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Optimization and Evaluation of Oleic Acid Based Unsaturated Fatty AcidLiposomes Gel 油酸基不饱和脂肪酸脂质体凝胶的优化与评价
Pub Date : 2017-05-25 DOI: 10.4172/JBB.1000336
N. Kaur, R. Garg
Oxiconazole loaded Unsaturated Fatty Acid Liposomes (UFL) was used as a transdermal formulation in treatment of chronic fungal infections. Oxiconazole has low oral bioavailability of drug and short half-life that’s why preferring this transdermal route for proper treatment against fungal infections. UFL was made by using oleic acid and tween 80 in different proportion, batches were developed by using a central composite design. The optimal UFL-6 formulation has shown maximum entrapment efficiency (61.05%) and good vesicle size (215 nm). The oxiconazole release from UFLG-6 gels, follow Higuchi model and drug permeation via a cellophane membrane was maximum in comparison to other gel formulations. The UFLG-6 formulation also shows maximum antifungal activity against Candida albicans fungus.
载氧康唑不饱和脂肪酸脂质体(UFL)作为一种透皮制剂用于治疗慢性真菌感染。奥昔康唑口服生物利用度低,半衰期短,这就是为什么更倾向于通过透皮途径治疗真菌感染的原因。以油酸和吐温80为原料,按不同比例配制UFL,采用中心复合设计研制出批次。优化后的UFL-6包封效率最高(61.05%),囊泡大小良好(215 nm)。与其他凝胶制剂相比,UFLG-6凝胶的oxiconazole释放量符合Higuchi模型,并且通过玻璃纸膜的药物渗透最大。UFLG-6配方也显示出对白色念珠菌真菌的最大抗真菌活性。
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引用次数: 3
Atypical Antipsychotics: Do Their Direct Actions on Adipocytes Contribute to Metabolic Disturbances? 非典型抗精神病药物:它们对脂肪细胞的直接作用是否会导致代谢紊乱?
Pub Date : 2017-05-22 DOI: 10.4172/JBB.1000334
Hugo Er, Ben Jonathan N
The introduction of Atypical Antipsychotics (AAP) has improved the treatment of many psychiatric disorders by reducing the incidence of extrapyramidal side effects, but it has come at the expense of developing severe metabolic disturbances. Although the AAP were initially developed for the treatment of schizophrenia, their use has been expanded to include treatment of bipolar disorder, autism, posttraumatic stress disorder, dementia, and as ‘off label’ therapy for major depression. The current dogma posits that both therapeutic and negative side-effects of the AAP are due to their exclusive actions within the brain. Here we argue that very little consideration has been given to the potential actions of the AAP in peripheral sites, constituting a serious deficit in our understanding of the full spectrum of the biological action of these drugs.
非典型抗精神病药(AAP)的引入通过减少锥体外系副作用的发生率改善了许多精神疾病的治疗,但它是以发展严重的代谢紊乱为代价的。虽然AAP最初是为治疗精神分裂症而开发的,但它们的用途已经扩大到治疗双相情感障碍、自闭症、创伤后应激障碍、痴呆,并作为“标签外”治疗重度抑郁症。目前的教条认为,AAP的治疗和负面副作用都是由于它们在大脑内的排他作用。在这里,我们认为很少考虑到AAP在外周部位的潜在作用,这构成了我们对这些药物的全谱生物学作用的理解的严重缺陷。
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引用次数: 1
Extrapyramidal Symptoms in Patients Treated with Antipsychotic Drugs 抗精神病药物治疗患者的锥体外系症状
Pub Date : 2017-05-10 DOI: 10.4172/jbb.1000333
F. Werner
Extrapyramidal symptoms are adverse effects of second-generation antipsychotic drugs which are generally used to treat schizophrenia and schizoaffective disorder. These adverse effects are due to the D2 receptor blockade. Neurotransmitter and neuropeptide alterations in the mesolimbic system and in the extrapyramidal system and the derived neural networks are described. M4 antagonists, GABAA agonists or NMDA antagonists can be used to treat the extrapyramidal symptoms because they improve the dopaminergic-cholinergic neurotransmitter imbalance in this neural system. Recently developed antipsychotic drugs such as aripiprazole and cariprazine cause less often and, to a lesser extent, extrapyramidal symptoms because they exert a partial agonism at the D2 receptor.
