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Antimicrobial studies on the stem-bark extracts of Ficus kamerunensis Warb. 滇榕茎皮提取物的抗菌研究。
Pub Date : 2017-01-01 DOI: 10.4314/JOPHAS.V14I3
U. Iliyasu, U. Danmalam, U. A. Katsayal, S. Shehu, H. Mshelia
Ficus kamerunensis is an epiphytic shrub or tree growing up to 20 m high. The plant is used in ethnomedicine to treat microbial infections of different kinds. Antimicrobial activity of methanol extract of the stem-bark of Ficus kamerunensis and fractions of the same (ethyl acetate, diethyl ether, n-butanol, aqueous) was studied. Agar diffusion method was used to screen the extracts while minimum inhibitory concentrations (MICs) of the extracts were determined at 0.5 scale Mc-farland’s turbidity standard and with standard ciprofloxacin as positive control. The diameter of zone of inhibition of the extracts against test microorganisms (in mm) was highest for the ethyl acetate, followed by diethyl ether then n-butanol extracts while the least was with the methanol extract. The zones of inhibition of the extracts were in the range of 18-31 mm. The MIC and MBC for the extracts were 6.25 mg/ml and 12.5 mg/ml respectively. Antimicrobial evaluation shows that the extracts have activity against E. coli, Candida albicans, Candida stellatodea, Corynebacterium ulcerans, MRSA, Neisseria gonorrheae, Pseudomonas aeruginosa Staphylococcus aureus while Candida tropicalis, Candida krusei, Proteus mirabilis and Streptococcus pyrogens were resistant. This therefore, supports the ethnomedical usage of the plant for the treatment of infectious diseases.Keywords: Ficus kamerunensis, Antimicrobial, MIC and MBC/ MFC
无花果是一种附生灌木或乔木,高可达20米。这种植物在民族医学中用于治疗不同种类的微生物感染。研究了无花果茎皮甲醇提取物及其提取物(乙酸乙酯、乙醚、正丁醇、水溶液)的抑菌活性。采用琼脂扩散法筛选提取物,以0.5标度Mc-farland浊度标准和标准环丙沙星为阳性对照测定提取物的最低抑菌浓度(mic)。乙酸乙酯提取物对试验微生物的抑制区直径最大(mm),其次为乙醚提取物,正丁醇提取物最小(mm)。提取物的抑制区在18 ~ 31 mm范围内。提取物的MIC和MBC分别为6.25 mg/ml和12.5 mg/ml。抗菌评价结果表明,提取物对大肠杆菌、白色念珠菌、星状念珠菌、溃疡杆状杆菌、MRSA、淋病奈瑟菌、铜绿假单胞菌、金黄色葡萄球菌均有抑菌活性,对热带念珠菌、克鲁氏念珠菌、神奇变形杆菌和热原链球菌均有耐药。因此,这支持了该植物用于治疗传染病的民族医学用途。关键词:无花果,抗菌,MIC, MBC/ MFC
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引用次数: 1
Evaluation of anticonvulsant activity of methanol leaf extract of Hymenocardia acida , Tul (Euphorbiaceae) in laboratory animals 大戟科酸膜心草(Hymenocardia acid, Tul)甲醇叶提取物对实验动物的抗惊厥活性评价
Pub Date : 2017-01-01 DOI: 10.4314/JOPHAS.V14I5
A. Haruna, U. Pateh, M. Sule, A. Musa, Y. Sani, M. Mohammed, M. Lawal, M. Garba
Pleurotus tuber regium , particularly the sclerotium is an important dietary component due to its nutritional value, since it is composed of micro- and macro- elements. Examples include potassium, magnesium, phosphorus, zinc, copper, iron, as well as classes of food such as protein, carbohydrate, vitamins (B1, B2, D2 and C), unsaturated fatty acids, low fat content, albumin, globulin, prolamines, and glutelin. This study is aimed at determining the effects of Pleurotus tuber regium on haematological indices of Albino Wistar rats. The Wistar rats were grouped and each group administered with aqueous and ethanol extracts of Pleurotus tuber regium respectively for a period of 14 days and blood samples obtained for complete blood count (CBC) using the Abacus Junior Haematology Analyser (S/N 111325). The rats fed with aqueous extracts recorded higher values of RBC (8.31±0.5x10 12 /L), haemoglobin (13.1±0.8g/DL), haematocrit (53.02±3.8%) as well as platelet count (788.6±157.4x10 9 /L) and plateletcrit (0.71±0.1%) compared to the ethanol and control groups with lower values. The aqueous group however recorded low WBC (8.68±3.22x10 9 /L) and Lymphocytes (5.16±2.0x10 9 /L) compared to the other two groups, with the ethanol groups recording the highest value for the lymphocyte (7.91±2.8x10 9 /L). The aqueous extract can thus serve as an ideal haematinics, since the values of RBC, haemoglobin and haematocrit are within the normal value for the female Wistar rats used. It could also serve as an immune booster due to the increased level of lymphocytes, because in the presence of pathogenic microbes, the body is primed to fight infection by releasing lymphocytes. Keywords:  Pleurotus tuber regium, Wistar rats, haematocrit, plant extract, blood count
