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Phytochemical screening and antimicrobial activities of leaf extracts of Mucuna pruriens 麻豆叶提取物的植物化学筛选及抑菌活性研究
Pub Date : 2019-12-18 DOI: 10.4314/JOPHAS.V16I4
O. Ushie, V. Okpashi, T. Azuaga, S. Iyen, E. Aikhoje, J. I. Lajaka
The aim of this study is to carry out phytochemical screening of the methanol, n-hexane and ethyl acetate leaf extracts of the plant Mucuna pruriens and to evaluate their antimicrobial activities. The crude extracts were tested on three bacterial species; Klebsiella aerogenes, E coli and Pseudomonas aeruginosa and two fungal isolates – Candida albicans and Aspergillus niger . The results revealed the presence for steroids, terpenes, alkaloids, saponins, tannins, and flavonoids in the extracts. Almost all the extracts inhibited Klebsiella aerogenes , Escherichia coli , and Pseudomonas aeruginosa . The implication is that these extracts can be used to cure diseases associated with the tested organisms. Methanol extract did not inhibit growth of Aspergillus niger but demonstrated high activity against Candida albicans . The result implies that the plant can actually be used to cure diseases associated those organisms such as diarrhea, stomach cramps, and nausea. Keywords: Phytochemical screening, Mucuna pruriens, antimicrobial studies, leaf extracts Journal of Pharmaceutical and Allied Sciences, Vol. 16 No.4 (2019)
本研究的目的是对麻豆叶中甲醇、正己烷和乙酸乙酯提取物进行植物化学筛选,并评价其抑菌活性。粗提物对3种细菌进行了检测;产气克雷伯氏菌,大肠杆菌和铜绿假单胞菌以及两种真菌分离株-白色念珠菌和黑曲霉。结果显示,提取物中存在类固醇、萜烯、生物碱、皂苷、单宁和黄酮类化合物。几乎所有提取物对产气克雷伯菌、大肠杆菌和铜绿假单胞菌均有抑制作用。这意味着这些提取物可以用来治疗与被测试生物相关的疾病。甲醇提取物对黑曲霉的生长没有抑制作用,但对白色念珠菌有较高的抑制作用。这一结果表明,这种植物实际上可以用来治疗与这些微生物有关的疾病,如腹泻、胃痉挛和恶心。关键词:植物化学筛选;毛粘虫;抗菌研究;
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引用次数: 1
A comparative study of floating drug delivery system of metronidazole formulated using effervescent and non effervescent techniques 用泡腾法和非泡腾法配制甲硝唑漂浮给药系统的比较研究
Pub Date : 2019-11-15 DOI: 10.4314/JOPHAS.V16I3
C. Airemwen, M. Uhumwangho
This study was carried out to compare effervescent and non-effervescent gastro-floating matrix tablets (GFMT) of metronidazole formulated using Azadirachta indica (Neem) gum (AIG). Neem gum was extracted by a method previously described. Granules were prepared by wet granulation technique using the extracted neem gum at varying concentrations (2, 4, 6 and 8% w/w). Sodium bicarbonate and tartaric acid were used as the gas generating agents for the GFMTs, while ammonium bicarbonate was used as the sublimating agent for the non-effervescent GFMTs. Formulations were either prepared alone with the natural gum or with the addition of 1.0% w/w of acrylate methacrylate copolymer (Eudragit® RL100). All granules were evaluated for micromeritic properties. The granules were compressed at an optimized compression pressure of 30 arbitrary unit on the tableting machine load scale and the non-effervescent GFMTs were sintered at 70 °C for 12 h in a hot-air oven. Tablets were evaluated for hardness, friability, floating lag time, in vitro buoyancy and drug release profiles. Drug-excipient compatibility study was done using Fourier Transform Infra-red Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). Scanning Electron Microscope (SEM) was used to analyze the pores and morphology of the tablets. Results revealed that all formulated floating matrix granules were free flowing, with angle of repose and Carr’s index ≤ 33.2o and ≤ 15.5% respectively. All floating matrix granules were compressible with tablet hardness ≤ 9.0 Kg/cm 2 . Generally, the percentage friability of the GFMTs decreased with increase in binder concentration (≤ 0.99%). The floating lag time for the effervescent GFMT tablets ranged from 2-7 min, while the non-effervescent formulations had zero floating lag time. FTIR and DSC studies showed that the excipients and the active pharmaceutical ingredient (API) i.e. metronidazole were compatible. SEM reveals the presence of pores and a smooth surface of the non-effervescent GFMTs, while smooth surface with no pores was revealed in the effervescent formulations. Gastro-floating matrix tablets of metronidazole were successfully formulated in this study using the effervescent and non-effervescent techniques and there was significant difference in the floating lag times (P 0.05). Keywords : Floating, matrix tablets, effervescent, non-effervescent, buoyancy.