锥体外系症状是第二代抗精神病药物的不良反应,通常用于治疗精神分裂症和分裂情感性障碍。这些不良反应是由于D2受体阻断。神经递质和神经肽的改变在中边缘系统和锥体外系统和衍生的神经网络被描述。M4拮抗剂、GABAA激动剂或NMDA拮抗剂可用于治疗锥体外系症状,因为它们可改善该神经系统的多巴胺能-胆碱能神经递质失衡。最近开发的抗精神病药物,如阿立哌唑和卡里吡嗪,引起锥体外系症状的次数较少,程度也较小,因为它们对D2受体发挥部分激动作用。
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引用次数: 1
Comparison of Pharmacokinetic and Pharmacodynamic Effects of Two Hydrofluoroalkane Formulations of Salmeterol 沙美特罗两种氢氟烷烃制剂的药动学和药效学效果比较
Pub Date : 2017-05-02 DOI: 10.4172/JBB.1000332
Nazma Morde, J. Rebello, B. Brashier, M. Garg, Raghu K. Naidu, A. Birhade, K. Iyer, R. Jadhav
Introduction: To compare the Pharmacokinetic (PK) and Pharmacodynamic (PD) effects of two Hydrofluoroalkane (HFA) formulations of salmeterol xinafoate (Test HFA formulation, Cipla Ltd., India; Reference HFA formulation, Allen and Hanburys, UK) administered using pressurized metered dose inhalers. Methods: Three separate randomized, crossover, PK studies and one PD study comparing the efficacy and safety of the two HFA formulations of salmeterol xinafoate (25 μg per actuation) in healthy subjects were conducted. The PK assessments of the two formulations were done without charcoal blockade, with charcoal blockade, and with a Volumatic spacer device using a single dose. A PD study was also conducted to evaluate the systemic exposure of the two formulations using three different doses (50 μg, 150 μg and 300 μg). Results: In the PK study without charcoal, the 90% CI for the difference between the two formulations for AUC0-t was within the bioequivalence limits of 80-125%; however, Cmax marginally exceeded the upper bioequivalence limit to 136%. In the PK study with charcoal, the 90% CI for the difference between the two formulations for Cmax was within the bioequivalence limits of 80-125%; however, AUC0-t marginally exceeded the upper bioequivalence limit to 128%. The impact of marginally higher systemic exposure was therefore further evaluated in the PD study. The PD study confirmed there were no greater systemic safety effects of the test formulation on the primary PD endpoints such as heart rate and serum potassium as well as on other safety PD endpoints such as blood glucose and QTc interval. The PK study with spacer demonstrated bioequivalence between the test and reference formulations. Both formulations were safe and well tolerated. Conclusion: The test HFA formulation of salmeterol was therapeutically equivalent to the reference HFA formulation of salmeterol when used with and without a spacer.
前言:比较沙美特罗两种氢氟烷烃制剂的药代动力学(PK)和药效学(PD)效果(Test HFA制剂,Cipla Ltd.,印度;参考HFA配方,Allen和Hanburys, UK)使用加压计量吸入器给药。方法:进行3个独立的随机、交叉、PK研究和1个PD研究,比较两种HFA制剂(25 μg /次)在健康受试者中的疗效和安全性。两种制剂的PK评估是在没有木炭阻断、木炭阻断和使用单剂量体积间隔装置的情况下进行的。研究人员还进行了PD研究,以评估两种制剂在三种不同剂量(50 μg、150 μg和300 μg)下的全身暴露。结果:在不加炭的PK研究中,AUC0-t两方差异的90% CI在80-125%的生物等效性范围内;Cmax略高于生物等效性上限136%。在用木炭进行的PK试验中,两种配方Cmax差异的90% CI在80-125%的生物等效性范围内;AUC0-t略高于生物等效性上限128%。因此,在PD研究中进一步评估了略高的全身暴露的影响。PD研究证实,试验配方对主要PD终点(如心率和血清钾)以及其他安全性PD终点(如血糖和QTc间期)没有更大的系统安全性影响。用间隔剂进行的PK研究表明,试验配方与参比配方具有生物等效性。两种制剂均安全且耐受性良好。结论:沙美特罗试验HFA制剂与沙美特罗参比HFA制剂在加或不加间隔剂时疗效相当。
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引用次数: 0
Comparison of Systemic and Pulmonary Bioavailability of Fluticasone Propionate HFA pMDI 250 Mcg per Actuation With and Without Spacer Device in Healthy Volunteers 健康志愿者每次驱动250 Mcg丙酸氟替卡松HFA pMDI的全身和肺部生物利用度比较,有无间隔装置
Pub Date : 2017-04-27 DOI: 10.4172/jbb.1000331
M. Garg, Raghu K. Naidu, A. Birhade, K. Iyer, R. Jadhav, J. Rebello, Nazma Morde, B. Brashier
