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Technological Innovation in Pharmaceutical Research Vol. 10最新文献

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Study on Anti-Diabetic effects of [10]-Gingerol in Streptozotocin and High-Fat Diet-Induced Diabetic Rats [10]-姜辣素对链脲佐菌素和高脂饮食诱导的糖尿病大鼠的抗糖尿病作用研究
Pub Date : 2021-08-03 DOI: 10.9734/bpi/tipr/v10/2516f
Ashutosh Yadav, Reetu, A. Garg
This experimental studies showed that its active components [10]-gingerol exert anti-diabetic effects against streptozotocin (STZ) and high-fat-diet (HFD) -induced diabetic rats. The occurrence of type 2 diabetes mellitus is rapidly rising around the world’s population. India is the ‘diabetes capital of the world’ with 62.4 million Indians having type 2 diabetes. The current treatment for type 2 diabetes includes insulin and oral hypoglycemic drugs i.e. sulfonylurea derivatives, thiazolidinediones, biguanides and (alpha)-glucosidase inhibitors but these medications have most of the side effects. Wistar rats (150-200 g) were group housed (n=6) under a standard 12 h light/dark cycle and controlled conditions of temperature and humidity (25±2°C, 55–65%). The histopathological illustration showed normal acini and normal cellular population in the islets of Langerhans in the pancreas of vehicle-treated rats. Our study suggested that [10]-gingerol dose-dependently produced antidiabetic activity. In this study might be helpful to understand the role of [10]-gingerol in the clinical treatment of diabetes mellitus.
本实验研究表明,其有效成分[10]-姜辣素对链脲佐菌素(STZ)和高脂饮食(HFD)诱导的糖尿病大鼠具有抗糖尿病作用。2型糖尿病的发病率在世界范围内迅速上升。印度是“世界糖尿病之都”,有6240万印度人患有2型糖尿病。目前2型糖尿病的治疗包括胰岛素和口服降糖药,即磺脲类衍生物、噻唑烷二酮类、双胍类和(alpha) -葡萄糖苷酶抑制剂,但这些药物的副作用最多。Wistar大鼠(150 ~ 200 g)分组饲养(n=6),标准明暗循环12 h,温湿度控制条件(25±2℃,55 ~ 65℃)%). The histopathological illustration showed normal acini and normal cellular population in the islets of Langerhans in the pancreas of vehicle-treated rats. Our study suggested that [10]-gingerol dose-dependently produced antidiabetic activity. In this study might be helpful to understand the role of [10]-gingerol in the clinical treatment of diabetes mellitus.
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引用次数: 0
Evaluation of Methanolic Leaf Extract of Parkia biglobosa (African locust bean, Jacg, Benth) Leaves against Trypanosoma evansi 刺槐叶甲醇提取物对伊氏锥虫的防治效果评价
Pub Date : 2021-08-03 DOI: 10.9734/bpi/tipr/v10/7218d-2
P. Shaba, N. P. Kurade, V. Bhanupraksah, R. Singh
In our ongoing research to determine the presence of antitrypanosomal compound(s) from medicinal plant, leaves of Parkia biglobosa were extracted with methanolic solvent at concentrations (250-1000 µg ml-1). Methanolic plant extract (MPE) obtained was tested against Trypanosoma evansi for trypanocidal activity. This was performed on Vero cells grown in Dulbecco's Modified Eagle Medium (DMEM) and supplemented with foetal calf serum (FCS) 20-40% at appropriate conditions. In vitro cytotoxicity test of P. biglobosa methanolic leaf extract at concentrations (1.56-100 µg ml-1) was done on Vero cells but without FCS. In vitro trypanocidal activity varied from immobilization, reduction and to the killing of trypanosomes in corresponding ELISA plate wells. At 250 µg ml-1of MPE of P. biglobosa, there was drastic reduction of average mean trypanosomes count in the extract (40.±0.0 to 7.000±0.33) as observed. At 500 µg ml-1 of the test extract of P. biglobosa, there was complete killing of trypanosomes (40.±0.0 to 0.00±0.00) at 9 h of incubation, which was statistically the same as diminazine aceturate (50 µg ml-1) at 4 h. Trypanosomes counts decreased in concentration and time –dependent manner with significant difference (P (le) 0.05 to 0. 01)). MPE of P, biglobosa and diminazine aceturate, standard drug, were cytotoxic to Vero cells except at concentrations of 12.5- 1.56 µg ml-1. Alkaloids, flavonoids, anthraquinones, tannins, phlobotannins and cardiac glycoside already isolated from P. biglobosa leaves and other parts of it could be responsible for higher antitrypanosmal activity.
