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Microbiological profile of lower respiratory tract infections in neurological intensive care unit of a tertiary care center from Central India. 下呼吸道感染的微生物谱在印度中部三级护理中心的神经重症监护病房。
Pub Date : 2013-06-01 DOI: 10.4103/0976-0105.118789
Trupti Bajpai, G Shrivastava, G S Bhatambare, A B Deshmukh, V Chitnis

Background: Lower respiratory tract infections (LRTI's) are the most frequent infections among patients in intensive care units. The consequences of increased drug resistance are far reaching since bacterial infection of the lower respiratory tract (LRT) is a major cause of death from infectious disease.

Objective: The study was conducted with the aim of determining the bacterial etiology of LRTI in the neuro intensive care unit (NICU) as well as to update the clinicians with the various antimicrobial alternatives available in the treatment of LRTI.

Subjects and methods: The study was conducted for the period of 3 years from January 2010 to December 2012 in the Microbiology Department of a Teaching Tertiary Care Hospital. The LRT specimens from 230 patients admitted in a NICU during the study period were processed. Following culture, the isolated organisms were identified and antimicrobial sensitivity was performed by standard methods.

Results: Out of the 230 LRT specimens evaluated, 198 (86.08%) were culture positive. A total of 254 pathogens were recovered with a predominance of Gram-negative isolates (n = 243; 96.05%) Pseudomonas aeruginosa was the most dominant pathogen followed by Klebsiella pneumoniae. Alarmingly high percentage of extended spectrum beta-lactamase and methicillin resistant Staphylococcus aureus isolates were detected. The resistance to cephalosporins, aminoglycosides and carbapenem were remarkable.

Conclusions: Therefore, we can conclude that for effective management of LRTI's, an ultimate and detailed bacteriological diagnosis and susceptible testing is required to overcome global problem of antibiotic resistance.

背景:下呼吸道感染(LRTI’s)是重症监护病房患者中最常见的感染。由于细菌感染下呼吸道(LRT)是传染病死亡的主要原因,耐药性增加的后果影响深远。目的:本研究的目的是确定神经重症监护病房(NICU)下呼吸道感染的细菌病因,并向临床医生提供治疗下呼吸道感染的各种可选抗菌药物。研究对象和方法:研究于2010年1月至2012年12月在某三级教学医院微生物科进行,为期3年。对研究期间入住NICU的230例患者的LRT标本进行处理。培养后,对分离的微生物进行鉴定,并采用标准方法进行抗菌敏感性测试。结果:230例LRT标本中,培养阳性198例(86.08%)。共检出254株病原菌,以革兰氏阴性菌株为主(n = 243;96.05%)铜绿假单胞菌是最大的病原菌,其次是肺炎克雷伯菌。检测到广谱β -内酰胺酶和耐甲氧西林金黄色葡萄球菌分离株的比例高得惊人。对头孢菌素类、氨基糖苷类和碳青霉烯类的耐药性显著。结论:为了有效管理LRTI,需要最终和详细的细菌学诊断和敏感检测,以克服抗生素耐药性的全球性问题。
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引用次数: 30
Antimicrobial resistance pattern in a tertiary care hospital: An observational study. 三级护理医院的抗菌药物耐药模式:一项观察性研究。
Pub Date : 2013-06-01 DOI: 10.4103/0976-0105.118797
Revathy Saravanan, Vinod Raveendaran

Context: The number of organisms developing resistance to commonly used antibiotics is increasing among the various generations. The exact national scenario of antimicrobial resistance (AMR) is not known in India owing to the absence of a central monitoring agency.

Aims: The aim of this study is to identify the group of organisms developing resistance, to know the classes of drugs against, which resistance has emerged and to assess the possible factors that can favor the development of AMR so that antibiotic policy can be formulated for the proper and effective use of antibiotics.

Settings and design: An observational study was conducted for a period of 1 year from August 2011 to July 2012 in a tertiary care hospital in Pondicherry.

Subjects and methods: Data regarding culture and sensitivity of the organisms isolated from different sources such as urine, blood, wound swab/pus, stool, sputum and tracheal aspirations were collected from the records of the Microbiology Department. Sample processing, identification of organisms to the genus and/or species level and antimicrobial sensitivity were carried out as per the Clinical and Laboratory Standards Institute guidelines on the 999 samples received.

