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Simultaneous Estimation and Validation of Niacin and Atorvastatin Calcium by UV-Spectroscopy in Pure and Tablet Dosage Form Using Methanol: Water Mixture as Solvent 以甲醇:水为溶剂,紫外光谱法同时测定烟酸和阿托伐他汀钙在纯剂型和片剂中的含量
Pub Date : 2014-08-25 DOI: 10.5530/RJPS.2014.2.6
M. Ranganath, R. Chowdary
Purpose of This paper: Two simple, precise, rapid, sensitive and accurate simultaneous estimation by UV spectrophotometric methods were developed and validated for niacin (NCN) and atorvastatin calcium (ATR) in pure and tablet dosage form using methanol: water (40:60 v/v)mixture as solvent. Design and methodology: Two methods were developed, Method 1: was based on the simultaneous equation (Veroirdt's) method where as Method 2:was based on Q-analysis method. Findings: The absorption maxima were found to be 262 nm and 246 nm for niacin and atorvastatin calcium respectively. Both the drugs showed isosbestic point at 250 nm. Beer’s range was in the concentration range of 10-50 μg/ml for niacin and 4-20 μg/ml for atorvastatin calcium with correlation coefficient within the range of 0.9974 – 0.9998 for both the drugs. Recovery studies were performed to assess the accuracy of the methods, the results were found to be between 99.39 ± 0.7614 and 100.63 ± 0.3876 for niacin; 97. 71 ± 0.3131 and 99.06 ± 0.5625 for atorvastatin calcium. Research implications/limitations: The above two methods has been validated according to ICH guidelines. Practical implications: Hence the above methods can be used for routine analysis of NCN and ATR in pharmaceutical industries and research institutions.
目的:以甲醇:水(40:60 v/v)为溶剂,建立了两种简便、精确、快速、灵敏、准确的紫外分光光度法同时测定烟酸(NCN)和阿托伐他汀钙(ATR)纯剂型和片剂剂型的方法,并进行了验证。设计与方法学:设计了两种方法,方法1采用Veroirdt联立方程法,方法2采用q分析法。结果:烟酸和阿托伐他汀钙的吸光度最大值分别为262 nm和246 nm。两种药物均在250 nm处出现等吸点。烟酸浓度范围在10 ~ 50 μg/ml,阿托伐他汀钙浓度范围在4 ~ 20 μg/ml,相关系数在0.9974 ~ 0.9998范围内。结果表明,烟酸的回收率在99.39±0.7614 ~ 100.63±0.3876之间;97. 阿托伐他汀钙为71±0.3131和99.06±0.5625。研究意义/局限性:上述两种方法已根据ICH指南进行了验证。实际意义:因此,上述方法可用于制药工业和研究机构的NCN和ATR的常规分析。
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引用次数: 4
Drug efficacy and safety research frontiers: soul of pharmaceutical care 药物疗效与安全性研究前沿:药学服务的灵魂
Pub Date : 2014-08-25 DOI: 10.5530/RJPS.2014.2.1
R. Thakur
To unveil more information about efficacy, safety and side effects of an approved new drug it is essential that all patients who are treated with such a drug are compulsorily supervised and monitored by prescribing physicians, dispensing pharmacists and nurses and duly documented for all major and minor events during the course of therapy to correlate real time safety and efficacy with clinical trial data, collected up to phase III. Mere dependence on spontaneous reporting is insufficient, because it suffers from the vice of poor-quality reports and underreporting. Moreover, it is difficult to estimate rates and frequencies of ADRs, on this basis. Drug’s effect on specific demographics should be specifically studied and documented to obtain real time data on safety and efficacy. Pregnant & lactating women and specially those taking other medications along with the new drug need to be studied as special populations to identify effects on the fetus, infants and interaction between the drugs. As a result of extensive treatment on large population, long-term and unique/rare events/effects may be identified, which may be instrumental in ensuring safety and efficacy of therapy. This also assists in finding new markets, new indications and product extension. Thus the research fields like post marketing surveillance (PMS) and Phase IV studies have vast opportunity and practice based research must focus on this. INTRODUCTION
