首页 > 最新文献

Clinical Pharmacology & Biopharmaceutics最新文献

英文 中文
Nerve Growth Factor Mediates the Vious Cycle between Hyperactivity ofGanglionated Plexus and Atrial Fibrillation 神经生长因子介导神经节丛亢进与心房颤动的循环
Pub Date : 2018-01-01 DOI: 10.4172/2167-065X.1000183
LiDong Cai, Shao-wen Liu
Ganglionated Plexus (GP) is a complex neural network composed by intrinsic cardiac autonomic nervous system (ANS) and is mainly located in fat pads around the antrum of the pulmonary veins (PVs). Recent studies demonstrated hyperactivity of GPs and atrial fibrillation (AF) formed a vicious cycle, to be specific, hyperactivity of the cardiac GPs facilitated the initiation and maintenance of AF and the activity of cardiac GPs increased as AF continued. In addition, research has confirmed that the Nav1.8 channel is highly expressed in GPs and is closely related to activity of GPs and the inducibility of AF. Nerve growth factor (NGF) is an important neurotrophic factor and the expression of NGF in GPs is up-regulated during AF over time, which could trigger the release of SP in the heart via TRPV1 signaling pathways. Besides, SP could rapidly increase the activity of the Nav1.8 channel, demonstrating the increment of Sensory nerve action potentials. Therefore, we hypothesized that up-regulated NGF during AF could increase the activity of GPs through TRPV1-SP-Nav1.8 channel pathways and contributes to stability of AF. If this hypothesis is proved to be correct, future studies based on this link may help to find new therapeutic targets for the treatment of AF.
神经节神经丛(Ganglionated Plexus, GP)是由心脏内在自主神经系统(ANS)组成的复杂神经网络,主要分布在肺静脉(pv)上腔周围的脂肪垫中。近期研究表明,心脏全科医生亢进与房颤形成恶性循环,心脏全科医生亢进促进房颤的发生和维持,随着房颤的持续,心脏全科医生亢进增加。此外,研究证实Nav1.8通道在GPs中高表达,与GPs的活性和AF的诱导密切相关。神经生长因子(NGF)是一种重要的神经营养因子,AF时,NGF在GPs中的表达随着时间的推移而上调,可通过TRPV1信号通路触发SP在心脏的释放。此外,SP能快速增加Nav1.8通道的活性,表现为感觉神经动作电位的增加。因此,我们假设房颤期间NGF的上调可以通过TRPV1-SP-Nav1.8通道通路增加gp的活性,有助于房颤的稳定性。如果这一假设被证明是正确的,未来基于这一联系的研究可能有助于寻找房颤治疗的新靶点。
{"title":"Nerve Growth Factor Mediates the Vious Cycle between Hyperactivity ofGanglionated Plexus and Atrial Fibrillation","authors":"LiDong Cai, Shao-wen Liu","doi":"10.4172/2167-065X.1000183","DOIUrl":"https://doi.org/10.4172/2167-065X.1000183","url":null,"abstract":"Ganglionated Plexus (GP) is a complex neural network composed by intrinsic cardiac autonomic nervous system (ANS) and is mainly located in fat pads around the antrum of the pulmonary veins (PVs). Recent studies demonstrated hyperactivity of GPs and atrial fibrillation (AF) formed a vicious cycle, to be specific, hyperactivity of the cardiac GPs facilitated the initiation and maintenance of AF and the activity of cardiac GPs increased as AF continued. In addition, research has confirmed that the Nav1.8 channel is highly expressed in GPs and is closely related to activity of GPs and the inducibility of AF. Nerve growth factor (NGF) is an important neurotrophic factor and the expression of NGF in GPs is up-regulated during AF over time, which could trigger the release of SP in the heart via TRPV1 signaling pathways. Besides, SP could rapidly increase the activity of the Nav1.8 channel, demonstrating the increment of Sensory nerve action potentials. Therefore, we hypothesized that up-regulated NGF during AF could increase the activity of GPs through TRPV1-SP-Nav1.8 channel pathways and contributes to stability of AF. If this hypothesis is proved to be correct, future studies based on this link may help to find new therapeutic targets for the treatment of AF.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2018-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77164571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Study of in vitro Therapeutic Equivalence of the 5 mg Glibenclamide Multi-source Tablets Respecting the Reference Medicine Product 格列本脲多源片5mg以参比品为参照的体外治疗等效性研究
Pub Date : 2017-12-16 DOI: 10.4172/2167-065X.1000180
Á. Alvarado-Yarasca, Ana Muñoz-Jauregui, L. Quiñones-Sepúlveda, F. Lizaraso-Soto, A. Salazar-Granara, Luis Sullón-Dextre, Juan J. Palomino-Jhong, Jorge Antonio García-Ceccarelli
