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A REVIEW ON AN EMERGIN TREND BILAYER FLOATING DRUG DELIVERY SYSTEM 新型双层漂浮给药系统的研究进展
Pub Date : 2021-07-08 DOI: 10.24092/crps.2021.110201
Anjali Chourasiya, Narendra Gehalot, S. Mahajan
NDDS is advanced drug delivery system which improves drug potency, control drug release to give a sustained therapeutic effect, provide greater safety, finally it is to target a drug specifically to a desired tissue. Novel drug delivery system have been developed to overcome the limitation of conventional drug delivery systems, such as of gastric retention by decreasing fluctuations in the concentration of the drug in blood,resulting in the reduction in unwanted toxicity and poor efficiency. As compared to traditional dosage forms bilayer tablets are more efficient for sequential release of two drugs that can be different or identical. Bilayer tablet is also capable of separating two incompatible substances and also for sustained release. Gastro retentive drug delivery system retains the period of dosage forms in the stomach or upper gastro intes-tinal tract ,as to improve bioavailability and the therapeutic efficacy of the drugs. Mainly the bilayer drug delivery system is suitable for drugs whose therapethic windows are narrow in the gastrointestinal tract (GIT) and also they have low elimination half life: 3-4 h. The purpose of this review is to disclose the challenges faced during the formulation of bilayer tablets. Finally, the whole article is firmly analyzed in a concluding paragraph. KEYWORDS: Conventional drug delivery systems, Bilayer tablet, Gastro retentive, Bioavailability
NDDS是一种先进的药物给药系统,它可以提高药物的效力,控制药物的释放,以获得持续的治疗效果,提供更大的安全性,最后是将药物特异性地靶向到所需的组织。新型给药系统的开发是为了克服传统给药系统的局限性,如胃潴留,通过减少药物在血液中的浓度波动,从而减少不必要的毒性和低效率。与传统剂型相比,双层片剂对于两种不同或相同的药物的顺序释放更有效。双层片剂还具有分离两种不相容物质和缓释作用。胃保留给药系统在胃或上消化道中保留剂型的时间,以提高药物的生物利用度和治疗效果。双层给药系统主要适用于胃肠道治疗窗口较窄且消除半衰期较低的药物(3-4小时)。本文的目的是揭示双层给药系统在制备过程中面临的挑战。最后,在结束语中对整篇文章进行了有力的分析。关键词:常规给药系统,双层片剂,胃保留剂,生物利用度
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引用次数: 0
Synthesis, Characterization and Antimicrobial Evaluation of some 1,2,4-Triazolo-5-Thione Derivatives 1,2,4-三唑-5-硫酮衍生物的合成、表征及抗菌性能评价
Pub Date : 2021-05-10 DOI: 10.24092/CRPS.2021.110103
Gurdeep Singh, N. Jain, K. Sahu
Due to this increasing predicament of antibiotic confrontation, the lot of distinct antibiotics available is dwindling and there are only smatterings of new antibiotics in the drug development channel. Therefore, an intense necessitate for new antimicrobial drugs. In current study, substituted 1,2,4-triazolo-5-thione derivatives were synthesized from substituted aromatic aldehydes, succinic acids and the structure of synthesized compounds were established by physicochemical (Melting Point, Rf value) and spectral analysis (IR, NMR & Mass). The title compounds were then evaluated for their antimicrobial activity against ciprofloxacin as a standard drug using agar plate method. Among all synthesized derivatives A5 and A6 found were found to possess very promising antimicrobial activity. Keywords: 1,2,4-triazolo-5-thione, anti-microbial, antibiotic, thione, Ciprofloxacin.
