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Synthesis, characterization and antimicrobial activity of novel tetrazoles clubbed with pyrimidine 新型嘧啶棒状四唑的合成、表征及抗菌活性研究
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.016
N. Bhoge, B. Magare, P. Mohite
An attempt was made to synthesize pyrimidine tetrazole derivatives of pharmaceutical interest by oxidative cyclization of chalcones with adequate yield and purity, prompted by the diversity of their wider usage and the fact that they are an integral part of genetic content. The present work involves the reaction of 5-(2,6-dimethylphenyl)-1H-tetrazole with acetic anhydride to yield 1-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl] ethanone (1) and which then treated with different aromatic aldehydes in presence of alkaline medium to chalcones (2a-f). Reaction of chalcones (2a-f) with urea and thiourea to produce 5-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl]-4-(substituted aryl ) pyrimidin-2-ol (3a-f) and 5-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl]-4-(substituted aryl) pyrimidin-2-thiol (4a-f) respectively. All compounds were characterized by infrared spectroscopy (IR), H nuclear magnetic resonance (NMR), and mass spectrometry (MS) to prove the structure and assessed in vitro for their efficacy as antibacterial and antifungal activity against four bacteria. The compounds 3c, 3d and 3f and compounds 4c, 4d and 4f possess very good activity against and E. coli and the compounds 3e, 3c and 3a and compounds 4e,4b and 4c possess very good activity against fungi and .
由于查尔酮具有广泛的用途,而且它们是遗传内容的一个组成部分,因此试图通过氧化环化法制备具有一定产量和纯度的具有药用价值的嘧啶四唑衍生物。本研究涉及5-(2,6-二甲基苯基)- 1h -四唑与乙酸酐反应生成1-[5-(2,6-二甲基苯基)- 1h -四唑-1-基]乙酮(1),然后在碱性介质中用不同的芳香醛处理得到查尔酮(2a-f)。查尔酮(2a-f)与尿素和硫脲反应分别生成5-[5-(2,6-二甲基苯基)- 1h -四唑-1-基]-4-(取代芳基)嘧啶-2-醇(3a-f)和5-[5-(2,6-二甲基苯基)- 1h -四唑-1-基]-4-(取代芳基)嘧啶-2-硫醇(4a-f)。通过红外光谱(IR)、核磁共振(NMR)和质谱(MS)对化合物进行了结构表征,并对其体外抗菌和抗真菌活性进行了评价。化合物3c、3d、3f和化合物4c、4d、4f对大肠杆菌具有很好的活性,化合物3e、3c、3a和化合物4e、4b、4c对真菌和大肠杆菌具有很好的活性。
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引用次数: 0
Nanotech drug delivery system: The perfect physio-Chemical deal for biological command 纳米技术药物输送系统:生物指令的完美物理化学交易
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.010
Yogranjan Singh, Kaustubh Gurnani, G. Satpute
The application of nanotechnology in drug delivery is offering several exhilarating possibilities not only in healthcare but also in agriculture. Nanoparticles combined with the therapeutic agents have a proven edge over problems associated with conventional therapy; however, some issues like side effects and toxicity are still under debate and are of prime concern in utilization in biological systems. Herein, we discuss the role of nanotech drug delivery system mostly in animal and plants- highlighting the comparative accounts of the key techniques for designing of drug in animals and plants, the challenges therein, the important nanoparticles being used in both the area and prospects of the field in the near future.
纳米技术在药物输送中的应用不仅在医疗保健领域,而且在农业领域提供了一些令人振奋的可能性。纳米粒子与治疗剂相结合,在与传统治疗相关的问题上具有已被证明的优势;然而,一些问题,如副作用和毒性仍在争论中,是在生物系统中利用的首要问题。在此,我们主要讨论了纳米技术在动物和植物中的作用,重点介绍了动物和植物药物设计的关键技术的比较,其中的挑战,重要的纳米颗粒在该领域的应用以及在不久的将来该领域的前景。
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引用次数: 1
A cohurt study on association and inflammatiory markers of cardio metabolic risk factors in pre and post menopausal women 绝经前和绝经后妇女心血管代谢危险因素的相关性和炎症标志物的队列研究
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.015
D. Jayarajan, V. Abirami
Pre and post menopause were the complications faced by women globally that not only interferes in physical health but also in mental health of a woman. The menopause factors includes many traditional CVD risk factors, including changes in body fat distribution from agynoid to an android pattern, reduced glucose tolerance, abnormal plasma lipids, increased blood pressure, increased sympathetic tone, endothelial dysfunction and vascular inflammation . Menopause is a risk factor for (CVD) because estrogen withdrawal has a detrimental effect on cardiovascular function and metabolism .The present study aimed for inflammatory markers of cardio metabolic risk factors in post menopausal women and premenopausal women and the results recorded the significant level of elevation in all parameters compared with case and control samples and the significance was given as student’s t test(p<0.001).