为了揭示关于已批准新药的疗效、安全性和副作用的更多信息,至关重要的是,所有接受这种药物治疗的患者都必须受到处方医生、配药药剂师和护士的强制性监督和监测,并对治疗过程中的所有重大和次要事件进行适当记录,以便将实时安全性和有效性与临床试验数据相关联,收集到第三期。仅仅依靠自发报告是不够的,因为它存在低质量报告和少报的弊端。此外,在此基础上很难估计不良反应的发生率和频率。药物对特定人群的影响应进行专门研究和记录,以获得有关安全性和有效性的实时数据。孕妇和哺乳期妇女,特别是与新药同时服用其他药物的妇女,需要作为特殊人群进行研究,以确定对胎儿、婴儿的影响以及药物之间的相互作用。由于对大量人群的广泛治疗,可能会发现长期和独特/罕见的事件/影响,这可能有助于确保治疗的安全性和有效性。这也有助于寻找新的市场,新的适应症和产品扩展。因此,像上市后监测(PMS)和IV期研究这样的研究领域有巨大的机会,基于实践的研究必须关注这一点。介绍
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引用次数: 0
In vitro Reactivation of Chlorpyrifos-inhibited Rat Brain Acetylcholinesterase from 2-Quinolone Substituted Thiazole derivatives 2-喹诺酮取代噻唑衍生物对毒死蜱抑制大鼠脑乙酰胆碱酯酶的体外再激活作用
Pub Date : 2014-08-25 DOI: 10.5530/RJPS.2014.2.4
M. Katagi, Jennifer Fernandes, D. Satyanarayana, Girish Bolakatti, Shivalingrao NagabhushanMamle
Organophosphate (OP) compounds exert inhibition of acetylcholinesterase (AChE) by irreversibly binding to catalytic site of an enzyme. Despite continued efforts to discover improved reactivators, there has been little success towards innovation of AChE reactivators. In the present investigation, new series of 2-quinolone fused thiazole derivatives 3a-3f and 4a-4f were evaluated for their in vitro reactivation efficacy against chlorpyrifos inhibited AChE using 2-PAM as standard. Even though the non oxime derivatives were not as effective as pralidoxime (2-PAM), but exhibited considerable AChE reactivation. The compounds, 3b, 3c, 3f, and 4f, showed promising reactivation against chlorpyrifos inhibited AChE.
有机磷化合物通过不可逆地结合酶的催化位点来抑制乙酰胆碱酯酶(AChE)。尽管不断努力发现改进的再活化剂,但在AChE再活化剂的创新方面几乎没有成功。本研究以2-PAM为标准,评价了新系列2-喹诺酮融合噻唑衍生物3a-3f和4a-4f对毒死蜱抑制乙酰胆碱酯酶的体外再活化效果。尽管非肟类衍生物的效果不如普拉度肟(2-PAM),但表现出相当大的AChE活性。化合物3b、3c、3f和4f对毒死蜱抑制的乙酰胆碱酯酶表现出有希望的再激活作用。
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引用次数: 0
Azadirachta indica: A Plant With Versatile Potential 印楝:一种具有多用途潜力的植物
Pub Date : 2014-08-25 DOI: 10.5530/RJPS.2014.2.2
S. Dubey, P. Kashyap
Purpose: The purpose of this article is to present a recent update on the various uses of the indigenous plant Azadirachta indica, and to highlight its importance in various therapeutic fields in traditional as well as modern system of medicine. Design/methodology/approach: The literature review of the plant has been presented covering all the fields of research where this plant has been exploited so far. Findings: The plant possesses powerful antidermatonic and anthelmintic, insect repellent, anti-bacterial, anti-fungal, anti-viral, anti-septic, anti-inflammatory, anti-ulcer and strengthens the body’s overall immune responses. It is widely used in treating chronic malaria, bed bugs ulcer, bad teeth, syphilis, leprosy, spermicidal in preventing pregnancies and other diseases. Externally it’s the oil applied as an antiseptic for urticaria and chronic skin diseases like eczema, scabies, ring worm and maggot infested wounds. It is also used for killing lice, fleas, ticks insecticide and bacterial growth in mouth. Research limitations/implications: This tree’s beneficial values have been known for 4000 years is described by the native as the village pharmacy due to its wide spectrum of medicinal qualities. Practical implications: Over 65 patents have been derived from its various uses, which clearly indicates its practical utility in our daily lives. Social Implications: It has been traditionally used by families for curing household ailments, spermicidal in preventing pregnancies. Originality/value: The paper is an overview of various researches being carried out on the Neem.
