本研究旨在首次在模拟实验室对学生进行标准患者的试点研究,并获得学生的反馈。本研究于2015年12月15-16日在22名药学技术人员、4名药学专业学生和4名标准患者中进行。我们使用了六种场景。研究结束后,与学生一起观看“学生与患者标准互动”的录像,以改进模拟实验室和计划进行的实践。在学生的反馈中,场地的物理特性、肢体语言的使用、与培训项目开发实践中的需求和感受相关的问题都得到了体现。将这一试点研究推广到两个学生群体是有益的,以沟通技巧开始他们的职业,并达到教育的黄金标准。
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引用次数: 4
Diclofop-methyl: A phenoxy propionate herbicide with multiple toxic effects in mouse embyro fibroblast (NIH/3T3) cell line 甲基双氯草:一种对小鼠胚胎成纤维细胞(NIH/3T3)具有多重毒性作用的苯氧基丙酸除草剂
Pub Date : 2017-12-01 DOI: 10.12991/mpj.2017.26
M. Çeliksöz, Bahar Ulus, Ezgi Öztaş, G. Özhan
Diclofop-methyl is a selective post-emergence graminicide from the phenoxy propionate group of herbicides to be developed for control of wild oats, millets, and other annual grass weeds. Diclofop-methyl usage is limited in various grass weed species due to its toxic effect and exposure risks. However, total annual usage of is approximately 750.000 pounds in United States, and more in Asia. Therefore, we aimed to investigate diclofopmethyl’s toxic potentials in vitro and the following assays were used; MTT assay for cytotoxicity, comet assay for genotoxicity, generation of reactive oxygen species (ROS), malondialdehyde (MDA) and glutathione (GSH) for the potential of oxidative damage in mouse embryo fibroblast (NIH/3T3) cell line. Diclofop-methyl was observed to reduce the cell viability in a concentration manner and the half maximal inhibitory concentration (IC50) value was 301.7 μM. Diclofop-methyl caused DNA damage and oxidative stress at the concentrations between 12.5-400 μM. Tail intensities were at the range of 1.24- 58.21% with increasing concentrations, which are approximately ≤ 1.63-fold of the negative control. Also, MDA levels were increased ≥ ³11.4-fold of the negative control that denotes lipid peroxidation was induced. However, there was no significant increment in the ROS and GSH levels at all concentrations. In view of the fact that ROS has not been detected, despite its level of MDA proffers, the idea that oxidative damage may have been caused by other mechanisms. Our results indicate that diclofopmethyl was cytotoxic, genotoxic and might have oxidative damage potential in vitro conditions.
甲基双氯草是丙酸苯氧基除草剂中的一种选择性萌发后除草剂,将被开发用于控制野生燕麦、小米和其他一年生杂草。由于其毒性作用和暴露风险,双氯灭在各种杂草中的使用受到限制。然而,在美国,每年的总使用量约为75万磅,在亚洲则更多。因此,我们旨在研究双氯磷甲基的体外毒性潜势,并采用以下方法:MTT法测定细胞毒性,comet法测定遗传毒性,生成活性氧(ROS)、丙二醛(MDA)和谷胱甘肽(GSH)测定小鼠胚胎成纤维细胞(NIH/3T3)的氧化损伤潜力。双氯吡肟有明显的降低细胞活力的作用,半数抑制浓度(IC50)为301.7 μM。在12.5 ~ 400 μM浓度范围内,甲基双氯草可引起DNA损伤和氧化应激。随着浓度的增加,尾部强度在1.24 ~ 58.21%之间,约为阴性对照的≤1.63倍。MDA水平较阴性对照组升高≥³11.4倍,提示脂质过氧化作用发生。然而,在所有浓度下,ROS和GSH水平均无显著升高。鉴于ROS未被检测到,尽管其MDA水平提供,氧化损伤可能是由其他机制引起的。结果表明,在体外条件下,双氯甲酯具有细胞毒性、遗传毒性和氧化损伤潜力。
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引用次数: 0
Influence of honey addition on the bioaccessibility of phenolic contents and antioxidant capacities of different coffee types 添加蜂蜜对不同咖啡品种酚类物质生物可及性及抗氧化能力的影响
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.15
E. Celep, E. Yeşilada