本研究对印楝胶配制的甲硝唑胃浮基质泡腾片和非泡腾片进行了比较。用前面描述的方法提取印楝胶。用不同浓度(2、4、6和8% w/w)提取印楝胶,采用湿造粒技术制备颗粒。采用碳酸氢钠和酒石酸作为气体生成剂,碳酸氢铵作为升华剂制备非起泡型石墨烯纳米管。配方要么单独使用天然胶,要么添加1.0% w/w的丙烯酸酯-甲基丙烯酸酯共聚物(Eudragit®RL100)。对所有颗粒进行微粒性评价。在压片机负荷量表上以任意30单位的优化压缩压力对颗粒进行压缩,并在热风烘箱中在70℃下烧结12 h。对其硬度、脆性、漂浮滞后时间、体外浮力和药物释放特性进行了评价。采用傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)研究了药物赋形剂的配伍性。采用扫描电镜(SEM)对片剂的孔隙和形貌进行了分析。结果表明:配制的悬浮基质颗粒均为自由流动,休止角≤33.2,卡尔指数≤15.5%;所有漂浮基质颗粒均可压缩,片剂硬度≤9.0 Kg/ cm2。一般情况下,GFMTs的脆性百分比随粘结剂浓度的增加而降低(≤0.99%)。泡腾片的漂浮滞后时间为2 ~ 7 min,而非泡腾片的漂浮滞后时间为零。FTIR和DSC研究表明,赋形剂与活性药物成分(API)甲硝唑是相容的。扫描电镜显示,非泡腾配方的GFMTs表面光滑,表面有气孔,而泡腾配方的GFMTs表面光滑,没有气孔。采用泡腾法和非泡腾法制备了甲硝唑胃漂浮基质片,其漂浮滞后时间差异有统计学意义(p0.05)。关键词:漂浮,基质片,泡腾剂,非泡腾剂,浮力。
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引用次数: 1
Amoxicillin loaded-sorbitan monostearate–alginate microparticles as mucoadhesive delivery system for anti-microbial therapy 载阿莫西林-山梨糖单硬脂酸-海藻酸盐微颗粒作为抗微生物治疗的黏附输送系统
Pub Date : 2019-04-09 DOI: 10.4314/JOPHAS.V16I1
E. Onuigbo, C. Ugwu, E. Ezeibe, Ifunanya Frank Mama
Antimicrobial resistance has been a challenge to effective antibiotic delivery. Highly technical approaches that meet therapeutic needs are being studied to improve drug bioavailability. This present work seeks to formulate and characterize amoxicillin - loaded sorbitan monostearate-sodium alginate microparticles as mucoadhesive drug delivery for antimicrobial therapy. Three optimized batches of mucoadhesive sorbitan monostearate-alginate microparticles were characterized for particle size, polydispersity index, encapsulation efficiency, viscosity, and mucoadhesivity. Sensitivity test, FTIR spectroscopy and in-vitro drug release were also performed. The particle sizes were between 457 and 872.3 nm. The mean polydispersity index was about 0.569. The encapsulation efficiencies were above 65 %. The pH, viscosity, shear stress and mucoadhesivity were high and decreased gradually with time. The FTIR showed stability and correlation between the formulations and materials used. Sensitivity test showed high susceptibility between 29.00 and 49.33 mm. The drug release followed mostly first order kinetics with R2 > 0.9. Mucoadhesive sorbitan monostearatealginate polymer can be explored as a novel construct for better delivery of amoxicillin.Keywords: sorbitan monostearate, sodium alginate, mucoadhesion, bioavailability, amoxicillin
抗菌素耐药性一直是有效抗生素递送的挑战。正在研究满足治疗需要的高技术方法,以提高药物的生物利用度。目前的工作旨在制定和表征阿莫西林负载山梨糖单硬脂酸-海藻酸钠微颗粒作为抗菌治疗的黏附药物递送。对优化后的三批山梨糖单硬脂酸海藻酸酯微颗粒进行了粒径、多分散指数、包封效率、粘度和粘接性能的表征。并进行了药敏试验、FTIR光谱和体外释药试验。粒径在457 ~ 872.3 nm之间。平均多分散性指数约为0.569。包封效率在65%以上。pH值、黏度、剪切应力和黏附力均较高,且随时间的延长逐渐降低。FTIR显示了配方和所用材料之间的稳定性和相关性。敏感性试验显示,29.00 ~ 49.33 mm间敏感性较高。药物释放主要服从一级动力学,R2 > 0.9。粘接山梨糖单硬脂酸海藻酸酯聚合物可以作为一种新的结构,以更好地传递阿莫西林。关键词:单硬脂酸山梨糖,海藻酸钠,黏附,生物利用度,阿莫西林
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引用次数: 0
Spectrophotometric assay of artesunate using benzaldehydes with electron withdrawing substituents 用带吸电子取代基的苯甲醛分光光度法测定青蒿琥酯
Pub Date : 2019-01-01 DOI: 10.4314/JOPHAS.V16I2
G. E. Aghayere, H. A. Okeri