Fluticasone Propionate (FP) is a topically active corticosteroid which shows little or no systemic activity after oral administration and is indicated for the prophylactic management of asthma of all severities. The aim of these studies was to evaluate systemic exposure and pulmonary deposition of two Hydrofluoroalkane (HFA) formulations of fluticasone propionate with and without a spacer device in, healthy volunteers. Study-1 was a, randomized, single dose, laboratory-blinded, 2-sequence, 4-period, crossover replicate design without volumatic spacer in 32 healthy volunteers under fasting conditions. Study-2 was a randomized, single dose, laboratory-blinded, 2-sequence, 2-period, crossover design with volumatic spacer in 28 healthy volunteers under fasting conditions. A washout period of 14 days was included in both the studies. Blood samples were collected up to 36 h post-dose for pharmacokinetic profiling. Safety evaluations included assessment of vital signs, clinical laboratory parameters and monitoring of adverse events. A validated LC-MS/MS method was used to measure the plasma concentrations of fluticasone propionate. The 90% CI of the difference between the test (T) and reference (R) for fluticasone propionate was 97.46-112.34 and 98.55-113.06 for Cmax, and AUC0-t respectively in study-1. The 90% CI of the difference between the test and reference for fluticasone propionate was 88.13-104.88, and 96.21-111.22 for Cmax, and AUC0-t respectively in study-2. The 90% CI (T/R) for fluticasone propionate for both Cmax and AUC0-t was within the bioequivalence limits of 80-125% in both the studies. Hence, it was concluded that test and reference formulations of fluticasone propionate HFA pMDI 250 mcg per actuation are equivalent in the systemic exposure and pulmonary deposition with and without a spacer device.
丙酸氟替卡松(FP)是一种局部活性皮质类固醇,口服后显示很少或没有全身活性,适用于所有严重程度哮喘的预防性治疗。这些研究的目的是评估两种丙酸氟替卡松氢氟烷烃(HFA)制剂在健康志愿者中有或没有间隔装置的全身暴露和肺沉积。研究1是一项随机、单剂量、实验室盲法、2序列、4周期、无体积间隔的交叉重复设计,在32名健康志愿者空腹条件下进行。研究2是一项随机、单剂量、实验室盲法、2序列、2期、有容量间隔的交叉设计,在28名健康志愿者空腹条件下进行。两项研究都有14天的洗脱期。给药后36小时采集血样进行药代动力学分析。安全性评估包括生命体征评估、临床实验室参数评估和不良事件监测。采用经验证的LC-MS/MS法测定丙酸氟替卡松血药浓度。研究1中丙酸氟替卡松Cmax和AUC0-t的试验(T)与参考(R)差异的90% CI分别为97.46-112.34和98.55-113.06。研究2中丙酸氟替卡松的Cmax、AUC0-t与对照差异的90% CI分别为88.13 ~ 104.88、96.21 ~ 111.22。两项研究中,丙酸氟替卡松Cmax和AUC0-t的90% CI (T/R)均在80-125%的生物等效性范围内。因此,得出的结论是,试验配方和参考配方丙酸氟替卡松HFA pMDI每次250微克在系统暴露和肺部沉积中是相同的,有无间隔装置。
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引用次数: 0
Pharmacological Evaluation of Ocimum sanctum 麝香的药理评价
Pub Date : 2017-04-24 DOI: 10.4172/JBB.1000330
Bano N, A. A, Tanveer M, Khandaker Gm, Ansari Mt
Tulsi is a Sanskrit word that means “matchless one”. Ocimum sanctum is a plant of family Lamiaceae, is commonly known as Holy Basil. Characteristically, the plant imparts a pungent, bitter, hot, light and dry effect. Holy Basil is extensively famous and has been used since centuries in Ayurvedic and Greek medicines owing to its beneficially diverse properties. O. sanctum (Tulsi in Hindi) has a significant place in Hindu culture, being used in an array of traditional medicaments and as a condiment. Online published articles, journals, internet sites, Pubmed, Scopus and Google Scholar were explored for data collection. Since Ayurveda times, various parts such as leaves, roots, seeds and whole plant has been recommended for treatment of a spectrum of diseases including bronchitis, dysentery, malaria, diarrhea, eye ailments, dermatological issues, rheumatoid arthritis, etc. Scientifically, it has been proven that O. sanctum possesses anticancer, anti-diabetic, anti-fertility, antifungal, antimicrobial, cardio protective, analgesic, antispasmodic and adaptogenic, immunomodulatory, antioxidant, hepatoprotective, antiallergic, antipyretic, antiviral, antiulcer, anti-inflammatory, CNS depressant and anti-arthritis activities. Its biologically active constituent is known as Eugenol (1-hydroxy-2-methoxy-4-allylbenzene) which is responsible for the mediation of therapeutic characteristics. This review is an attempt to summarize the botanical, pharmacological, phytochemical, ethno medicinal, and toxicological information. This is an effort to help researchers and clinicians to be aware of the magical properties and the effectiveness of Tulsi.
