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Synthesis, Molecular Modeling and In vitro Antimicrobial Evaluation of New Quinolin-4yl-hydrazones 新型喹啉-4酰腙的合成、分子模拟及体外抗菌评价
Pub Date : 2019-10-15 DOI: 10.37285/ijpsn.2020.13.1.4
Shivani Pola, A. Garlapati
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引用次数: 0
Preparation and Evaluation of Oral Dispersible Strips of Teneligliptin Hydrobromide for Treatment of Diabetes Mellitus 氢溴替尼格列汀治疗糖尿病口服分散片的制备及评价
Pub Date : 2019-10-07 DOI: 10.37285/ijpsn.2020.13.1.2
Malviya V.R, M. Tawar
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引用次数: 51
"Green Synthesis and Characterization of Silver Nano- conjugates using Some Common Medicinal Weeds Leaf Aqueous Extracts" 《几种常用药用杂草叶水提物纳米银缀合物的绿色合成及表征》
Pub Date : 2019-10-07 DOI: 10.37285/ijpsn.2020.13.1.3
P. Ghosh, Moumita Saha, Subhadra Nandi, Titav Sengupta, Sohini Kulavi, Shaktijit Das, Sirshendu Chatterjee
Nanotechnology is one of the most rapidly progressing fields of technology, and it has opened up many new frontiers of research for modern society. It deals with the nanoparticles having a size of 1-100 nm in one dimension. These nano-conjugates can be prepared easily by different chemical, physical, and biological approaches. However, the green synthesis approach is the most favoured one because this method is more natural, less hazardous, and eco-friendly. Our present study gives an overview of some common medicinal weeds Heliotropium indicum (Family: Boraginaceae), Tridax procumbens (Family: Asteraceae), Cleome rutidosperma (Family: Cleomaceae), Commelina benghalensis (Family: Commelinaceae), and Euphorbia hirta (Family: Euphorbiaceae) leaf aqueous extract mediated green synthesis of silver nano-conjugates. After synthesis, silver nanoparticles were examined by using advanced characterization techniques, including UV-Vis Spectrophotometer, DLS, and FT-IR. The UV-Vis absorption spectroscopy results highlighted a single peak within the range of 402-429 nm for all the five nanoconjugates. The DLS data highlighted that the particle size of the nano-conjugates ranges between 18.17 nm105.7 nm. Whereas the similarities between the FT-IR data of the sample and nanoparticle confirm the conjugation of different bioactive compounds of the aqueous leaf extracts with the metal nanoparticles.
纳米技术是发展最为迅速的技术领域之一,它为现代社会开辟了许多新的研究领域。它处理一维尺寸为1-100纳米的纳米颗粒。这些纳米缀合物可以很容易地通过不同的化学,物理和生物方法制备。然而,绿色合成方法是最受欢迎的一种方法,因为这种方法更自然,危害更小,更环保。本研究综述了一些常见的药用杂草:梧桐(Boraginaceae)、原藜(Tridax proumbens Family: Asteraceae)、山毛榉(Cleomaceae)、山毛榉(Commelina benghalensis Family: Commelinaceae)和大戟(euphorbita Family: Euphorbiaceae)叶片水提物介导的银纳米缀合物的绿色合成。合成后,使用先进的表征技术,包括紫外可见分光光度计,DLS和FT-IR对银纳米颗粒进行了检测。紫外可见吸收光谱结果表明,5种纳米缀合物在402 ~ 429 nm范围内均有一个单峰。DLS数据显示,纳米共轭物的粒径范围在18.17 nm ~ 105.7 nm之间。而样品和纳米颗粒的FT-IR数据之间的相似性证实了不同的生物活性化合物与金属纳米颗粒的结合。
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引用次数: 4
Formulation and Evaluation of Metoprolol Tartrate Sustained Release Matrix Tablets 酒石酸美托洛尔缓释基质片的研制及评价
Pub Date : 2019-09-30 DOI: 10.37285/ijpsn.2019.12.5.7
Y ShravanKumar, G. Shireesha, S. Harika
The objective of the present work was to develop sustained release matrix tablets of Metoprolol tartrate using different polymers viz. Guar gum, Xanthan gum, Kondagogu gum and HPMC K100M. The release rates were modulated by combination of two different rates controlling material and triple mixture of two different rate controlling materials. After evaluation of physical properties of tablet, the in-vitro release study was performed in phosphate buffer pH 6.8 up to 12 hrs. Dissolution data was analyzed for release kinetics. It was observed that matrix tablets contained polymer Xanthan gum was successfully sustained the release of drug up to 12 hrs. Among all the formulations, F6 which contains 45 % of Xanthan gum, release of drug which follows zero order kinetics via, swelling, diffusion and the release profile of formulation F6 was compared with marketed product. The FTIR study revealed that there was no chemical interaction between drug and excipient.