目的:本文的目的是介绍土着植物印楝的各种用途的最新进展,并强调其在传统和现代医学系统中各种治疗领域的重要性。设计/方法/途径:该植物的文献综述涵盖了迄今为止该植物已被开发的所有研究领域。发现:该植物具有强大的抗皮肤病和驱虫药,驱虫,抗菌,抗真菌,抗病毒,抗脓毒症,抗炎,抗溃疡和增强人体的整体免疫反应。广泛用于治疗慢性疟疾、臭虫溃疡、坏牙、梅毒、麻风病、杀精预防怀孕等疾病。在外部,它是一种用于荨麻疹和慢性皮肤病如湿疹、疥疮、环虫和蛆感染伤口的防腐剂。它也被用来杀死虱子,跳蚤,蜱虫,杀虫剂和口腔中的细菌生长。研究局限/启示:这种树的有益价值已经被人们知道了4000年,由于其广泛的药用品质,当地人将其描述为乡村药房。实际意义:超过65项专利来源于它的各种用途,这清楚地表明它在我们日常生活中的实用性。社会影响:传统上,它被家庭用于治疗家庭疾病,杀精预防怀孕。原创性/价值:本文概述了对印楝树进行的各种研究。
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引用次数: 17
Formulation and In vitro Evaluation of Loratadine Gels for Ophthalmic Use 眼用氯雷他定凝胶的制备及体外评价
Pub Date : 2014-08-25 DOI: 10.5530/RJPS.2014.2.5
A. El-Gawad, O. Soliman, M. Shams, D. Maria
Background: Loratadine is an oral H 1 antihistaminic drug which exhibits poor water solubility and very low dissolution rate. Objectives: An attempt was made in the current research study to prepare loratadine as ophthalmic gels for the treatment of ocular allergic conjunctivitis. Method: Loratadine ophthalmic gels were prepared using different polymers in various proportions and combinations. The solubility study, partition coefficient, drug content, viscosity and pH of the prepared formulations as well as the release characteristics of the drug in phosphate buffer solution having pH 7.4 were measured and its release kinetics was analyzed. Results: The solubility of loratadine increased linearly as a function of b-cyclodextrin (b-CyD) concentration. Gels containing loratadine-b-CyD complex had lower viscosity relative to gels containing free drug only. The pH values of the prepared gel formulations were within the acceptable range. Loratadine released from gel formulations containing its complex in a percentage higher than that released from gel formulations containing free drug only. This indicates a higher solubilizing effect of b-CyD. Conclusion: The obtained results encouraged a further In vivo study to investigate the efficacy of loratadine in these gel formulations for the treatment of ocular allergic conjunctivitis.
背景:氯雷他定是一种水溶性差、溶出率极低的口服h1抗组胺药。目的:本研究尝试制备氯雷他定眼用凝胶治疗眼部变应性结膜炎。方法:采用不同的聚合物以不同的比例和组合制备氯雷他定眼用凝胶。测定了所制制剂的溶解度、分配系数、药物含量、黏度、pH值以及药物在pH为7.4的磷酸盐缓冲液中的释放特性,并分析了其释放动力学。结果:氯雷他定的溶解度随b-环糊精(b-CyD)浓度线性增加。含有氯雷他定-b- cyd复合物的凝胶相对于仅含游离药物的凝胶粘度更低。所得凝胶制剂的pH值均在可接受范围内。氯雷他定从含其复合物的凝胶制剂中释放的百分比高于仅含游离药物的凝胶制剂释放的百分比。这表明b-CyD具有较高的增溶作用。结论:所得结果鼓励进一步的体内研究,以调查氯雷他定凝胶制剂治疗眼部过敏性结膜炎的疗效。
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引用次数: 1
Liposomal Drug Delivery System-A Review 脂质体给药系统综述
Pub Date : 2014-08-25 DOI: 10.5530/RJPS.2014.2.3
Deepthi, K. An
Purpose of this paper: Liposomes have received a lot of attention during the past 30 years as pharmaceutical carriers of great potential. More recently, many developments have been seen in the area of liposomal drugs-from clinically approved products to new experimental applications. For further successful development of this field, promising trends must be identified and exploited, with a clear understanding of the limitations of these approaches. Design/methodology/approach: This review presents a panoramic view of current status of research in this field to serve as a ready reference for future researchers. Practical implications: The treasure of information provided in this review find wide utility by future researchers and will serve as basis for further improvement in methodology and design of better formulations as well as evaluation methods. What is original/value of paper: In this article, basic characteristics, method of preparation and marketed formulations of liposomes are discussed. The success of liposomes as drug carriers has been reflected in a number of liposome based formulations, which are commercially available, or are currently undergoing clinical trials.