This study was designed to assess the effect of honey addition to the antioxidant capacity and in vitro bioaccessibility of phenolic content of both brewed and soluble coffee. Floral and pine honey were used in the assay. The antioxidant capacities of the samples were evaluated with three different methods: DPPH radical scavenging activity, cupric reducing capacity and total antioxidant capacity tests. In order to measure the antioxidant metabolites of the samples, total phenolic and flavonoid contents were appraised. In vitro gastrointestinal digestion simulation procedure was conducted to mimic the physiochemical and biochemical factors of the gastrointestinal tract. During the digestion process, components in the food matrix are exposed to significant structural changes and certain amount of them are effectively absorbed and reach the circulation. To that end, the importance of studies concerning the simulated gastrointestinal digestion increases. The results of this study revealed that honey addition to coffee samples induced increases in antioxidant capacities, total phenolic and flavonoid contents.
本研究旨在评估添加蜂蜜对煮咖啡和溶咖啡的抗氧化能力和酚类物质体外生物可及性的影响。实验采用花蜂蜜和松蜂蜜。通过DPPH自由基清除能力、铜还原能力和总抗氧化能力三种不同的方法来评价样品的抗氧化能力。为了测定样品的抗氧化代谢产物,测定了总酚和类黄酮的含量。采用体外胃肠消化模拟程序,模拟胃肠道的理化生化因素。在消化过程中,食物基质中的成分发生了明显的结构变化,其中一定数量的成分被有效吸收并进入循环。为此,研究模拟胃肠道消化的重要性增加了。本研究结果表明,在咖啡样品中加入蜂蜜可以提高咖啡的抗氧化能力、总酚和类黄酮含量。
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引用次数: 3
Phytochemicals and biological activities of Macaranga hosei and Macaranga constricta (Euphorbiaceae) 大黄姜和大戟姜(大戟科)的植物化学成分及生物活性
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.11
W. Salleh, N. D. A. Razak, F. Ahmad
Phytochemicals and biological activities of the leaves of Macaranga hosei and Macaranga constricta have been studied. Fractionation and purification of the extracts of M. hosei afforded two triterpenoids, lupenone (1) and β-sitostenone (2) and two flavonoids, 5-hydroxy-7,4’-dimethoxyflavone (3) and 5-hydroxy-6,7,4’-trimethoxyflavone (4). Three triterpenoids characterized as taraxerone (5), taraxerol (6) and β-amyrin (7) were isolated from M. constricta. The structures of these compounds were established by analysis of their spectroscopic data, as compared to that of reported compounds. Biological activities which include antibacterial, α-glucosidase inhibition and antioxidant were also carried out. The antibacterial activities have demonstrated that all extracts and isolated compounds exhibited weak inhibition against the tested bacterial strains with MIC value exceeded 500 μg/mL. Evaluation of α-glucosidase inhibition activity using ρ-nitrophenyl-ρ-D-glucopyranosidase on extracts exhibited α-glucosidase inhibitory potential. The most potent α-glucosidase activity was exhibited by the petroleum ether extract of M. hosei with inhibitory concentration at 50% (IC50) of 25.3 ppm compared with quercetin (4.5 ppm) and acarbose (12.6 ppm). The antioxidant activity was conducted through DPPH radical scavenging activity and total phenolic content. All the extracts displayed positive results and the methanol extract of M. hosei displayed the highest scavenging activity with scavenging concentration at 50% (SC50) value of 25.8 ppm. The methanol extract of M. hosei also gave the highest total phenol content with 347.7 mg GAE/g.