在我们正在进行的研究中,以确定药用植物中抗锥虫化合物的存在,用甲醇溶剂(250-1000µg ml-1)提取了大叶Parkia biglobosa的叶子。研究了甲醇植物提取物(MPE)对伊文氏锥虫的杀虫活性。这是在Dulbecco's Modified Eagle培养基(DMEM)中生长的Vero细胞上进行的,并添加了胎牛血清(FCS) 20-40% at appropriate conditions. In vitro cytotoxicity test of P. biglobosa methanolic leaf extract at concentrations (1.56-100 µg ml-1) was done on Vero cells but without FCS. In vitro trypanocidal activity varied from immobilization, reduction and to the killing of trypanosomes in corresponding ELISA plate wells. At 250 µg ml-1of MPE of P. biglobosa, there was drastic reduction of average mean trypanosomes count in the extract (40.±0.0 to 7.000±0.33) as observed. At 500 µg ml-1 of the test extract of P. biglobosa, there was complete killing of trypanosomes (40.±0.0 to 0.00±0.00) at 9 h of incubation, which was statistically the same as diminazine aceturate (50 µg ml-1) at 4 h. Trypanosomes counts decreased in concentration and time –dependent manner with significant difference (P (le) 0.05 to 0. 01)). MPE of P, biglobosa and diminazine aceturate, standard drug, were cytotoxic to Vero cells except at concentrations of 12.5- 1.56 µg ml-1. Alkaloids, flavonoids, anthraquinones, tannins, phlobotannins and cardiac glycoside already isolated from P. biglobosa leaves and other parts of it could be responsible for higher antitrypanosmal activity.
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引用次数: 0
Investigating the Trypanocidal Activity of Purified Precocene I by Reverse-Phase High-Performance Liquid Chromatography from Essential Oil of Ageratum houstonianum Aerial Parts 用反相高效液相色谱法研究鹰爪草挥发油中纯化的早熟素I的杀锥虫活性
Pub Date : 2021-08-03 DOI: 10.9734/bpi/tipr/v10/7218d-3
P. Shaba, N. Pandey, O. Sharma, N. Pandy, J. Rao, S. Dey, B. Mandal, N. P. Kurade, R. Singh, V. Bhanuprakash, P. Chaudary
Ageratum houstonianum leaves are a common poisonous weeds found on the vast valley of Kangra in Palampur, Himachal Pradesh State, India. Freshly harvested leaves sample of Ageratum houstonionum were dried under shade and powdered. Leaf sample of A. houstonionum was extracted by process of hydrodistillation using a Clevenger-type apparatus for the preparation of essential oil. Extract from A. houstonianum was prepared by dissolving 5 µL of the essential oil in 10 mL methanol. All the sample was filtered through a Whatman (Maidstone, England) stainless steel syringe assembly using a 0.22 µm Durapore (Millipore: Milford, USA) membrane filter. Purification processes via column chromatography, thin layer chromatography and preparative thin layer chromatography were done. Reverse phase HPLC analysis was carried out via a Waters HPLC system consisting of model 510 and 515 pumps, a Rheodyne injector, a Novapak C18 column (250 x 4.6 mm i.d.; 4 µm), a model 490E multi-channel detector and Millennium 2010 sata manager. The mobile phase constituents were filtered using a Durapore 0.22 µm membrane filter. The elution was carried out with a linear gradient of acetonitrile: water (40:60) to pure acetonitrile in 60 min at a flow rate of 1 mL/min. detection was at 210, 240, 280 and 320 nm. The precocene was eluted within 25 min, the peak areas showed good reproducibility (average relative standard deviation were 0.78%), and the calibration curves (i.e. mass of precocene standard injected vs. peak area detected at 210 nm) were linear over the range of 0.05-10 µg (for precocene I, y = 6654454 x + 176626, r2 = 0.99 and for precocene II, y = 4618457 x + 133472, r2 = 0.99). Standard sample containing precocene I (1 mg/mL) and precocene II (1 