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Mesoporous Silica as a Carrier for Amorphous Solid Dispersion 介孔二氧化硅作为非晶固体分散的载体
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/33553
S. P. Chaudhari, A. Gupte
In the past decade, the discovery of active pharmaceutical substances with high therapeutic value but poor aqueous solubility has increased, thus making it challenging to formulate these compounds as oral dosage forms. The bioavailability of these drugs can be increased by formulating these drugs as an amorphous drug delivery system. Use of porous media like mesoporous silica has been investigated as a potential means to increase the solubility of poorly soluble drugs and to stabilize the amorphous drug delivery system. These materials have nanosized capillaries and the large surface area which enable the materials to accommodate high drug loading and promote the controlled and fast release. Therefore, mesoporous silica has been used as a carrier in the solid dispersion to form an amorphous solid dispersion (ASD). Mesoporous silica is also being used as an adsorbent in a conventional solid dispersion, which has many useful aspects. This review focuses on the use of mesoporous silica in ASD as potential means to increase the dissolution rate and to provide or increase the stability of the ASD. First, an overview of mesoporous silica and the classification is discussed. Subsequently, methods of drug incorporation, the stability of dispersion and, much more are discussed.
在过去的十年中,具有高治疗价值但水溶性差的活性药物物质的发现越来越多,因此,将这些化合物配制成口服剂型具有挑战性。这些药物的生物利用度可以通过将这些药物配制成无定形给药系统来提高。利用介孔二氧化硅等多孔介质作为增加难溶性药物的溶解度和稳定非晶给药系统的潜在手段已被研究。这些材料具有纳米级毛细血管和大表面积,使材料能够适应高载药量,促进控制和快速释放。因此,介孔二氧化硅被用作固体分散体的载体,形成非晶固体分散体(ASD)。介孔二氧化硅也被用作传统固体分散体中的吸附剂,具有许多有用的方面。本文综述了介孔二氧化硅在ASD中的应用,作为提高ASD溶解速度和提供或增加ASD稳定性的潜在手段。首先,介绍了介孔二氧化硅的研究概况和分类。随后,讨论了药物掺入方法、分散稳定性等。
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引用次数: 25
Hepatoprotective activity of leaf and leaf callus extracts of orthosiphon aristatus (Blume) Miq. 石菖蒲叶及愈伤组织提取物的保肝活性。
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/32191
N. Reshi, Sudarshana Mysore Shankarsingh, Girish Vasanaika Hodiyala
Aim: The study was carried out to evaluate the in vitro hepatoprotective activity of leaf and leaf callus extracts of Orthosiphon aristatus against alcohol induced toxicity using HepG2 cell line. Materials and Methods: Leaf segments were cultured on Murashige and Skoog solid medium fortified with different auxins alone and in combination. Prior to the determination of hepatoprotective property leaf and leaf callus extracts were subjected to the toxic dose study. The degree of hepatoprotection of extracts was determined by measuring cell viability percentage by MTT assay. Leaf and leaf callus extracts were subjected to the preliminary phytochemical analysis. Results: Maximum percentage of callus formation (94%) was obtained in MS medium augmented with 2 mg/L of 2,4-D. HepG2 cells were pretreated with the different concentrations (below toxic dose) of leaf and leaf callus extracts for 72 hrs. followed by alcohol intoxication. Results revealed that aqueous leaf extract pretreated HepG2 cells show 90% cell viability compared to the standard silymarin pretreated HepG2 cells which showed 81% cell viability. Leaf callus extracts also showed significant hepatoprotective activity where ethanolic callus extract pretreated HepG2 cells showed82% viability after intoxication with alcohol. Results revealed that HepG2 cell viability percentage is dose dependent. Phytochemical studies revealed the presence of different secondary metabolites in leaf and leaf callus extracts. Conclusion: The bio-efficacy study confirms the presence of secondary metabolites of hepatoprotective nature. Callus mediated tissues show hepatoprotection which paves a way for the mass production of desired biologically active principles.