本文研究了麦卡兰(Macaranga hosei)和麦卡兰(Macaranga constricta)叶片的植物化学成分和生物活性。从缢草提取物中分离纯化得到两种三萜类化合物:lupenone(1)和β- sitoneone(2),以及两种黄酮类化合物:5-羟基-7,4′-二甲氧基黄酮(3)和5-羟基-6,7,4′-三甲氧基黄酮(4)。从缢草中分离得到三萜类化合物:taraxerone(5)、taraxerol(6)和β-amyrin(7)。这些化合物的结构是通过分析它们的光谱数据来确定的,并与已报道的化合物进行了比较。并进行了抗菌、α-葡萄糖苷酶抑制和抗氧化等生物活性研究。抑菌活性表明,所有提取物和分离化合物对MIC值大于500 μg/mL的细菌均有较弱的抑制作用。ρ-硝基苯-ρ- d -葡萄糖苷酶对提取物α-葡萄糖苷酶抑制活性评价显示α-葡萄糖苷酶抑制潜力。与槲皮素(4.5 ppm)和阿卡波糖(12.6 ppm)相比,石蜡石油醚提取物的α-葡萄糖苷酶活性最高,抑制浓度为50% (IC50),为25.3 ppm。通过DPPH自由基清除能力和总酚含量测定其抗氧化活性。所有提取物均呈阳性,其中鹤尾草甲醇提取物的清除率最高,其50% (SC50)值为25.8 ppm。甲醇提取物总酚含量最高,为347.7 mg GAE/g。
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引用次数: 3
Comparison of two topical medications, on pain relief due to fistula cannulation in hemodialysis patients 两种外用药物缓解血液透析患者瘘管插管疼痛的比较
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.23
F. Malekshahi, Shirzad Fallahi, M. Mohseni, M. Almasian
Patients with end stage renal failure consider the pain caused by recurrent fistula cannulations as the most intense stress they experience from their treatment and the biggest concern in their lives. One of the fundamental objectives of the nursing procedures is to relieve this pain. Therefore, this study aimed to determine the impact of two topical medications, namely Piroxicam and EMLA cream, on the pain caused by fistula cannulation among hemodialysis patients. This was a clinical trial conducted on 75 patients referring to the dialysis unit of the Shohadaye Ashayer Hospital of Khorramabad, West of Iran, in 2013. The patients were randomly divided into three groups: group A (Piroxicam), group B (EMLA cream), and group C (placebo). The data collection instrument was a questionnaire consisting of three parts: demographic information, the visual analog scale (VAS) for pain assessment, and a checklist for the likely side effects of the medications. The severity of pain during fistula cannulation was assessed in the three groups in two stages (before and after the intervention). To analyze the data, the Kruscal-Wallis and the Mann-Whitney statistical tests and SPSS 19 were used. The median for pain relief was obviously higher in the EMLA cream group than in either the Piroxicam or the placebo group and this difference was statistically significant (p<0.001). Comparing the Piroxicam and the placebo showed that the pain reduction median was much higher in the Piroxicam group than the placebo group, but the difference was not significant. The results of this study showed that the EMLA cream is more effective than the Piroxicam gel in the reduction of pain caused by fistula cannulation among hemodialysis patients. Therefore, based on the results of the present study, it can be suggested that the EMLA cream, as a simple treatment method which can be applied by the patient himself/herself, be used to relieve pain during fistula cannulation of hemodialysis patients.