由于抗生素对抗的困境日益加剧,可用的独特抗生素数量正在减少,药物开发渠道中只有少数新抗生素。因此,迫切需要开发新的抗菌药物。本研究以取代的芳香醛、琥珀酸为原料合成了取代的1,2,4-三唑-5-硫酮衍生物,并通过理化分析(熔点、Rf值)和光谱分析(IR、NMR和Mass)确定了合成化合物的结构。然后用琼脂平板法评价标题化合物对环丙沙星作为标准药物的抗菌活性。在所有已合成的衍生物中,发现A5和A6具有很好的抗菌活性。关键词:1,2,4-三唑-5-硫酮,抗菌药物,抗生素,硫酮,环丙沙星
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引用次数: 0
Formulation and Evaluation of Curcumin Loaded Nanoliposome on Brain Targeted 脑靶向姜黄素纳米脂质体的制备与评价
Pub Date : 2021-05-10 DOI: 10.24092/CRPS.2021.110104
J. Kumari, Lovely Chaurasia
The present work aimed to produce Curcumin based nanoliposomes that nanoliposome can target the site via the brain in a controlled manner. Nanoliposomes are important in controlling the carriage; Curcumin which is an active constituent of curcuminoids thus also provides an effective treatment for the central nervous system and plays a crucial role. The interaction of the drug was ruled out by FT-IR studies and no incompatibility and lipids and surfactant. To optimize the formulation, factors affecting the physical appearance of Nanoliposomes were investigated. Curcumin-loaded Nanoliposomes were formulated using cholesterol by physical dispersion method and characterized for particle size, drug content, stability, production yield. Prepared nanoliposomes gave the better physical, morphological concerning the concentration of the lipids, surfactant, and ratio of lipid and surfactant. Six different formulations of Nanoliposomes F1-F6 were formulated to obtain the optimized formulation. The TEM (Transmission Electron Microscopy) of Nanoliposomes showed that they were rounded in shape and porous in texture. In-vitro drug release of formulation indicates that formulation F6 was selected as an optimized formulation for incorporation into the nanoliposomes among all the six formulations and liposome showed drug release in a controlled manner at the end of 10 hours. Keywords: Curcumin, Nanoliposomes, Physical Dispersion Method, Brain Targeting, Blood-Brain Barrier, Cholesterol, Bioavailability, In vitro Release.
目前的工作旨在生产基于姜黄素的纳米脂质体,纳米脂质体可以通过大脑以可控的方式靶向该部位。纳米脂质体在控制运输中起重要作用;姜黄素是姜黄素类的一种活性成分,对中枢神经系统也有有效的治疗作用,起着至关重要的作用。FT-IR研究排除了药物的相互作用,也没有脂质和表面活性剂的不相容性。为了优化配方,研究了影响纳米脂质体物理外观的因素。以胆固醇为原料,采用物理分散法制备了载姜黄素纳米脂质体,并对其粒径、药物含量、稳定性和产率进行了表征。制备的纳米脂质体在脂质浓度、表面活性剂浓度、脂质与表面活性剂的比例等方面表现出较好的物理形态特征。对F1-F6纳米脂质体进行了6种不同配方的配制,得到了最佳配方。纳米脂质体的透射电镜(TEM)分析表明,纳米脂质体呈圆形,具有多孔结构。体外释药结果表明,6个剂型中选择F6为纳米脂质体入药的最佳剂型,10小时后脂质体释药可控。关键词:姜黄素,纳米脂质体,物理分散法,脑靶向,血脑屏障,胆固醇,生物利用度,体外释放
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引用次数: 0
A brief Overview of a Fatal Disease Namely Cancer 一种致命疾病即癌症的简要概述
Pub Date : 2021-04-08 DOI: 10.24092/CRPS.2021.110102
Himanshu, Pradumn Kumar Maddheshiya, Mukesh Kumar
In today era cancer is a dangerous and terrible disease which cause due to rapid increment of unusual cells within the body. Cancer is the second influential cause of death in the world. It has become very difficult overcome cancerous disease. 10 million people died per year from cancer. The major cause of cancer is sudden change in DNA within the cells. As a result normal cells convert into cancerous cells which enhance the process of metastasis. There are some treatments of this dangerous disease but cancer treatments are so expensive not everyone and the common man can get. So, it’s our responsibility to spread awareness and convince people about such a disease. Its simple purpose is that after reading people should know more about it. And whatever, things are follow in our daily life to avoid cancer disease. Keywords: Neoplasm, Carcinoma, Leukemia, Chemotherapy, Radiation therapy.