Introduction: Therapeutic equivalence of medications is carried out through in vitro and in vivo studies called bioequivalence studies. Objective: To determine the in vitro therapeutic equivalence of the 5 mg glibenclamide multi-source tablets respecting the reference medicine. Materials and methods: Both, the multi-source drug 5 mg glibenclamide and the reference 5 mg Glidiabet are made in Peru, and were acquired in a drugstore of Ica city (Peru). Reagents and an analytical grade standard were used. The Ultraviolet absorption method at 300 nm was used on each of the three dissolution media. Results: Neither the multi-source drug T nor the reference R dissolved by 85% at pH 1.2 and at pH 4.5, during 15 or 30 minutes. However, at pH 6.8 dissolution occurs. These results correspond to Food and Drug Administration and United States Pharmacopoeia criteria. The similarity factor value was within the acceptance range (50-100) for the three tested pHs. Dissolution efficiency was 68.66% (pH 1.2), 56.59% (pH 4.5) and 95.98% (pH 6.8). The mean of in vitro dissolution time was 28.56 min (pH 1.2), 39.97 min (pH 4.5) and 4.54 min (pH 6.8). Conclusion: According to the similarity factor (f2) and the efficiency of dissolution, it is concluded that the multisource drug 5 mg glibenclamide of the present study is therapeutically equivalent in vitro to the reference 5 mg Glidiabet.
药物的治疗等效性是通过体外和体内研究进行的,称为生物等效性研究。目的:以对照药为参照,确定5 mg格列本脲多源片的体外治疗等效性。材料与方法:多源药物格列本脲5mg和参比药物glidiabetes 5mg均为秘鲁产,购自秘鲁伊卡市一家药店。使用试剂和分析级标准。三种溶出介质均采用300 nm紫外吸收法。结果:在pH为1.2和pH为4.5的条件下,多源药物T和对照药物R在15分钟和30分钟内均未溶解85%。然而,在pH为6.8时发生溶解。这些结果符合美国食品和药物管理局和美国药典的标准。三个试验ph值的相似因子值均在可接受范围(50-100)内。溶出率分别为68.66% (pH 1.2)、56.59% (pH 4.5)和95.98% (pH 6.8)。平均体外溶出时间分别为28.56 min (pH 1.2)、39.97 min (pH 4.5)和4.54 min (pH 6.8)。结论:根据相似因子(f2)和溶出效率,得出本研究多源药物5mg格列本脲与参比药物5mg glidiabetes体外治疗等效的结论。
{"title":"Study of in vitro Therapeutic Equivalence of the 5 mg Glibenclamide Multi-source Tablets Respecting the Reference Medicine Product","authors":"Á. Alvarado-Yarasca, Ana Muñoz-Jauregui, L. Quiñones-Sepúlveda, F. Lizaraso-Soto, A. Salazar-Granara, Luis Sullón-Dextre, Juan J. Palomino-Jhong, Jorge Antonio García-Ceccarelli","doi":"10.4172/2167-065X.1000180","DOIUrl":"https://doi.org/10.4172/2167-065X.1000180","url":null,"abstract":"Introduction: Therapeutic equivalence of medications is carried out through in vitro and in vivo studies called bioequivalence studies. \u0000Objective: To determine the in vitro therapeutic equivalence of the 5 mg glibenclamide multi-source tablets respecting the reference medicine. \u0000Materials and methods: Both, the multi-source drug 5 mg glibenclamide and the reference 5 mg Glidiabet are made in Peru, and were acquired in a drugstore of Ica city (Peru). Reagents and an analytical grade standard were used. The Ultraviolet absorption method at 300 nm was used on each of the three dissolution media. \u0000Results: Neither the multi-source drug T nor the reference R dissolved by 85% at pH 1.2 and at pH 4.5, during 15 or 30 minutes. However, at pH 6.8 dissolution occurs. These results correspond to Food and Drug Administration and United States Pharmacopoeia criteria. The similarity factor value was within the acceptance range (50-100) for the three tested pHs. Dissolution efficiency was 68.66% (pH 1.2), 56.59% (pH 4.5) and 95.98% (pH 6.8). The mean of in vitro dissolution time was 28.56 min (pH 1.2), 39.97 min (pH 4.5) and 4.54 min (pH 6.8). \u0000Conclusion: According to the similarity factor (f2) and the efficiency of dissolution, it is concluded that the multisource drug 5 mg glibenclamide of the present study is therapeutically equivalent in vitro to the reference 5 mg Glidiabet.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83976327","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Pharmacogenomics: The Scientific Basis of Rational Drug Development and Prescribing 药物基因组学:合理药物开发和处方的科学依据
Pub Date : 2017-11-16 DOI: 10.4172/2167-065X.1000179
S. Abraham, H. Jethwa
“It is more important to know what sort of a patient has a disease than what sort of a disease a patient has” (Hippocrates 460 BC-370 BC). The holy grail of drug discovery is to ensure that an individual responds positively to an investigational drug with minimal or no adverse events. This could then translate to newly discovered drugs being licenced for prescribing as safe and effective therapeutics. Pharmacogenomics may herald the technology for this aspiration to become reality. Uniting the disciplines of pharmacology and genomics, pharmacogenomics provides a mechanism to understand and predict the response of an individual to a drug or group of drugs. This is based on the premise that an individual’s genotype affects the pharmacokinetics, pharmacodynamics and, ultimately, the individual’s their response to a drug. This review will begin by reviewing the history of drug development and then proceed to discuss the use of pharmacogenomics in drug development through case studies in oncology, respiratory and vaccinology. It will then go on to discuss how pharmacogenomics presently influences prescribing practices and how this technology may have the potential to enhance patient safety when medicines are administered.