摘要:脂质体作为一种极具潜力的药物载体,在过去的30年里受到了广泛的关注。最近,从临床批准的产品到新的实验应用,在脂质体药物领域取得了许多进展。为了进一步成功地发展这一领域,必须确定和利用有希望的趋势,并清楚地了解这些方法的局限性。设计/方法/方法:本文综述了该领域的研究现状,为未来的研究者提供了一个现成的参考。实际意义:本综述提供的宝贵信息对未来的研究人员有广泛的应用价值,并将作为进一步改进方法学和设计更好的配方和评价方法的基础。本文讨论了脂质体的基本特性、制备方法和上市配方。脂质体作为药物载体的成功已经反映在许多基于脂质体的配方中,这些配方已经上市,或者目前正在进行临床试验。
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引用次数: 19
Design and Evaluation of Orodispersible Tablets of Sumatriptan Succinate 琥珀酸舒马匹坦多孔分散片的设计与评价
Pub Date : 2012-10-04 DOI: 10.5530/RJPS.2012.3.4
Sreenivasa Rao, Patil Kg, Dattatreya B. Udgirkar, P. Patil, K. V. Biradar
The demand for Orodispersible tablet (ODT) has been growing during the last decade. Sumatriptan Succinate used in the treatment of migraine and cluster headache. Sumatriptan Succinate is a 5-HT 1 receptor agonist, undergo extensive fi rst pass metabolism with an oral bioavailability of 14%. In present work an attempt has been made to prepare Orodispersible tablets of Sumatriptan Succinate with increased rate of dissolution May leads to increase bioavailability by using sodium starch glycolate, Crosscarmellose sodium and Crospovidone as Superdisintegrants by direct compression methods. The prepared tablets were evaluated for various parameters like hardness, friability, average weight, thickness, in vitro disintegration time, wetting time, water absorption ratio, uniformity of drug content, in vitro dissolution study, drug-polymer interaction, in vitro drug release, IR studies and short term stability and compatibility studies. Superdisintegrant of Croscarmellose sodium containing Sumatriptan Succinate compressed tablets showed highest in vitro drug release of 93% within 30 min. and there is no variation in the position of characteristic absorption bands it reveals that there is no interaction between drug and polymer.
在过去的十年中,对口服分散片(ODT)的需求一直在增长。琥珀酸舒马匹坦用于治疗偏头痛和丛集性头痛。琥珀酸舒马匹坦是一种5-羟色胺受体激动剂,具有广泛的第一次代谢,口服生物利用度为14%。本研究尝试以乙醇酸淀粉钠、交叉卡蜜糖钠和交叉维酮为强力崩解剂,采用直接压缩法制备琥珀酸舒马普坦的体外分散片,提高其溶出率,提高生物利用度。对制备的片剂进行硬度、脆度、平均重量、厚度、体外崩解时间、润湿时间、吸水率、药物含量均匀性、体外溶出度、药物-聚合物相互作用、体外释药、红外光谱研究、短期稳定性和相容性研究等指标的评价。含琥珀酸舒马普坦压缩片的交联棉糖钠超崩解剂在30 min内的体外释药率最高,达到93%,特征吸收带的位置无变化,说明药物与聚合物之间无相互作用。
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引用次数: 4
Phytochemical Screening, Antimicrobial and Antioxidant Activity of Indigofera Linnaei 林奈靛蓝植物化学筛选及抗菌抗氧化活性研究
Pub Date : 2012-10-04 DOI: 10.5530/RJPS.2012.3.11
Sandhyavali, P. Sivakamisundari, P. Sharma, V. Murugan
The present study deals with the preliminary phytochemical study of Indigofera linnaei of family Fabaceae which is commonly known as Birdsville indigo. The Indigofera species has been cited in various literatures for its use in treating rheumatism, arthritis, infl ammation, tumor and liver diseases. The Pharmacognostical study revealed presence of important constituents like alkaloids, saponins, fl avonoids, terpenoids, steroids and tannins. The aerial part of the plant was macerated with methanol to get the methanolic extract. The Antimicrobial Activity of methanolic extract of Indigofera linnaei was performed using agar well diffusion method. The extract was tested against 4 different species of human pathogenic bacteria including two species of gram-negative (E.coli and Klebsiella pneumoniae) and two species of gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis). The zone of inhibition was observed and the response was compared with the standard drug, Streptomycin. The observations revealed that the extract showed considerable antibacterial activity against Bacillus subtilis. The extract exhibited moderate activity in case of Staphylococcus aureus. However, very mild activity was observed against gram negative organisms. The two extracts i.e. chloroform and methanol extract of Indigofera linnaei were studied for their antioxidant potential. The activityof two extracts were compared by in vitro methods namely DPPH and Hydrogen Peroxide Assay. Ascorbic acid was used as standard in DPPH method. The in vitro antioxidant study revealed that the extract showed good antioxidant activity as compared to the chloroform extract which showed less inhibitory effect in DPPH method while in hydrogen peroxide assay, chloroform extract showed good antioxidant activity compared to methanol extract.