块状侧耳,特别是其菌核是由微量元素和宏量元素组成的,具有丰富的营养价值,是重要的膳食成分。例子包括钾、镁、磷、锌、铜、铁,以及各种食物,如蛋白质、碳水化合物、维生素(B1、B2、D2和C)、不饱和脂肪酸、低脂肪含量、白蛋白、球蛋白、脯氨酸和谷蛋白。本研究旨在探讨白化Wistar大鼠白化侧耳菇对血液学指标的影响。将Wistar大鼠分组,每组分别给予侧耳菇水提液和乙醇提液14天,并使用Abacus Junior血液学分析仪(S/N 111325)采集全血细胞计数(CBC)血样。大鼠红细胞(8.31±0.5 × 10 12 /L)、血红蛋白(13.1±0.8g/DL)、红细胞压积(53.02±3.8%)、血小板计数(788.6±157.4 × 10 9 /L)和血小板压积(0.71±0.1%)均高于乙醇组和对照组。然而,与其他两组相比,水组的WBC(8.68±3.22 × 10 9 /L)和淋巴细胞(5.16±2.0 × 10 9 /L)较低,其中乙醇组的淋巴细胞(7.91±2.8 × 10 9 /L)最高。因此,水提取物可以作为理想的血液学,因为红细胞、血红蛋白和红细胞压积值在雌性Wistar大鼠的正常值之内。由于淋巴细胞水平的增加,它也可以作为免疫增强剂,因为在病原微生物存在的情况下,身体会通过释放淋巴细胞来对抗感染。关键词:平菇,Wistar大鼠,红细胞压积,植物提取物,血细胞计数
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引用次数: 0
Prescription pattern and cost analysis of antipsychotics in a tertiary hospital in south- South Nigeria. 南尼日利亚某三级医院抗精神病药物处方模式及成本分析。
Pub Date : 2016-01-01 DOI: 10.4314/JOPHAS.V13I1
P. Osahon, A. C. Baye-Osagie, I. C. Ediae, P. Erah
The aim of this study was to formulate metformin as a floating drug delivery system using Irvingia gabonesis gum in order to increase its bioavailability and enhance its site-specific absorption. Floating matrix granules of metformin were prepared by wet granulation technique using the extracted natural gum from Irvingia gabonensis at varying concentrations (2, 4, 6 and 8 %w/w). Sodium bicarbonate (30%) and tartaric acid (5%) were incorporated as the gas generating agents. Formulations were either prepared alone with the natural gum or with the addition of 1.0 %w/w of acrylatemethacrylate copolymer (Eudragit RL100). All granules were evaluated for micromeritic properties i.e. bulk and tapped densities, Hausner’s ratio, Carr’s index, and angle of repose. Granules were compressed at an optimized compression pressure of 35 arbitrary unit on the tableting machine load scale. Tablets were evaluated for hardness, friability, floating lag time, in vitro buoyancy and drug release profiles. Release data were subjected to analysis by four different mathematical models namely, – zero order flux, first order, Higuchi square root of time relationship and Korsmeyer-Peppas equation. Drug-excipient compatibility study was done using Fourier Transform Infra-red Spectroscopy (FTIR). From the results obtained, all formulated gastroretentive floating matrix (GRFM) granules were free flowing with angle of repose and Carr’s index ≤ 30.2o and ≤ 11% respectively. The floating lag time for GRFM tablets formulated with Irvingia gabonesis was ≤ 850 s. The in vitro buoyancy times of GRFM tablets formulations using Irvingia gabonesis gum alone (i.e. without the incorporation of acrylatemethacrylate copolymer) were 12 h. All GRFM granules were compressible with tablet hardness between 2.2 – 6.3 Kpa. There was a significant difference in tablet hardness with increase in binder concentration (p 0.45, hence their release mechanism was by Non-Fickian diffusion. FTIR studies show that the excipients and the active pharmaceutical ingredient (API) i.e. metformin were compatible. Irvingia gabonesis gum has been investigated in the formulation of gastroretentive floating matrix tablets of metformin which may find useful application in sustained release drug delivery particularly for drugs with short biological half-life that require frequent administration.Keywords: Floating drug delivery system (FDDS), Irvingia gabonesis gum, Metformin hydrochloride, Gastroretentive floating matrix tablets (GRFMTs).