“了解什么样的病人得了什么样的病比了解病人得了什么样的病更重要”(希波克拉底公元前460 -公元前370)。药物发现的终极目标是确保个体对研究药物产生积极反应,而不良事件最少或没有。然后,这可能会转化为新发现的药物,作为安全有效的治疗药物被许可开处方。药物基因组学可能预示着这一愿望成为现实的技术。结合药理学和基因组学的学科,药物基因组学提供了一种机制来理解和预测个体对一种药物或一组药物的反应。这是基于一个前提,即个体的基因型影响药代动力学、药效学,并最终影响个体对药物的反应。本综述将首先回顾药物开发的历史,然后通过肿瘤学、呼吸学和疫苗学的案例研究讨论药物基因组学在药物开发中的应用。然后,它将继续讨论药物基因组学目前如何影响处方实践,以及这项技术如何有可能在给药时提高患者的安全。
{"title":"Pharmacogenomics: The Scientific Basis of Rational Drug Development and Prescribing","authors":"S. Abraham, H. Jethwa","doi":"10.4172/2167-065X.1000179","DOIUrl":"https://doi.org/10.4172/2167-065X.1000179","url":null,"abstract":"“It is more important to know what sort of a patient has a disease than what sort of a disease a patient has” (Hippocrates 460 BC-370 BC). \u0000The holy grail of drug discovery is to ensure that an individual responds positively to an investigational drug with minimal or no adverse events. This could then translate to newly discovered drugs being licenced for prescribing as safe and effective therapeutics. Pharmacogenomics may herald the technology for this aspiration to become reality. \u0000Uniting the disciplines of pharmacology and genomics, pharmacogenomics provides a mechanism to understand and predict the response of an individual to a drug or group of drugs. This is based on the premise that an individual’s genotype affects the pharmacokinetics, pharmacodynamics and, ultimately, the individual’s their response to a drug. \u0000This review will begin by reviewing the history of drug development and then proceed to discuss the use of pharmacogenomics in drug development through case studies in oncology, respiratory and vaccinology. It will then go on to discuss how pharmacogenomics presently influences prescribing practices and how this technology may have the potential to enhance patient safety when medicines are administered.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81676008","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Study of Storage Conditions Effect (Light-Heat) on Natamycin Co ntent and Stability in Some Dairy Products (Cheese-Yoghurt) 储存条件(光热)对某些乳制品(奶酪-酸奶)中纳他霉素含量及稳定性的影响
Pub Date : 2017-09-30 DOI: 10.4172/2167-065X.1000177
A. Nihad, M. Salami
The study aims to determine changes of Natamycin content in some dairy products (cheese-yoghurt) from different local companies in refrigeration conditions (4oC ± 2oC) or different temperatures (25oC ± 2oC , 40oC ± 2oC) and during exposure to sunlight at room temperature (25oC ± 2oC) using ultraviolet spectrophotometer method. This study was based on the collection of samples at the same day (the same type from the same batch) and used to study the effect of temperature and light on natamycin content in these pervious products. Results of analysis showed that exposure to sunlight and different temperature conditions significantly affected the stability of natamycin. A significant negative correlation exists between natamycin and storage time. Natamycin content was more stable in cheese and yoghurt products when stored under refrigeration conditions (4oC ± 2oC) in a dark place. A little significant effect on natamycin content during exposure to room temperature (25oC ± 2oC) without exposure to sunlight. A more significant effect on natamycin content was found during exposure to high temperatures (40oC ± 2oC) compared to effect of sunlight at 25oC ± 2oC. These results showed that dairy products containing natamycin should be kept away from sunlight and high temperatures.
