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Spectrophotometric Determination of Amprenavir by ComplexFormation in Bulk Drug and Formulation Samples 分光光度法测定原料药和制剂样品中安非那韦的含量
Pub Date : 2017-07-25 DOI: 10.25258/ijpcr.v9i7.8785
T. Padmini, L. Satyanarayana
A validate rapid, economical and sensitive visible spectrophotometric method has been developed for quantitative determination of amprenavir in bulk drug and formulation samples. This method is validated for irinotecan with chromogenic reagent 3-methyl benzothiazolinone hydrazine (MBTH). The calibration curve was linear over Beer’sconcentration range of 25-350 µg/ml. The relative standard deviation is less than 1% and average recovery is above 99.80%. Efficient visible spectrophotometric detection at the respective absorption maxima enabled determination with no interference from tablet excipients .The proposed method is fast, sensitive, precise, accurate and efficient and can be used for analysis in quality control laboratories.
建立了一种快速、经济、灵敏的可见分光光度法定量测定原料药和制剂样品中安非那韦的方法。用显色试剂3-甲基苯并噻唑啉酮肼(MBTH)对该方法进行了验证。在啤酒浓度25 ~ 350µg/ml范围内,校准曲线呈线性。相对标准偏差小于1%,平均回收率在99.80%以上。该方法具有快速、灵敏、精密度高、准确、高效的特点,可用于质量控制实验室的分析。
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引用次数: 2
Formulation, Optimization and Evaluation of Capecitabine Tablet for Colon Specific Drug Delivery System 结肠特异性给药系统卡培他滨片的处方、优化及评价
Pub Date : 2017-07-25 DOI: 10.25258/IJPCR.V9I7.8788
Hussain Mobarak, D. Biswajit, Chakraborty Jashabir
Aim: The present research is focused on development and optimization of colon specific, fast disintegrating Capecitabine tablet for the treatment of Colon cancer. Methods: Colon targeted core tablet of Capecitabine was prepared by using CCS (Croscarmellose sodium) as a super disintegrating agent by direct compression method and coating was done over the core tablets by using pectin in different ratios by compression coating method. The colon targeted coating was done on the compression coated tablets by using ES100 and CAP (Cellulose acetate phthalate) in different ratios by dip coating method. In vitro swelling studies were carried out at different pH (1.2, 6.8 and 7.4). The Design Expert software (v.10) was used to optimise the best formulation and an in vitro cumulative percentage of drug release in different dissolution media (pH 1.2,6.8 and 7.4) with respect to the time interval (2hr, 7hr and 9hr) as dependable variable. Results: Optimized formulation of Capecitabine tablet shows satisfactory result with respect to all pre and post compression test parameters and it was significantly stable during stability studies conducted for 30and 60 days. Conclusion: From the above research it was found that, the optimised formulation of less half-life period anticancer drug Capecitabine can be properly targeted to colon area with the help of pectin and eudragit S 100.