为了促进发展中国家的合理用药,重要的是利用世界卫生组织(世卫组织)的药物使用指标来评估药物使用模式。因此,本研究的主要目的是利用世卫组织的一些核心药物使用指标,评估贝宁市联邦神经精神病医院的处方模式并进行药物成本分析。这是一个回顾性的,横断面调查和样本选择采用系统随机抽样。对2014年1月- 2014年9月收治的540例患者进行回顾性分析。每次就诊的平均处方药物数为2.3种,范围在1至6种之间。处方抗生素或注射的比例分别为2.0% (n=11)和40.9% (n=221)。按仿制名开具处方的占92.5% (n=1165),按基本药物清单开具处方的占70.0% (n=880)。处方的口服抗精神病药物(86%)包括氟哌啶醇、氯丙嗪、三氟拉嗪、硫硝嗪、奥氮平和利培酮。储备制剂为癸酸氟非那嗪和癸酸氟辛醇(17%)。处方费用从N90-N18, 405不等。我们的研究表明,所研究的医院的处方模式不符合世卫组织的指导方针。非典型性药物非常昂贵,对研究环境中的大多数患者来说是负担不起的。这表明需要采取措施降低较新的精神药物的成本,增加其可得性和使用,以提高尼日利亚精神病患者的生活质量。:处方模式,抗精神病药物,合理用药
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引用次数: 7
Pharmacokinetics and drug interactions of herbal medicines: the effect of Garcinia kola and Carmellia sinensis on norfloxacin use in the treatment of urinary tract infections 中草药的药代动力学及药物相互作用:枸橼酸和山楂对诺氟沙星治疗尿路感染的影响
Pub Date : 2016-01-01 DOI: 10.4314/JOPHAS.V13I2
C. Ihekwereme, S. Nduka, Ifeanyi E Okoye, C. Esimone, M. Adikwu
People consume herbal products such as Garcinia kola seed (GKS) or Carmellia sinensis (tea) while on conventional or orthodox medication. Urinary tract infections are frequently treated using norfloxacin. This work investigated the clinical outcome of co-administration of norfloxacin, and either Garcinia kola seed (GKS) or Carmellia sinensis (tea) on the urinary clearance of E. coli using human volunteers. Three parallel groups were used for the study. The urinary excretion rate, urinary concentration-time profile, cumulative amount of drug excreted in urine and reciprocal urinary inhibitory titer (RUIT) were clinically determined for norfloxacin. Urine samples were collected at intervals (up to 24 h) from 3 groups (n = 4) of healthy volunteers (norfloxacin alone, norfloxacin and either GKS or tea) and used for the studies. The results indicated that both herbs reduced the peak excretion rate and peak urinary concentrations of norfloxacin. The percentage of norfloxacin recovered in the urine of subjects decreased from 2.3 ± 0.4% (without herb) to 2.0± 0.3 % (G. kola) and 1.5 ± 0.3% (C. sinensis) when herbs were administered concomitantly. Tea enhanced antibacterial activity at 1st and 3rd hours, while GKS maintained antibacterial activity much longer than the other groups. Although, all the groups had equal antibacterial potency at the 7th hour, only GKS could sustain it until the 10th hour. The highest bacteriostatic potency in urine was from subjects that consumed the antibiotics concomitantly with tea, suggesting that tea enhanced the potency of norfloxacin. The urinary concentration and hence bactericidal potency of norfloxacin was significantly influenced by tea and GKS, which may be beneficial in the treatment of urinary tract infections. Thus co-administration of tea and norfloxacin in the treatment of UTI may result in increased bacterial clearance, rapid recovery, and possibly some pharmacoeconomic advantagesKeywords: Drug-Herb Interactions, Pharmacokinetics, Urinary tract Infections, Pharmacotherapy, Synergism