本研究旨在利用紫外分光光度计法测定当地不同公司的部分乳制品(奶酪-酸奶)在冷藏条件(4℃±20℃)、不同温度(25℃±20℃、40℃±20℃)和室温(25℃±20℃)光照条件下纳他霉素含量的变化。本研究是在同一天(同一批次同一类型)采集样品的基础上,研究温度和光照对这些产品中纳他霉素含量的影响。分析结果表明,光照和不同温度条件对纳他霉素的稳定性有显著影响。纳他霉素与贮藏时间呈显著负相关。在冷藏条件(4℃±2℃)下,奶酪和酸奶产品中纳他霉素含量较稳定。室温(25℃±20℃)无光照对纳他霉素含量影响不显著。高温(40℃±20℃)比光照(25℃±20℃)对纳他霉素含量的影响更为显著。这些结果表明,含有纳他霉素的乳制品应远离阳光和高温。
{"title":"Study of Storage Conditions Effect (Light-Heat) on Natamycin Co ntent and Stability in Some Dairy Products (Cheese-Yoghurt)","authors":"A. Nihad, M. Salami","doi":"10.4172/2167-065X.1000177","DOIUrl":"https://doi.org/10.4172/2167-065X.1000177","url":null,"abstract":"The study aims to determine changes of Natamycin content in some dairy products (cheese-yoghurt) from different local companies in refrigeration conditions (4oC ± 2oC) or different temperatures (25oC ± 2oC , 40oC ± 2oC) and during exposure to sunlight at room temperature (25oC ± 2oC) using ultraviolet spectrophotometer method. This study was based on the collection of samples at the same day (the same type from the same batch) and used to study the effect of temperature and light on natamycin content in these pervious products. Results of analysis showed that exposure to sunlight and different temperature conditions significantly affected the stability of natamycin. A significant negative correlation exists between natamycin and storage time. Natamycin content was more stable in cheese and yoghurt products when stored under refrigeration conditions (4oC ± 2oC) in a dark place. A little significant effect on natamycin content during exposure to room temperature (25oC ± 2oC) without exposure to sunlight. A more significant effect on natamycin content was found during exposure to high temperatures (40oC ± 2oC) compared to effect of sunlight at 25oC ± 2oC. These results showed that dairy products containing natamycin should be kept away from sunlight and high temperatures.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82039135","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
The Use of H2-Blockers in Intensive Care h2受体阻滞剂在重症监护中的应用
Pub Date : 2017-08-31 DOI: 10.4172/2167-065X.1000176
P. Kaur, A. Mukherjee, Rutkevich As, Rutkevich Eu, PredkAA Va, Gerasimchik Pa
Treatment plan for a patient in ICU is quite complicated as doctors from different specialities take part in it with advanced methods and machines. But the intensive treatment and diseases of the patient also has complications in itself.
ICU患者的治疗方案是非常复杂的,不同专业的医生参与其中,使用先进的方法和机器。但患者的强化治疗和疾病本身也有并发症。
{"title":"The Use of H2-Blockers in Intensive Care","authors":"P. Kaur, A. Mukherjee, Rutkevich As, Rutkevich Eu, PredkAA Va, Gerasimchik Pa","doi":"10.4172/2167-065X.1000176","DOIUrl":"https://doi.org/10.4172/2167-065X.1000176","url":null,"abstract":"Treatment plan for a patient in ICU is quite complicated as doctors from different specialities take part in it with advanced methods and machines. But the intensive treatment and diseases of the patient also has complications in itself.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78691517","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation of Extended-Release Theophylline for Gastric Tube Administration Significantly Impairs Gradual Resorption 胃管给药缓释茶碱的制备显著损害逐渐吸收
Pub Date : 2017-08-31 DOI: 10.4172/2167-065X.1000175
PapieAA Adriana, Sramek Vladimir, Pesakova Edita, MatiAAakova Libuse, S. Pavel
Background: Although Extended Release (ER) dosage forms are not suitable for administration via Nasogastric Tube (NGT), they are used in critically ill patients. The aim of this study is to compare pharmacokinetics of intact and crushed ER theophylline capsules and tablets. Methods: Open-label, randomized controlled trial with two parallel groups was conducted on 10 healthy volunteers. They were randomized into Theo plus® 300 (ER tablets) and Eupyllin CR N® 300 (capsules with ER pellets) group. Each group took the same drug orally twice-first prepared (for the NGT administration) by crushing and secondly as an intact dosage form. Theophylline serum levels were taken at baseline, 30 min, 60 min, 2 h, 4 h, 6 h, 9 h and 12 h after drug administration. maximum serum concentration (Cmax), time to reach Cmax (Tmax) and area under the serum concentration-time curves over 12 h (AUC12h) were calculated. Data are presented as mean ± SD. Results: Crushing increased Cmax in both Euphyllin (43.8 ± 6.5 vs. 26.5 ± 1.6 μmol/l; p<0.01) and Theoplus (45.2 ± 3.6 vs. 29.4 ± 4.8 μmol/l; p=0.013) groups. Tmax was significantly shorter after administration of crushed dosage forms in Euphyllin (0.9 ± 0.7 vs. 5.6 ± 0.9 h; p<0.001) and Theoplus (1.1 ± 0.5 vs. 9.6 ± 2.5 h; p<0.01) group. Concordantly, drug crushing augmented AUC12 h by 40% in both drugs. Conclusion: Crushing destroyed ER properties of theophylline tablets and capsules and their pharmacokinetic profiles were comparable with immediate release forms.