绝经前和绝经后是全球妇女面临的并发症,不仅会干扰妇女的身体健康,还会干扰妇女的精神健康。更年期因素包括许多传统的心血管疾病危险因素,包括体脂分布从甲状腺样向人形变化、糖耐量降低、血脂异常、血压升高、交感神经张力增加、内皮功能障碍和血管炎症。绝经是心血管疾病的危险因素,因为雌激素的停药对心血管功能和代谢有不利影响。本研究旨在检测绝经后和绝经前妇女心血管代谢危险因素的炎症标志物,结果显示,与病例和对照组相比,所有参数均显著升高,并采用学生t检验(p<0.001)。
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引用次数: 0
Removal of dye by using activated charcoal prepared by kitchen waste 用厨余制备的活性炭去除染料
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.017
Shravani Sunil Sontakke, Anushka Shailesh Rupwate, M. Baile, Ashish Jain
The given research study explains about the removal of methyl red dye from aqueous solution. Using activated carbon prepared from kitchen waste. Garlic husk which was used in this work is cost effective and easily available kitchen waste for the production of activated carbon. HCl solution was used as activating agent. Various characterization procedures such as FT-IR, XRD, moisture content, ash value, volatile matter content, pH, iodine value of prepared activated carbon was studied. The adsorption property of activated carbon using different measurement studies like contact time study, effect of concentration, effect of dose of adsorbent was also studied.
本文研究了甲基红染料在水溶液中的脱除。使用由厨余垃圾制备的活性炭。本研究中所使用的大蒜壳是一种经济有效且易于获得的厨余垃圾,可用于生产活性炭。采用盐酸溶液作为活化剂。对制备的活性炭进行了FT-IR、XRD、水分、灰分、挥发物、pH、碘值等表征方法的研究。采用接触时间、吸附剂浓度、吸附剂剂量对活性炭吸附性能的影响进行了研究。
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引用次数: 0
Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion 美沙拉胺水溶液溶解度和溶出度的富集:固体分散体的体外评价
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.018
A. Pawar, Pralhad Vitthalrao Mundhe, V. Deshmukh, R. Pandhare, T. Nandgude
The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.
本研究的目的是制备美沙拉胺的固体分散体(SD),以提高其水溶性和溶出率。美沙拉明用于治疗急性溃疡性结肠炎和预防活动性溃疡性结肠炎复发。本研究以不同的聚合物为原料,采用熔融和溶剂蒸发法制备了美沙拉胺的固体分散体。用实际产率、药物含量、溶解度、红外光谱(FT-IR)、粉末X射线衍射(PXRD)、扫描电镜(SEM)、体外溶出度和稳定性研究对SD进行了表征。采用融合和固体分散法制备的美沙拉胺固体分散体(FM47、FM67、SE47和SE67)的释药率为1:7,分别为81.36±0.41、86.29±0.64、82.45±0.57和87.25±1.14。两种方法均能显著提高美沙拉胺固体分散体的溶解度和释药率。PXRD表明,固体分散体中存在的纯药物结晶度明显降低,导致美沙拉明的水溶性和溶出率增加。在固相分散体系中,加入peg4000和peg6000后,药物的结晶度降低,无聚集和结块现象,润湿性增强,分散性良好,使得美萨拉明的水溶性和溶解速率显著提高。
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引用次数: 3
Potentially inappropriate medications in nursing homes of iraqi elders: Pharmacists’ assessment and intervention based on 2019 beers criteria 伊拉克老年人疗养院中可能不适当的药物:药剂师基于2019年啤酒标准的评估和干预
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.013
Hussein Naqash
The number of elderly people worldwide is growing with the increasing life expectancy of the human population; in Iraq, the number of elderly people aged ≥65 years was estimated to be 1.34 million in 2019. The use of potentially inappropriate medications (PIMs) is high among older adults, which is associated with an increased risk of adverse drug reactions. This study investigated the use of PIMs among elderly nursing home (NH) residents in Iraq based on 2019 Beers criteria and the application of the criteria and intervention by pharmacists. An interventional study was conducted from January 2019 to April 2019 at 2 NHs in Baghdad, Iraq. A total of 109 NH residents aged ≥65 years that were using ≥1 daily medicine were included. Patients discharged before completion of the assessment were excluded. Patients with PIMs were using significantly more medications (5.7±3.2) than those without PIMs (2.0 ±1.46) (p<0.0001). The total number of PIMs identified according to the 2019 Beers criteria was 163; for 140 of these (85.9%), pharmacists recommended changing the prescription, with 112 (68.7%) discontinued/changed as a result for an acceptance rate of 80% by physicians. Our results indicate that the use of PIMs for the treatment of Iraqi NH residents is associated with polypharmacy. Thus, prescriptions for elderly people in Iraq with polypharmacy or multiple concurrent diagnoses should be reviewed for PIMs by pharmacists to reduce the risk of adverse events.