Results: Out of 999 samples, 125 (12.5%) showed significant growth of organisms exhibiting resistance to either single or multiple drugs. Out of 84 (67.2%) in-patients and 41 (32.8%) out-patient samples, Escherichia was the most common organism isolated with a total of 41 (32.8%), followed by Methicillin sensitive Staphylococcus aureus, 26 (20.8%), Klebsiella 25 (20%), Methicillin resistant Staphylococcus aureus 17 (13.6%), Pseudomonas 10 (8%), Proteus 2 (1.6%), 1 (0.8%) each of Citrobacter and Enterococci. Maximum resistance was observed with commonly used first line antimicrobials such as co-trimoxazole, ampicillin, amoxicillin, amoxyclav, fluoroquinolones, third generation cephalosporins and nalidixic acid. Least resistant or highly sensitive were amikacin, nitrofurantoin, gentamycin and doxycycline among the gram-negative bacteria. Macrolides, clindamycin, gentamycin, nitrofurantoin, vancomycin were the most sensitive antimicrobials against the gram-positive bacteria. Lack of knowledge on the consequences of inappropriate use of antibiotics was exhibited by 63% of subjects in our study.

Conclusions: AMR was more with hospital acquired organisms and against commonly used antibiotics that are available since long period. Variation of resistance and sensitivity pattern with time and geographical location is identified. Periodic AMR monitoring and rotation of antibiotics are suggested to restrict further emergence of resistance.

背景:在不同的世代中,对常用抗生素产生耐药性的生物体数量正在增加。由于缺乏中央监测机构,目前尚不清楚印度国内抗菌素耐药性的确切情况。目的:本研究的目的是确定产生耐药性的微生物群体,了解对哪些药物产生耐药性,并评估可能有利于抗菌素耐药性发展的因素,以便制定抗生素政策,正确有效地使用抗生素。背景和设计:本研究于2011年8月至2012年7月在本地治里的一家三级保健医院进行了为期1年的观察性研究。对象和方法:从不同来源(如尿液、血液、伤口拭子/脓液、粪便、痰液和气管分泌物)分离的微生物培养和敏感性数据从微生物科的记录中收集。我们按照临床及实验室标准学会的指引,对收到的999个样本进行样本处理、鉴定属及/或种级别的生物及抗菌药物敏感性。结果:在999份样本中,125份(12.5%)显示出对单一或多种药物耐药的微生物显著生长。在84例(67.2%)住院患者和41例(32.8%)门诊患者的样本中,最常见的是埃希菌,共41例(32.8%),其次是甲氧西林敏感金黄色葡萄球菌26例(20.8%),克雷伯菌25例(20%),耐甲氧西林金黄色葡萄球菌17例(13.6%),假单胞菌10例(8%),变形杆菌2例(1.6%),柠檬酸杆菌和肠球菌各1例(0.8%)。常用一线抗菌药如复方新诺明、氨苄西林、阿莫西林、阿莫克拉夫、氟喹诺酮类药物、第三代头孢菌素和萘啶酸耐药性最大。革兰氏阴性菌中耐药最少或高敏感的是阿米卡星、呋喃妥因、庆大霉素和强力霉素。大环内酯类、克林霉素、庆大霉素、呋喃妥英、万古霉素对革兰氏阳性菌最敏感。在我们的研究中,63%的受试者对不适当使用抗生素的后果缺乏了解。结论:抗菌素耐药性多发生在医院获得性微生物和长期使用的常用抗生素上。确定了电阻和灵敏度随时间和地理位置的变化规律。建议定期监测抗菌素耐药性并轮换使用抗生素,以限制耐药性的进一步出现。
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引用次数: 29
Drug utilization pattern in an Omani pediatric population. 阿曼儿科人群的药物利用模式。
Pub Date : 2013-06-01 DOI: 10.4103/0976-0105.118808
K A Al Balushi, F Al-Sawafi, F Al-Ghafri, I Al-Zakwani

Objective: Evidence suggests that medication errors have a higher incidence in children and infants than in adults. At present, there is limited local data that investigates the drug prescription trends in pediatric populations. This study aims at understanding drug utilization patterns in pediatric patients at Sultan Qaboos University Hospital (SQUH), Oman.

Materials and methods: A retrospective cross-sectional study was conducted in the outpatient pediatric clinics and inpatient pediatric wards at SQUH, a tertiary care hospital attached to the Sultan Qaboos University Medical College, Oman.