人们在服用常规或正统药物的同时,也会食用草药产品,如Garcinia kola种子(GKS)或Carmellia sinensis(茶)。尿路感染常用诺氟沙星治疗。本研究研究了诺氟沙星与藤黄籽(GKS)或山茶花(茶)共同给药对人类志愿者尿中大肠杆菌清除的临床效果。研究中使用了三个平行组。临床测定诺氟沙星的尿排泄率、尿浓度-时间谱、尿中累积药物排泄量和尿互抑效价(RUIT)。每隔一段时间(最长24小时)从3组(n = 4)健康志愿者(单独使用诺氟沙星,诺氟沙星和GKS或茶)中收集尿液样本并用于研究。结果表明,两种中药均能降低诺氟沙星排泄峰率和尿中诺氟沙星浓度。受试者尿液中诺氟沙星回收率由未配药组(2.3±0.4%)降至合用中药组(2.0±0.3%)和合用中药组(1.5±0.3%)。茶在第1和第3小时的抑菌活性增强,而GKS的抑菌活性维持时间明显长于其他各组。虽然在第7小时,所有组的抑菌力相同,但只有GKS能维持到第10小时。尿液中抑菌效力最高的是与茶同时服用抗生素的受试者,这表明茶可以增强诺氟沙星的效力。茶水和GKS对诺氟沙星的尿浓度和杀菌效力有显著影响,这可能对尿路感染的治疗有益。因此,茶和诺氟沙星联合使用治疗尿路感染可能会增加细菌清除率,快速恢复,并可能具有一些药物经济学优势。关键词:药物-草药相互作用,药代动力学,尿路感染,药物治疗,协同作用
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引用次数: 0
Assessment Of The Microbial Load And Some Physico-Chemical Parameters Of Some Finished Herbal Liquid Products 部分中药饮料液的微生物负荷及理化参数评价
Pub Date : 2015-03-07 DOI: 10.4314/JOPHAS.V12I1
O. Uwumarongie, H. A. Okeri
Despite the benefits derived from herbal products, they may be contaminated with various impurities. It is therefore important to assess the microbial quality and heavy metal content of herbal preparations, especially liquid preparations and determine their safety profile. Herbal liquid preparations made locally by herbalists and sold to patients in herbal homes were used for this study. One bottle of each of seventeen (17) different liquid herbal preparations was purchased. From each bottle, three aliquot samples were assessed for microbial presence and total viable count. Isolation and identification of the contaminants were also carried out, while other determinations like pH, phytoconstituents, heavy metal and elemental contents were performed using standard methods of analyses. Results showed that, 4 (23.53%) had no microbial contaminants, while 13 (76.47%) were contaminated with various microbes. Of these contaminated preparations, 10 (58.82%) had single contaminants each, of which 1 (10%) had Staphylococcus aureus ; 2 (20%) had Escherichia coli ; 2 (20%) had Pseudomonas aeruginosa and 5 (50%) had C andida albicans . The remaining 3 (17.65%) had 2 contaminants each, of which 1 (33.33%) had E. coli and P. aeruginosa ; 1 (33.33%) had E. coli and Staph. aureus ; and 1 (33.33%) had Klebsiella pneumonia and Candida albicans . Total viable count and pH values of the different preparations ranged from 1.75 x 10 5 – 7.50 x 10 8 organisms/ml and 3.63 – 8.89, respectively. Phytochemical analysis revealed the presence of useful phytoconstituents while elemental analysis revealed the presence of valuable elements whose values all fall within stipulated limits. Thus, the presence of microbes (above limits specified) in a greater percentage of the preparations despite the presence of useful phytoconstituents and elements, could adversely affect the health status of consumers of such herbal liquid preparations.  Keywords : Assessment, Microbial load, Physico-Chemical parameters, Herbal products.