背景:虽然缓释(ER)剂型不适合通过鼻胃管(NGT)给药,但它们用于危重患者。本研究的目的是比较完整的和粉碎的内质网茶碱胶囊和片剂的药代动力学。方法:对10名健康志愿者进行开放标签、随机对照、两组平行试验。随机分为Theo plus®300 (ER片剂)组和Eupyllin CR N®300 (ER胶囊)组。各组口服同一药物两次,第一次为NGT给药,第二次为完整剂型。分别于给药后基线、30 min、60 min、2 h、4 h、6 h、9 h、12 h测定血清茶碱水平。计算最大血药浓度(Cmax)、达到Cmax所需时间(Tmax)和12h血药-时间曲线下面积(AUC12h)。数据以mean±SD表示。结果:粉碎后两种物质的Cmax均升高(43.8±6.5 vs. 26.5±1.6 μmol/l);p<0.01)和Theoplus(45.2±3.6∶29.4±4.8 μmol/l);p = 0.013)。给药后的Tmax显著缩短(0.9±0.7 vs. 5.6±0.9 h);p<0.001)和Theoplus(1.1±0.5∶9.6±2.5;p < 0.01)。同时,药物粉碎使两种药物的AUC12 h增加了40%。结论:茶碱片剂和胶囊的粉碎破坏内质网性质与立即释放制剂的药动学特征相当。
{"title":"Preparation of Extended-Release Theophylline for Gastric Tube Administration Significantly Impairs Gradual Resorption","authors":"PapieAA Adriana, Sramek Vladimir, Pesakova Edita, MatiAAakova Libuse, S. Pavel","doi":"10.4172/2167-065X.1000175","DOIUrl":"https://doi.org/10.4172/2167-065X.1000175","url":null,"abstract":"Background: Although Extended Release (ER) dosage forms are not suitable for administration via Nasogastric Tube (NGT), they are used in critically ill patients. The aim of this study is to compare pharmacokinetics of intact and crushed ER theophylline capsules and tablets. \u0000Methods: Open-label, randomized controlled trial with two parallel groups was conducted on 10 healthy volunteers. They were randomized into Theo plus® 300 (ER tablets) and Eupyllin CR N® 300 (capsules with ER pellets) group. Each group took the same drug orally twice-first prepared (for the NGT administration) by crushing and secondly as an intact dosage form. Theophylline serum levels were taken at baseline, 30 min, 60 min, 2 h, 4 h, 6 h, 9 h and 12 h after drug administration. maximum serum concentration (Cmax), time to reach Cmax (Tmax) and area under the serum concentration-time curves over 12 h (AUC12h) were calculated. Data are presented as mean ± SD. \u0000Results: Crushing increased Cmax in both Euphyllin (43.8 ± 6.5 vs. 26.5 ± 1.6 μmol/l; p<0.01) and Theoplus (45.2 ± 3.6 vs. 29.4 ± 4.8 μmol/l; p=0.013) groups. Tmax was significantly shorter after administration of crushed dosage forms in Euphyllin (0.9 ± 0.7 vs. 5.6 ± 0.9 h; p<0.001) and Theoplus (1.1 ± 0.5 vs. 9.6 ± 2.5 h; p<0.01) group. Concordantly, drug crushing augmented AUC12 h by 40% in both drugs. \u0000Conclusion: Crushing destroyed ER properties of theophylline tablets and capsules and their pharmacokinetic profiles were comparable with immediate release forms.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79717629","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Comparative Study of the Protective Effect of Metformin and Sitagliptin against Doxorubicin-Induced Cardiotoxicity in Rats 二甲双胍与西格列汀对阿霉素致大鼠心脏毒性保护作用的比较研究
Pub Date : 2017-08-25 DOI: 10.4172/2167-065X.1000174
Mahmoud M. Kamel, Lubna Omar El-Farouk, A. Osman, O. Khorshid, Mohamed El Shabrawy-Abdo
Background and aim: Cancer patients treated with doxorubicin are at high risk to develop cardiotoxicity and hyperglycemia. The present study was designed to compare the effect of the two anti-hyperglycemia drugs; metformin and Sitagliptin, in the prevention of doxorubicin-induced cardiotoxicity in rats. Methods: Cardiotoxicity was induced in male Wistar rats by intraperitoneal injection of cumulative dose of doxorubicin (15 mg/kg over 3 weeks). Metformin or sitagliptin was administrated orally concomitant with intraperitoneal doxorubicin for 3 weeks. Mean body weight, systolic blood pressure, electrocardiographic changes, serum lactate dehydrogenase and creatine kinase-myocardium band, blood glucose and cardiac malondialdhyde level, cardiac