Results: The average number of drugs per prescription was 2.3 ± 1.5, and it was almost similar in all age groups and in both males and females. About 16% of the study group received antibiotics. Paracetamol was the most prescribed drug in the patients (13%). Respiratory system drugs were the most prescribed class of drugs (22%) and salbutamol was the most prescribed drug in this class.

Conclusions: This study will help in assessing rational usage and cost control of various medications used in the pediatric setting.

目的:有证据表明,儿童和婴儿的用药错误发生率高于成人。目前,调查儿科人群药物处方趋势的当地数据有限。本研究旨在了解阿曼苏丹卡布斯大学医院(SQUH)儿科患者的药物使用模式。材料和方法:在阿曼苏丹卡布斯大学医学院附属的三级保健医院sqh的儿科门诊和儿科住院病房进行了一项回顾性横断面研究。结果:处方平均用药数为2.3±1.5种,各年龄组、男女用药数基本一致。大约16%的研究组接受了抗生素治疗。对乙酰氨基酚是患者使用最多的处方药(13%)。呼吸系统药物是处方最多的一类药物(22%),沙丁胺醇是该类药物中处方最多的一类药物。结论:本研究有助于评估各种儿科用药的合理使用和成本控制。
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引用次数: 21
A conventional HPLC-MS method for the simultaneous determination of ofloxacin and cefixime in plasma: Development and validation. HPLC-MS同时测定血浆中氧氟沙星和头孢克肟的方法:建立与验证。
Pub Date : 2013-03-01 DOI: 10.4103/0976-0105.113606
Mahesh V Attimarad, Ahmed O Alnajjar

Objective: A simple, rapid, and sensitive high performance liquid chromatography-mass spectrometry (HPLC-MS) method was developed and validated for the simultaneous determination of ofloxacin (OFL) and cefixime (CEF) in human plasma using the moxifloxacin as internal standard.

Methodology: Analytes were separated using an Agilent LCMS system equipped with a Zorbax eclipse XBD C18 column (150 mm × 4.6 mm i.d., 5 μm) and using a mobile phase consisting of a mixture of acetonitrile, methanol and 0.5% formic acid in a ratio of 23:10:67% v/v and flow rate was set at 0.6 mL/min. Plasma samples were extracted using the protein precipitation with acetonitrile and analyzed by positive ion mode.

Results: The linearity of the proposed method was investigated in the concentration range of 4-500 ng/mL (r = 0.9996) for OFL and 40-6000 ng/mL (r = 0.9998) for CEF. The lower limits of quantification were 4 ng/mL and 40 ng/mL for OFL and CEF respectively, which reach the level of both drugs possibly found in human plasma. Further, the reported method was validated as per the ICH guidelines and found to be well within the acceptable range.

Conclusion: The proposed method is simple, rapid, accurate, precise, and appropriate for pharmacokinetic and therapeutic drug monitoring in the clinical laboratories.