目的:研究结肠癌特异性快速崩解卡培他滨片的研制与优化。方法:以交联棉糖钠(CCS)为超级崩解剂,采用直接加压法制备卡培他滨结肠靶向核心片,并采用不同比例的果胶加压包衣法制备核心片。采用浸渍包衣法,将ES100与邻苯二甲酸纤维素(CAP)按不同比例进行结肠靶向包衣。在不同pH值(1.2、6.8和7.4)下进行体外肿胀研究。使用Design Expert软件(v.10)优化最佳配方,并以时间间隔(2hr, 7hr和9hr)为可靠变量,确定药物在不同溶出介质(pH 1.2,6.8和7.4)中的体外累积释放百分比。结果:优化后的卡培他滨片在压缩前、压缩后的各项试验参数均达到满意的效果,且在30、60天的稳定性研究中具有显著的稳定性。结论:通过以上研究发现,缩短半衰期的抗癌药物卡培他滨的优化配方可以在果胶和乌木糖s100的帮助下,适当地靶向结肠区域。
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引用次数: 4
Computational Study of Substituted 5[H] - Phenanthradin-6-Ones as Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors by Analog and Structure Based Methods 取代5[H] -菲蒽醌-6-酮作为聚(adp -核糖)聚合酶-1 (PARP-1)抑制剂的模拟和结构计算研究
Pub Date : 2017-07-25 DOI: 10.25258/IJPCR.V9I7.8783
K. Ravindrachary, M. Ramesh, T. Parthasarathy
The poly (ADP-ribose) polymerase-1 (PARP-1) is an abundant nuclear protein involved in DNA repair and programmedcell death. Substituted 5(H) phenanthradin-6-one analogs were found to be potent PARP-1 inhibitors. Semiempiricalmethods were used to estimate various physicochemical parameters. The hydration energy (HE), ionization potential (IP),electrophilic index (ω) and partition coefficient ( LogP ) were resulted as independent variables for inhibitory activity ofthe analogs. The overall increase of HE, IP, and EI and overall decrease of LogP enhance the efficacy of inhibitory natureof these analogs to PARP-1. Docking studies of 5(H) phenanthradin-6-one analogs with PARP-1 were also performed insupport of the findings of QSAR studies. Analysis of results of both QSAR and docking studies suggested that remarkableinhibitory activity is exhibited by molecules 9b, 10b1 and 10b2. The hydrogen bond interactions along with hydrophobicand electrostatic interactions are mapped to confirm their potencies.
聚adp核糖聚合酶-1 (PARP-1)是一种丰富的核蛋白,参与DNA修复和程序性细胞死亡。取代的5(H)菲蒽醌6- 1类似物被发现是有效的PARP-1抑制剂。采用半经验方法估计各种理化参数。以水合能(HE)、电离势(IP)、亲电指数(ω)和分配系数(LogP)作为抑制活性的自变量。HE、IP和EI的总体升高和LogP的总体降低增强了这些类似物对PARP-1的抑制作用。5(H)菲蒽醌-6- 1类似物与PARP-1的对接研究也支持了QSAR研究的结果。QSAR和对接研究结果分析表明,分子9b、10b1和10b2表现出显著的抑制活性。氢键相互作用以及疏水和静电相互作用被映射以确认它们的效力。
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引用次数: 0
Synthesis of Novel Cinnoline Fused Mannich Bases: Pharmacological Evaluation of Antibacterial, Analgesic and Anti-Inflammatory Activities 新型肉桂碱融合曼尼希碱的合成:抗菌、镇痛和抗炎活性的药理评价
Pub Date : 2017-07-25 DOI: 10.25258/IJPCR.V9I7.8784
G. Kalyani, S. Bethi, K. V. Sastry, V. Kuchana
In the present study, we have designed and synthesized a series of novel cinnoline fused Mannich bases by the condensationreaction of 4-methyl-3-acetyl cinnoline with different secondary aromatic and aliphatic amines with and the structures ofcompounds were characterized by H1-NMR, IR and Mass spectral analysis. The biological potentials of the newlysynthesized compounds are evaluated for their antibacterial activity against Staphylococcus aureus (Gram positive), andEeshricia coli (Gram negative) bacteria, in vivo analgesic and anti-inflammatory activities. Compounds 4 and 3, which arehaving larger hydrophobic amino substitutions resulted in relatively higher antibacterial against S. aureus and E. coli whencompared to streptomycin. Similarly, compound 4 reported higher analgesic activity when compared to diclofenac at 120mins and 180 mins. From anti-inflammatory evaluations, dose level of 50 mg/kg of test compounds reported significantlyhigher activity when compared to dose level of 20 mg/kg. Moreover, compound 4 (50 mg/kg) resulted in similar antiinflammatoryactivity when compared with celecoxib (20 mg/kg).
