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Development of microparticles and microparticulated tablets containing piperine 含胡椒碱微颗粒及微颗粒片剂的研制
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-05-08 DOI: 10.1590/s2175-97902023e21265
A. Schneider, Carlos Eduardo de Souza Brener, N. Daudt, L. Cruz, C. B. Silva
Piper nigrum (black pepper) is used in Indian traditional medicine and its main alkaloid, Piperine (PIP), presents antioxidant, antitumor and neuroprotective pharmacological properties. This substance is insoluble in aqueous media and can irritate the gastrointestinal tract. Aiming to avoid these inconvenient characteristics and enable PIP oral administration, this study suggested the PIP microencapsulation through the emulsion-solvent evaporation method and the preparation of microparticulated tablets by direct compression. An UV-spectroscopy method was validated to quantify PIP. Microparticles and microparticulated tablets were successfully obtained and the microparticles exhibited excellent flow. The scanning electron microscopy images showed that PIP microparticles were intact after compression. The in vitro release showed a controlled release of PIP from microparticles and PIP microparticles from tablets in comparison to PIP and PIP tablets. The release profiles of PIP microparticles and the microparticulated tablets were similar. Therefore, tablets containing PIP microparticles are promising multiparticulated dosage forms because a tablet allows microparticles administration and the intact ones promote a controlled release, decreasing its irritating potential on the mucosa.
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引用次数: 0
A Hospital-based Observational Study of Newly diagnosed Sthula Prameha Subjects with special reference to type 2 Diabetes Mellitus from Maharashtra, India 印度马哈拉施特拉邦新诊断的2型糖尿病患者的医院观察研究
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-05-08 DOI: 10.1590/s2175-97902023e21230
N. Munishwar, Rakesh Bramhankar, N. N. Raju
The aim of this study is to provide a real picture of the disease burden of Prameha in society. The study was performed in Government Ayurved College and Hospital, Nagpur, Maharashtra during Oct 2015-Mar 2016. Total 60 patients of newly diagnosed type 2 diabetes mellitus attending the Kayachikitsa Opd of GAC Nagpur were included for the study. The subjects details were recorded in case report form. The CRF included many variables such as sociodemographic factors, presenting symptoms, risk factors such as hypertension, obesity and glycaemic status, family history of diabetes and physical activity. Other parameters like BMI, glycosylated haemoglobin, fasting and post prandial blood sugar and fasting lipid profile were documented. Descriptive and bivariate analyses were carried out using the XLSTAT software (2020). Amongst 60 subjects, 65% were male and 93.3% were adults. 78% of subjects were following sedentary lifestyle and 40% had family history of diabetes. The results revealed that, obesity, family history of diabetes, uncontrolled glycemic status, sedentary lifestyles, and hypertension were prevalent among the Prameha subjects. The characterization of this risk profile and early detection of prameha by observing poorvarupa will contribute to designing more effective and specific strategies for screening and controlling Prameha in Maharashtra, India.
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引用次数: 0
In vitro antibacterial-antibiofilm effect of Hypericum atomarium Boiss and chemical composition 金丝桃体外抗菌-抗菌膜作用及化学成分研究
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-05-08 DOI: 10.1590/s2175-97902023e20412
E. Önem, A. Özaydın, H. Sarısu
Treatment with plant is considered an effective option against increased antibiotic resistance. In this study antibiofilm activity of methanol (CH 3 OH), chloroform (CHCl 3 ), ethyl acetate (EtOAc) and water (H 2 O) extracts of Hypericum atomarium Boiss. which is member of Hypericum genus was evaluated in Pseudomonas aeruginosa PAO1 and antibacterial performance against Gram (+) and Gram (-) strains and also bioactive compounds of extract were analysed using by HPLC and GC-MS. According to antibacterial activity test results the extracts were effective all Gram (+) bacteria and Gram (-) Chromobacterium violaceum (MICs ranging from 0.42 µg/ ml to 4.3 mg). Inhibition effect of biofilm formation was found to be different rate in extracts (methanol-63%, chloroform-52%). The major flavonoids were detected (−)-epicatechin (2388.93 µg/ml) and (+)-catechin (788.94 µg/ml). The main phenolic acids were appeared as caffeic acid 277.34 µg/ml and chlorogenic acid 261.79 µg/ml. And according to GC results α-pinene was found main compound for three solvent extracts methanol, chloroform and ethyl acetate 67.05, 62.69, 49.28% rate respectively.