mg/mL) obtained from Sigma (St Louis, MO, USA) were prepared in methanol. Identified precocene I was screened against Trypanosoma evansi for trypanocidal activity on Vero cells grown in Dulbecco's Modified Eagle Medium (DMEM) and supplemented with foetal calf serum (FCS) 20-40% at appropriate conditions. In vitro cytotoxicity test of precocene I at concentrations (1.56-100 µg ml-1) was done on Vero cells but without FCS. In vitro trypanocidal activity varied from immobilization, reduction and to the killing of trypanosomes in corresponding ELISA plate wells. At 250 µg ml-1of purified precocene I, there was drastic reduction of average mean trypanosomes count to complete killing of trypanosomes (40.±0.0 to 0.00±0.00) at 9 h of incubation, which was statistically the same as diminazine aceturate (50 µg ml-1) at 4 h. Trypanosomes counts decreased in concentration and time –dependent manner with significant difference (P (le) 0.05 to 0. 01)). During in vitro cytotoxicity test, Purified precocene I and diminazine aceturate standard drug, were cytotoxic to Vero cells at all concentrations except at concentrations of 6.25-1.56 µg ml-1 and 1.56 µg ml-1, respectively. Precocene I was responsible for higher anti-trypanosomal activity. Preco
在印度喜马偕尔邦的Palampur, Ageratum houstonianum的叶子是一种常见的毒草。将刚采收的灰隼叶样品在阴凉处晒干,制成粉末。采用Clevenger-type装置,采用加氢蒸馏法提取胡芦巴叶样品。取5µL精油,用10 mL甲醇溶解制得冬冬提取物。所有样品通过Whatman (Maidstone, England)不锈钢注射器组件,使用0.22µm Durapore (Millipore: Milford, USA)膜过滤器过滤。采用柱层析、薄层析和制备薄层析进行纯化。反相HPLC分析通过Waters HPLC系统进行,该系统由510型和515型泵,Rheodyne进样器,Novapak C18色谱柱(250 x 4.6 mm id;4µm),型号490E多通道检测器和Millennium 2010 sata管理器。流动相成分采用Durapore 0.22µm膜过滤器过滤。以乙腈:水(40:60)线性梯度洗脱至纯乙腈,洗脱时间为60 min,流速为1ml /min。检测波长分别为210、240、280、320 nm。在25 min内洗脱,峰面积重现性好(平均相对标准偏差为0.78)%), and the calibration curves (i.e. mass of precocene standard injected vs. peak area detected at 210 nm) were linear over the range of 0.05-10 µg (for precocene I, y = 6654454 x + 176626, r2 = 0.99 and for precocene II, y = 4618457 x + 133472, r2 = 0.99). Standard sample containing precocene I (1 mg/mL) and precocene II (1 mg/mL) obtained from Sigma (St Louis, MO, USA) were prepared in methanol. Identified precocene I was screened against Trypanosoma evansi for trypanocidal activity on Vero cells grown in Dulbecco's Modified Eagle Medium (DMEM) and supplemented with foetal calf serum (FCS) 20-40% at appropriate conditions. In vitro cytotoxicity test of precocene I at concentrations (1.56-100 µg ml-1) was done on Vero cells but without FCS. In vitro trypanocidal activity varied from immobilization, reduction and to the killing of trypanosomes in corresponding ELISA plate wells. At 250 µg ml-1of purified precocene I, there was drastic reduction of average mean trypanosomes count to complete killing of trypanosomes (40.±0.0 to 0.00±0.00) at 9 h of incubation, which was statistically the same as diminazine aceturate (50 µg ml-1) at 4 h. Trypanosomes counts decreased in concentration and time –dependent manner with significant difference (P (le) 0.05 to 0. 01)). During in vitro cytotoxicity test, Purified precocene I and diminazine aceturate standard drug, were cytotoxic to Vero cells at all concentrations except at concentrations of 6.25-1.56 µg ml-1 and 1.56 µg ml-1, respectively. Precocene I was responsible for higher anti-trypanosomal activity. Precocene I could be near future trypanocidal compound for a new trypanocide. To attest its full and firm trypanocidal activity potential, in vivo test need to be conducted alongside the in vitro method.