本研究通过4-甲基-3-乙酰基肉桂啉与不同的仲芳香胺和脂肪胺缩合反应,设计并合成了一系列新型肉桂啉曼尼希碱,并用H1-NMR、IR和质谱对化合物的结构进行了表征。新合成的化合物对金黄色葡萄球菌(革兰氏阳性)和大肠杆菌(革兰氏阴性)的抑菌活性、体内镇痛和抗炎活性进行了生物学电位评价。与链霉素相比,化合物4和3具有较大的疏水氨基取代,对金黄色葡萄球菌和大肠杆菌的抗菌作用相对较高。同样,与双氯芬酸相比,化合物4在120分钟和180分钟的镇痛活性更高。从抗炎评估来看,与20 mg/kg剂量水平相比,50 mg/kg剂量水平的试验化合物报告了显著更高的活性。此外,与塞来昔布(20 mg/kg)相比,化合物4 (50 mg/kg)具有相似的抗炎活性。
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引用次数: 4
Colourants and Additives: Existing and Emerging Safety Concerns 着色剂和添加剂:现有和新出现的安全问题
Pub Date : 2017-07-25 DOI: 10.25258/IJPCR.V9I7.8786
Manish Kumar, M. Venkatesh, T. M. Kumar
Colour additives have long been used as a means of enhancing the aesthetic value of foods, beverages, and cosmetics and of identifying drugs and other products. Naturally occurring substances such as turmeric, paprika, saffron, and inorganic mineral pigments have been used for thousands of years. In the middle of the nineteenth century, synthetic organic dyes were developed, creating an economical and extensive array of color additives. Certified color additives are synthetic organic compounds. Most exempt colorants are derived from vegetable or mineral sources and are therefore often called "natural"; they can also be made synthetically, however it requires FDA to hold both types of color additives to the same safety standard. Colour additives exempt from certification (also known as ‘natural Colour additives’) are commonly used in the United States to colour foods, drugs and cosmetics. The US Food and Drug Administration established regulations governing the use of these colour additives, and the labelling of the products that contain them. The safety of these colour additives has been demonstrated by safety testing programs that have yielded a significant amount of toxicology data, and also by a long and well documented history of safe use in the United States and elsewhere. In this study the data supporting the safety of the colour additives that are exempt from certification and approved for use in the USA, and conclude that the safety of these colour additives are well supported by the literature.
长期以来,颜色添加剂一直被用作提高食品、饮料和化妆品的审美价值以及识别药物和其他产品的手段。天然存在的物质,如姜黄、红辣椒、藏红花和无机矿物颜料已经使用了数千年。在19世纪中叶,合成有机染料被开发出来,创造了一系列经济而广泛的颜色添加剂。经过认证的颜色添加剂是合成的有机化合物。大多数豁免着色剂是从植物或矿物质中提取的,因此通常被称为“天然”;它们也可以合成,但它要求FDA将两种类型的颜色添加剂保持在相同的安全标准。免认证的颜色添加剂(也称为“天然颜色添加剂”)在美国通常用于给食品、药品和化妆品着色。美国食品和药物管理局制定了有关这些颜色添加剂使用的法规,并对含有这些添加剂的产品进行了标签管理。这些色素添加剂的安全性已经得到了安全测试项目的证明,这些测试项目产生了大量的毒理学数据,而且在美国和其他地方也有长期的安全使用记录。在本研究中,数据支持的安全性的颜色添加剂,免除认证,并批准在美国使用,并得出结论,这些颜色添加剂的安全性是由文献很好地支持。
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引用次数: 5
Antibacterial Potential and Phytochemical Analysis of Barleria lupulina Lindl. (Aerial Parts) Extracts Against Respiratory Tract Pathogens 狼疮芽孢杆菌抑菌潜能及植物化学分析。(空中部分)抗呼吸道病原体提取物
Pub Date : 2017-07-25 DOI: 10.25258/IJPCR.V9I7.8787
Ajeet Singh, Navneet
The antibacterial and phytochemical investigation of Barleria lupulina Lindl. aerial parts extracts were examined against common respiratory tract pathogens i.e., Streptococcus pneumoniae (MTCC 655), Staphylococcus aureus (MTCC 1144), Pseudomonas aeruginosa (MTCC 2474), Streptococcus pyogens (MTCC 442), Haemophillus influenzae (MTCC 3826). The plant material was extracted with solvents i.e., petroleum ether (PET), acetone (ACE), methanol (MeOH) and aqueous (H2O) with increasing polarity by Soxhlet apparatus and removed the solvent using vacuum evaporator at 30˚C. Antibacterial activity and minimum inhibitory concentration (MICs) were examined by Agar well diffusion two fold serialdilution method respectively. The maximum inhibition zone was found against S. aureus (17.34±0.78 mm) of methanol extract and minimum against S. pyogens (9.44±0.32 mm). MICs were observed for MeOH extract between 3.12 to 12.5 mg/mL against S. pneumoniae and S. pyogens respectively. Phytochemical examination of plant extracts showed the occurrence of alkaloids, saponins, steroids, flavonoids, glycosides, tannins, resins and phenolic compounds. The antimicrobial activity of the crude extracts of plant represents a significant outcome for the treatment of respiratory tract diseases.