图尔西是一个梵语单词,意思是“无与伦比的”。罗勒(Ocimum sanctum)是兰科植物,俗称圣罗勒。这种植物具有辛辣、苦涩、炎热、清淡和干燥的特点。圣罗勒非常有名,几个世纪以来一直用于阿育吠陀和希腊药物中,因为它有益的多种特性。O. sanctum(印地语中的Tulsi)在印度文化中占有重要地位,被用于一系列传统药物和调味品中。研究人员对在线发表的文章、期刊、网站、Pubmed、Scopus和Google Scholar进行了数据收集。自阿育吠陀时代以来,叶子、根、种子和整株植物等不同部位被推荐用于治疗一系列疾病,包括支气管炎、痢疾、疟疾、腹泻、眼疾、皮肤病、类风湿性关节炎等。科学研究证明,荆芥具有抗癌、抗糖尿病、抗生育、抗真菌、抗菌、心脏保护、镇痛、抗痉挛和适应、免疫调节、抗氧化、保护肝脏、抗过敏、解热、抗病毒、抗溃疡、抗炎、中枢神经系统抑制和抗关节炎等作用。其生物活性成分被称为丁香酚(1-羟基-2-甲氧基-4-烯丙基苯),它负责调解治疗特性。本文综述了其在植物学、药理学、植物化学、民族医药和毒理学等方面的研究进展。这是一项帮助研究人员和临床医生意识到图尔西的神奇特性和有效性的努力。
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引用次数: 43
The Hidden Ingredients Affecting Cancer Patients Outcome and the Mathematical Journey to Their Uncover 影响癌症患者预后的隐藏因素及其揭示的数学之旅
Pub Date : 2017-04-20 DOI: 10.4172/jbb.1000329
Siegelmann Danieli N, Siegelmann H
2) Basic biology events of normal cycling cells [5], and principals involved in cancer pathogenesis named "hallmarks of cancer," including sustaining proliferative signaling, evading growth suppressors, resisting cell death, enabling replicative immortality, angiogenesis, activating invasion and metastasis, and recently expanded to include also reprogramming of energy metabolism and evading immune destruction [6,7];
2)正常循环细胞的基本生物学事件[5],以及被称为“癌症标志”的癌症发病机制中涉及的原则,包括维持增殖信号,逃避生长抑制因子,抵抗细胞死亡,使复制不朽,血管生成,激活入侵和转移,最近扩展到包括能量代谢的重编程和逃避免疫破坏[6,7];
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引用次数: 0
The Investigation of the Oxidative Stress-Related Parameters in High Doses Methotrexate-Induced Albino Wistar Rats 大剂量甲氨蝶呤诱导的白化Wistar大鼠氧化应激相关参数的研究
Pub Date : 2017-04-07 DOI: 10.4172/JBB.1000327
S. Saka, O. Aouacheri
Methotrexate (MTX) is used as a chemotherapeutic agent used to treat many cancer types. Methotrexate was known for its toxic effects involving most of the body organs including liver, kidney, intestines and blood components. The aim of the present study was to investigate the antioxidant status during oxidative stress via biological, biochemical and haematological parameters in rats subjected to oral high-doses of methotrexate. Forty male albino rats were equally divided at random into four groups; the first group was the control and the other three groups were treated per os for 7 days with three different doses (1/10, 2/10 and 3/10 of an LD50) of MTX respectively. The methotrexate-treatment of rats caused critical changes in the biological, biochemical and haematological markers. Mainly, an increase in the organo-somatic indexes (organo-megaly), a decrease in urine output value (nephotoxicity) and also a perturbation in most blood components (haematoxicity) were appeared. In addition, MTX has a prooxidant effect, which was indicated by a decrease of the antioxidant parameters in different studied tissues. In view of these results, a close relationship was shown between the increasing MTX-doses and the oxidative stress intensity, characterized by perturbations in biochemical and haematological markers.