Different analytical methods have been reported for the assay of artesunate. However, these methods require the use of sophisticated and expensive equipment and reagents which are not readily available in many developing countries like Nigeria. This study is aimed at developing a method that is accurate, simple and cost effective using readily available reagents for the assay of artesunate in pure form and in pharmaceutical formulations. The developed spectrophotometric assay method is based on the fact that reactive methylene centre of the acid decomposed product of artesunate readily donates a proton that reacts with benzaldehyde to form a chromogen. This study involves the use of two benzaldehydes with electron withdrawing substituents, 3-bromobenzaldehyde and 4-chlorobenzaldehyde. Both gave immediate yellow coloured products and the wavelength of maximum absorption for the product obtained using 3-bromobenzaldehyde was 452 nm, while it was 456 nm for the product obtained with 4-chlorobenzaldehyde. However, the dissolution of 3-bromobenzaldehyde was incomplete in the acidic medium. The result obtained with 4-chlorobenzaldehyde revealed that Beer’s law was obeyed at the range of 20-100 μg/ml artesunate concentration with a linear coefficient of 0.9996 and the molar absorptivity was 2.1261×10 3 mol -1 cm -1 . The limits of detection and quantification were 1.3832 μg/ml and 4.6109 μg/ml, respectively. The method required water as diluent. The result obtained from recovery studies by standard addition method confirmed that there was no interference from pharmaceutical excipients. The developed method was used to assay five brands of artesunate tablets successfully. The results compared favourably well with those obtained using the method described in the International Pharmacopoeia. Keywords: Artesunate, Benzaldehydes, spectrophotometry, recovery studies
不同的分析方法已报道的测定青蒿琥酯。然而,这些方法需要使用复杂和昂贵的设备和试剂,而这些设备和试剂在尼日利亚等许多发展中国家并不容易获得。本研究旨在开发一种准确、简单和成本有效的方法,使用现成的试剂来测定纯形式和药物制剂中的青蒿琥酯。所开发的分光光度测定方法是基于青蒿琥酯酸分解产物的活性亚甲基中心容易提供一个质子与苯甲醛反应形成显色剂的事实。本研究涉及使用两种具有吸电子取代基的苯甲醛,3-溴苯甲醛和4-氯苯甲醛。用3-溴苯甲醛制得的产物的最大吸收波长为452nm,用4-氯苯甲醛制得的产物的最大吸收波长为456nm。而3-溴苯甲醛在酸性介质中溶解不完全。以4-氯苯甲醛为溶剂,在青蒿琥酯浓度20 ~ 100 μg/ml范围内符合比尔定律,线性系数为0.9996,摩尔吸光度为2.1261×10 3 mol -1 cm -1。检测限为1.3832 μg/ml,定量限为4.6109 μg/ml。这种方法需要水作为稀释剂。标准加样法回收率研究结果证实,该方法不受药用辅料的干扰。该方法成功地测定了5个牌号的青蒿琥酯片的含量。结果与用国际药典中所描述的方法得到的结果比较良好。关键词:青蒿琥酯,苯甲醛,分光光度法,回收率研究
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引用次数: 0
In vitro antimicrobial activity of Citrus Sinensis (orange), Citrus Limetta (sweet lime) and Citrus Limon (lemon) fruit peel oil extracts on selected causal organisms of urinary tract infection 柑桔、酸橙和柠檬果皮油提取物对尿路感染病原菌的体外抑菌活性研究
Pub Date : 2018-12-19 DOI: 10.4314/JOPHAS.V15I3
J. Appah, V. O. Aina, Ayuba.O Karen
Oils from the fruit peels of Citrus sinensis (Orange), Citrus limetta (Lime) and Citrus limon (Lemon) were extracted and investigated for their antimicrobial activities against some selected microorganisms ( Escherichia coli, Staphylococcus aureus, Klebsiella pneumonia, Pseudomonas aeruginosa and Candida albicans ). Phytochemical analysis of the oil extracts shows the presence of tannins, saponins, flavonoids, terpenoids, cardiac glycosides, alkaloids, carbohydrates (reducing sugar) and phenol. Flavonoids occurred in the highest amount in C. sinensis . Infrared spectroscopy revealed the various functional groups present in the extracted oils.. antimicrobial studies showed that the extracted oils had antimicrobial effect on the test organisms, which is attributed to the phytochemicals and functional groups of the oil. The oils in combination showed synergistic antimicrobial effects on the organisms tested. With C. sinensis essential oil (1.5 ml), the zone of inhibition was highest on Staphylococcus aureus. With C. limetta (1.0 ml), the inhibition zone (27 mm) was also