狼疮芽孢杆菌的抑菌及植物化学研究。检测气参提取物对常见呼吸道病原菌肺炎链球菌(MTCC 655)、金黄色葡萄球菌(MTCC 1144)、铜绿假单胞菌(MTCC 2474)、致病菌链球菌(MTCC 442)、流感嗜血杆菌(MTCC 3826)的抑制作用。以石油醚(PET)、丙酮(ACE)、甲醇(MeOH)和极性递增的水(H2O)为溶剂,用索氏装置提取植物材料,在30℃的温度下用真空蒸发器除去溶剂。采用琼脂孔扩散两倍连续稀释法分别测定其抑菌活性和最低抑菌浓度(mic)。甲醇提取物对金黄色葡萄球菌的抑制区最大(17.34±0.78 mm),对病原菌的抑制区最小(9.44±0.32 mm)。MeOH提取物对肺炎链球菌和化脓性链球菌的mic值分别为3.12 ~ 12.5 mg/mL。植物化学检测表明,植物提取物中含有生物碱、皂苷、甾体、黄酮类、苷类、单宁类、树脂类和酚类化合物。植物粗提取物的抗菌活性是呼吸道疾病治疗的重要成果。
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引用次数: 1
Formulation and Evaluation of Bilayered Tablets Containing Immediate Release Layer of Glimepiride Complexed with Mangifera indica Gum and Sustained Release Layer Containing Metformin HCL by Using HPMC as Release Retardant 以HPMC为缓释剂的格列美脲与芒果胶配速释层与盐酸二甲双胍缓释层双层片的研制及评价
Pub Date : 2017-06-25 DOI: 10.25258/IJPCR.V9I6.8775
S. Hemalatha, P. Srikanth, G. Sai
In present investigation an attempt has been made to design and develop the Bilayered tablet of Glimepiride and Metformin using Mangifera Indica Gum (MIG) and HPMC as Immediate Release and Sustained Release Layer polymers. Glimepiride and Metformin are oral-hypoglycaemic drugs which lower blood glucose level and have been selected to prepare Bilayered tablets. Glimepiride immediate release layer was prepared using MIG by wet granulation technique and Metformin sustained release layer was prepared using HPMC by dry granulation technique. Prepared Bilayered tablets were evaluated for parameters like thickness, diameter, weight variation, hardness, friability, disintegration and in-vitro release studies. All the prepared tablets were of smooth surface and elegant texture. The weights of the tablets were in the range of 540±0.551 mg. The thicknesses of the tablet were in the range of 4±0.05mm. The drug content uniformity study showed uniform dispersion of drug throughout the formulation in the range of 97.16±0.50%. The hardness was in the range of 4.0±0.5 kg/cm2 and friability is in the range of 0.67±0.06%. The bilayered tablets were also subjected to model fitting analysis to know the order and mechanism of drug release from the formulation by treating the data according to zeroorder, first-order, Higuchi and peppas equations.The bioequivalence studies conducted between prepared and marketed (Glycomate) bilayered tablet showed the similarity factor value of 70.120 for IR layer and 57.689 for SR layer.