随着人类预期寿命的延长,世界范围内老年人的数量正在增长;在伊拉克,2019年65岁以上老年人的数量估计为134万。老年人使用潜在不适当药物(PIMs)的比例很高,这与药物不良反应的风险增加有关。本研究基于2019 Beers标准、标准的应用和药剂师的干预,调查了伊拉克老年养老院(NH)居民对pim的使用情况。2019年1月至2019年4月,在伊拉克巴格达的2个NHs进行了一项介入性研究。共纳入109例年龄≥65岁、每日用药≥1种的NH居民。在评估完成前出院的患者被排除在外。有PIMs的患者使用的药物(5.7±3.2)明显多于无PIMs的患者(2.0±1.46)(p<0.0001)。根据2019年Beers标准确定的pim总数为163个;其中140例(85.9%),药剂师建议更改处方,112例(68.7%)停止或更改处方,医生接受率为80%。我们的结果表明,使用pim治疗伊拉克NH居民与多药有关。因此,在伊拉克,药剂师应该对有多种药物或多种并发诊断的老年人的处方进行pim审查,以减少不良事件的风险。
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引用次数: 0
Muntingia calabura: A comprehensive review 卡拉芒廷:全面回顾
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.011
M. Kuchekar, Mohini C. Upadhye, R. Pujari, S. Kadam, Priyanka Gunjal
Medicinal plants are well-known sources of important therapeutic aid for alleviate human disorders. (Elaeocarpaceae) is the widely used in the ayurvedic system of the medicine as very sweet, musky, fig-like flavour. also known as Jamaica cherry, is a small and evergreen tree. The necessity of plant in human ailments is illustrious in old medicinal practices. The secondary metabolites are obtained from the different parts of plant alkaloids, flavonoids, tannin, phenolic compound etc. are traditional medicinal uses have been reported for the leaves (headaches, prostate problems, reduce gastric ulcers), bark (antiseptic), flowers (antiseptic, reduce swelling, antispasmodic), and fruits (respiratory problems, antidiarrheic). The present study gives an overview on plant and its pharmacological activities were documented.
众所周知,药用植物是缓解人类疾病的重要治疗援助来源。(elaecarpaceae)是广泛应用于阿育吠陀系统的药物,非常甜,麝香,类似无花果的味道。也被称为牙买加樱桃,是一种小的常青树。在古老的医学实践中,植物治疗人类疾病的必要性是显而易见的。次生代谢物是从植物的不同部位获得的生物碱,类黄酮,单宁,酚类化合物等,传统的药用用途已被报道为叶子(头痛,前列腺问题,减少胃溃疡),树皮(防腐),花(防腐,消肿,止痉),和水果(呼吸问题,止泻)。本文对该植物进行了综述,并对其药理活性进行了文献报道。
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引用次数: 2
Ocular drug delivery system (ODDS): Exploration the challenges and approaches to improve ODDS 眼部给药系统(ODDS):探讨提高ODDS的挑战和途径
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.012
Suraj Mandal, Km Shiva, K. P. Kumar, Sweta Goel, Ramesh Patel, Shweta Sharma, Renu Chaudhary, Arti Bhati, Netra Pal, Ashwani Dixit
The remarkable life structures and physiology of the eye presents huge difficulties to researchers in the field of visual medication conveyance frameworks. Nearby infusion is the most fitting and proper medication organization technique for the treatment of foremost front sickness. There are two kinds of hindrances in ophthalmic medication conveyance frameworks: static boundaries and dynamic obstructions. Static lamellae contain corneal, dermal, retinal, and retinal vessels while dynamic lamellae contain placental blood stream, conjunctiva, tear evacuation, and lymphatic seepage. These limitations influence the bioavailability of the medication. This article examines the limits of customary ophthalmic practice and the central point affecting the pharmacokinetics of the eye. Likewise, eye salves, gels, prodrugs, intranasal infusions, thickeners, entrance energizers, liposomes, microparticles, nanoparticles, visual infusions, inserts, nanoparticles, nanostructures, microemulsions, gels and periocular infusions. It guarantees the bioavailability of the medication and the controlled and constant control of the medication in the foremost and back alveoli.