目的:以HepG2细胞株为实验对象,研究石菖蒲叶及其愈伤组织提取物对酒精毒性的体外保护作用。材料与方法:分别在添加不同生长素的Murashige和Skoog固体培养基上培养叶片。在确定其肝保护作用之前,对其叶片和愈伤组织提取物进行了毒性剂量研究。MTT法测定细胞存活率,测定提取物的保肝作用。对叶片和愈伤组织提取物进行了初步的植物化学分析。结果:在添加2mg /L 2,4- d的MS培养基中愈伤组织形成率最高(94%)。用不同浓度(低于中毒剂量)的叶片和愈伤组织提取物预处理HepG2细胞72小时。其次是酒精中毒。结果表明,水飞蓟素预处理的HepG2细胞存活率为81%,水飞蓟素预处理的HepG2细胞存活率为90%。叶片愈伤组织提取物也显示出显著的肝保护作用,乙醇愈伤组织提取物预处理HepG2细胞后,酒精中毒后的存活率为82%。结果显示HepG2细胞存活率呈剂量依赖性。植物化学研究表明,叶片和愈伤组织提取物中存在不同的次生代谢物。结论:生物功效研究证实了其具有保肝作用的次生代谢产物。愈伤组织介导的组织显示出肝脏保护作用,这为大量生产所需的生物活性原理铺平了道路。
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引用次数: 1
Human Drug Targets Identification in Breast Cancer by Computationally Based DNA Microarray Analysis 基于计算的DNA微阵列分析在乳腺癌人类药物靶点鉴定中的应用
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/32138
S. Muhammad, N. Fatima, Hasan Afzaal, Z. Shah, Amjad Ali
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引用次数: 1
Factors Predicting Erythropoietin Responsiveness among Maintenance Hemodialysis Patients: Prospective Longitudinal Study 维持性血液透析患者促红细胞生成素反应性的预测因素:前瞻性纵向研究
Pub Date : 2017-01-10 DOI: 10.9734/bjpr/2017/33144
A. Ebid, Amira M. Elsawy, Waled Taha
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引用次数: 0
Effects of Piper guineense (Schumach) Leaf and Xylopia aethiopica Seed Extracts on Gastric Acid Secretion in Ibuprofen-Treated Wistar Rats 舒马赫胡椒叶和青木籽提取物对布洛芬治疗Wistar大鼠胃酸分泌的影响
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/29150
E. O. Agbai, C. Njoku, C. O. Nwanegwo, P. Onyebuagu, J. Ekezie, C. Eke, A. Arthur
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引用次数: 2
Haematological and Biochemical Properties of Methanolic Extract of Citrullus lanatus Seeds 瓜籽甲醇提取物血液学和生化特性研究
Pub Date : 2017-01-10 DOI: 10.9734/bjpr/2017/32346
G. Adedeji, O. Bamidele, A. Ogunbiyi
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引用次数: 3
Ameliorative Effect of Fennel Oil on Cyclophosphamide Induced Hepatotoxicity in Albino Rats 茴香油对环磷酰胺所致白化大鼠肝毒性的改善作用
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/34197
S. Sakr, Somaya Y. Shalaby, Rawan H. Beder
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引用次数: 1
Antioxidant Activity of Cnestis ferruginea and Uvaria chamae Seed Extracts 铁锈蕨和狼耳蕨种子提取物的抗氧化活性研究
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/32924
B. Ita
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引用次数: 11
Anti-inflammatory and Analgesic Effects of an Aqueous Extract of Lannea acida Stem Bark 水提物的抗炎镇痛作用
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/33266
G. Owusu, Jones Ofori-Amoah
Background: Different parts of Lannea acida A. Rich (fam: Anarcadiaceae) are used traditionally to treat various ailments including inflammation, facial pain, schistosomiasis, haemorrhoids and toothache. Objective: This study was carried out to investigate the anti-inflammatory and analgesic effects of an aqueous extract of the stem bark of Lannea acida. Methodology: Rats were given sub-plantar injection of prostaglandin E2 to induce oedema, which was measured using calipers over 21⁄2 hours at 30 min interval. In the acetic acid–induced abdominal writhing test, mice were given intraperitoneal injection of acetic acid and writhing movements were recorded. Oedema test was run for both prophylactic and curative protocols. In both paw oedema and writhing test models, inhibitory effects of the plant extract were compared Original Research Article Owusu and Ofori-Amoah; BJPR, 16(6): 1-8, 2017; Article no.BJPR.33266 2 with diclofenac. Results: Aqueous extract (30 – 300 mg/kg) of Lannea acida stem bark significantly reduced prostaglandin E2–induced paw oedema in both prophylactic and curative protocols. The extract also significantly inhibited acetic acid–induced abdominal writhing movement in Imprint Control Region (ICR) mice. Conclusion: The aqueous extract of Lannea acida stem bark inhibited prostaglandin E2–induced paw oedema in rats and acetic acid–induced writhing behaviour in ICR mice; indicating a possible anti-inflammatory and analgesic activities.
背景:Lannea acida . Rich (family: Anarcadiaceae)的不同部位传统上用于治疗各种疾病,包括炎症、面部疼痛、血吸虫病、痔疮和牙痛。目的:研究酸铃兰茎皮水提物的抗炎镇痛作用。方法:在大鼠足底下注射前列腺素E2诱导水肿,每隔30 min用卡尺测量21⁄2 h。在醋酸致小鼠扭腹实验中,小鼠腹腔注射醋酸,记录小鼠扭腹运动。对预防和治疗方案进行水肿试验。在两种足跖水肿和扭体实验模型中,比较了植物提取物奥乌苏和奥福瑞-阿莫阿的抑制作用;生物工程学报,16(6):1-8,2017;文章no.BJPR。33266 2双氯芬酸。结果:水提物(30 - 300 mg/kg)可显著降低前列腺素e2诱导的足跖水肿,无论是预防还是治疗方案。该提取物还能显著抑制醋酸诱导的印记控制区小鼠腹部扭体运动。结论:枸橼酸茎皮水提物对前列腺素e2诱导的大鼠足部水肿和醋酸诱导的ICR小鼠扭体行为有抑制作用;提示可能具有抗炎和镇痛作用。
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引用次数: 7
Development and Validation of UV-Spectrophoto-metric Method for Determination of Palladium Content in Rasagiline Mesylate 甲磺酸雷沙吉兰中钯含量的紫外分光光度测定方法的建立与验证
Pub Date : 2017-01-10 DOI: 10.9734/BJPR/2017/32254
S. Hussain, A. Gosar, Tabrez Shaikh
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引用次数: 0
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British journal of pharmaceutical research
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