highest on S. aureus. Concentration of 2.0 ml gave the highest inhibition (15.5 mm) on S. aureus . The zones of inhibition with different quantities of orange peel oil, against the selected microbes were not significantly different (P-Value - 0.013). There was also no significant difference in the zone of inhibition of microbes at different concentrations of lime and lemon essential oils, with PValues of 0.0956 and 0.01225 respectively. It may be concluded that essential oils of C. sinensis, C. limetta and C. limon have antimicrobial properties and may be applied in the treatment of diseases induced by the pathogens. Further research is needed to achieve appropriate formulation into dosage forms, of the test oils. The superior antimicrobial properties demonstrated by the oil blends can be exploited further with a view to generating new effective antimicrobial compounds. Keywords: Antimicrobial Activity, Urinary Tract Infections, Citrus limetta, Column Chromatography, Candida albicans.
从柑橘(Citrus sinensis)、柠檬(Citrus limtta)和柠檬(Citrus limon)的果皮中提取精油,研究其对大肠杆菌、金黄色葡萄球菌、肺炎克雷伯菌、铜绿假单胞菌和白色念珠菌的抑菌活性。植物化学分析表明,油提取物中含有单宁、皂苷、黄酮类、萜类、心苷、生物碱、碳水化合物(还原糖)和苯酚。黄酮类化合物的含量最高。红外光谱揭示了提取油中存在的各种官能团。抑菌研究表明,精油对试验生物具有抑菌作用,这与精油中含有的植物化学物质和官能团有关。两种油的组合对被试生物具有协同抑菌作用。以中华香薷挥发油(1.5 ml)对金黄色葡萄球菌的抑制作用最大。用C. limetta (1.0 ml)对金黄色葡萄球菌的抑制区(27 mm)也最高。浓度为2.0 ml时对金黄色葡萄球菌的抑制作用最高(15.5 mm)。不同用量的橙皮油对所选微生物的抑制区差异不显著(p值为- 0.013)。不同浓度的青柠精油和柠檬精油对微生物的抑制区也无显著差异,p值分别为0.0956和0.01225。由此可见,柑橘、酸橙和柠檬精油具有抑菌作用,可用于病原菌所致疾病的治疗。需要进一步的研究,以实现适当的配方成剂型的试验油。所述油共混物所显示的优越抗菌性能可以进一步开发,以产生新的有效抗菌化合物。关键词:抗菌活性,尿路感染,柑橘酸橙,柱层析,白色念珠菌
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引用次数: 1
Phytochemical Screening and Antibacterial Activity of Citrus Sinensis Peel Extracts on Clinical Isolates of Staphylococcus Aureus and Salmonella Typhi 柑桔皮提取物对金黄色葡萄球菌和伤寒沙门氏菌临床分离株的植物化学筛选及抑菌活性研究
Pub Date : 2018-10-25 DOI: 10.29199/japs.101014
The study was conducted to determine the phytochemical composition, antibacterial activity and activity index orange (Citrus sinensis (L) Osbeck) peel extracts against clinical isolates of Staphylococcus aureus and Salmonella typhi. The result of phytochemical screening of the peel extracts showed the presence of alkaloid, glycoside, saponin, tannin, flavonoid, terpenoid and phenol. The result of the antibacterial efficacy of the extracts against the isolates indicated the extracts were active against the isolates with higher activity in ethanol extract (with average zone of inhibition of 15 mm) when compared to aqueous extract (12.25 mm). The result of susceptibility of the isolates to the extracts showed Staphylococcus aureus was more sensitive to the extract with average zone of inhibition of 15.25 mm when compared to Salmonella typhi with average zone of inhibition of 12.00 mm. The minimum inhibitory concentration (MIC) of the extracts showed that dilutions of various concentrations of aqueous and ethanol of peel extracts can inhibit the growth or kill the isolates at a concentration of between 2.125 – 20 mg/ ml. the average activity index of the extracts on the test isolates was found to be 0.64 which indicated that the plant extract can compete with the standard antibiotic used. Statistical analysis of the results indicated that there is no significant different in the activity of the extracts against the isolates used at p<0.05. Findings from this study support the use of orange peel extracts for medicinal purposes.