本研究以芒果胶(MIG)和HPMC为缓释层聚合物,设计并制备格列美脲-二甲双胍双层片剂。格列美脲和二甲双胍是一种降低血糖水平的口服降糖药,已被选择制成双层片。采用MIG湿造粒法制备格列美脲速释层,采用HPMC干造粒法制备二甲双胍缓释层。对制备的双层片进行了厚度、直径、重量变化、硬度、脆性、崩解度和体外释放度等参数的评价。所制片剂表面光滑,质构美观。片剂质量范围为540±0.551 mg。片剂厚度范围为4±0.05mm。药物含量均匀性研究表明,在97.16±0.50%范围内,药物在整个制剂中分散均匀。硬度范围为4.0±0.5 kg/cm2,脆性范围为0.67±0.06%。通过零阶、一阶、Higuchi和peppas方程对数据进行处理,对双层片进行模型拟合分析,了解其缓释顺序和释药机理。制备的糖苷酸双层片与上市的糖苷酸双层片的生物等效性研究表明,红外层的相似系数为70.120,SR层的相似系数为57.689。
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引用次数: 0
The Correlation of Fc-gamma Receptor I (CD64) Expression and Procalcitonin in Early Onset Neonatal Sepsis 早期新生儿败血症中fc - γ受体I (CD64)表达与降钙素原的相关性
Pub Date : 2017-06-25 DOI: 10.25258/IJPCR.V9I6.8774
Zenia Angelina, E. Sulistijono, L. Fitri
Objective: The aim of this study is to prove the relationship of FcγRI (CD64) expression and Procalcitonin value in earlyonset neonatal sepsis to assist in diagnosis of early-onset neonatal sepsis. Method: A descriptive and analytical case control study was conducted in dr. Saiful Anwar General Hospital Malang. There were 40 children divided into two groups: 1). Group of infants with neonatal risk factors who express signs of SIRS and proven by blood culture; 2). Group of infants with neonatal risk factors who showed no sign for SIRS. Both groups were performed examination of FcγRI (CD64) expression with flowcytometry and Procalcitonin value with ELISA. Data were statistically analyzed using normality test (Kolmogorov-Smirnov), chi square test, t test and Pearson correlation. We used SPSS 16 for this analysis. Results: The study showed that the FcγRI (CD64) expression and Procalcitonin value were higher in the infants group with proven early-onset neonatal sepsis (p less than 0.05). There was a significant relationship between FcγRI (CD64) expression and the Procalcitonin value (p=0.036). Conclusions: We conclude that expression of FcγRI (CD64) and Procalcitonin value were higher in the infants group with proven early-onset neonatal sepsis. There is a positive relationship between FcγRI (CD64) expression and Procalcitonin value in early onset neonatal sepsis
目的:本研究旨在证实fc γ - ri (CD64)表达与降钙素原值在新生儿早发性脓毒症中的关系,以辅助对新生儿早发性脓毒症的诊断。方法:采用描述性和分析性病例对照研究。40例患儿分为两组:1)有SIRS体征并经血培养证实的新生儿危险因素组;2)有新生儿危险因素但未出现SIRS症状的婴儿组。两组均采用流式细胞术检测fc - γ - ri (CD64)表达,ELISA检测降钙素原值。数据采用正态性检验(Kolmogorov-Smirnov)、卡方检验、t检验和Pearson相关进行统计学分析。我们使用SPSS 16进行分析。结果:早发新生儿脓毒症患儿组fc γ - ri (CD64)表达及降钙素原值升高(p < 0.05)。fc γ - ri (CD64)表达与降钙素原值有显著相关(p=0.036)。结论:我们认为fc γ - ri (CD64)的表达和降钙素原值在早发性新生儿败血症的婴儿组中较高。早期新生儿败血症中fc γ - ri (CD64)表达与降钙素原呈正相关
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引用次数: 2
Diabetic Risk Score and Fasting Plasma Glucose Testing in the Screening for Type 2 Diabetes Mellitus Risk 糖尿病风险评分和空腹血糖检测在筛查2型糖尿病风险中的作用
Pub Date : 2017-06-25 DOI: 10.25258/IJPCR.V9I6.8771