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引用次数: 1
An Observational Study on Intensive Care Unit Prophylaxis and Its Outcome in a Rural Tertiary Care Hospital 某农村三级医院重症监护病房预防及其结果的观察性研究
Pub Date : 2021-08-03 DOI: 10.9734/bpi/tipr/v10/2907f
P. Ananth, Surendra Kumar Bouddh
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引用次数: 0
Impairment in Acetylcholinesterase Activity in Different Brain Parts of Female Mice, Mus musculus Following 17 α-Methyltestosterone (Anabolic- Androgenic Steroid) 17 α-甲基睾酮(合成代谢雄激素)对雌性小家鼠不同脑区乙酰胆碱酯酶活性的影响
Pub Date : 2021-08-03 DOI: 10.9734/bpi/tipr/v10/9888d
Sachin Patil, Praveenkumar Kondaguli, L. S. Inamdar
Objective: Anabolic androgenic steroids (AAS) are synthetic derivatives of the male sex hormone testosterone. In the present investigation, we studied the impact of one of the AAS compounds 17(alpha)-methyltestosterone on acethylcholinesterase (AChE) enzyme activity in different parts of mice brain viz. forebrain, hippocampus, midbrain, and hindbrain. Methods: The adult female mice were assigned to four experimental groups to which different doses of 17(alpha)-Methyltestosterone (17(alpha)-MT- 0.5, 5.0 and 7.5 mg/kg bwt, respectively) were administrated s.c. for 30 days. Results: A significant increase in AChE activity in forebrain and midbrain (low and medium dose treatment) suggests a reduction of cholinergic neurotransmission efficiency due to a decrease in acetylcholine levels in the trans-synaptic cleft. Further, a concurrent reduction in AChE activity was observed in the whole brain, hippocampus and hindbrain of 17(alpha)-MT treated mice suggest the impairment in neuronal transmission. Since the regulation of cholinergic system through acetylcholine hydrolysis has been largely attributed to AChE activity, a significant reduction in its activity may lead to stress-related anxiety, memory loss with some cognitive and behavioral aspects in the mice. Conclusion: Based on the observed results we propose that 17(alpha)-MT an alkylated steroid compound has a negative impact on AChE enzyme activity in different parts of mice brain leading to impairment in neuronal transmission.