尽管草药产品有很多好处,但它们可能被各种杂质污染。因此,评估草药制剂,特别是液体制剂的微生物质量和重金属含量并确定其安全性是很重要的。本研究使用的是当地草药师制作的草药液体制剂,并在草药家中出售给患者。购买了17种不同的液体草药制剂各一瓶。从每个瓶子中,评估三个等分样品的微生物存在和总活菌数。还对污染物进行了分离和鉴定,同时使用标准分析方法进行了pH、植物成分、重金属和元素含量等其他测定。结果显示,4份(23.53%)未发现微生物污染,13份(76.47%)存在各种微生物污染。其中10份(58.82%)为单一污染物,1份(10%)为金黄色葡萄球菌;2例(20%)感染大肠杆菌;铜绿假单胞菌2例(20%),白色念珠菌5例(50%)。其余3例(17.65%)各检出2种污染物,其中大肠杆菌和铜绿假单胞菌各检出1例(33.33%);1例(33.33%)检出大肠杆菌和葡萄球菌。葡萄球菌;肺炎克雷伯菌和白色念珠菌1例(33.33%)。不同制剂的总活菌数和pH值分别为1.75 × 10.5 ~ 7.50 × 108个生物体/ml和3.63 ~ 8.89。植物化学分析显示存在有用的植物成分,元素分析显示存在有价值的元素,其值均在规定的范围内。因此,尽管存在有用的植物成分和元素,但在更大比例的制剂中存在微生物(超过规定的限度)可能对此类草药液体制剂的消费者的健康状况产生不利影响。关键词:评价;微生物负荷;理化参数;
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引用次数: 0
Evaluation of antimicrobial activity and mode of action of Laportea aestuans extracts against urogenital, gut and pulmonary pathogens 拉乌茶提取物对泌尿生殖器、肠道和肺部病原体的抑菌活性及作用方式的评价
Pub Date : 2015-01-01 DOI: 10.4314/JOPHAS.V12I2
U. Ekong, R. Martins
Phytochemical screening and antimicrobial activities of Laportea aestuans leaves, stem-bark and whole-plant aqueous, methanol and ethanol extracts were carried-out using standard phytochemical and microbiological methods. The phytochemical procedures indicated the presence of saponins, tannins, phlobatannins, flavonoids, alkaloids and cardiac-glycosides. The yields of the whole-plant extracts were significantly(p ethanol>methanol. The antimicrobial activities of the aqueous, methanol and ethanol extracts of Laportea aestuans leaves, stem-bark and whole-plant against the auchthocthonous urogenital, gut and pulmonary test organisms: Staphylococcus aureus , Staphylococcus saprophyticus , Streptococcus pneumoniae , Escherichia coli , Pseudomonas aeruginosa , Proteus mirabilis , Salmonella typhi , Vibrio cholerae , Shigella dysenteriae , Candida albicans and Aspergillus niger ; assayed by the modified agar-well diffusion technique indicated broad-spectrum antimicrobial activities. Analysis of the antimicrobial activities of the extracts by activity-index, indicated that the leaf extracts, have significantly (p stem-bark extracts >whole- plant extracts. Similarly by activity-index, the ethanol extracts recorded significantly (p methanol extracts>aqueous extracts. The minimum inhibitory concentrations (MIC) of the leaves extracts, assayed by the macrobroth-dilution technique was lowest against Shigella dysentariae ( 1.25 mg/ml),and generally between 2.50 - 5.0 mg/ml against the other bacterial and fungal species tested for both methanol and ethanol extracts; while the aqueous extracts was inactive. Equally, the minimum biocidal concentrations (MBC), and the establishment of mode of activity of the bioactive leaves extracts, assayed by the macrobroth-dilution technique, indicated predominantly static activity for the methanol extract, and a predominantly cidal activity for the ethanol extract. Both methanol and ethanol leaves extracts of Laportea aestuans showed significant (p<0.05) antimicrobial activities compared to the standard antibiotics: chloramphenicol and fluconazole. Keywords: Antimicrobial potency, Activity –spectra, Laportea aestuans Extracts, Auchthocthonous urogenital, gut and pulmonary pathogens
采用标准的植物化学和微生物学方法对拉乌茶叶片、茎皮和全株水提取物、甲醇提取物和乙醇提取物进行了植物化学筛选和抗菌活性研究。植物化学程序表明,存在皂苷、单宁、白丹宁、黄酮类、生物碱和心脏苷。全株提取物的产率显著(p)乙醇>甲醇。紫竹叶、茎皮和整株水、甲醇和乙醇提取物对原性泌尿生殖系统、肠道和肺部试验生物的抑菌活性:金黄色葡萄球菌、腐生葡萄球菌、肺炎链球菌、大肠杆菌、铜绿假单胞菌、奇异变形杆菌、伤寒沙门氏菌、霍乱弧菌、痢疾志贺氏菌、白色念珠菌和黑曲霉;改良琼脂孔扩散法测定其抗菌活性具有广谱性。活性指数分析表明,叶提取物的抑菌活性显著高于茎皮提取物。同样,从活性指数上看,乙醇提取物显著高于甲醇提取物。用大液稀释法测定的叶提取物对痢疾志贺氏菌的最低抑制浓度(MIC)为1.25 mg/ml,甲醇和乙醇提取物对其他细菌和真菌的最低抑制浓度一般在2.50 ~ 5.0 mg/ml之间;而水提物无活性。同样,通过大液稀释技术测定的最低生物杀灭浓度(MBC)和生物活性叶提取物的活性模式的建立表明,甲醇提取物的主要是静态活性,乙醇提取物的主要是杀灭活性。与标准抗生素氯霉素和氟康唑相比,茶叶甲醇提取物和乙醇提取物的抑菌活性均显著(p<0.05)。关键词:抑菌效价,活性谱,茯苓提取物,泌尿生殖、肠道和肺部原发病原体