{"title":"In vitro antibacterial-antibiofilm effect of Hypericum atomarium Boiss and chemical composition","authors":"E. Önem, A. Özaydın, H. Sarısu","doi":"10.1590/s2175-97902023e20412","DOIUrl":"https://doi.org/10.1590/s2175-97902023e20412","url":null,"abstract":"Treatment with plant is considered an effective option against increased antibiotic resistance. In this study antibiofilm activity of methanol (CH 3 OH), chloroform (CHCl 3 ), ethyl acetate (EtOAc) and water (H 2 O) extracts of Hypericum atomarium Boiss. which is member of Hypericum genus was evaluated in Pseudomonas aeruginosa PAO1 and antibacterial performance against Gram (+) and Gram (-) strains and also bioactive compounds of extract were analysed using by HPLC and GC-MS. According to antibacterial activity test results the extracts were effective all Gram (+) bacteria and Gram (-) Chromobacterium violaceum (MICs ranging from 0.42 µg/ ml to 4.3 mg). Inhibition effect of biofilm formation was found to be different rate in extracts (methanol-63%, chloroform-52%). The major flavonoids were detected (−)-epicatechin (2388.93 µg/ml) and (+)-catechin (788.94 µg/ml). The main phenolic acids were appeared as caffeic acid 277.34 µg/ml and chlorogenic acid 261.79 µg/ml. And according to GC results α-pinene was found main compound for three solvent extracts methanol, chloroform and ethyl acetate 67.05, 62.69, 49.28% rate respectively.","PeriodicalId":9218,"journal":{"name":"Brazilian Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":1.3,"publicationDate":"2023-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"67737702","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Anti-hyperglycemic fraction from Alternanthera sessilis L. leaves gets elucidated following bioassay-guided isolation and mass spectrometry 利用生物测定引导分离和质谱分析技术,从无梗莲叶中分离出抗高血糖成分
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-05-08 DOI: 10.1590/s2175-97902023e21283
R. A. M. Manalo, E. C. Arollado, Francisco M. Heralde III
Abstract The anecdotal use of Alternanthera sessilis L. as a relief for diabetes has been known in the Philippines for generations, and antidiabetic activity of similar varieties in other countries is likewise documented. However, the compounds responsible for this activity remain unclear. This study aims to isolate the anti-hyperglycemic fraction of local A. sessilis leaves and identify the compounds in this fraction. Methanol extract of A. sessilis leaves and its hexane, ethyl acetate (ASE), and water fractions were administered to alloxan-induced diabetic mice. ASE (250mg/kg) had the highest anti-hyperglycemic activity at 6-h post-treatment (25.81%±12.72%), with almost similar blood glucose reduction rate as metformin (30.13±3.75%, p=0.767). Repeated fractionation employing chromatographic separation techniques followed by in vivo anti-hyperglycemic assay yielded partially purified subfractions. A. sessilis ethyl acetate subfraction 4-2 (100mg/kg) displayed remarkable suppression of blood glucose rise in diabetic mice at 6-h post-treatment (26.45±3.75%, p<0.0001), with comparable activity with metformin (100mg/kg, 27.87±5.65%, p=0.652). Liquid chromatography/mass spectrometry showed eight distinct peaks, with four peaks annotated via the Traditional Chinese Medicine library and custom library for A. sessilis. Among these, luteolin, apigenin, ononin, and sophorabioside were identified as putative compounds responsible for the anti-hyperglycemic activity. This result provided basis for the reported anecdotal claims and potential utility of the local variety of A. sessilis leaves as sources of anti-hyperglycemic agents.