以瓜尔胶、黄原胶、孔大谷胶和HPMC K100M为原料,制备酒石酸美托洛尔缓释片。通过两种不同控释材料的联合和两种不同控释材料的三重混合来调节释药速度。在评价片剂的物理性能后,在pH 6.8的磷酸盐缓冲液中进行体外释放研究。对溶出度数据进行释放动力学分析。观察到含有高分子黄原胶的基质片能成功地缓释药物达12小时。以黄原胶含量为45%的F6为研究对象,通过溶胀、扩散等零级动力学释放药物,并与市售产品进行了比较。红外光谱研究表明,药物与辅料之间不存在化学相互作用。
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引用次数: 0
Formulation and Evaluation of Chlorpheniramine Maleate Troches 马来酸氯苯那敏制剂的研制及评价
Pub Date : 2019-09-30 DOI: 10.37285/ijpsn.2019.12.5.6
K. Rajitha, G Rashmitha, B. Sharanya, A. Swathi
The present study was sought to prepare Chlorphenamine (also called chlorpheniramine) maleate troches. Chlorpheni-ramine maleate (CPM) is a first-generation alkyl amine anti histamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticarial having oral bio availability about 25-50%, it undergoes first pass metabolism. Troches containing CPM was prepared by non-aqueous granulation technology using Xanthum gum, Gum acacia, HPMC K4M and tragacanth and guar gum as the polymers.  The effect of varying the concentration of polymer on release of Chlorpheniramine maleate (CPM) from troches was investigated. Differential scanning calorimetry and X-ray powder diffraction spectroscopy were used for physicochemical characterization. Tablets prepared were evaluated for different parameters such as average weight, hardness, Carr’s index, tapped density, friability, disintegration, content uniformity test. All the parameters were found within the specifications. The drug content was estimated by UV spectrophotometer at 261 nm. In vitro drug release studies of troches formulations were performed in artificial saliva pH 6.8 at 37±1oC. Among the all polymers used the highest drug release is shown with xanthum gum due to its less binding capacity. The in vitro release data was subjected to zero order, first order, Higuchi, Korsemeyer-Peppas, Hixon crowell and erosion model in order to establish the drug release mechanism and kinetics of drug release from the lozenge tablets.
本研究旨在制备马来酸氯苯那敏(又称氯苯那敏)制剂。马来酸氯苯胺(Chlorpheni-ramine maleate, CPM)是第一代烷基胺抗组胺药,用于预防鼻炎和荨麻疹等过敏性疾病的症状,口服生物利用度约为25-50%,经过一次代谢。以黄原胶、金合胶、HPMC K4M、黄原胶和瓜尔胶为聚合物,采用非水造粒技术制备了含CPM的微球。研究了不同聚合物浓度对马来酸氯苯那敏(CPM)释放的影响。采用差示扫描量热法和x射线粉末衍射光谱法进行了理化表征。对所制片剂的平均质量、硬度、卡尔氏指数、轻叩密度、脆性、崩解性、含量均匀性等参数进行了评价。所有的参数都在规格书中。用紫外分光光度计在261 nm处测定药物含量。在37±10℃、pH值为6.8的人工唾液中对制剂进行体外释药研究。在所有使用的聚合物中,由于黄原胶的结合能力较小,药物释放量最高。采用零级、一级、Higuchi、korsemyer - peppas、Hixon crowell、糜烂等体外释放模型,建立含片的释药机理和释药动力学。
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引用次数: 0
Review of Atypical Lipoma and its Natural Treatment 非典型脂肪瘤及其自然治疗综述
Pub Date : 2019-09-30 DOI: 10.37285/ijpsn.2019.12.5.1
Brijesh Dasvani, A. Khristi, Vanniyer Thiyagarajan
Atypical lipomatous are rare tumors that typically arise out of soft tissues in the body and common in adults. Most lipomas comprise of mature fat cells that exhibit characteristic of benign tumor by nature. They are round, motile, non-painful slow growing masses, with a characteristic soft and soggy feel, usually appear in the hypodermic area of skin. Atypical lipomas, though uncommon and slow growing can be associated with syndromes such as multiple hereditary lipomatosis, colorless adipose, Gardner's syndrome and Madelung's disease. While surgery has been the primary treatment modality, doctors have managed few patients with radiation therapy (RT). Median age of diagnosis was found in the range: 36–76 years but intramuscular lipomas may occur irrespective of age group, right from childhood to old age. However, the occurrence dominancy was found between the ages of 42 and 72 years, with the average age at presentation reported as 47 to 57 years.