histopathological examination and in vitro cardiac contractility in response to isoprenaline were be assessed. Results: Doxorubicin induced marked cardiotoxicity evidenced by significant deterioration in body weight, systolic blood pressure and heart rate, elevation of ST segment, prolongation of QT interval, elevation in the serum level of creatine kinase-myocardiac band and lactate dehydrogenase, blood glucose and cardiac malondialdhyde level and reduced in vitro cardiac contractility in response to isoprenaline compared to control untreated rats. These changes were associated with histopathological evidence of cardiotoxicity. Administration of either metformin or sitagliptin with doxorubicin resulted in significant improvement in all tested parameters compared with doxorubicin treated rats. Metformin treated rats showed more significant improvement in systolic blood pressure, ST segment elevation, serum enzymes, cardiac malondialdhyde, histopathological finding and in vitro cardiac contractility than sitagliptin treated rats. Conclusion: The present study showed that metformin ameliorated doxorubicin-induced cardiotoxicity better than sitagliptin.
背景和目的:接受阿霉素治疗的癌症患者发生心脏毒性和高血糖的风险很高。本研究旨在比较两种抗高血糖药物的效果;二甲双胍和西格列汀在预防阿霉素引起的大鼠心脏毒性中的作用。方法:雄性Wistar大鼠腹腔注射累积剂量阿霉素(15mg /kg,持续3周)致心脏毒性。二甲双胍或西格列汀口服,同时腹腔注射阿霉素3周。评估各组平均体重、收缩压、心电图变化、血清乳酸脱氢酶和肌酸激酶-心肌带、血糖和心脏丙二醛水平、心脏组织病理学检查和异丙肾上腺素对体外心脏收缩力的影响。结果:阿霉素诱导了明显的心脏毒性,表现为与对照组相比,异丙肾上腺素对大鼠的体重、收缩压和心率明显恶化,ST段升高,QT间期延长,血清肌酸激酶-心肌带水平和乳酸脱氢酶水平升高,血糖和心脏丙二醛水平升高,体外心脏收缩力降低。这些变化与心脏毒性的组织病理学证据有关。与阿霉素治疗的大鼠相比,二甲双胍或西格列汀与阿霉素联合用药可显著改善所有测试参数。与西格列汀治疗大鼠相比,二甲双胍治疗大鼠在收缩压、ST段抬高、血清酶、心脏丙二醛、组织病理学检查和体外心脏收缩力方面均有更显著的改善。结论:二甲双胍比西格列汀更能改善阿霉素引起的心脏毒性。
{"title":"Comparative Study of the Protective Effect of Metformin and Sitagliptin against Doxorubicin-Induced Cardiotoxicity in Rats","authors":"Mahmoud M. Kamel, Lubna Omar El-Farouk, A. Osman, O. Khorshid, Mohamed El Shabrawy-Abdo","doi":"10.4172/2167-065X.1000174","DOIUrl":"https://doi.org/10.4172/2167-065X.1000174","url":null,"abstract":"Background and aim: Cancer patients treated with doxorubicin are at high risk to develop cardiotoxicity and hyperglycemia. The present study was designed to compare the effect of the two anti-hyperglycemia drugs; metformin and Sitagliptin, in the prevention of doxorubicin-induced cardiotoxicity in rats. \u0000Methods: Cardiotoxicity was induced in male Wistar rats by intraperitoneal injection of cumulative dose of doxorubicin (15 mg/kg over 3 weeks). Metformin or sitagliptin was administrated orally concomitant with intraperitoneal doxorubicin for 3 weeks. Mean body weight, systolic blood pressure, electrocardiographic changes, serum lactate dehydrogenase and creatine kinase-myocardium band, blood glucose and cardiac malondialdhyde level, cardiac histopathological examination and in vitro cardiac contractility in response to isoprenaline were be assessed. \u0000Results: Doxorubicin induced marked cardiotoxicity evidenced by significant deterioration in body weight, systolic blood pressure and heart rate, elevation of ST segment, prolongation of QT interval, elevation in the serum level of creatine kinase-myocardiac band and lactate dehydrogenase, blood glucose and cardiac malondialdhyde level and reduced in vitro cardiac contractility in response to isoprenaline compared to control untreated rats. These changes were associated with histopathological evidence of cardiotoxicity. Administration of either metformin or sitagliptin with doxorubicin resulted in significant improvement in all tested parameters compared with doxorubicin treated rats. Metformin treated rats showed more significant improvement in systolic blood pressure, ST segment elevation, serum enzymes, cardiac malondialdhyde, histopathological finding and in vitro cardiac contractility than sitagliptin treated rats. \u0000Conclusion: The present study showed that metformin ameliorated doxorubicin-induced cardiotoxicity better than sitagliptin.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90620794","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