终末期肾衰竭患者认为复发性瘘管插管引起的疼痛是他们在治疗过程中经历的最大压力,也是他们生活中最大的担忧。护理程序的基本目标之一是减轻这种疼痛。因此,本研究旨在确定两种外用药物Piroxicam和EMLA乳膏对血液透析患者瘘管插管疼痛的影响。这是一项2013年在伊朗西部霍拉马巴德Shohadaye Ashayer医院透析病房进行的75名患者的临床试验。将患者随机分为3组:A组(吡罗昔康)、B组(EMLA乳膏)、C组(安慰剂)。数据收集工具是一份由三部分组成的问卷:人口统计信息、用于疼痛评估的视觉模拟量表(VAS)和药物可能副作用的清单。三组患者分别在干预前和干预后两个阶段评估瘘管插管时疼痛的严重程度。采用Kruscal-Wallis和Mann-Whitney统计检验及SPSS 19进行数据分析。EMLA乳膏组疼痛缓解的中位数明显高于吡罗西康组和安慰剂组,差异有统计学意义(p<0.001)。吡罗昔康与安慰剂组比较,吡罗昔康组疼痛减轻中位数明显高于安慰剂组,但差异不显著。本研究结果表明,EMLA乳膏在减轻血透患者瘘管插管引起的疼痛方面比吡罗昔康凝胶更有效。因此,根据本研究的结果,可以建议使用EMLA乳膏作为一种简单的治疗方法,可由患者自行应用,用于缓解血液透析患者瘘管插管时的疼痛。
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引用次数: 3
Anti-adenovirus activity, antioxidant potential, and phenolic content of dried flower buds of Syzygium aromaticum extract in HEp2 cell line 香合子提取物对HEp2细胞株的抗腺病毒活性、抗氧化能力和酚类物质含量
Pub Date : 2017-12-01 DOI: 10.12991/MPJ.2017.4
M. Moradi, A. Karimi, S. Alidadi, L. Hashemi
The aim of this study is to evaluate in vitro anti-adenovirus property, antioxidant potential, and total phenolic content of dried flowers buds of Syzygium aromaticum crude extract. The crud extract was prepared and its anti-adenovirus activity was investigated on HEp2 cell line using MTT (3-[4,5-dimethylthiazol–2-yl]-2,5-diphenyltetrazolium bromide) assay. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, Folin-Ciocalteu method and aluminum chloride colorimetric method was used to determine antioxidant activity, total phenol content, flavonoids and flavonols content of the extract, respectively. Based on results, the 50% cytotoxicity concentration (CC50) and the 50% inhibitory concentration (IC50) of the extract were 97.66±11.4 and 4.73±1.6 μg/ml, respectively, with the selectivity index (SI) of 20.64. The crud extract inhibited adenovirus replication in post-adsorption step (p<0.05). The extract showed remarkable scavenging activity with IC50 values of 10.05±1.93 μg/ml. Total phenolic, flavonoid and flavonol content of the crude extract was 255.8±3.95 mg GAE/g, 63.9±2.35 mg RUT/g and 62±2.35 mg RUT/g, respectively. The results of the present study indicated that S. aromaticum crude extract exhibited anti-adenovirus activity with inhibitory effect on adenovirus replication
本研究的目的是评价香合欢粗提物的体外抗腺病毒特性、抗氧化潜力和总酚含量。制备粗提物,采用MTT(3-[4,5-二甲基噻唑-2 -基]-2,5-二苯基溴化四唑)法测定其抗腺病毒活性。采用2,2-二苯基-1-苦味酰肼(DPPH)法、福林- ciocalteu法和氯化铝比色法分别测定了提取物的抗氧化活性、总酚含量、总黄酮含量和黄酮醇含量。结果表明,提取物的50%细胞毒浓度(CC50)为97.66±11.4 μg/ml, 50%抑制浓度(IC50)为4.73±1.6 μg/ml,选择性指数(SI)为20.64。粗提物对腺病毒吸附后复制有抑制作用(p<0.05)。提取物具有明显的清除率,IC50值为10.05±1.93 μg/ml。粗提物总酚、类黄酮和黄酮醇含量分别为255.8±3.95 mg GAE/g、63.9±2.35 mg RUT/g和62±2.35 mg RUT/g。结果表明,香参粗提物具有抗腺病毒活性,对腺病毒复制有抑制作用
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引用次数: 5
期刊
Marmara Pharmaceutical Journal
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