摘要:在菲律宾,人们世代都知道互花菊(Alternanthera sessilis L.)作为一种缓解糖尿病的轶事,在其他国家,类似品种的抗糖尿病活性也有类似的记录。然而,导致这种活性的化合物仍不清楚。本研究的目的是分离和鉴定当地无尾木叶的抗高血糖成分。以四氧嘧啶诱导的糖尿病小鼠为研究对象,采用四氧嘧啶诱导的四氧嘧啶诱导的无叶荷叶甲醇提取物及其己烷、乙酸乙酯(ASE)和水馏分。ASE (250mg/kg)在治疗后6 h的降糖活性最高(25.81%±12.72%),降糖率与二甲双胍基本相当(30.13±3.75%,p=0.767)。采用色谱分离技术进行重复分离,然后进行体内抗高血糖测定,得到部分纯化的亚组分。无尾草乙酸乙酯亚段4-2 (100mg/kg)对糖尿病小鼠治疗后6 h的血糖升高有显著的抑制作用(26.45±3.75%,p<0.0001),与二甲双胍(100mg/kg, 27.87±5.65%,p=0.652)相当。液相色谱/质谱分析显示8个不同的峰,其中4个峰通过中药文库和自定义文库标注。其中,木犀草素、芹菜素、芥子苷和槐总皂苷被认为是具有抗高血糖活性的化合物。这一结果为报道的轶事索赔和当地品种的无梗无梗叶作为抗高血糖药的来源的潜在效用提供了基础。
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引用次数: 1
Oral and nasal vaccination: current prospects, challenges, and impact of nanotechnology-based delivery systems 口服和鼻腔疫苗接种:目前的前景、挑战和基于纳米技术的递送系统的影响
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-05-08 DOI: 10.1590/s2175-97902023e21769
Natália Floriano Paiva, F. Vicentini
Abstract Currently, mucosal vaccine administration has stood out as an easier and non-invasive application method. It can also be used to induce local and systemic immune responses. In the COVID-19 pandemic context, nasal and oral vaccines have been developed based on different technological platforms. This review addressed relevant aspects of mucosal vaccine administration, with emphasis on oral and nasal vaccinations, in addition to the importance of using nanotechnology-based delivery systems to enable these strategies.
目前,粘膜疫苗给药作为一种较为简便、无创的应用方法而备受关注。它也可用于诱导局部和全身免疫反应。在COVID-19大流行背景下,基于不同的技术平台开发了鼻用和口服疫苗。这篇综述讨论了粘膜疫苗给药的相关方面,重点是口服和鼻腔疫苗接种,以及使用基于纳米技术的递送系统来实现这些策略的重要性。
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引用次数: 0
Use of bacaba peel for the development of hydroelectrolytic beverages and their consumer acceptance 利用芭蕉皮开发电解水饮料及其消费者接受度
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-04-28 DOI: 10.1590/s2175-97902023e21762
L. Baldissera, B. W. Debiasi, J. S. Agostini, C. R. Andrighetti, M. M. Sugui, E. B. Ribeiro, D. M. S. Valladão
The hydroelectrolytic beverages segment has been expading its market and introducing new flavors in order to meet the demand for new products. However, experimental studies find concerns about the chemical compositions of these drinks. The aim of this study was to develop a drink without synthetic coloring or flavoring, with functional attributes based on the bacaba ( Oenocarpus bacaba Mart.) peel extract. Two hydroelectrolytic drinks were developed, one hypotonic and the other isotonic, containing 0.5 and 1.0% of bacaba peel extract. Physicochemical characterization, determination of total phenolic compounds, anthocyanins, and antioxidant capacity were perfomed, in addition to color evaluation, as well as sensory analysis by means of preference tests. The developed formulations showed potential antioxidant activity and natural red coloring due to the phenolic compounds and anthocyanins present in the beverages. The sensory evaluation indicated positive acceptance by the tasters regarding the addition of the bacaba peel extract to the beverage formulations. The developed formulations demonstrated that the use of the bacaba peel is a viable option for the production of sports drinks, acting as a natural dye and offering health benefits due to its bioactive compounds.