目的:合成代谢雄激素类固醇(AAS)是雄性激素睾酮的合成衍生物。本实验研究了一种AAS化合物17 (alpha) -甲基睾酮对小鼠前脑、海马、中脑和后脑不同部位乙酰胆碱酯酶(AChE)活性的影响。方法:将成年雌性小鼠分为4个实验组,分别给予不同剂量的17 (alpha) -甲基睾酮(17 (alpha) - mt - 0.5、5.0和7.5 mg/kg bwt),连续30 d。结果:前脑和中脑(低、中剂量治疗)乙酰胆碱酯酶活性显著增加,表明胆碱能神经传递效率降低,这是由于突触间隙中乙酰胆碱水平降低所致。此外,17只(alpha) -MT处理小鼠全脑、海马和后脑同时观察到AChE活性降低,提示神经元传递受损。由于乙酰胆碱水解对胆碱能系统的调节在很大程度上归因于乙酰胆碱酯酶的活性,乙酰胆碱酯酶活性的显著降低可能导致小鼠出现与压力相关的焦虑、认知和行为方面的记忆丧失。结论:基于观察结果,我们提出烷基化类固醇化合物17 (alpha) -MT对小鼠脑不同部位乙酰胆碱酯酶活性有负面影响,导致神经元传递受损。
{"title":"Impairment in Acetylcholinesterase Activity in Different Brain Parts of Female Mice, Mus musculus Following 17 α-Methyltestosterone (Anabolic- Androgenic Steroid)","authors":"Sachin Patil, Praveenkumar Kondaguli, L. S. Inamdar","doi":"10.9734/bpi/tipr/v10/9888d","DOIUrl":"https://doi.org/10.9734/bpi/tipr/v10/9888d","url":null,"abstract":"Objective: Anabolic androgenic steroids (AAS) are synthetic derivatives of the male sex hormone testosterone. In the present investigation, we studied the impact of one of the AAS compounds 17(alpha)-methyltestosterone on acethylcholinesterase (AChE) enzyme activity in different parts of mice brain viz. forebrain, hippocampus, midbrain, and hindbrain. \u0000Methods: The adult female mice were assigned to four experimental groups to which different doses of 17(alpha)-Methyltestosterone (17(alpha)-MT- 0.5, 5.0 and 7.5 mg/kg bwt, respectively) were administrated s.c. for 30 days. \u0000Results: A significant increase in AChE activity in forebrain and midbrain (low and medium dose treatment) suggests a reduction of cholinergic neurotransmission efficiency due to a decrease in acetylcholine levels in the trans-synaptic cleft. Further, a concurrent reduction in AChE activity was observed in the whole brain, hippocampus and hindbrain of 17(alpha)-MT treated mice suggest the impairment in neuronal transmission. Since the regulation of cholinergic system through acetylcholine hydrolysis has been largely attributed to AChE activity, a significant reduction in its activity may lead to stress-related anxiety, memory loss with some cognitive and behavioral aspects in the mice. \u0000Conclusion: Based on the observed results we propose that 17(alpha)-MT an alkylated steroid compound has a negative impact on AChE enzyme activity in different parts of mice brain leading to impairment in neuronal transmission.","PeriodicalId":22326,"journal":{"name":"Technological Innovation in Pharmaceutical Research Vol. 10","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78448473","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: 0
Study on Preparation and Optimization of Fast Dissolving HPMC/PVA Blended films of Loperamide Hydrochloride 盐酸洛哌丁胺HPMC/PVA速溶共混膜的制备及优化研究
Pub Date : 2021-08-03 DOI: 10.9734/bpi/tipr/v10/11504d
P. Patil, V. Jadhav, Rasika Rane, Amruta V. Shelar, Sainath S. Nair, Aniruddha Gurchal, Sujay Kanitkar
Since discovering new chemical entities is a complex, expensive, and time-consuming process, current trends have shifted toward designing and developing improved drug delivery methods for existing drugs. Recent times, fast dissolving oral films were introduced to the market, attracting the attention of a large number of pharmaceutical companies due to their numerous advantages over other oral dosage forms, including ease of administration, better patient compliance, rapid drug absorption, and rapid onset of action with instant bioavailability. Aside from these advantages, quick dissolving oral films can be employed in children, the geriatric, and bedridden patients who have difficulties swallowing tablets or capsules. Initially, fast-dissolving oral films of breath strips, confectionary, and oral care treatments were developed, but it has now evolved into an innovative and widely accepted technique for delivering both OTC and prescription drugs.  