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Investigations on noval method for the formulation of solid dispersions part- I Formulation, characterization and selection 固体分散体配方新方法的研究——第一部分:配方、表征和选择
Pub Date : 2017-10-31 DOI: 10.5138/09750215.2173
Rakesh Sharma, A. Middha
The solid dispersions of indomethacin with hydrophilic polymers were prepared by lyophilization. The polymers used in the investigation were HPMC, PVP K30, CBR and PLF 127. The solubility and dissolution of indomethacin from prepared lyophilized solid dispersions were investigated in 0.1 N HCl, purified water and USP-NF dissolution media.  Out of fifteen lyophilized formulations from F1 to F15, five formulations F2, F5, F8, F12 and F14 showed highest solubility in purified water. Formulation F2, F8 failed to comply with the USP-NF dissolution test for indomethacin capsules. Formulation F14 showed maximum dissolution in the respective dissolution media within 60 min.  Sustained drug release was observed for 6 h with formulations F2 and F8 in USP-NF media. The formulations F2, F5, F8, F12 and F14 were characterized by modulated DSC and FT-IR spectroscopy. Some Formulations on stability testing were found physico-chemically stable at accelerated temperature conditions.
采用冻干法制备了吲哚美辛亲水性聚合物固体分散体。研究中使用的聚合物有HPMC、PVP K30、CBR和PLF 127。研究了制备的冻干固体分散体在0.1盐酸、纯净水和USP-NF溶出介质中的溶解度和溶出度。从F1到F15的15个冻干制剂中,F2、F5、F8、F12和F14 5个制剂在纯净水中的溶解度最高。处方F2、F8不符合吲哚美辛胶囊的USP-NF溶出度试验。F14在溶出介质中溶出时间为60min, F2和F8在USP-NF介质中缓释时间为6h。采用调制DSC和FT-IR对配方F2、F5、F8、F12和F14进行了表征。稳定性试验表明,某些配方在加速温度条件下是物理化学稳定的。
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引用次数: 0
In vitro cytotoxicity, in vivo pharmacokinetic studies and tissue distribution studies of multifunctional citric acid dendrimers using the drug Cytarabine 使用阿糖胞苷的多功能柠檬酸树状大分子的体外细胞毒性、体内药代动力学研究和组织分布研究
Pub Date : 2017-10-06 DOI: 10.5138/09750215.2128
K. Reddy, B Narasimha Rao, KB Chandra Sekhar
Dendrimers are considered the emerging polymeric architectures, known for their well defined molecular-weight, polydispersity, uniformity and high-surface functionality. These nano-architectures are capable of encapsulating low-high molecular-weight drug moieties in their interior or exterior through covalent bonding and host-guest interactions. Further, large surface volume made researchers to implicate dendrimers in biomedical and therapeutic applications. Regardless of the massive applications, sometimes its use is limited because of the cytotoxicity produced.  Considering this, the present research is focused on the synthesis and PEGylation of citric acid dendrimers. PEGylation is an act of conjugating polyethylene glycol to dendrimers that completely eliminates the toxicity issues associated with dendrimers and render them biocompatible. Cytarabine was loaded in the dendritic architecture to target specifically the tumor cells. Dendrimers are made tumor specific by incorporating certain agents that get cleaved in tumor environment. Synthesized dendrimers were studied for its effect on acute cytotoxicity, tissue-distributions and pharmacokinetic parameters.
树状大分子被认为是新兴的聚合物结构,以其明确的分子量、多分散性、均匀性和高表面功能而闻名。这些纳米结构能够通过共价键和主客体相互作用在其内部或外部封装低分子量药物部分。此外,大的表面体积使研究人员将树状大分子应用于生物医学和治疗领域。尽管有大量的应用,但由于其产生的细胞毒性,有时其使用受到限制。考虑到这一点,目前的研究重点是柠檬酸树状大分子的合成和聚乙二醇化。聚乙二醇化是一种将聚乙二醇偶联到树状大分子上的行为,它完全消除了与树状大分子相关的毒性问题,并使它们具有生物相容性。阿糖胞苷被装载在树突结构中,以特异性靶向肿瘤细胞。树状大分子是通过结合某些在肿瘤环境中被切割的试剂而产生肿瘤特异性的。研究了合成树状大分子对急性细胞毒性、组织分布和药代动力学参数的影响。
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引用次数: 0
Regulatory aspects of medical devices in India 印度医疗器械的监管方面
Pub Date : 2017-10-06 DOI: 10.5138/09750215.2147
Monika Targhotra, G. Aggarwal, H. Popli, Madhu Gupta
Today millions of patients depend on medical device based treatment for the management and diagnose of several diseases. Quality and safety of device is depends upon the regulatory guidelines. Medical device manufacturing in India should be taken seriously due to large population and the potential severity of the consequences of introducing inferior and unsafe products to the market-place. Therefore a law containing adequate guidelines of rules and regulations are required for monitoring the entry of such devices into the use in public health. The regulations define requirements of medical device design, development and manufacture to ensure that products reaching market are safe and effective. Presently in India regulatory body CDSCO is governing regulation for regulation of devices which with time, amendment introducing in the law will provide safety assurance to public health. This review provides a study on different regulatory aspects of medical device implemented in India. The present review discuss about the classification of medical devices and regulations aspects in India.