Techit Thavorasak, Paphanin Kamkaen, Araya Rattanasri, S. Tangvarasittichai
Type 2 diabetes mellitus (T2DM) is a common metabolic disorder and one of the leading causes of morbidity and mortality in both developed and developing countries. Early recognition and intervention will be helpful in reducing the personal and financial cost of the disease. We used the diabetic risk score (DRS) and fasting plasma glucose test (FPGT) for identification the risk of T2DM. A total of 142 female participants were randomly participated in the present study. These participants were identified as 39 (27.5%) high risk (Gr-III) and 71 (50%) very high risk (Gr-IV) for T2DM groups according to the DRS. In addition with 13 (9.2%) and 2 (1.4%) were newly diagnosed as having HT and T2DM. Both HT and T2DM participants were older than the normal participants. BMI and WC were not significantly different in the comparison of T2DM with Non-T2DM and HT with Non-HT patients. The DRS would be practical to use as tool for T2DM risk screening while FPGT was used to identify impaired fasting glucose and T2DM onset. Then, we recommended FPGT for the individuals with high and very high DRS groups.
2型糖尿病(T2DM)是一种常见的代谢紊乱,是发达国家和发展中国家发病率和死亡率的主要原因之一。早期识别和干预将有助于减少该疾病的个人和经济成本。我们使用糖尿病风险评分(DRS)和空腹血糖测试(FPGT)来识别T2DM的风险。本研究随机选取142名女性受试者。根据DRS,这些参与者被确定为T2DM组的高风险(Gr-III) 39人(27.5%)和非常高风险(Gr-IV) 71人(50%)。此外,13名(9.2%)和2名(1.4%)新诊断为HT和T2DM。HT和T2DM参与者都比正常参与者年龄大。T2DM组与非T2DM组、HT组与非HT组比较,BMI和WC无显著差异。DRS可作为T2DM风险筛查的实用工具,而FPGT用于识别空腹血糖受损和T2DM发病。然后,我们推荐对DRS高和非常高的个体进行FPGT。
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引用次数: 0
Self-Assembling Peptides- Notion and Medical Applications: A Review 自组装肽的概念和医学应用综述
Pub Date : 2017-06-25 DOI: 10.25258/ijpcr.v9i6.8776
Ankita Sharma, D. V. Gowda, N. Gupta, R. Osmani
Peptides are the building blocks which are widely used owing to their biology as well as their chemistry. They provide a vast platform in the area of medicine. Self-assembling peptides are peptide biomaterials which are pacing in the field of diagnosis, therapeutics, tissue regeneration and vaccine. Self-assembling peptides provide an excellent alternative to the conventional methods for the drug delivery and the treatment. In this article, we discuss about the various medical applications of self-assembling peptide as they have excellent biocompatibility and resemblance with the proteins in the biological system. These are constructed and modified using various amino acid sequences depending upon the type of the application for which it is being used
多肽由于其生物学和化学性质而被广泛应用。它们为医学领域提供了一个广阔的平台。自组装肽是一种肽类生物材料,在诊断、治疗、组织再生和疫苗等领域有着广泛的应用前景。自组装肽为药物传递和治疗提供了一种极好的替代方法。由于自组装肽具有良好的生物相容性和与生物系统中蛋白质的相似性,本文讨论了自组装肽的各种医学应用。根据所使用的应用类型,使用各种氨基酸序列构建和修改这些序列
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引用次数: 0
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