非典型脂肪瘤是一种罕见的肿瘤,通常发生在身体的软组织中,在成人中很常见。多数脂肪瘤由成熟脂肪细胞组成,具有良性肿瘤的特征。它们是圆形的、可动的、无痛的、生长缓慢的肿块,具有柔软和潮湿的感觉,通常出现在皮肤的皮下区域。非典型脂肪瘤虽然不常见且生长缓慢,但可与多种遗传性脂肪瘤病、无色脂肪、加德纳综合征和马德隆病等综合征相关。虽然手术一直是主要的治疗方式,但医生对放疗(RT)患者的管理很少。中位诊断年龄范围为36-76岁,但肌肉内脂肪瘤可能发生在任何年龄组,从儿童到老年。然而,主要发生在42至72岁之间,报告的平均发病年龄为47至57岁。
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引用次数: 0
Development and Validation of Stability Indicating RP-HPLC Method for Determination of Enzalutamide 恩杂鲁胺稳定性指示反相高效液相色谱法的建立与验证
Pub Date : 2019-09-30 DOI: 10.37285/ijpsn.2019.12.5.3
P. Nerkar, Sameer Ansari, S. Chalikwar
A simple, isocratic, and accurate reversed phase HPLC method was developed for the quantitative determination of enzalutamide. The chromatographic separation was achieved on an Qualisil BDS C18 (250 mm x 4.6mm, 5 μm) column using methanol: ammonium acetate buffer pH 4.2 adjusted with glacial acetic acid: (60:40, v/v) as a mobile phase, at a flow rate of 1 ml/min and detection at 236nm. The linear range for enzalutamide were 2.0 to        10 μg/mL was obtained with correlation coefficients ≥ 0.998. The retention time was found to be 6.30min. Enzalutamide was subjected to stress conditions hydrolysis (acid, base) oxidation, photolysis and thermal degradation and the stressed samples were analysed by the developed method. The method was validated for the precision, accuracy, linearity and robustness. The developed stability indicating method for enzalutamide was validated as per ICH guidelines.
建立了一种简便、等浓度、准确的反相高效液相色谱法测定恩杂鲁胺的含量。色谱柱为Qualisil BDS C18 (250 mm × 4.6mm, 5 μm),流动相为甲醇:醋酸铵缓冲液pH 4.2,冰醋酸:(60:40,v/v),流速为1 ml/min,检测波长为236nm。恩杂鲁胺在2.0 ~ 10 μg/mL范围内呈线性关系,相关系数≥0.998。停留时间为6.30min。对恩杂鲁胺进行了水解(酸、碱)、氧化、光解和热降解等应激条件,并对应激样品进行了分析。验证了该方法的精密度、准确度、线性度和鲁棒性。根据ICH指南验证了所建立的恩杂鲁胺稳定性指示方法。
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引用次数: 1
Efficacy of Silver Nanoparticles Synthesized from Hymenocallis species (Spider Lilly) Leaf Extract as Antimicrobial Agents 膜藻叶提取物合成纳米银抗菌效果研究
Pub Date : 2019-09-30 DOI: 10.37285/ijpsn.2019.12.5.4
K. Gupta, N. Kumari, N. Sinha, Akruti Gupta
Biogenic synthesis of silver nanoparticles synthesized from Hymenocallis species (Spider Lilly) leaf extract was subjected for investigation of its antimicrobial property against four bacterial species (E. coli, Salmonella sp., Streptococcus sp. & Staphylococcus sp.). The results revealed that synthesized nanoparticles solution very much justify the color change property from initial light yellow to final reddish brown during the synthesis producing a characteristics absorption peak in the range of 434-466 nm. As antimicrobial agents, their efficacy was evaluated by analysis of variance in between the species and among the different concentration of AgNPs solution, which clearly showed that there was significant variation in the antibiotic property between the four different concentrations of AgNPs solution and also among four different species of bacteria taken under studies. However, silver nanoparticles solution of 1: 9 and 1:4 were proved comparatively more efficient as antimicrobial agents against four species of bacteria.
以膜虫属植物(蜘蛛礼来)叶片提取物为原料合成纳米银颗粒,研究其对大肠杆菌、沙门氏菌、链球菌和葡萄球菌等4种细菌的抗菌性能。结果表明,合成的纳米粒子溶液在合成过程中具有从最初的淡黄色到最终的红棕色的变色特性,在434 ~ 466 nm范围内产生特征吸收峰。作为抗菌药物,我们通过菌种间和不同浓度AgNPs溶液间的方差分析来评价它们的抗菌效果,结果清楚地表明,四种不同浓度AgNPs溶液之间以及所研究的四种不同细菌之间的抗菌性能存在显著差异。然而,1:9和1:4的纳米银溶液对四种细菌的抗菌效果相对较好。
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引用次数: 0
Enhancement of Nimodipine Solubility by Self-Nano-emulsifying Drug Delivery System 自纳米乳化给药系统增强尼莫地平溶解度的研究