Commercializing Biosimilar: Challenges, Strategies and Finding Path toSuccess 生物仿制药商业化:挑战、策略和成功之路
Pub Date : 2017-08-21 DOI: 10.4172/2167-065X.1000173
Prashant A Pandya
Biosimilars and reference biologics have the same amino acid sequences. Differences in clinically inactive components are generally quite minor. Developments of Bio similar involve a series of complex decision and anyone of which have significant impact on Organization success. Early risk identification allows companies to put preventive measures in place to save development time and maximize return on investment. There are numerous development and regulatory constraints associated with biosimilar development affecting decision of commercialization. It is important to optimize commercialization strategies as regulations are still evolving hence it is vital for the companies to quickly modify biosimilar development strategies matching with the regulatory scenario.
生物仿制药和参比生物制剂具有相同的氨基酸序列。临床无活性成分的差异通常相当小。生物相似的开发涉及一系列复杂的决策,其中任何一个决策都对组织的成功产生重大影响。早期的风险识别允许公司采取适当的预防措施,以节省开发时间并最大化投资回报。与生物类似药开发相关的许多开发和监管限制影响了商业化决策。优化商业化战略非常重要,因为法规仍在不断发展,因此公司快速修改与监管情景相匹配的生物类似药开发战略至关重要。
{"title":"Commercializing Biosimilar: Challenges, Strategies and Finding Path toSuccess","authors":"Prashant A Pandya","doi":"10.4172/2167-065X.1000173","DOIUrl":"https://doi.org/10.4172/2167-065X.1000173","url":null,"abstract":"Biosimilars and reference biologics have the same amino acid sequences. Differences in clinically inactive components are generally quite minor. Developments of Bio similar involve a series of complex decision and anyone of which have significant impact on Organization success. Early risk identification allows companies to put preventive measures in place to save development time and maximize return on investment. There are numerous development and regulatory constraints associated with biosimilar development affecting decision of commercialization. It is important to optimize commercialization strategies as regulations are still evolving hence it is vital for the companies to quickly modify biosimilar development strategies matching with the regulatory scenario.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89282481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Importance of Bioavailable Calcium and Other Minerals to Reduce the Calcium Deficiency Symptoms, Aging, and Other Pertinent Diseases 生物可利用钙和其他矿物质对减少缺钙症状、衰老和其他相关疾病的重要性
Pub Date : 2017-08-12 DOI: 10.4172/2167-065X.1000172
M. Reddy
In this review/research article the effect of supplementation of bioavailable calcium to treat or eliminate osteopenia and osteoporosis has been discussed. Various aliments which can be corrected through supplementation of the bioavailable calcium have been documented. The transport of bioavailable calcium (both active and passive) and the conditions under which such transport systems get hampered have also been discussed. The importance of Multiple Mixed Strain Probiotics to improve not only the bioavailability but also absorption and assimilation of calcium and other major and minor minerals has also been stressed.