目的:建立以莫西沙星为内标同时测定人血浆中氧氟沙星(OFL)和头孢克肟(CEF)含量的高效液相色谱-质谱(HPLC-MS)方法,并进行验证。方法:采用安捷伦LCMS系统,配备Zorbax eclipse XBD C18色谱柱(150 mm × 4.6 mm,直径5 μm),流动相为乙腈、甲醇和0.5%甲酸的混合物,比例为23:10:67% v/v,流速为0.6 mL/min。血浆样品用乙腈蛋白沉淀法提取,用正离子模式分析。结果:本方法在OFL浓度范围4 ~ 500 ng/mL (r = 0.9996)和CEF浓度范围40 ~ 6000 ng/mL (r = 0.9998)内具有良好的线性关系。OFL和CEF的定量下限分别为4 ng/mL和40 ng/mL,达到两种药物在人血浆中可能存在的水平。此外,根据ICH指南对报告的方法进行了验证,发现其完全在可接受的范围内。结论:该方法简便、快速、准确、精密度高,适用于临床实验室药代动力学和治疗药物监测。
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引用次数: 19
Brief examination of psychopharmacology. 精神药理学简介。
Pub Date : 2013-03-01 DOI: 10.4103/0976-0105.113611
Abimbola Farinde
Abimbola Farinde Address for correspondence: Dr. Abimbola Farinde, 500 Medical Center blvd, Webster, Texas, USA. E-mail: aofpharm420@hotmail.com Since the 1970s, psychiatry has experienced a transformation with regards to available treatment options which have led to the creation of practitioners who are well-trained and versed in psychopharmacology.[1] Each new year brings the opportunity for new psychotropic medications to be approved for release and marketing to the general public. The decision to initiate a particular psychotropic medication in any given patient can be influenced by many factors but pharmacology is regarded as a significant influential factor in psychiatric treatment decisions. The study of psychopharmacology may serve to answer questions that mental health providers may have about the use of drug treatments for emotional, cognitive, and behavioral disturbances.[2] Previous and current studies that have focused on the study of psychopharmacology have led to the development of several landmark psychotropic medications which have significantly improved the quality of life of many individuals who suffer from different mental illnesses. The quality of life of individuals diagnosed with depression and bipolar disorder have been extensively studied in the literature with both disorders being associated with pervasive impairments in psychosocial functioning.[3] While research struggles to define quality of life related to mental illness due to its consistently evolving nature, psychopharmacology is being recognized as a rapidly developing subject in relation to quality of life measurement. It is becoming increasingly important due to the ongoing evaluation that is required for new drugs that are released on the market, and the need to achieve a balance between therapeutic effects and adverse side-effects.[4] The advent of available psychotropic medications in the various formulations that can aid with the treatment of affective symptoms, mood or behavioral disturbances have improved the lives of many individuals that are diagnosed with a psychiatric, behavioral or emotion disorder.[5] The observed improvements in mental health conditions can be largely attributed to the study of psychopharmacology. [5] From a scientific perspective, psychopharmacology consists of two separate areas that are also clearly related, and this is the influence of drugs on the psychological functioning and the mechanism by which these drugs produce their effects.[6] It is a multifaceted process that examines the influence that drugs have on emotional states, psychological functioning, and psychomotor performance in psychiatric patients, normal patients, and animals.[6] The intended purpose is to examine the therapeutic use or identify the evidence of the effectiveness of these drugs on the regulation of the psychiatric and emotional disorders.[7] The class of drugs that are the primary focus of psychopharmacology for psychiatric and related disorders consi
{"title":"Brief examination of psychopharmacology.","authors":"Abimbola Farinde","doi":"10.4103/0976-0105.113611","DOIUrl":"https://doi.org/10.4103/0976-0105.113611","url":null,"abstract":"Abimbola Farinde Address for correspondence: Dr. Abimbola Farinde, 500 Medical Center blvd, Webster, Texas, USA. E-mail: aofpharm420@hotmail.com Since the 1970s, psychiatry has experienced a transformation with regards to available treatment options which have led to the creation of practitioners who are well-trained and versed in psychopharmacology.[1] Each new year brings the opportunity for new psychotropic medications to be approved for release and marketing to the general public. The decision to initiate a particular psychotropic medication in any given patient can be influenced by many factors but pharmacology is regarded as a significant influential factor in psychiatric treatment decisions. The study of psychopharmacology may serve to answer questions that mental health providers may have about the use of drug treatments for emotional, cognitive, and behavioral disturbances.