今天,数以百万计的患者依靠基于医疗设备的治疗来管理和诊断几种疾病。设备的质量和安全取决于法规的指导方针。印度的医疗设备制造应受到重视,因为印度人口众多,而且向市场引入劣质和不安全产品可能造成严重后果。因此,需要一项载有适当规则和条例准则的法律来监测这类装置进入公共卫生领域的使用情况。该法规规定了医疗器械设计、开发和制造的要求,以确保进入市场的产品安全有效。目前在印度,监管机构CDSCO正在管理设备监管法规,随着时间的推移,法律中引入的修正案将为公众健康提供安全保障。这篇综述提供了在印度实施的医疗器械的不同监管方面的研究。本综述讨论了印度医疗器械的分类和法规方面的问题。
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引用次数: 3
Synthesis and in vitro drug release studies on substituted polyphosphazene conjugates of lumefantrine. 甲基苯胺取代聚磷腈缀合物的合成及体外释药研究。
Pub Date : 2017-10-06 DOI: 10.5138/09750215.2133
Sahil Kumar, Alka Sharma, R. Singh, D. Prasad, T. Bhardwaj
The present study pertains to the delivery of antimalarial drug (Lumifantrine). In this, polyphosphazene has been used in the synthesis of polyphosphazene-linked conjugates of Lumifantrine. These polymer-linked Conjugates have been synthesized and characterized by modern analytical techniques. The in-vitro drug release of Lumifantrine drug conjugates: p -Amino benzoic acid ester substituted polyphosphazene drug conjugate (15) and Glycine methyl ester substituted polyphosphazene drug conjugate (21) have been found to be 6.00 % and 5.96% (pH 1.2), 88.52% and 79.86% (pH 7.4), respectively. These drug conjugate may prove an effective delivery system for the treatment of malaria.
本研究涉及抗疟疾药物(鲁米曲明)的给药。在本研究中,聚磷腈被用于合成聚磷腈连接的鲁米芬汀缀合物。这些聚合物连接的共轭物已经被合成并通过现代分析技术进行了表征。对氨基苯甲酸酯取代聚磷腈药物偶联物(15)和甘氨酸甲酯取代聚磷腈药物偶联物(21)的体外释放度分别为6.00%和5.96% (pH值1.2)、88.52%和79.86% (pH值7.4)。这些药物偶联物可能被证明是治疗疟疾的有效给药系统。
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引用次数: 1
Nanoparticle preparation and characterization of Haruan fish ( Channa striata ) exctract contains albumin from south Kalimantan with ionic gelation method 离子凝胶法制备南加里曼丹白蛋白哈云鱼提取物及其表征
Pub Date : 2017-10-06 DOI: 10.5138/09750215.2070
D. Rahmawanty, A. Risa, N. Malikhatun, Prima Hr, K. Nani, A. Effionora
Snakehead fish ( Channa striata ) has been reported to be used for wound healing by people in South Borneo because it contains albumin. Snakehead fish extract ( Channa striata ) has hydrophillic property and poor stability. Nanoparticle technology has been started to be developed as an alternative solution to improve drug delivery profile. The purpose of this study was to determine the formulation that obtained best characterization for nanoparticle. Nanoparticles were prepared by ionic gelation method, that was prepared by doing optimize ratio between snakehead fish extract : chitosan and pH of chitosan solvent.Nanoparticles were characterized using Particle Size Analyzer for particle size and particle size distribution, measurement of entrapment efficiency, determined Zeta potential using Particle Size Analyzer, and observation of particle’s morphology using Transmission Electron Microscope. The result showed that the chosen formula was formula 6 which  ratio of extract : chitosan 1:2 with chitosan solvent pH 3, particle size 152.3 nm, polidispersity index 0.778, percentage of entrapment efficiency 51.3961 %, Zeta potential +35.9 mV, and round shape of particles.