本研究旨在测定柑桔皮提取物对临床分离的金黄色葡萄球菌和伤寒沙门菌的植物化学成分、抑菌活性和活性指数。果皮提取物的植物化学筛选结果表明,其中含有生物碱、糖苷、皂苷、单宁、黄酮类、萜类和酚类化合物。结果表明,乙醇提取液对分离菌株的抑菌效果优于水提液(平均抑制区为12.25 mm),乙醇提取液的平均抑制区为15 mm。结果表明,金黄色葡萄球菌对提取物的平均抑制区为15.25 mm,而伤寒沙门氏菌对提取物的平均抑制区为12.00 mm。最低抑菌浓度(MIC)表明,在2.125 ~ 20 mg/ ml的浓度范围内,不同浓度的果皮提取物的水溶液和乙醇溶液对分离株均有抑制或杀伤作用,提取物对分离株的平均活性指数为0.64,表明该植物提取物可与标准抗生素竞争。统计分析结果表明,提取物对不同分离物的活性差异无统计学意义(p<0.05)。这项研究的结果支持橘皮提取物的药用用途。
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引用次数: 1
Evaluating the ethyl-acetate fraction of crude methanol leaf extract of Ocimum gratissimum formulated as ointments for wound healing properties using the excision wound model 采用切除创面模型,评价粗甲醇叶提取物醋酸乙酯组分作为创面软膏的创面愈合性能
Pub Date : 2018-01-01 DOI: 10.4314/JOPHAS.V15I1
E. Ibezim, M. Momoh, V. Onyishi, I. Nwabunike, D. Odimegwu, N. Ibezim, N. J. Nzekwe
Ointment formulations of the ethyl acetate fraction of the crude methanol leaf extract of Ocimum gratissimum was in this study evaluated for wound healing activities in rat using the excision wound model. The air-dried and pulversied leaves were extracted with methanol in a Soxhlet extraction apparatus to obtain the crude methanol extract. This was  subsequently shaken with ethyl acetate and to obtain the ethyl acetate fraction, which was later dried and used in two different concentrations ( 1% w/w and 2 % w/w to formulate simple ointments. The ointments were evaluated for wound healing properties using male albino rats (65 – 180 g) aged 3 – 4 months. Prior to this, the crude methanol extract and ethyl acetate fraction were subjected to phytochemical studies to ascertain their phyto-constituents .The phytochemical studies showed the presence of alkaloids, tannins, flavonoids and resins and absence of glycosides and saponins. The ointment formulations had wound healing activities which were time-dependent, but concentration independent. The ointment formulations containing the extracts showed more effective wound healing than the positive control, Cicatrin® a standard wound healing agent, with the ointment containing 1 % w/w extract having superior effects than the batch containing 2 % w/w, implying that the extract, at 1 % w/w concentration, can be exploited in ointment form, as a potential wound healing remedy. Keywords : wound healing, ointment, ethyl acetate fraction, methanol extract, Ocimum gratissimum, Cicatrin®
本研究采用大鼠切除伤口模型,评价了竹叶粗甲醇提取物乙酸乙酯部分软膏配方对大鼠伤口愈合的活性。在索氏提取装置中,用甲醇提取风干和粉碎的叶片,得到粗甲醇提取物。随后用乙酸乙酯摇匀,得到乙酸乙酯部分,随后干燥,并以两种不同的浓度(1% w/w和2% w/w)配制简单的软膏。用3 - 4月龄雄性白化大鼠(65 - 180 g)评估软膏的伤口愈合性能。在此之前,对粗甲醇提取物和乙酸乙酯提取物进行了植物化学研究,确定了它们的植物成分,植物化学研究表明,它们含有生物碱、单宁、类黄酮和树脂,不含糖苷和皂苷。药膏制剂的伤口愈合活性与时间有关,但与浓度无关。含有提取物的软膏配方比阳性对照——标准伤口愈合剂Cicatrin®更有效地愈合伤口,其中含有1% w/w提取物的软膏比含有2% w/w的软膏具有更好的效果,这意味着1% w/w浓度的提取物可以制成软膏形式,作为潜在的伤口愈合药物。关键词:创面愈合,软膏,乙酸乙酯馏分,甲醇提取物,大红花,Cicatrin®
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引用次数: 1
Colorimetric determination of zidovudine in bulk and tablet dosage forms using potassium dichromate 重铬酸钾比色法测定散装和片剂齐多夫定的含量
Pub Date : 2018-01-01 DOI: 10.4314/JOPHAS.V15I2
U. Ogbeide, H. A. Okeri, C. Eboka