[2] Previous and current studies that have focused on the study of psychopharmacology have led to the development of several landmark psychotropic medications which have significantly improved the quality of life of many individuals who suffer from different mental illnesses. The quality of life of individuals diagnosed with depression and bipolar disorder have been extensively studied in the literature with both disorders being associated with pervasive impairments in psychosocial functioning.[3] While research struggles to define quality of life related to mental illness due to its consistently evolving nature, psychopharmacology is being recognized as a rapidly developing subject in relation to quality of life measurement. It is becoming increasingly important due to the ongoing evaluation that is required for new drugs that are released on the market, and the need to achieve a balance between therapeutic effects and adverse side-effects.[4] The advent of available psychotropic medications in the various formulations that can aid with the treatment of affective symptoms, mood or behavioral disturbances have improved the lives of many individuals that are diagnosed with a psychiatric, behavioral or emotion disorder.[5] The observed improvements in mental health conditions can be largely attributed to the study of psychopharmacology. [5] From a scientific perspective, psychopharmacology consists of two separate areas that are also clearly related, and this is the influence of drugs on the psychological functioning and the mechanism by which these drugs produce their effects.[6] It is a multifaceted process that examines the influence that drugs have on emotional states, psychological functioning, and psychomotor performance in psychiatric patients, normal patients, and animals.[6] The intended purpose is to examine the therapeutic use or identify the evidence of the effectiveness of these drugs on the regulation of the psychiatric and emotional disorders.[7] The class of drugs that are the primary focus of psychopharmacology for psychiatric and related disorders consi","PeriodicalId":15046,"journal":{"name":"Journal of Basic and Clinical Pharmacy","volume":"4 2","pages":"49-50"},"PeriodicalIF":0.0,"publicationDate":"2013-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/31/af/JBCP-4-49.PMC3979262.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"32323476","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Management of coronary artery disease in a Tertiary Care Hospital. 三级医院冠状动脉疾病的管理。
Pub Date : 2013-03-01 DOI: 10.4103/0976-0105.113605
Pranay Wal, Ankita Wal, Vandana R Nair, A K Rai, Umeshwar Pandey
Aims: The objective of the study was to study the prescribing patterns of drugs used in the coronary artery disease (CAD) and to identify, which drug is mostly prescribed at that hospital. Settings and Design: This was a prospective observational survey including case series analysis of patients with CAD who met the inclusion criteria. It was conducted in the cardiology unit of multidisciplinary Tertiary Care Hospital in Kanpur. Materials and Methods: Data of patients who met the inclusion criteria was collected in specially designed case record forms. It was designed to include the patient data such as, demographics, risk factors, clinical and biochemical characteristics, procedures and investigations performed during the hospital stay, in-hospital and discharge drug therapy. Statistical Analysis Used: Descriptive statistics were performed for baseline characteristics, risk factors and medication use. All the analyses were performed using Statistical Package for Social Sciences version 16.0. Results: Subjects of age groups 65-74 (33.34%) were found to be more susceptible to CAD. In this study, we see that Aspirin, Clopidogrel and Statins were mostly prescribed in this hospital. Conclusions: In this study, Aspirin and Clopidogrel were mostly prescribed. According to 2009 focused updates of American College of Cardiology/American Heart Association (ACC/AHA) guidelines for the management of patients with ST-elevation Myocardial Infarction. So in this hospital prescription for CAD were according to the guideline.
目的:本研究的目的是研究冠状动脉疾病(CAD)药物的处方模式,并确定该医院最常用的药物。背景和设计:这是一项前瞻性观察性调查,包括对符合纳入标准的CAD患者进行病例系列分析。该研究在坎普尔多学科三级保健医院的心脏病科进行。材料与方法:采用专门设计的病例记录表收集符合纳入标准的患者资料。其目的是纳入患者数据,如人口统计、风险因素、临床和生化特征、住院、住院和出院药物治疗期间进行的程序和调查。采用的统计分析:对基线特征、危险因素和用药情况进行描述性统计。所有分析均使用Statistical Package for Social Sciences version 16.0进行。结果:65 ~ 74岁人群(33.34%)易患冠心病。在这项研究中,我们看到阿司匹林、氯吡格雷和他汀类药物主要是在这家医院开的。结论:本研究以阿司匹林和氯吡格雷为主。根据2009年美国心脏病学会/美国心脏协会(ACC/AHA) st段抬高型心肌梗死患者管理指南的重点更新。所以在这家医院,CAD的处方是根据指南的。
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引用次数: 12
A review on proniosomal drug delivery system for targeted drug action. 综述用于靶向药物作用的代膜给药系统。
Pub Date : 2013-03-01 DOI: 10.4103/0976-0105.113609
G V Radha, T Sudha Rani, B Sarvani