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引用次数: 0
Evaluation of Socio-Demographic Characteristics of HIV/AIDS Patients in a Tertiary Hospital 某三级医院HIV/AIDS患者社会人口特征评价
Pub Date : 2014-06-09 DOI: 10.4314/JOPHAS.V11I1
OW Aitalegbe, M. Femi-Oyewo
The HIV/AIDS epidemic in Nigeria has rapidly gained momentum and is now a public health concern. This study was carried out to assess the socio-demographics of HIV/AIDS patients who accessed treatment at OOUTH, Sagamu, Ogun, Nigeria. It involved a retrospective review of medical records obtained from the Community Medicine and Primary Care Unit which contained information on patients who received treatment between January 2007 and December 2009. The total number of case notes studied was 362. The result indicated that 61% of the study population were females. Age range, 20-40 years of both the female and male groups had the highest representations of 41% and 21% respectively. Majority (45%) were married, 38% had no formal education while, 33% were traders. The study showed a higher HIV/AIDS prevalence within the ages of 21 and 60 years and females were mostly affected. This study thus suggests a system for implementation of specific and focused educational programs among this age range. Keywords: Socio-demographics, HIV/AID, Retrospective, Teaching hospital
艾滋病毒/艾滋病在尼日利亚迅速蔓延,现已成为一个令人关切的公共卫生问题。本研究旨在评估在尼日利亚奥贡Sagamu的youth接受治疗的艾滋病毒/艾滋病患者的社会人口统计学特征。它涉及对从社区医学和初级保健股获得的医疗记录进行回顾性审查,其中载有2007年1月至2009年12月期间接受治疗的患者的信息。研究的病例记录总数为362份。结果表明,61%的研究人群为女性。在20-40岁年龄组中,女性和男性的比例最高,分别为41%和21%。大多数(45%)已婚,38%没有受过正规教育,33%是商人。该研究显示,21岁和60岁人群中艾滋病毒/艾滋病的患病率较高,其中女性感染率最高。因此,本研究建议在这一年龄范围内实施具体和重点教育计划的系统。关键词:社会人口学;HIV/ aids;回顾性
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引用次数: 0
Phytochemical Studies And Antimicrobial Properties Of Methanolic And Aqueous Extracts Of Lemon Grass Leaves ( Cymbopogon Citratus ) 柠檬草叶醇提物和水提物的植物化学研究及抑菌性能
Pub Date : 2014-01-01 DOI: 10.4314/JOPHAS.V11I3
V. Aina, M. Ibrahim, A. Adewumi, M. Abdulsalami, Adejo Godwin, A. Shehu
Binders, disintegrants and compression pressures play important roles in producing good tablets. The interactions between these three factors were analyzed to observe how they contribute to tablet properties. The concentration levels of the factors were determined using 2 3 factorial study designs by wet granulation method of tableting. The binder and disintegrant levels were used in narrow differences at 2 % w/w & 4 % w/w and 5 % w/w & 10 % w/w respectively. While for wide differences, 1 % w/w & 5 % w/w 5 % w/w & 20 % w/w respectively. Compression pressure was used at 8.0 MT & 9.5 MT for narrow and wide levels respectively. For each tablet property determined, interaction by two of the factors was calculated by finding the differences between the mean of four combinations in which the two factors occur as both “high” or “low” levels together from the mean of the remaining four combinations in which the two factors occur in combination of “high” and “low” levels. A student t-test was then used to calculate the significance of such interactions. The results show that at narrow differences in levels of factors, compression pressure determined good tablet properties, but as the differences