A colorimetric method involving the oxidation of zidovudine (ZDV) using potassium dichromate in sulphuric acid has been developed for the determination of ZDV in bulk and tablet dosage forms. The wavelength of maximum absorption (λ max ) of the oxidation product was determined and concentrations of sulphuric acid, potassium dichromate and amount/duration of heat were optimized. Beers plot was constructed at the λ max and used in the recovery studies for pure drug sample. Two methods (acid and methanol extraction) were used to extract ZDV from tablet samples. The developed method was then used to determine the percentage content of the drug in the tablets. The method was validated using the International Council for Harmonization of Technical Requirement for registration of Pharmaceuticals for Human Use (ICH) guideline. The λ max of the oxidation product was found to be 602 nm. The optimized conditions were as follows: 0.083M (potassium dichromate), 12 M (sulphuric acid) and heating at 90oC for 30 mins. The regression equation for the Beer’s plots is: A = 0.4313C + 0.0018 (R 2 =0.9995) for ZDV. The recovery of ZDV from standard solutions was 100.36%±0.36. Thus the developed method was accurate and precise. The percentage contents determined for different brands of ZDV tablets were 99.07%±0.83, 98.70%±0.76, 93.46%±0.72 for the three brands of ZDV. These values compared well with results obtained with use of another method of assay. These values are within the specifications of the British Pharmacopoeia (90-110%). The limits of detection and limits of quantification were 0.004 and 0.014 mg/ml respectively. The developed method is simple, accurate, and utilizes readily available chemicals and equipment, and is inexpensive. It could therefore be used for the routine determination of ZDV. Keywords: Zidovudine, Oxidation, Colorimetric, Absorbance
建立了用重铬酸钾在硫酸中氧化齐多夫定(ZDV)的比色法测定原料药和片剂的含量。测定了氧化产物的最大吸收波长(λ max),优化了硫酸、重铬酸钾的浓度和加热时间。在λ max处建立了Beers图,并将其用于纯药物样品的回收率研究。采用酸萃取和甲醇萃取两种方法从片剂样品中提取ZDV。然后用所建立的方法测定该药物在片剂中的百分含量。采用国际人用药品注册技术要求协调委员会(ICH)指南对该方法进行了验证。氧化产物的λ max为602 nm。优化条件为:0.083M(重铬酸钾),12 M(硫酸),90℃加热30 min。Beer’s plot的回归方程为:ZDV的A = 0.4313C + 0.0018 (r2 =0.9995)。标准溶液中ZDV的回收率为100.36%±0.36。因此,所开发的方法是准确和精确的。ZDV不同品牌的含量分别为99.07%±0.83、98.70%±0.76、93.46%±0.72。这些值与用另一种测定方法得到的结果比较良好。这些值在英国药典(90-110%)的规定范围内。检测限和定量限分别为0.004和0.014 mg/ml。所开发的方法简单、准确,利用现成的化学品和设备,而且价格低廉。该方法可用于ZDV的常规测定。关键词:齐多夫定,氧化,比色,吸光度
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引用次数: 0
Analgesic and anti-inflammatory activities of the n-butanol fraction of Vernonia glaberrima 山梨正丁醇部分的镇痛和抗炎作用
Pub Date : 2017-10-02 DOI: 10.4314/JOPHAS.V14I2
I. Nasir, A. Yusuf, M. Abdullahi, A. Uba, A. Muntaka, S. S. Bello, A. Umar, A. Alhasan, C. Alebiosu, M. Yahaya, Mohammad Shah Hafez Kabir, C. Ottah, S. Ibrahim
The n-butanol leaf fraction of Vernonia glaberrima was evaluated for its toxicity, analgesic and anti-inflammatory effects. The leaves of V. glaberrima were collected, identified and extracted with methanol using maceration method and the resulting crude methanol extract was then partitioned using different solvents of increasing polarity (hexane, chloroform, ethyl acetate and n-butanol respectively). Preliminary phytochemical screening was conducted on the n-butanol fraction (BF) using standard procedures. The median lethal dose (LD50) of the fraction was determined using Lorke’s method and the analgesic effect was evaluated using acetic