本文对豆科靛蓝(俗称伯氏靛蓝)的植物化学进行了初步研究。靛蓝属植物因其治疗风湿病、关节炎、炎症、肿瘤和肝脏疾病而在各种文献中被引用。生药学研究揭示了生物碱、皂苷、类黄酮、萜类、类固醇和单宁等重要成分的存在。将植物的地上部分用甲醇浸渍,得到甲醇提取物。采用琼脂孔扩散法对青靛甲醇提取物进行抑菌活性研究。该提取物对4种不同的人类致病菌进行了检测,包括两种革兰氏阴性菌(大肠杆菌和肺炎克雷伯菌)和两种革兰氏阳性菌(金黄色葡萄球菌和枯草芽孢杆菌)。观察其抑菌区,并与标准药链霉素进行比较。结果表明,该提取物对枯草芽孢杆菌具有较强的抑菌活性。提取物对金黄色葡萄球菌具有中等活性。然而,观察到对革兰氏阴性菌的活性非常轻微。研究了蓝靛的氯仿和甲醇提取物的抗氧化活性。采用体外DPPH法和过氧化氢法比较两种提取物的活性。DPPH法以抗坏血酸为标准品。体外抗氧化研究表明,在DPPH法中,三氯甲烷提取物具有较好的抗氧化活性,而在过氧化氢法中,三氯甲烷提取物具有较好的抗氧化活性,而甲醇提取物具有较好的抗氧化活性。
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引用次数: 1
Navigating Your Way Through Online Resources for Biomedical Research 通过生物医学研究的在线资源导航你的方式
Pub Date : 2012-10-04 DOI: 10.5530/RJPS.2012.3.2
P. Balakumar, Sharon Marcus, G. Jagadeesh
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引用次数: 2
Microspheres: Mucoadhesion Based Controlled Drug Delivery System 微球:基于黏附的受控给药系统
Pub Date : 2012-10-04 DOI: 10.5530/RJPS.2012.3.3
N. Jain, Neha Gulati, D. Kumar, Upendra Nagaich
A well designed controlled drug delivery system can overcome several problems of conventional therapy and also enhance the therapeutic effi cacy of active pharmaceutical compounds. There are various approaches for the delivery of therapeutic substance to the target site in a controlled release fashion. One such approach is using microspheres as carriers for drugs or active pharmaceutical compound. However, the success of this drug delivery system is limited due to their short residence time at the site of absorption. Thus, mucoadhesion characteristics are coupled to microspheres to develop a novel delivery system referred to as “mucoadhesive microspheres”. These mucoadhesive carriers provide an intimate contact with the mucus layer and specifi c targeting of drugs to the absorption site. In recent years, mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal for either systemic or local effects. Present work highlights the numerous aspects of microspheres i.e. method of preparation, delivery route, various polymers used for preparation and applications. Moreover, recent patents granted till now are also discussed in detail.
一个设计良好的受控给药系统可以克服常规治疗的一些问题,也可以提高活性药物化合物的治疗效果。以受控释放方式将治疗物质递送到靶部位的方法有多种。其中一种方法是使用微球作为药物或活性药物化合物的载体。然而,这种药物传递系统的成功是有限的,因为它们在吸收部位停留时间短。因此,黏附特性与微球相结合,开发了一种称为“黏附微球”的新型递送系统。这些黏附载体提供了与黏液层的密切接触和药物对吸收部位的特异性靶向。近年来,黏附微球已被开发用于口腔、口腔、鼻腔、眼、直肠和阴道的全身或局部作用。目前的工作重点是微球的许多方面,即制备方法,输送途径,用于制备和应用的各种聚合物。此外,还详细讨论了到目前为止授权的最新专利。
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引用次数: 9
期刊
RGUHS Journal of Pharmaceutical Sciences
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