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引用次数: 1
Effect of Lyophilization on Stability of PEG-Protein Conjugate: A Case Study with Peginterferon alfa-2b 冻干对聚乙二醇-蛋白偶联物稳定性的影响:以聚乙二醇干扰素α -2b为例
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-04-28 DOI: 10.1590/s2175-97902023e201120
Patel Chintan, P. Gayatri
The purpose of the present study was to develop stable lyophilized formulation of peginterferon alfa-2b which is acquiescent to the short lyophilization process. The present study evaluates the effect of buffering components and cryoprotectant(s) on depegylation of the peginterferon alfa-2b in combination with lyophilization process. Finally, a short lyophilization process was identified which can produce a stable pharmaceutical form of peginterferon alfa-2b without any depegylation during long-term storage. Formulations were analyzed mainly for depegylation by HP-size exclusion chromatography and in-vitro antiviral activity. Residual moisture content in the lyophilized product was also used as a key indicating parameter to check its role with respect to depegylation upon storage under various temperature conditions. It was observed that the peginterferon alfa-2b when formulated in presence of cryoprotectant like sucrose requires longer lyophilization process of about 5 days, irrespective of the buffering components used, to reduce the level of residual moisture content and thereby to produce the stable formulation without depegylation. A stable formulation in presence of high concentration of lactose as a cryoprotectant was developed which can withstand stresses exerted to protein-polymer conjugate during lyophilization phases without any significant depegylation. A short lyophilization process of about 48 hours can be utilized for peginterferon alfa-2b when formulated in presence of lactose as a cryoprotectant through which a stable lyophilized formulation can be produced as against longer process required when sucrose is used a cryoprotectant, which is essential from commercial point of view as lyophilization is a costly process.
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引用次数: 0
Effect of combined sedation using multiple drugs on inflammatory cytokines in patients with acute respiratory distress syndrome 多药联合镇静对急性呼吸窘迫综合征患者炎症因子的影响
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-04-28 DOI: 10.1590/s2175-97902023e21461
Xiangbi Nie, Liqiong Lou, Huijie Xu, Wei Xiong, Zenggeng Wang
The innate immune response plays an important role in the pathophysiology of acute respiratory distress syndrome (ARDS); however, no drug has been proven to be beneficial in the management of ARDS. Therefore, the aim of this study was to investigate the effects of using combined sedatives on systemic inflammatory responses in patients with ARDS. A total of 90 patients with ARDS and an intubation time of > 120 h were randomly divided into the propofol group (group P), midazolam group (group M), and combined sedation group (group U). Patients in groups P and M were sedated with propofol and midazolam, respectively, whereas patients in group U were sedated with a combination of propofol, midazolam, and dexmedetomidine. The dosage of sedatives and vasoactive drugs, duration of mechanical ventilation, and incidence of sedative adverse reactions were documented. The dosage of sedatives and vasoactive drugs, as well as the incidence of sedative adverse reactions in group U, was significantly lower than those in groups P and M. Similarly, the duration of mechanical ventilation in group U was significantly shorter than that in groups P and M. Hence, inducing sedation through a combination of multiple drugs can significantly reduce their adverse effects, improve their sedative effect, inhibit systemic inflammatory responses, and improve oxygenation in patients with ARDS.
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引用次数: 0
Effect of quercetin and role of nitric oxide pathway in chloroquine-induced scratching 槲皮素在氯喹致抓伤中的作用及一氧化氮通路的作用
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-04-28 DOI: 10.1590/s2175-97902023e201085
O. Kukula, Caner Günaydın
Nitric oxide (NO) is an abundant mediator which is demonstrated to be involved in pruritus. Assuming that the increased NO also mediates chloroquine-induced pruritus, which is a frequent complication seen in the chronic chloroquine treatment, the current study aimed to investigate the effect of quercetin and the role of NO in chloroquine-induced pruritus in C57BL/6 mice. Model was created with subcutaneous chloroquine (400µg/site) injection to the nape of the mice. Effect of quercetin and role of NO were investigated with administration of quercetin, and co-administration with L-NAME, 7-NI and L-arginine before chloroquine injection. Locomotor activity was assessed by activity cage and number of the scratching bouts after chloroquine injection was recorded for 30 minutes. Our results show that quercetin significantly reduced scratching bouts at the doses of 10, 20, 40 and 80 mg/kg. Locomotor activity was decreased at the 40 and 80 mg/kg doses of quercetin. Additionally, decrease of the number of scratching bouts by quercetin prevented by L-arginine treatment, while L-NAME and 7-NI enhanced the anti-pruritic effect of sub-effective doses of quercetin. Therefore, our study demonstrated that acute injection of quercetin significantly diminished chloroquine-induced scratching behavior, and this effect is partly mediated by inhibition of neuronal nitric oxide synthase enzyme.