acid-induced writhing test in mice, while the anti-inflammatory activity was assessed using carrageenan-induced paw oedema in rats. Secondary metabolites including saponins, tannins, alkaloids, glycosides and flavonoids were found in the fraction. The LD50 of the fraction was 2154 mg/kg indicating the fraction to be moderately toxic. The fraction at 150 mg/kg exhibited 77.6 % inhibition of writhes, higher than the standard drug, piroxicam (10 mg/kg) which had 53.7 % inhibition. The n-butanol fraction at 150 and 250 mg/kg significantly inhibited the carrageenan-induced paw oedema at the 2nd and 4th hour, respectively, while there was no significant inhibition at 500 mg/kg of the fraction. The standard drug was only able to inhibit oedema at the 1st hour. The results showed the n-butanol fraction of V. glaberrima to possess significant analgesic and anti-inflammatory activities thereby validating its traditional use in the treatment of pain and inflammation.
研究了光水仙花正丁醇叶提取物的毒性、镇痛和抗炎作用。采用浸渍法对光蓝叶片进行收集、鉴定和甲醇提取,然后用极性递增的不同溶剂(分别为己烷、氯仿、乙酸乙酯和正丁醇)对粗甲醇提取物进行分离。采用标准程序对正丁醇馏分(BF)进行初步植物化学筛选。采用Lorke法测定其中位致死剂量(LD50),采用醋酸致小鼠扭体实验评价其镇痛作用,采用卡拉胶致大鼠足跖水肿实验评价其抗炎作用。次生代谢产物包括皂苷、单宁、生物碱、糖苷和黄酮类化合物。该馏分的LD50为2154 mg/kg,为中毒性。在150 mg/kg浓度下,其对扭体的抑制率为77.6%,高于标准药物吡罗昔康(10 mg/kg)的53.7%。150和250 mg/kg正丁醇组分分别在第2和第4小时显著抑制卡拉胶诱导的足跖水肿,而500 mg/kg正丁醇组分无显著抑制作用。标准药物仅能在第1小时抑制水肿。结果表明,光灰草正丁醇部分具有显著的镇痛和抗炎活性,从而验证了其在治疗疼痛和炎症方面的传统用途。
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引用次数: 0
Influence of ampicllin/cloxacilin combination on pharmacokinetics of metformin in type II diabetic patients 氨苄林/氯西林联合用药对2型糖尿病患者二甲双胍药动学的影响
Pub Date : 2017-01-01 DOI: 10.4314/JOPHAS.V14I4
M. Garba, M. T. Bakare-Odunola, M. Garba, A. I. Yakasai, A. Musa, M. Usman, S. S. Bello, B. Rabiyu, A. Haruna
The study was aimed at determining the antibacterial activity of stem bark and leaf extracts of Azadirachta indica on laboratory isolates of Escherichia coli and Staphylococcus aureus obtained from spoiled cabbage. The phytochemical constituents of the extracts were screened. The aqueous and methanol extracts from the leaves and stem bark of the plant were then tested using agar well diffusion method for their antibacterial activity against laboratory isolates of Escherichia coli and Staphylococcus aureus obtained from spoiled cabbage. The result showed that the extracts were active against the microorganisms tested. The methanolic extract of stem bark showed the highest zones of inhibition against tested organisms (average of 17.25 mm) compared to the aqueous extract (average of 15.81 mm). Statistical analysis of the result shows that the extracts demonstrated high antibacterial activity against the isolates tested with the average zone of inhibition of 15.75 mm and 17.31 mm for E. coli and Staphylococcus aureus respectively. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of the extracts ranged between 6.25 – 25 mg/ml. Preliminary phytochemical analysis showed that both stem bark and leaf extracts contain alkaloid, tannin, anthraquinone, flavonoid, phenols and terpenoid. The extracts of the plant demonstrated antibacterial activity due to presence of phytochemical constituents hence, the application of the decoction of leaf and stem bark of the plant in ethnomedicine is justified. Keywords:  Azadirachta indica ; phytochemical; well diffusion; antibacterial activity; Escherichia coli and Staphylococcus aureus