眼睛独特的生命结构和生理特征给视觉药物传输框架的研究带来了巨大的困难。就近输液是治疗前列病最合适、最合理的用药组织技术。眼科药物输送框架存在两种障碍:静态边界和动态边界。静态片层包含角膜、真皮、视网膜和视网膜血管,而动态片层包含胎盘血流、结膜、泪液排出和淋巴渗漏。这些限制影响药物的生物利用度。本文考察了习惯眼科实践的局限性和影响眼睛药代动力学的中心点。同样,眼膏、凝胶、前药、鼻内输液、增稠剂、入口能量剂、脂质体、微颗粒、纳米颗粒、视觉输液、插入物、纳米颗粒、纳米结构、微乳液、凝胶和眼周输液。保证了药物的生物利用度,保证了药物在前肺泡和后肺泡的可控和恒定控制。
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引用次数: 1
Drug withdrawal a common feature attributed to patient safety 药物戒断是患者安全的一个共同特征
Pub Date : 2021-11-15 DOI: 10.18231/j.jpbs.2021.009
S. Chaudhry
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引用次数: 0
Evaluation of some pharmacognostic parameters of the herbs for a traditional hematinic (Haematol -B) powdered formulation in Ogbomoso, Nigeria 尼日利亚Ogbomoso一种传统血碱(Haematol -B)粉状制剂的一些生药学参数评价
Pub Date : 2021-07-15 DOI: 10.18231/J.JPBS.2021.007
J. E. Ideh, A. Ogunkunle, G. Olaniran, F. O. Olu
The traditional hematinic oral powdered herbal drug (Haematol-B) from Ogbomoso, Nigeria had been characterized in terms of its botanical constituents, ascorbic acid and mineral elements composition, but there is inadequate information on the pharmacognostic properties of the ten herbal materials for its formulation. Therefore the objective of this study was to evaluatethe bark and wood anatomy (as appropriate) of seven of these herbs with a view to highlighting the diagnostic markers for their authentication. Following the conventional anatomical procedures of transverse sectioning (TS) and tissue maceration (TIM), a total of 21 characters were drawn from the barks (root or stem as appropriate) of the seven woody species studied, while 41 characteristics of the wood in the roots of three of the species were compiled using TS, transverse longitudinal sectioning (TLS), radial longitudinal sectioning (RLS) and TIM techniques. Staining, mounting and microscopic examinations followed, and the observed features were taxonomically described in accordance with the provisions of International Association of Wood Anatomists. Their diagnostic values among the medicinal herbs studied were also explored. The bark anatomical features that can be used to diagnose the species studied were those of the secondary cortex, phloem rays, axial parenchyma, sclereids and resin ducts. The wood anatomical markers included features of the vessels in the TS and variable ray characteristics in the TLS. The two artificial keys constructed from discontinuities in qualitative and quantitative anatomical features of the barks and the wood are useful tools for avoiding misidentification of the herbal materials studied.
尼日利亚Ogbomoso的传统血液科口服粉状草药(Haematol-B)在其植物成分、抗坏血酸和矿物元素组成方面具有特征,但关于其配方的十种草药材料的生药学性质的资料不足。因此,本研究的目的是评估七种草药的树皮和木材解剖(如适当),以突出其认证的诊断标记。采用传统的横切面(TS)和组织浸渍(TIM)的解剖方法,从7种木本植物的树皮(根或茎)中提取了21个特征,并利用横切面、横切面、径向纵切面和横切面技术对其中3种木本植物的根系进行了41个特征的整理。随后进行染色、安装和显微镜检查,并根据国际木材解剖学家协会的规定对观察到的特征进行分类描述。探讨了它们在所研究的中草药中的诊断价值。树皮的次生皮质、韧皮部射线、轴向薄壁、硬核和树脂导管等解剖特征可用于诊断所研究树种。木材解剖标记包括TS中的血管特征和TLS中的变射线特征。利用树皮和木材在定性和定量解剖特征上的不连续构造的两个人工键,可以有效地避免对所研究的药材的误认。
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引用次数: 0
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Research journal of pharmaceutical, biological and chemical sciences
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