一氧化氮(NO)是一种丰富的介质,被证明参与瘙痒。假设NO的升高也介导了氯喹性瘙痒,这是慢性氯喹治疗中常见的并发症,本研究旨在探讨槲皮素在C57BL/6小鼠氯喹性瘙痒中的作用和NO的作用。小鼠颈背皮下注射氯喹(400µg/位点)造模。在注射氯喹前,分别用槲皮素和L-NAME、7-NI、l -精氨酸联合给药,考察槲皮素的作用和NO的作用。采用活动笼法评估运动活动,记录注射氯喹30 min后抓痒次数。我们的研究结果表明,槲皮素在10、20、40和80 mg/kg剂量下显著减少抓痕次数。40和80 mg/kg剂量的槲皮素使运动活性降低。此外,l -精氨酸处理可防止槲皮素引起的抓痒次数减少,而L-NAME和7-NI可增强槲皮素亚有效剂量的止痒作用。因此,我们的研究表明,急性注射槲皮素可以显著减少氯喹引起的抓痕行为,这种作用部分是通过抑制神经元一氧化氮合酶来介导的。
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引用次数: 0
University Pharmacy: from the foundation to the Pandemic times of Covid-19 大学药学:从建校到新冠肺炎大流行时期
IF 1.3 4区 医学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-04-28 DOI: 10.1590/s2175-97902023e21425
E. Ricci-Júnior, Denise A. Garofalo,, Maria Amélia Geraldes Bordalo Mont´Alverne, Melanie Tavares, Márcia Maria Barros dos Passos, Z. Freitas, E. P. Santos, M. Monteiro
Abstract The University Pharmacy Program (FU), from the Federal University of Rio de Janeiro (UFRJ), was created based on the need to offer a curricular internship to students of the Undergraduate Course at the Faculty of Pharmacy. Currently, it is responsible for the care of about 200 patients/day, offering vacancies for curricular internships for students in the Pharmacy course, it has become a reference in the manipulation of many drugs neglected by the pharmaceutical industry and provides access to medicines for low-income users playing an important social function. Research is one of the pillars of FU-UFRJ and several master and doctoral students use the FU research laboratory in the development of dissertations and theses. As of 2002, the Pharmaceutical Care extension projects started to guarantee a rational and safe pharmacotherapy for the medicine users. From its beginning in 1982 until the current quarantine due to the COVID-19 pandemic, FU-UFRJ has been adapting to the new reality and continued to provide patient care services, maintaining its teaching, research, and extension activities. The FU plays a relevant social role in guaranteeing the low-income population access to special and neglected medicines, and to pharmaceutical and education services in health promotion.
里约热内卢联邦大学(UFRJ)的大学药学项目(FU)是基于为药学院本科学生提供课程实习的需要而创建的。目前,每天负责照顾约200名患者,为药学课程的学生提供课程实习的空缺,成为制药行业忽视的许多药物操纵的参考,并为低收入用户提供药品,发挥着重要的社会功能。研究是复旦大学- ufrj的支柱之一,许多硕士生和博士生利用复旦大学的研究实验室进行学位论文和论文的开发。2002年开始实施“药学服务推广工程”,为广大患者提供合理、安全的药物治疗。从1982年建校到目前因新冠肺炎疫情而实行隔离,复旦大学附属医院一直适应新的现实,继续提供病人护理服务,保持教学、研究和推广活动。妇联在保障低收入人口获得特殊药品和被忽视药品以及获得促进健康方面的医药和教育服务方面发挥着相关的社会作用。
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引用次数: 0
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Brazilian Journal of Pharmaceutical Sciences
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