在当今时代,癌症是一种危险而可怕的疾病,是由于体内异常细胞的快速增加而引起的。癌症是世界上影响最大的第二大死因。战胜癌症已经变得非常困难。每年有1000万人死于癌症。癌症的主要原因是细胞内DNA的突然变化。结果,正常细胞转化为癌细胞,从而加快了转移的过程。这种危险的疾病有一些治疗方法,但癌症治疗太昂贵了,不是每个人都能得到。所以,我们有责任传播意识,让人们相信这种疾病。它的目的很简单,那就是人们在阅读之后应该对它有更多的了解。无论如何,在我们的日常生活中要遵循以下几点来避免癌症。关键词:肿瘤,癌,白血病,化疗,放疗
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引用次数: 0
FORMULATION, DEVELOPMENT AND CHARACTERIZATION OF EFFECTIVE NIOSOMAL DRUG DELIVERY SYSTEM FOR THE TREATMENT OF DIABETES MELLITUS 治疗糖尿病的有效niosomal给药系统的研制与表征
Pub Date : 2020-12-31 DOI: 10.24092/crps.2020.100402
Nida Musheer, Vikrant Gupta
In the present study, gliclazide-loaded niosomes are formulated and evaluated for their in vitro as well as in vivo characteristic in an attempt to improve the oral bioavailability of the drug. Formulation of niosomes was optimized for highest percentage of drug entrapment. Microscopic observation confirmed that all particles were uniform in size and shape. The entrapment efficiency was determined by separating the unentrapped drug using dialysis. The in vitro release studies of drug from niosomes exhibited a prolonged drug release as observed over a period of 24 h. The positive values of zeta potential indicated that the gliclazide niosomes were stabilized by electrostatic repulsive forces. Results from stability study have shown that the drug leakage from the vesicles was least at 4ºC followed by 25 and 37ºC. The niosomes showing maximum entrapment and suitable release rate were selected for in vivo evaluation. In conclusion, the niosomal formulation could be a promising delivery system for gliclazide with improved bioavailability and prolonged drug release profile. KEYWORDS: Heme Oxygenase Inhibitor, HO-1, 2D QSAR, 3D QSAR, kNN-MFA
在本研究中,为了提高药物的口服生物利用度,我们制定了格列齐特负载niosomes,并对其体外和体内特性进行了评估。以药物包封率最高为目标,优化了乳质体的配方。显微镜观察证实,所有的颗粒在大小和形状上都是均匀的。通过透析分离未包裹的药物来确定包裹效率。体外药物释放研究显示,在24小时的时间内,药物释放时间较长。zeta电位的阳性表明,格列齐特乳小体在静电斥力的作用下是稳定的。稳定性研究结果表明,药物在4℃时渗漏最少,其次是25℃和37℃。选择具有最大包裹度和合适释放率的乳质体进行体内评价。综上所述,niosomal制剂具有提高格列齐特生物利用度和延长药物释放时间的优点,是一种很有前景的给药系统。关键词:血红素加氧酶抑制剂,HO-1, 2D QSAR, 3D QSAR, kNN-MFA
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引用次数: 0
FORMULATION AND DEVELOPMENT OF BILAYER FLOATING TABLET OF AMOXICILLIN 阿莫西林双层漂浮片的研制
Pub Date : 2020-12-31 DOI: 10.24092/crps.2020.100403
Priyanka Jartolia, S. Kondalkar, A. Kondalkar, Muraree Lal
Bilayer floating tablet of amoxicillin was formulated successfully and evaluated under suitable parameters. All the batches of tablet produced were found to exhibit short floating lag times. The tablet of batch F2 exhibited a longer floating lag time of 23 minutes. Relationship between the dependent and independent variables was further elucidated using contour and response surface plots. Dissolution profiles that the tablets of batch F3, F7, and F12 exhibits initial burst phase during the first hour of dissolution. The burst phase was followed by a limited drug release for the rest of the period. Also it was observed during the dissolution studies that tablets of all three batches eroded quickly with increased effervescence. Time required for 50 % drug to get released (T50%) and %CR10hrs were found to be in the range of 0.7 to 8.6 hours and 57.35 ± 3.89 to 99.93 ± 0.07 respectively, value of “Prob > F” less than 0. 05. Response surface plots and Contour plot indicated that at a fixed level of B (35 mg) and low level of A (amount of HPMC), % CR10hrs increases from 68.11 to 90.00 % and T50% decrease from 6.86 to 1.66 as the amount of citric acid (C) increases from 0 to 10 mg. Stability study was performed for optimized formulation and it was found that formulation was stable for 6 week at 25 °C/ 60% RH. KEYWORDS: Bilayer floating tablet, amoxicillin, Evaluated, Multi-layered tablet, Stability