Pub Date : 2019-09-30 DOI: 10.37285/ijpsn.2019.12.5.5
S. Gande, S. Reddy, B. D. V. R. N.
Self-nanoemulsifying drug delivery system (SNEDDS) of Nimodipine was developed with the purpose of improving the bioavailability of the drug. Based on the results of Nimodipine solubility studies Peceol, Transcutol P and PEG 400 were optimized as oil, surfactant and co-surfactant for the formulation and Pseudo ternary plots was constructed by Chemix software. Fifteen formulations of Nimodipine SNEDDS prepared and analyzed for particle size, emulsification time, percentage drug release, percentage transmittance, in vitro drug dissolution studies and thermodynamic stability. The optimized Nimodipine SNEDDS formulation (F13) subjected to drug-excipient compatibility studies by FTIR. They are analyzed for zeta potential, SEM and stability. The particle size of optimized Nimodipine SNEDDS formulation was 25.9 nm, PDI is 0.382 and zeta potential -12.7 mV that are optimal for the stability of emulsion. SEM studies of Nimodipine SNEDDS indicated spherical shape and uniform particle distribution. The drug release of formulation F13 (98.25±4.77%) was higher than pure drug (38.49±3.88%). The stability studies indicated no change in drug content, drug release, emulsifying properties and appearance. Hence a potential SNEDDS formulation of Nimodipine developed with increased dissolution rate, bioavailability and solubility.
为了提高尼莫地平的生物利用度,研制了尼莫地平自纳米乳化给药系统。在尼莫地平溶解度研究的基础上,优化了Peceol、Transcutol P和peg400作为制剂油、表面活性剂和助表面活性剂,并利用化学软件构建了伪三元图。制备了15种尼莫地平SNEDDS制剂,并对其粒径、乳化时间、释药率、透过率、体外溶出度及热力学稳定性进行了分析。采用FTIR对优化后的尼莫地平SNEDDS (F13)进行了药物与辅料的配伍研究。对它们进行了zeta电位、SEM和稳定性分析。优化后的尼莫地平SNEDDS处方粒径为25.9 nm, PDI为0.382,zeta电位为-12.7 mV。尼莫地平SNEDDS的SEM研究表明其呈球形,颗粒分布均匀。F13制剂释放度(98.25±4.77%)高于纯药(38.49±3.88%)。稳定性研究表明,其药物含量、药物释放、乳化性能和外观均无变化。因此,一种潜在的尼莫地平sndds制剂具有更高的溶出率、生物利用度和溶解度。
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引用次数: 0
Pharmaceutical Applications and Safety Review of Dendrimers 树状大分子的药物应用及安全性综述
Pub Date : 2019-07-31 DOI: 10.37285/ijpsn.2019.12.4.1
Jyotimayee Nayak, P. Tripathi, N. Verma, J. Mishra
This article describes the innovative approaches to overcome the cationic toxicity inherently associated with the dendrimers. A dendrimer is a macromolecule characterized by its highly branched 3D structure that provides a high degree of surface functionality and versatility. The toxicity is attributed to the interaction of surface cationic charge of dendrimers with negatively charged biological membranes in vivo. Dendrimer toxicity in biological system is generally characterized by hemolytic toxicity, cytotoxicity and hematological toxicity. To minimize this toxicity, two strategies have been utilized; first, designing and synthesis of biocompatible dendrimers; and second, masking of peripheral charge of dendrimers by surface engineering. Biocompatible dendrimers can be synthesized by employing biodegradable core and branching units or utilizing intermediates of various metabolic pathways. Dendrimer biocompatibility has been evaluated in vitro and in vivo for efficient presentation of biological performance. Neutral and negatively charged dendrimers do not interact with biological environment and hence are compatible for clinical applications as elucidated by various studies examined in this review. Chemical modification of the surface is an important strategy to overcome the toxicity problems associated with the dendrimers.
本文介绍了克服树突分子固有的阳离子毒性的创新方法。树状大分子是一种高分子,其特点是其高度分支的三维结构,提供了高度的表面功能性和多功能性。树状大分子表面的正电荷与带负电荷的生物膜在体内相互作用而产生毒性。树状大分子在生物系统中的毒性主要表现为溶血毒性、细胞毒性和血液学毒性。为了尽量减少这种毒性,采用了两种策略;首先,生物相容性树状大分子的设计与合成;其次,利用表面工程技术对树状大分子的外围电荷进行掩蔽。生物相容性树状大分子可以通过采用可生物降解的核心和分支单位或利用各种代谢途径的中间体来合成。树状大分子的生物相容性已经在体外和体内进行了评估,以有效地呈现生物性能。中性和带负电荷的树状大分子不与生物环境相互作用,因此可以用于临床应用。表面化学修饰是克服树枝状大分子毒性问题的重要策略。
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引用次数: 0
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International Journal of Pharmaceutical Sciences and Nanotechnology
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