Proniosomes are dry formulation of water soluble carrier particles that are coated with surfactant. They are rehydrated to form niosomal dispersion immediately before use on agitation in hot aqueous media within minutes. Proniosomes are physically stable during the storage and transport. Drug encapsulated in the vesicular structure of proniosomes prolong the existence of drug in the systematic circulation and enhances the penetration into target tissue and reduce toxicity. From a technical point of view, niosomes are promising drug carriers as they possess greater chemical stability and lack of many disadvantages associated with liposomes, such as high- cost and variable purity problems of phospholipids. The present review emphasizes on overall methods of preparation characterization and applicability of proniosomes in targeted drug action.

前列异构体是由表面活性剂包覆的水溶性载体颗粒组成的干燥制剂。使用前,在热的水介质中搅拌几分钟,它们就会重新水化形成药膜分散体。前糖体在储存和运输过程中具有物理稳定性。药物被包裹在代糖体的囊泡结构中,延长了药物在系统循环中的存在时间,增强了对靶组织的渗透,降低了毒性。从技术角度看,代糖体具有更高的化学稳定性,而且没有脂质体的许多缺点,如成本高、磷脂纯度不稳定等问题,因此是一种很有前途的药物载体。本综述重点介绍了前生物体的总体制备方法、特征和在靶向药物作用中的适用性。
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引用次数: 0
Study of pharmacological activities of methanol extract of Jatropha gossypifolia fruits. 麻疯树果实甲醇提取物的药理活性研究。
Pub Date : 2012-12-01 DOI: 10.4103/0976-0105.109404
Apurba Sarker Apu, Faruq Hossain, Farhana Rizwan, Shakhawat Hossan Bhuyan, Maima Matin, A T M Jamaluddin

Objective: The present study was carried out to investigate the possible in vivo analgesic, neuropharmacological and anti-diarrheal activities of the methanol extract of Jatropha gossypifolia fruits.

Materials and methods: The analgesic activity was measured by acetic acid induced writhing inhibition test. The neuropharmacological activities were evaluated by hole cross, hole-board, and elevated plus-maze (EPM) tests and the anti-diarrheal activity was assessed by castor oil induced diarrhea inhibition method.

Findings: The extract showed highly significant (P < 0.001) analgesic activity with % inhibitions of writhing response at doses 200 and 400 mg/kg body weight were 77.86% and 71.25%, respectively. The extract at both doses showed significant (P < 0.05) sedative effect in-hole cross test. In-hole board test, the extract showed highly significant (P < 0.001) anxiolytic activity at lower dose whereas this activity was observed at higher dose in EPM test. The extract also showed highly significant (P < 0.001) anti-diarrheal activity.

Conclusion: The findings of the study clearly indicate the presence of significant analgesic, neuropharmacological and anti-diarrheal properties of the plant, which demands further investigation including, compound isolation.

目的:研究麻疯树果实甲醇提取物的体内镇痛、神经药理和抗腹泻活性。材料与方法:采用醋酸扭体抑制试验测定其镇痛活性。采用交叉孔法、孔板法、升高正迷宫法(EPM)评价其神经药理活性,采用蓖麻油致泻法评价其抗泻活性。结果:黄芪提取物具有极显著的镇痛作用(P < 0.001), 200和400 mg/kg体重组的扭体反应抑制率分别为77.86%和71.25%。孔内交叉试验中,2个剂量的提取物均有显著的镇静作用(P < 0.05)。在孔板试验中,低剂量组表现出极显著的抗焦虑活性(P < 0.001),高剂量组表现出抗焦虑活性。其抗腹泻活性也极显著(P < 0.001)。结论:本研究结果明确表明该植物具有显著的镇痛、神经药理和抗腹泻作用,有待进一步研究,包括化合物分离。
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引用次数: 39
Isolation of anticancer drug TAXOL from Pestalotiopsis breviseta with apoptosis and B-Cell lymphoma protein docking studies. 短拟盘多毛孢中抗癌药物TAXOL的分离与细胞凋亡与b细胞淋巴瘤蛋白的对接研究。
Pub Date : 2012-12-01 DOI: 10.4103/0976-0105.109402
G Kathiravan, Sripathi M Sureban, Harsha N Sree, V Bhuvaneshwari, Evelin Kramony

Background: Extraction and investigation of TAXOL from Pestalotiopsis breviseta (Sacc.) using protein docking, which is a computational technique that samples conformations of small molecules in protein-binding sites. Scoring functions are used to assess which of these conformations best complements the protein binding site and active site prediction.

Materials and methods: Coelomycetous fungi P. breviseta (Sacc.) Steyaert was screened for the production of TAXOL, an anticancer drug.

Results: TAXOL PRODUCTION WAS CONFIRMED BY THE FOLLOWING METHODS: Ultraviolet (UV) spectroscopic analysis, Infrared analysis, High performance liquid chromatography analysis (HPLC), and Liquid chromatography mass spectrum (LC-MASS). TAXOL produced by the fungi was compared with authentic TAXOL, and protein docking studies were performed.

Conclusion: The BCL2 protein of human origin showed a higher affinity toward the compound paclitaxel. It has the binding energy value of -13.0061 (KJ/Mol) with four hydrogen bonds.