成功研制了阿莫西林双层漂浮片,并在适宜的工艺参数下进行了评价。生产的所有批次的片剂均出现较短的漂浮滞后时间。F2批次片剂的漂浮滞后时间较长,为23分钟。利用等高线图和响应面图进一步阐明了因变量和自变量之间的关系。溶出曲线显示F3、F7、F12批次片剂在溶出的第一个小时内呈现初始爆发阶段。爆发期之后的其余时间是有限的药物释放。在溶出度研究中还观察到,所有三批的片剂都被迅速侵蚀,起泡增加。50%药物释放所需时间(T50%)为0.7 ~ 8.6小时,%CR10hrs为57.35±3.89 ~ 99.93±0.07小时,“Prob > F”值均小于0。05. 响应面图和等高线图显示,在固定水平B (35 mg)和低水平a (HPMC用量)下,随着柠檬酸(C)用量从0 mg增加到10 mg, % CR10hrs从68.11%增加到90.00 %,T50%从6.86降低到1.66。对优化后的配方进行稳定性研究,结果表明,在25℃/ 60% RH条件下,该配方稳定6周。关键词:双层漂浮片,阿莫西林,评价,多层片,稳定性
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引用次数: 0
THE ROLE, SCOPE, HEALTH BENEFITS AND MARKET GROWTH OF NUTRACEUTICALS: AN OVERVIEW 营养保健品的作用、范围、健康效益和市场增长:概述
Pub Date : 2020-10-08 DOI: 10.24092/crps.2020.100301
Ramila Prajapati, Sanjeev Kumar
Nutraceuticals are products used as medicines in addition to nutrition. Nutraceuticals can be defined as substances that have physiological benefits or provide protection against chronic disease. Nutraceuticals can be used to improve health, slow down the aging process, prevent chronic diseases, increase life expectancy or support body structure or function. Nutraceuticals are getting a lot of attention these days because of their potential nutritional, safety and therapeutic benefits. Recent studies have shown that these compounds have promising results in various complications. In this review, we have made a great effort in proposing new concepts for nutraceuticals based on disease indications. Highlights herbal remedies that are effective for harsh therapeutic conditions associated with oxidative stress, including allergies, Alzheimer's disease, cardiovascular disease, cancer, diabetes, eye, immunity, inflammation, and Parkinson's disease and obesity. These nutraceuticals are used in various diseases, their application, and current market demand. Examples of fish oil preparations, prebiotics and probiotics reviewed. KEYWORDS: Nutraceutical, Dietary supplements, Antioxidants, Probiotics, Health benefits
营养品是除营养品外用作药物的产品。营养保健品可以定义为具有生理益处或提供预防慢性疾病的物质。营养保健品可用于改善健康,延缓衰老过程,预防慢性疾病,延长预期寿命或支持身体结构或功能。营养保健品由于其潜在的营养、安全性和治疗效益而受到广泛关注。最近的研究表明,这些化合物对各种并发症有很好的疗效。在这篇综述中,我们在提出基于疾病适应症的营养保健品的新概念方面做了很大的努力。重点介绍了对与氧化应激相关的恶劣治疗条件有效的草药疗法,包括过敏、阿尔茨海默病、心血管疾病、癌症、糖尿病、眼睛、免疫、炎症、帕金森病和肥胖。这些营养保健品用于各种疾病,它们的应用,以及目前的市场需求。综述了鱼油制剂、益生元和益生菌的实例。关键词:营养保健品,膳食补充剂,抗氧化剂,益生菌,健康益处
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引用次数: 0
EVALUATION OF ANTHELMINTIC ACTIVITY OF BAUHINIA VARIEGATA LINN METHANOLIC ROOT EXTRACT ON PHERETIMA POSTHUMA 紫荆花甲醇根提取物对后脑虫的驱虫活性评价
Pub Date : 2020-10-08 DOI: 10.24092/crps.2020.100302
A. Jain
Methanolic extracts from roots of Bauhinia variegata linn were investigated for their anthelmintic activity by using three concentrations (10, 25, & 50mg/ml) as test worms. Results were expressed in terms of time of paralysis and time of death of worms and the activity was compared with albendazole as reference standard & Normal saline served as control. Dose dependent decreased paralyzing time and death time was observed. The results of present study indicated that crude methanolic root extract significantly demonstrated paralysis and also caused death of worms especially at higher concentration of (50 mg/ml), Bauhinia variegata showed the best anthelmintic activity. The use of the roots as anthelmintic has been established and further studies are recommended to isolate the active principles answerable for the activity. KEYWORDS: Anthelmintic activity, Pheretima Posthuma, Bauhinia variegata linn