在这篇综述/研究文章中讨论了补充生物可利用钙治疗或消除骨质减少和骨质疏松症的效果。可以通过补充生物可利用钙来纠正的各种营养物质已被记录在案。生物可利用钙(活性和被动)的运输以及这种运输系统受到阻碍的条件也进行了讨论。强调了多种混合菌株益生菌对提高生物利用度和钙及其他主要和次要矿物质的吸收和同化的重要性。
{"title":"Importance of Bioavailable Calcium and Other Minerals to Reduce the Calcium Deficiency Symptoms, Aging, and Other Pertinent Diseases","authors":"M. Reddy","doi":"10.4172/2167-065X.1000172","DOIUrl":"https://doi.org/10.4172/2167-065X.1000172","url":null,"abstract":"In this review/research article the effect of supplementation of bioavailable calcium to treat or eliminate osteopenia and osteoporosis has been discussed. Various aliments which can be corrected through supplementation of the bioavailable calcium have been documented. The transport of bioavailable calcium (both active and passive) and the conditions under which such transport systems get hampered have also been discussed. The importance of Multiple Mixed Strain Probiotics to improve not only the bioavailability but also absorption and assimilation of calcium and other major and minor minerals has also been stressed.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75776960","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 4
Influence of Bile Salts as Excipients in Ranitidine, Aminophylline and Phenobarbital Tablets on Dissolution Rate 胆汁盐作为辅料对雷尼替丁、氨茶碱、苯巴比妥片溶出度的影响
Pub Date : 2017-05-31 DOI: 10.4172/2167-065X.1000171
M. Pocuca, J. Cvejić, S. Vukmirović, N. Stilinović, K. Kuhajda, S. Kevrešan, M. Mikov
Aim: The aim of this study is to investigate the influence of bile salts, sodium cholate, sodium 12-ketocholate and sodium dehydrocholate, as excipients in ranitidine, aminophylline and phenobarbital tablets on dissolution rate. Methods: Four groups of tablets (control without bile salts and three investigational groups containing different bile salts) were prepared for three different drug substances: ranitidine, aminophylline and phenobarbital. Dissolution rate was measured. Results: Dissolution rate is increased significantly in all investigational groups comparing to the control group in all three drug substances. Discussion: Presented results are very favourable and encouraging in case of dissolution enhancing and should be further investigated, especially in drug substances that are classified in class II and IV as per Biopharmaceutical Classification System (BCS) classification. Conclusion: Bile acid salts are very promising excipients, proven to act as surfactants and as lubricants. Running title: Bile salts as excipients in ranitidine, aminophylline and phenobarbital tablets.
目的:考察胆盐、胆酸钠、12-酮胆酸钠和去氢胆酸钠作为辅料在雷尼替丁、氨茶碱和苯巴比妥片中的溶出度。方法:采用雷尼替丁、氨茶碱、苯巴比妥三种不同原料药配制四组片剂(不含胆盐的对照组和含不同胆盐的试验组)。测定溶出率。结果:三种原料药的溶出率在各研究组均较对照组显著提高。讨论:在溶出度增强的情况下,目前的结果是非常有利和令人鼓舞的,应该进一步调查,特别是根据生物制药分类系统(BCS)分类被分类为II类和IV类的原料药。结论:胆汁酸盐是一种很有前景的赋形剂,具有表面活性剂和润滑剂的作用。标题:胆汁盐作为雷尼替丁、氨茶碱和苯巴比妥片的辅料。
{"title":"Influence of Bile Salts as Excipients in Ranitidine, Aminophylline and Phenobarbital Tablets on Dissolution Rate","authors":"M. Pocuca, J. Cvejić, S. Vukmirović, N. Stilinović, K. Kuhajda, S. Kevrešan, M. Mikov","doi":"10.4172/2167-065X.1000171","DOIUrl":"https://doi.org/10.4172/2167-065X.1000171","url":null,"abstract":"Aim: The aim of this study is to investigate the influence of bile salts, sodium cholate, sodium 12-ketocholate and sodium dehydrocholate, as excipients in ranitidine, aminophylline and phenobarbital tablets on dissolution rate. \u0000Methods: Four groups of tablets (control without bile salts and three investigational groups containing different bile salts) were prepared for three different drug substances: ranitidine, aminophylline and phenobarbital. Dissolution rate was measured. \u0000Results: Dissolution rate is increased significantly in all investigational groups comparing to the control group in all three drug substances. \u0000Discussion: Presented results are very favourable and encouraging in case of dissolution enhancing and should be further investigated, especially in drug substances that are classified in class II and IV as per Biopharmaceutical Classification System (BCS) classification. \u0000Conclusion: Bile acid salts are very promising excipients, proven to act as surfactants and as lubricants. Running title: Bile salts as excipients in ranitidine, aminophylline and phenobarbital tablets.","PeriodicalId":10410,"journal":{"name":"Clinical Pharmacology & Biopharmaceutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2017-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83816211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
期刊
Clinical Pharmacology & Biopharmaceutics
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1