据报道,在南婆罗洲,人们用蛇头鱼(Channa striata)来治疗伤口,因为它含有白蛋白。黑鱼提取物具有亲水性,稳定性差。纳米颗粒技术已经开始发展,作为一种替代解决方案,以改善药物的输送。本研究的目的是确定获得最佳表征纳米颗粒的配方。采用离子凝胶法制备了纳米颗粒,优化了鱼头鱼提取物与壳聚糖的比例和壳聚糖溶剂的pH值。采用粒径分析仪对纳米颗粒进行了粒径和粒径分布的表征,测定了包封效率,测定了Zeta电位,透射电镜观察了纳米颗粒的形貌。结果表明:壳聚糖提取率为1:2,壳聚糖溶剂pH为3,粒径为152.3 nm,多分散度指数为0.778,包封率为51.3961%,Zeta电位+35.9 mV,颗粒形状为圆形。
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引用次数: 1
Biosynthesis, Characterization and Antibacterial activity of Silver nanoparticles of Excoecaria agallocha L. fruit extract 沉香果提取物纳米银的合成、表征及抗菌活性研究
Pub Date : 2017-06-21 DOI: 10.5138/09750215.2094
P. Nagababu, V. U. Rao
In this present study, Excoecaria agallocha fruit aqueous extract was used to synthesize Silver Nano Particles (Ag NPs/SNPs) which has proven as eco-friendly, nontoxic, less time consuming and energy saving. The synthesized SNPs were characterized by UV-Visible spectroscopy, FTIR and SEM studies. The SNPs were checked for the antibacterial activity against both Gram positive and Gram negative bacteria. The characterization studies clearly revealed the formation and synthesis of SNPs which also showed the inhibitory activity on the tested bacteria.  SNPs of Excoecaria agallocha fruit showed higher zone of inhibition against Micrococcus luteus , Arthrobacter protophormiae , Rhodococcus rhodochrous , Bacillus subtilis , Alcaligens faecalis , Enterobacter aerogenes , Proteus mirabilis and Salmonella enterica when compared to that of standard antibiotic, Streptomycin.
本研究以无尾银果水提液为原料合成了环保、无毒、省时、节能的银纳米颗粒(Ag NPs/SNPs)。通过紫外可见光谱、红外光谱和扫描电镜对合成的SNPs进行了表征。snp对革兰氏阳性菌和革兰氏阴性菌的抗菌活性进行了检测。表征研究清楚地揭示了SNPs的形成和合成,并显示了对被试细菌的抑制活性。与标准抗生素链霉素相比,黄体微球菌、原生疣节杆菌、红红球菌、枯草芽孢杆菌、粪钙原菌、产气肠杆菌、奇异变形杆菌和肠沙门氏菌的SNPs具有更高的抑制区。
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引用次数: 1
The Future of Biosimilars 生物仿制药的未来
Pub Date : 2017-06-21 DOI: 10.5138/09750215.1930
L. El-Bakry
Biosimilars are to Biologic products what generic drugs are to chemical products, a more affordable solution to the increasing drug pricing without sacrificing the quality of the treatment.There is much debate in the health care industry as to whether Biosimilars will deliver on the same success achieved by the generic products, which can amount to up to 80% in some cases.   It is my view though that Biosimilars provide a viable path to cost reduction, quality improvement and affordable accessibility to medication.  In fact, the introduction of lower costs Biologics as intended by the Biosimilar market will force competition within the therapeutics treatment market that will both exertpricing pressure as well as inspire innovation in the entire ecosystem.
生物仿制药之于生物制品,就像仿制药之于化学制品一样,在不牺牲治疗质量的情况下,是一种更实惠的解决方案,可以应对不断上涨的药品价格。在医疗保健行业,关于生物仿制药是否能取得与仿制药相同的成功存在很多争论,在某些情况下,仿制药的成功率可高达80%。在我看来,生物仿制药为降低成本、提高质量和负担得起的药物提供了一条可行的途径。事实上,生物仿制药市场所期望的低成本生物制剂的引入将迫使治疗药物治疗市场内的竞争,这既会施加价格压力,也会激发整个生态系统的创新。
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引用次数: 5
One-Pot Multicomponent Synthesis of β-Acetamido Ketones Using BF3-Et2O as Catalyst 以BF3-Et2O为催化剂一锅多组分合成β-乙酰氨基酮
Pub Date : 2017-06-21 DOI: 10.5138/ijaps.v4i2.903
P. Rawat, P. Rawat, Piyush Kumar
Starting from different ketones 1a-1f , aldehyde 2a-2g , and acetonitriles 3a-3d we synthesize some bioactive β- Acetamido carbonyl compounds 4a-4h . We also attempted to synthesize these compounds by using phenylacetone and deoxybenzoins in place of ketones to afford the products 4i-4j . 1 H-NMR spectra are presented. On the basis of QSAR studies, some compounds were tested for their anti-thrombotic activity in mice. Compound 4f , 4h and 4j were found to exhibit less percentage protection.