以紫荆根甲醇提取物为试虫,分别以10、25、50mg/ml为试虫浓度,对其驱虫活性进行了研究。以蠕虫麻痹时间和死亡时间表示结果,并与阿苯达唑为参比标准,生理盐水为对照进行活性比较。麻痹时间和死亡时间呈剂量依赖性缩短。结果表明,紫荆粗甲醇根提取物具有明显的麻痹性和致虫性作用,其中高浓度(50 mg/ml)紫荆的驱虫活性最强。根作为驱虫剂的用途已经确定,建议进一步研究以分离出导致活性的活性原理。关键词:驱虫活性,白花菊,紫荆花
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引用次数: 0
PHARMACOLOGICAL INVESTIGATIONS OF CYPERUS ROTUNDUS TUBER EXTRACT IN MONOSODIUM GLUTAMATE INDUCED EXPERIMENTAL ANIMAL 香附提取物对味精诱导实验动物的药理作用研究
Pub Date : 2020-04-08 DOI: 10.24092/crps.2020.100102
Munesh Kumar, M. Rani, B. Meher
Nowadays obesity is the major health problem due to food habit and life style of people. Nature and natural compounds possess lots of health benefits. To explore the therapeutic benefit of Cyperus rotundus in this work, we have evaluated the anti-obesity potential on Monosodium glutamate (MSG) induced obese rats. Methanolic extract of tubers of Cyperus rotundus was administered at the dose of 250 and 500 mg/kg/oral after 45 d of treatment and a significant improvement in body weight, organs and lipid profile was observed as compared with MSG induced obese rats. Nowadays obesity is a common metabolic disorder in developed and developing countries. It was observed that Cyperus rotundus tuber possesses anti-obesity potential and protective action on heart and liver.
由于人们的饮食习惯和生活方式,肥胖是当今主要的健康问题。自然和天然化合物对健康有很多好处。为了探索圆草的治疗作用,我们对味精诱导的肥胖大鼠进行了抗肥胖潜力的评价。给药45 d后,分别给药250和500 mg/kg/口服香附块茎甲醇提取物,与味精诱导的肥胖大鼠相比,其体重、脏器和血脂均有显著改善。如今,肥胖在发达国家和发展中国家都是一种常见的代谢性疾病。观察到香附块茎具有抗肥胖潜力和对心脏、肝脏的保护作用。
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引用次数: 0
NANOSPONGES: A PROMISING NANOCARRIER SYSTEMS FOR DRUG DELIVERY 纳米海绵:一种很有前途的药物递送纳米载体系统
Pub Date : 2020-04-08 DOI: 10.24092/crps.2020.100101
Mukesh Kumar, Priya, Anoop Kumar, Shobhit Kumar
Nanoengineered drug delivery system is generally used to solubilize the hydrophobic drugs. They also carry the drug to the target site and release the drug according to need of patient. These are very effective drug carriers which minimize and resolve the problems of drug toxicity and poor bioavailability as they can load both hydrophilic and hydrophobic drugs. Nanosponges are tiny in size with three dimensional networks. These are highly porous in nature and entrap active moieties and provide an advantage of programmable release. These are prepared by cross linking using many type of cyclodextrin with carbonyl and dicarboxylate compound like cross linker. Nanosponges are used for enhancing the bioavailability of drug and delivery of drug via oral, topical and parenteral routes. These are also used as a carrier for release of enzyme, protein, vaccines and antibiotics.
纳米工程给药系统通常用于疏水药物的增溶。它们还携带药物到靶部位,并根据患者的需要释放药物。它们是一种非常有效的药物载体,可以同时装载亲水性和疏水性药物,从而最大限度地减少和解决药物毒性和生物利用度差的问题。纳米海绵的尺寸很小,具有三维网络。这些材料具有高度多孔性,可捕获活性成分,并具有可编程释放的优势。它们是用多种类型的环糊精与羰基和二羧酸盐化合物如交联剂交联而成的。纳米海绵用于提高药物的生物利用度,并通过口服、局部和肠外途径给药。它们也被用作释放酶、蛋白质、疫苗和抗生素的载体。
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引用次数: 2
期刊
Current Research in Pharmaceutical Sciences
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