甲氨蝶呤(MTX)是一种用于治疗多种癌症的化疗药物。甲氨蝶呤以其毒性作用而闻名,涉及大多数身体器官,包括肝、肾、肠和血液成分。本研究旨在通过口服大剂量甲氨蝶呤的生物学、生化和血液学参数研究氧化应激大鼠的抗氧化状态。40只雄性白化大鼠随机分为4组;第一组为对照组,其余三组分别给予三种不同剂量(LD50的1/10、2/10和3/10)的甲氨蝶呤,每组治疗7天。甲氨蝶呤治疗大鼠引起了生物、生化和血液学指标的重大变化。主要表现为器官躯体指数(organo-megaly)升高,尿输出值(ne光毒性)降低,大部分血液成分(haemattoxic)紊乱。此外,MTX还具有促进氧化的作用,这可以通过降低不同组织的抗氧化参数来证明。鉴于这些结果,mtx剂量的增加与氧化应激强度之间存在密切关系,其特征是生化和血液学标志物的扰动。
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引用次数: 27
Wakaskar RR (2017) Types of Nanocarriers–Formulation Method and Applications. Wakaskar RR(2017)纳米载体的种类-制备方法及应用。
Pub Date : 2017-04-07 DOI: 10.4172/JBB.10000E77
Wakaskar Rr
Colloidal nanocarriers have provided a plethora of opportunities in terms of advancing the drug delivery field based on their immense biocompatibility, size, target-specific delivery and increased efficacy. The current passage entails an in-depth discussion regarding the varied types of nanocarriers such as dendrimers, polymeric micelles, solid-lipid nanoparticles along with their conventional formulation strategies and their specific applications. These nanoparticles have been extensively researched, till date, for their different diagnostic as well as therapeutic uses and their recent developments have been covered in this short review.
胶体纳米载体由于其巨大的生物相容性、大小、靶向性和更高的功效,在推进药物递送领域提供了大量的机会。本文将深入讨论各种类型的纳米载体,如树状大分子、聚合物胶束、固体脂质纳米颗粒,以及它们的常规配方策略和具体应用。迄今为止,这些纳米颗粒已被广泛研究,用于不同的诊断和治疗用途,这篇简短的综述涵盖了它们的最新发展。
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引用次数: 4
Au/Ag NPS Decorated PANI For Electrochemical and Biomedical Applications Au/Ag NPS修饰聚苯胺的电化学和生物医学应用
Pub Date : 2017-04-07 DOI: 10.4172/JBB.1000328
P. Singh, Rajan Patel, K. Kumari, G. K. Mehrotra
Polyaniline (PANI) has number of electronic structure and it depends on the doping. PANI composites containing Fe3O4NPs are regularly studied as the PANI having electrical and magnetic features. Herein, PANI was prepared from aniline and HCl by means of solution mixing using ammonium persulphate as oxidizing agent and catalyst. Composites of polyaniline with calcium carbonate and Au/Ag NPs were prepared. Nanocomposites of PANI were characterized using FTIR, SEM, EDX, electrical conductivity measurement techniques. The incorporation of CaCO3 and Au/Ag NPs in polyaniline matrix was confirmed by SEM, FT-IR and EDX results. CaCO3 act as binder and provide strength to the composite which can be clearly understood by SEM microgram. Electrochemical study of composite has been done which showed that on decorating PANI with gold/silver NPs, the conducting properties increases. We successfully tested the antimicrobial activity of nanocomposite via paper disk diffusion method against Escherichia coli and Staphylococcus aureus.
聚苯胺(PANI)具有若干个电子结构,并与掺杂有关。含Fe3O4NPs的聚苯胺复合材料作为具有电、磁特性的聚苯胺,经常被研究。以过硫酸铵为氧化剂和催化剂,以苯胺和盐酸为原料,通过溶液混合法制备聚苯胺。制备了聚苯胺与碳酸钙和金/银纳米粒子的复合材料。采用FTIR、SEM、EDX、电导率等测试技术对聚苯胺纳米复合材料进行了表征。通过SEM、FT-IR和EDX分析证实了CaCO3和Au/Ag NPs在聚苯胺基体中的掺入。CaCO3作为粘结剂,为复合材料提供了强度,这一点可以通过SEM微图清楚地理解。对复合材料的电化学研究表明,用金/银纳米粒子修饰聚苯胺后,其导电性能有所提高。采用纸片扩散法对纳米复合材料对大肠杆菌和金黄色葡萄球菌的抑菌活性进行了测试。
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引用次数: 3
期刊
Journal of Bioequivalence & Bioavailability
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