以不同的酮类1a-1f、醛类2a-2g、乙腈类3a-3d为起始原料,合成了具有生物活性的β-乙酰氨基羰基化合物4a-4h。我们还尝试用苯丙酮和脱氧苯甲酸代替酮合成这些化合物,得到产物4i-4j。给出了H-NMR谱图。在QSAR研究的基础上,对一些化合物在小鼠体内的抗血栓活性进行了测试。化合物4f、4h和4j的保护率较低。
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引用次数: 0
Role of Quercetin in chemoprevention against wide range of carcinogens and mutagens 槲皮素在化学预防多种致癌物和诱变物中的作用
Pub Date : 2017-06-21 DOI: 10.5138/09750215.2040
S. Shivakumar, Yasodha Lakshmi Tadakaluru, Raja Ratna Reddy Yakkanti, S. Suresh, P. C. Sekhar
Quercetin is a ubiquitous plant flavoniod with significant pharmacological and clinical activity. In this study we determined to demonstrate the protective role of quercetin against range of mutagens and carcinogens in a combination of in vitro and in vivo studies via different mechanisms. Quercetin demonstrated significant protective role against sodium azide, benzo(a)pyrene, cyclophosphamide monohydrate, methyl methane sulphonate and etoposide compared to other mutagens. Quercetin is effective in both in vitro and in vivo test conditions and also in the presence as well as in the absence of metabolic activation system (Rat liver S9).  Auto oxidation, antioxidant properties, inhibition of pro-mutagens metabolism by CYP1A activity and multiple antimutagenic and adaptive response, mechanisms of quercetin may account for its protective role in cancer prevention. In conclusion, the results clearly indicate that quercetin plays a significant role against mutagens that act by direct DNA binding (form DNA adducts), pro-mutagens and alkylating agents with free radical generation; which could be the rationale for its potent anticancer activity against particular cancer types.
槲皮素是一种普遍存在的植物类黄酮,具有重要的药理和临床活性。在这项研究中,我们决定通过不同的机制在体外和体内研究中证明槲皮素对一系列诱变剂和致癌物质的保护作用。槲皮素对叠氮化钠、苯并(a)芘、一水环磷酰胺、甲烷磺酸甲酯和叶黄醇具有显著的抗诱变作用。槲皮素在体外和体内试验条件下都有效,在存在和不存在代谢激活系统的情况下也有效(大鼠肝脏S9)。槲皮素的自氧化、抗氧化特性、通过CYP1A活性抑制促诱变剂代谢以及多种抗诱变和适应性反应等机制可能解释了槲皮素在癌症预防中的保护作用。综上所述,槲皮素对直接结合DNA(形成DNA加合物)的诱变剂、促诱变剂和产生自由基的烷基化剂具有显著的抑制作用;这可能是其对特定癌症类型有效的抗癌活性的基本原理。
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引用次数: 1
Formulation and evaluation of floating bioadhesive Doxofylline tablets 多索茶碱漂浮型生物黏附片的研制及评价
Pub Date : 2017-02-28 DOI: 10.5138/09750215.1871
B. Nagaraju, B. Ramu, S. Saibaba, B. Rajkamal
In the present work, an attempt has been made to develop gastro retentive floating tablets of Doxofylline . HPMC K4M and carbopol were used as controlled release polymers . All the formulations were prepared by direct compression method on 12 station rotary tablet punching machine. The blend of all the formulations showed god flow properties such as angle of repose, bulk density, tapped density. The prepared tablets were shown good post compression parameters and they passed all the quality control evaluation parameters as per I.P limits. FH 5 was the best optimized floating formulation because it released drug completely in 12hrs.It was also observed that the increasing concentration of polymers had a retarding effect on the drug release from the polymer matrices.
本研究尝试研制多索茶碱胃内保留漂浮片。以HPMC - K4M和卡波波尔为控释聚合物。在12工位旋转冲压机上采用直接压缩法制备。各配方的共混物在休止角、容重、出丝密度等方面表现出良好的流动性能。所制片剂的后压缩参数良好,并通过了所有质量控制评价参数。fh5在12h内完全释放,是最佳的漂浮制剂。同时还观察到,聚合物浓度的增加对药物从聚合物基质中的释放有延缓作用。
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引用次数: 1
期刊
International Journal of Drug Delivery
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