感染在糖尿病中很常见,氨苄西林/氯西林联合用药(氨苄西林®)通常与二甲双胍联合用药。该研究检查了单剂量(2 × 500 mg)氨苄氯与(2 × 500 mg)二甲双胍胶囊同时给药对II型糖尿病患者二甲双胍药代动力学的影响。这项研究的批准是由尼日利亚扎里亚Ahmadu Bello大学教学医院伦理委员会批准的。6名年龄在25 - 55岁之间,体重在50-70公斤之间的II型糖尿病患者参加了这项研究。6例患者每隔2周接受以下治疗:单独服用1克二甲双胍片,同时服用氨苄氯胶囊。每隔0 ~ 8 h采集血样,在- 40℃保存后进行分析。采用高效液相色谱法测定样品中二甲双胍的血药浓度,并对其进行了改进和验证。样品采用Agilent Technologies 1120 Compact LG型高效液相色谱,色谱柱为Eclipse x BD C-8,色谱柱为4.6 x 150 nm,流动相乙腈:正磷酸二氢钾(79:21),紫外检测器。研究结果表明,在tmax 3.0 h时,二甲双胍的血药浓度(cmax)从1140.43±0.52增加到1379.55±0.4 ng/ml, AUC从4388.81±0.52增加到5179.71±0.80 ng/ml/hr,消除半衰期从3.8增加到5.1 hr -1,具有统计学意义(P < 0.5)。分布体积从333,852.19.28±0.27 ml减少到283,061±0.02 ml,具有统计学意义。氨苄氯胺一定抑制了二甲双胍的肾脏分泌,导致循环血浆浓度升高。服用二甲双胍的患者需要氨苄氯,因此需要监测以避免治疗失败。关键词:氨氯,糖尿病,高效液相色谱,二甲双胍,药代动力学
{"title":"Influence of ampicllin/cloxacilin combination on pharmacokinetics of metformin in type II diabetic patients","authors":"M. Garba, M. T. Bakare-Odunola, M. Garba, A. I. Yakasai, A. Musa, M. Usman, S. S. Bello, B. Rabiyu, A. Haruna","doi":"10.4314/JOPHAS.V14I4","DOIUrl":"https://doi.org/10.4314/JOPHAS.V14I4","url":null,"abstract":"The study was aimed at determining the antibacterial activity of stem bark and leaf extracts of Azadirachta indica on laboratory isolates of Escherichia coli and Staphylococcus aureus obtained from spoiled cabbage. The phytochemical constituents of the extracts were screened. The aqueous and methanol extracts from the leaves and stem bark of the plant were then tested using agar well diffusion method for their antibacterial activity against laboratory isolates of Escherichia coli and Staphylococcus aureus obtained from spoiled cabbage. The result showed that the extracts were active against the microorganisms tested. The methanolic extract of stem bark showed the highest zones of inhibition against tested organisms (average of 17.25 mm) compared to the aqueous extract (average of 15.81 mm). Statistical analysis of the result shows that the extracts demonstrated high antibacterial activity against the isolates tested with the average zone of inhibition of 15.75 mm and 17.31 mm for E. coli and Staphylococcus aureus respectively. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of the extracts ranged between 6.25 – 25 mg/ml. Preliminary phytochemical analysis showed that both stem bark and leaf extracts contain alkaloid, tannin, anthraquinone, flavonoid, phenols and terpenoid. The extracts of the plant demonstrated antibacterial activity due to presence of phytochemical constituents hence, the application of the decoction of leaf and stem bark of the plant in ethnomedicine is justified. Keywords:  Azadirachta indica ; phytochemical; well diffusion; antibacterial activity; Escherichia coli and Staphylococcus aureus","PeriodicalId":16719,"journal":{"name":"Journal of Pharmaceutical and Allied Sciences","volume":"126 1","pages":"2616-2624"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76827475","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
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Journal of Pharmaceutical and Allied Sciences
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