Fast dissolving films are gaining interest as an alternative to fast dissolving tablets. The films are designed to disintegrate in a matter of seconds when they come into touch with a wet surface, such as the tongue, allowing the user to eat the food without the need for extra liquid. This ease of use gives a marketing benefit as well as greater patient compliance. Since the medicine is absorbed straight into the systemic circulation, it avoids gastrointestinal degradation and the first-pass impact.Solvent casting is used to make the Loperamide hydrochloride mouth dissolving film. The ingredient used for formulation Loperamide hydrochloride as a Anti-Diarrheal, HPMC-E50, HPMC-E15-LV and PVA as film forming polymer, propylene glycol as a plasticizer, Sodium starch glycolate (2-8%) as super disintegrant, lemon oil (2-5%) as a flavoring agent, citric acid (2-6%) as a Saliva Stimulating Agent, methylparaben (0.015%) as a preservative. Tensile strength, disintegration time, and percentage drug dissolution were chosen as independent variables, whereas tensile strength, disintegration time, and percentage drug dissolution were chosen as response variables. Mass uniformity, thickness, percent drug content, folding endurance, surface pH, moisture uptake, % swelling, percentage elongation, tensile strength, in vitro disintegration time, and in vitro percentage drug dissolution were all considered when evaluating the formulations. Loperamide was discovered to be a viable candidate for development of Fast Mouth Dissolving Films. The solvent casting procedure used to create Loperamide oral films is simple and cost-effective. It was deemed acceptable by the super disintegrants who were used in this study. FT-IR tests of drug-excipient compatibility indicated no physicochemical interaction. The obtained oral films were clear, had sufficient physical strength, and had a suitable disintegration time. In vitro dissolution experiments of all formulations revealed a superior release profile than pure medicines.Based on the
由于发现新的化学实体是一个复杂、昂贵和耗时的过程,目前的趋势已经转向为现有药物设计和开发改进的给药方法。近年来,速溶口服膜被引入市场,吸引了大量制药公司的注意,因为它比其他口服剂型有许多优点,包括易于给药、更好的患者依从性、快速的药物吸收、快速起效和即时的生物利用度。除了这些优点外,快速溶解的口服薄膜还可用于吞咽片剂或胶囊有困难的儿童、老年人和卧床不起的患者。最初,快速溶解的口腔薄膜呼吸条,糖果和口腔护理治疗被开发出来,但它现在已经发展成为一种创新和广泛接受的技术,用于输送非处方药和处方药。快速溶解薄膜作为快速溶解片剂的替代品正引起人们的兴趣。这种薄膜的设计初衷是,当它们接触到潮湿的表面(比如舌头)时,几秒钟内就会分解,这样使用者就可以在不需要额外液体的情况下吃下食物。这种易用性为市场营销带来了好处,并提高了患者的依从性。由于药物被直接吸收进入体循环,它避免了胃肠道降解和第一次影响。采用溶剂铸造法制备盐酸洛哌丁胺口腔溶膜。盐酸洛哌丁胺抗腹泻剂,HPMC-E50, HPMC-E15-LV和PVA成膜聚合物,丙二醇作为增塑剂,乙醇酸淀粉钠(2-8%)作为超级崩解剂,柠檬油(2-5%)作为调味剂,柠檬酸(2-6%)作为唾液刺激剂,对羟基苯甲酸甲酯(0.015%)作为防腐剂。以抗拉强度、崩解时间和药物溶出度百分比为自变量,以抗拉强度、崩解时间和药物溶出度百分比为响应变量。质量均匀性、厚度、药物含量百分比、折叠耐力、表面pH、吸湿率、溶胀率、伸长率、抗拉强度、体外崩解时间、体外药物溶出率是评价制剂的主要因素。洛哌丁胺被发现是开发快速口溶膜的可行候选物。溶剂铸造工艺用于制造洛哌丁胺口服薄膜是简单和经济有效的。在这项研究中使用的超级崩解剂认为这是可以接受的。傅里叶变换红外光谱测试显示药物与赋形剂的相容性没有物理化学相互作用。所制得的口腔膜透明,具有足够的物理强度,崩解时间合适。所有制剂的体外溶出度实验均显示出优于纯药物的释放谱。根据试验结果,确定含HPMC E15和PVA成膜剂的F7成膜剂为最佳配方。
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引用次数: 1
期刊
Technological Innovation in Pharmaceutical Research Vol. 10
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