背景:利用蛋白质对接技术对短拟盘多毛孢(Sacc.)中紫杉醇的提取和研究。蛋白质对接是一种检测蛋白质结合位点小分子构象的计算技术。评分函数用于评估这些构象中哪一个最能补充蛋白质结合位点和活性位点预测。材料与方法:空腔菌属短叶假单胞菌(Sacc.)对Steyaert进行了筛选,以产生抗癌药物紫杉醇。结果:通过紫外(UV)光谱分析、红外(ir)光谱分析、高效液相色谱(HPLC)和液相色谱质谱(LC-MASS)等方法证实了紫杉醇的生产。将该真菌产的紫杉醇与正品紫杉醇进行了比较,并进行了蛋白对接研究。结论:人源BCL2蛋白对化合物紫杉醇具有较高的亲和力。它与4个氢键的结合能为-13.0061 (KJ/Mol)。
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引用次数: 15
Formulation and evaluation of controlled porosity osmotic pump for oral delivery of ketorolac. 口服给药酮酸控制孔隙度渗透泵的研制及评价。
Pub Date : 2012-12-01 DOI: 10.4103/0976-0105.109398
Fatima Sanjeri Dasankoppa, Mahesh Ningangowdar, Hasanpasha Sholapur

Background: The osmotic drug delivery systems suitable for oral administration typically consist of a compressed tablet core that is coated with a semipermeable membrane that has an orifice drilled on it by means of a laser beam or mechanical drill. Ketorolac is a nonsteroidal agent with powerful analgesic. Oral bioavailability of ketorolac was reported to be 90% with very low hepatic first-pass elimination; the biological half-life of 4-6 hours requires frequent administration to maintain the therapeutic effect.

Aim: The aim of the current study was to design a controlled porosity osmotic pump (CPOP)based drug delivery system for controlled release of an NSAID agent, ketorolac tromethamine, which is expected to improve patient compliance due to reduced frequency; it also eliminates the need for complicated and expensive laser drilling and maintain continuous therapeutic concentration.

Design: The CPOP was designed containing pore-forming water-soluble additives in the coating membrane, which after coming in contact with water, dissolve, resulting in an in situ formation of a micro porous structure.

Materials and methods: The effect of different formulation variables, namely level of pore former (PVP), plasticizer (dibutyl phthalate) in the membrane, and membrane weight gain were studied.

Results and conclusion: Drug release was inversely proportional to the membrane weight but directly related to the initial concentration of pore former (PVP) in the membrane. Drug release was independent of pH and agitational intensity, but dependent on the osmotic pressure of the release media. Based on the in vitro dissolution profile, formulation F3C1 (containing 0.5 g PVP and 1 g dibutyl phthalate in coating membrane) exhibited Peppas kinetic with Fickian diffusion-controlled release mechanism with a drug release of 93.67% in 12 hours and hence it was selected as optimized formulation. SEM studies showed the formation of pores in the membrane. The formulations were stable after 3 months of accelerated stability studies. CPOP was designed for effective administration of drugs for prolonged period of time.

背景:适用于口服给药的渗透给药系统通常由压缩的片剂芯组成,片剂芯涂有半透膜,半透膜上有通过激光束或机械钻在其上钻孔的孔。酮咯酸是一种非甾体类强效镇痛药。据报道,酮咯酸的口服生物利用度为90%,肝脏首过消除率极低;生物半衰期为4-6小时,需要经常给药以维持治疗效果。目的:本研究的目的是设计一种基于可控孔隙渗透泵(CPOP)的非甾体抗炎药酮咯酸三甲胺的控释给药系统,由于频率降低,该系统有望提高患者的依从性;它还消除了复杂和昂贵的激光钻孔的需要,并保持持续的治疗浓度。设计:CPOP的涂层膜中含有成孔水溶性添加剂,该添加剂与水接触后溶解,在原位形成微孔结构。材料与方法:研究了不同配方变量对膜中孔隙成形剂(PVP)、增塑剂(邻苯二甲酸二丁酯)含量、膜增重的影响。结果与结论:药物释放量与膜质量成反比,而与膜中孔隙原(PVP)的初始浓度直接相关。药物释放不受pH值和搅拌强度的影响,而取决于释放介质的渗透压。基于体外溶出度分析,处方F3C1(包膜中含有0.5 g PVP和1 g邻苯二甲酸二丁酯)具有Peppas动力学和Fickian扩散控制释放机制,12 h释药率为93.67%,优选处方F3C1。扫描电镜研究表明,膜上形成了孔隙。经过3个月的加速稳定性研究,配方是稳定的。CPOP是为长期有效给药而设计的。
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引用次数: 25
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Journal of Basic and Clinical Pharmacy
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