widens, binder action dominates. Enlarging the differences between the factors also showed the increasing influence of disintegrant action for good table properties with increasing concentration levels. In all the batches however, none showed any significant interactions among the factors. Therefore, the levels of tablet factors, binder, disintegrant and compression pressure shows interactions on tablet friability, hardness and disintegration time by both being additive or opposing and their effects depend on the differences in the levels of the factors in the formulation.  Keywords: Binder, disintegrant, compression pressure, tablet, interaction
对香茅水提液和醇提液进行了植物化学研究。采用琼脂孔扩散法评价提取物对选定病原菌的抑菌效果。甲醇提取物在不同浓度(50 mg%、25 mg%、12.5 mg%、6.25 mg%)下对沙门氏菌的平均抑制区(mm)分别为31.75、26.00、21.50和15.00;假单胞菌分别为25.25、19.25、16.25和12.25。水提物对假单胞菌(20.75、14.75和10.50)和金黄色葡萄球菌(13.25)的平均抑制区(mm)最小。沙门氏菌、金黄色葡萄球菌和假单胞菌的甲醇和水提物的最低抑菌浓度MIC (minimum Inhibitory Concentration)分别为25% v/v和50% v/v,相应的MBC分别为50% v/v和75% v/v。植物化学筛选表明,水提液和甲醇提液均含有生物碱、心苷、黄酮类化合物、单宁和白丹宁5种有效成分。关键词:柠檬草,琼脂孔扩散,植物化学分析,白色念珠菌,心脏苷
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引用次数: 5
Determination of binding affinities of some approved drugs to Ascaris suum mitochondrial rhodoquinol-fumarate reductase by in silico molecular docking 硅分子对接法测定一些获批药物与猪蛔虫线粒体富马酸还原酶的结合亲和力
Pub Date : 2014-01-01 DOI: 10.4314/JOPHAS.V11I2
I. Uzochukwu, O. Olubiyi, CO Akpojotor
The binding affinity of a drug for a receptor describes how avidly the drug binds to the receptor. Drugreceptor binding determines the ability to produce a pharmacological response and to some extent the size of that response. The study investigated the binding affinities of some approved drugs to Ascaris suum  mitochondrial rhodoquinol-fumarate reductase(MRFR), an essential Ascaris enzyme, by in silico molecular docking simulations. Twenty eight approved drugs were carefully selected based on the possibility of their pharmacological action on Ascaris smooth muscles or antiparasitic activities. Selected drugs were obtained from ZINC ® database as mol2 files and further prepared for docking simulations using AutoDock tools v. 1.5.6. Ascaris MRFR was obtained as pdb file (3vra) from the Protein Data Bank and further prepared for docking simulations using both Chimera v. 1.8.1 and AutoDock tools v. 1.5.6. In order to validate the docking protocol, the binding of atpenin, an experimental anthelmintic compound, to MRFR was successfully reproduced in silico . Docking simulations were performed using AutoDockVina 4.0 on a Linux platform. Docking results were analyzed using PyMol v.0.99r c6. Molecular dynamics was employed for the validation of complexed frontrunner approved drugs. Binding free energies of -8.60, -7.75 and -7.50 kcal/mol were obtained for atovaquone, carvedilol and atpenin respectively. Zero binding free energies were recorded for tinidazole, piperazine, bithionol, thiabendazole and metronidazole. Molecular dynamics simulations of atovaquone and carvedilol complexed with the reductase enzyme revealed a strongly favourable binding with likely favourable entropic term in the case of carvedilol. Atovaquone and carvedilol were thus predicted as frontrunner approved drugs with possible anthelmintic activities comparable to atpenin. In vitro and in vivo investigations into the anthelmintic activities of atovaquone and carvedilol are recommended. Key-words : Ascaris, docking, molecular dynamics, anthelmintics, drug repurposing.
药物与受体的结合亲和力描述了药物与受体的结合程度。药物受体结合决定了产生药理学反应的能力,并在某种程度上决定了反应的大小。本研究通过硅分子对接模拟研究了一些获批药物与Ascaris suum线粒体富马酸rhodoquinol-fumarate reductase(MRFR)的结合亲和力,MRFR是Ascaris必不可少的酶。28种批准的药物是根据其对蛔虫平滑肌的药理作用或抗寄生虫活性的可能性精心选择的。从ZINC®数据库中获得选定的药物作为mol2文件,并使用AutoDock工具v. 1.5.6进行对接模拟。从蛋白质数据库中获得Ascaris MRFR为pdb文件(3vra),并使用Chimera v. 1.8.1和AutoDock工具v. 1.5.6进行对接模拟。为了验证对接方案,在硅中成功地复制了atpenin(一种实验性驱虫药化合物)与MRFR的结合。在Linux平台上使用AutoDockVina 4.0进行对接模拟。对接结果使用PyMol v.0.99r c6进行分析。采用分子动力学方法对已获批的复杂先导药物进行验证。阿托伐醌、卡维地洛和阿霉素的结合自由能分别为-8.60、-7.75和-7.50 kcal/mol。替硝唑、哌嗪、比硫醇、噻苯达唑和甲硝唑均记录了零结合自由能。对阿托伐醌和卡维地洛与还原酶络合的分子动力学模拟表明,卡维地洛具有很强的亲和性,并且可能具有有利的熵项。因此,阿托伐酮和卡维地洛被预测为领先的批准药物,可能具有与肾上腺素相当的驱虫活性。建议对阿托伐醌和卡维地洛的体内和体外驱虫活性进行研究。关键词:蛔虫,对接,分子动力学,驱虫药,药物再利用
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引用次数: 4
Training needs analysis for pharmacists in Nigeria – A case study of Warri, Delta State 尼日利亚药剂师培训需求分析——以三角洲州瓦里为例
Pub Date : 2013-06-21 DOI: 10.4314/JOPHAS.V10I1
V. Imieje, I. Igbe, A. Falodun
Pharmacists in Nigeria do not seem to exhibit the expertise, skills, poise and assertiveness necessary to function effectively as drug experts in the health care team. This posture could be due to knowledge deficiency. Bridging the knowledge gap could be an important step in improving the confidence of practicing pharmacists irrespective of the practice setting. The objective of the present study was to identify areas of knowledge deficiency among practicing pharmacists in Nigeria with respect to drug therapy of diseases of contemporary interest - hypertension, HIV/AIDS, thrombosis, cancer and epilepsy. A census of all pharmacists that met the inclusion criteria was done. Knowledge was assessed using a 52 item pre-tested questionnaire exploring basic aspects of pharmacotherapy of various disease states. Response rate was 73%. Majority of pharmacists surveyed had no additional qualifications. Even though over 75% of pharmacists claimed to be computer literate, self rated internet skills was below average. Knowledge scores were high for hypertension, diabetes and retroviral disease while pharmacists were found to be knowledge deficient in the areas of lipid lowering drugs, anti cancer drugs and anticoagulant therapy . Pharmacists with Doctor of Pharmacy degree and those in hospital pharmacy practice consistently had higher knowledge scores than those without further qualifications and who are in community pharmacy practice. There is a need for pharmacists, particularly those in the community setting, to undergo more specialized training in the area of lipid management, epilepsy, anticoagulation therapy and treatment of cancers if they are to meet the challenges of contemporary practice . Keywords : Training needs, Pharmacists, knowledge deficiency, Nigeria
尼日利亚的药剂师似乎没有表现出作为保健队的药物专家有效发挥作用所必需的专业知识、技能、沉着和自信。这种姿势可能是由于缺乏知识。弥合知识差距可能是提高执业药师信心的重要一步,无论执业环境如何。本研究的目的是确定尼日利亚执业药剂师在当代关注的疾病——高血压、艾滋病毒/艾滋病、血栓形成、癌症和癫痫——的药物治疗方面缺乏知识的领域。对所有符合纳入标准的药剂师进行普查。知识评估采用52项预测问卷,探讨各种疾病状态的药物治疗的基本方面。有效率为73%。接受调查的大多数药剂师没有额外资格。尽管超过75%的药剂师声称自己精通电脑,但他们自测的互联网技能却低于平均水平。药师对高血压、糖尿病和逆转录病毒疾病的知识得分较高,对降脂药物、抗癌药物和抗凝治疗的知识得分较低。具有药学博士学位的药师和在医院药学实习的药师的知识得分始终高于未取得进一步资格的药师和在社区药学实习的药师。药剂师,特别是社区药剂师,如果要应对当代实践的挑战,就需要在血脂管理、癫痫、抗凝治疗和癌症治疗方面接受更多的专业培训。关键词:培训需求;药师;知识缺失
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引用次数: 2
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Journal of Pharmaceutical and Allied Sciences
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