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Comparative Dissolution and Disintegration Study of Different Brands of Linezolid 600 mg Tablets Available in Karachi, Pakistan 巴基斯坦卡拉奇市不同品牌利奈唑胺600 mg片剂溶出度与崩解度比较研究
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000602
Uddin As
The dissolution and disintegration tests (USP) are extensively useful for the determination of the safe and effective drugs as well as used for the stability and quality of the drug product. The purpose of the study was to observe the disintegration and dissolution profile (UV spectrophotometer), and estimation of the quality through weight variation and hardness test of different brands of Linezolid 600 mg tablets from Karachi, Pakistan. The weight variation test for all the brands was found to be under normal limits and the hardness of all the brands was also within normal limits. The tablet disintegration time was as per the specifications and all the tablets were disintegrated within 30 minutes except for brand C3, which disintegrates within 3.98 minutes and provided better disintegration time. Although, all the brands showed better dissolution rate, but the percent drug release of C1 was found to be the best, i.e. 100% drug was dissolved in 30 minutes in contrast to the different brands. Dissolution test is comparatively an efficient and cost effective in vitro approach that can be helpful in the assessment of the release attributes of formulation. It was found that brand C1 and C2 exhibited better dissolution profile as compared to other brands. Although, C3 and C4 were also found to be under the limits i.e. 80 % of the label amount of the drug.
溶出崩解试验(USP)广泛用于安全有效药物的测定以及药品的稳定性和质量。研究了产自巴基斯坦卡拉奇的利奈唑胺600 mg片剂的崩解、溶出度,并通过重量变化和硬度试验对其质量进行了评价。所有品牌的重量变化试验均在正常范围内,所有品牌的硬度也在正常范围内。崩解时间按规格执行,除C3品牌崩解时间为3.98 min外,其余片剂均在30 min内崩解,崩解时间较长。虽然各品牌的溶出率均较好,但与不同品牌相比,C1的释药百分率最好,即30分钟内药物100%溶出。溶出度试验是一种较为有效和经济的体外方法,可用于评价制剂的释放特性。结果表明,与其他品牌相比,C1和C2品牌具有更好的溶出度。虽然,C3和C4也被发现在限制范围内,即药物标签量的80%。
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引用次数: 1
Role of Blood Retinal Barrier in Drug Absorption 血液视网膜屏障在药物吸收中的作用
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000585
Tyagi A, S. Pk, Malviya R
The blood-retinal barrier is the one of the earliest retinal changes in diabetes. The blood retinal barrier is a physiological barrier that regulates ion, protein and water flux in inner and outer retina. In blood-retinal barrier function vitreous fluorophotometry technique is an excellent technique to quantitate. The two most relevant retinal diseases are diabetic retinopathy and age related macular degeneration (AMD), are directly associated with alterations of the Blood retinal barrier (BRB). In this review, the authors also mentioned tracer molecules for evaluating the blood retinal barrier integrity.
血视网膜屏障是糖尿病患者视网膜最早的变化之一。血视网膜屏障是调节视网膜内外离子、蛋白质和水通量的生理屏障。在血视网膜屏障功能中,玻璃体荧光光度法是一种很好的定量方法。两种最相关的视网膜疾病是糖尿病视网膜病变和年龄相关性黄斑变性(AMD),它们与血液视网膜屏障(BRB)的改变直接相关。在这篇综述中,作者还提到了用于评估血液视网膜屏障完整性的示踪分子。
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引用次数: 5
Implementing Laboratory Safety in the Academic Settings 在学术环境中实施实验室安全
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000E195
Purohit Ss
Safety in the chemistry laboratory is undoubtedly a primary concern as safe environment at any workplace ensures the better quality and productivity. The death of Marie Curie due to aplastic anemia brought on by exposure to radiation while carrying test tubes of radium in her pockets during her research is a wellknown example that proves the importance of safety in the field of chemistry. Fatal accidents occurred in the academic laboratories in the recent past have drawn the attention of federal authorities and media and have thus highlighting the importance of teaching and implementation of laboratory safety in the academic settings [1-8]. It is crucial to develop a genuine safety culture in research and teaching laboratories in the academic institutions. Hence, formalized safety training must be enforced not just to the students but also to the faculty and nonteaching staff personnel.
化学实验室的安全无疑是一个首要问题,因为任何工作场所的安全环境都能确保更好的质量和生产力。居里夫人(Marie Curie)在进行研究时,口袋里装着镭试管,由于受到辐射而死于再生障碍性贫血,这是一个众所周知的例子,证明了安全在化学领域的重要性。最近发生在学术实验室的致命事故引起了联邦当局和媒体的注意,因此强调了学术环境中实验室安全教学和实施的重要性[1-8]。在学术机构的研究和教学实验室中建立真正的安全文化至关重要。因此,正式的安全培训必须强制执行,不仅对学生,而且对教师和非教学人员。
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引用次数: 1
Design of Sustained Action Dosage Forms; Mini-Review 持续作用剂型的设计本文着重
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000593
Aah Abdellatif
Greatest idealized per-oral sustained action products have been formulated in the form of oral dosage forms such as capsules or tablets. The characteristic trouble of preparing sustained action liquids has controlled the availability of such dosage forms. Encapsulated long-acting dosage forms have two particular benefits over capsules and tablet designs. Firstly, the inability to be disintegrated which may persist in the stomach for long periods of time, extremely suspending in the stomach and retard the absorption of maintenance dose. Secondly, the disintegration of the capsule shell in the gastric fluid releases particles that pass across the pyloric valve. Also, the release of drug by a meaningful fraction of the granules is highly possible. If a tablet fails to release drug, the entire maintenance dose is lost. This review discusses the different methods for enhancing the sustained drug action.
最理想的口服持续作用产品是以口服剂型如胶囊或片剂的形式配制的。制备持续作用液体的特有困难控制了这种剂型的可用性。与胶囊和片剂设计相比,封装的长效剂型有两个特别的好处。一是不能分解,在胃中存留时间较长,在胃中极度悬浮,延缓维持剂量的吸收。其次,胃液中胶囊壳的解体释放出穿过幽门阀的颗粒。此外,药物释放的颗粒的一个有意义的部分是非常可能的。如果片剂不能释放药物,整个维持剂量就失去了。本文综述了提高药物持续作用的不同方法。
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引用次数: 1
Development and Validation of a Liquid Chromatographic Method for the Quantification of Related Compounds in Cyclophosphamide 环磷酰胺中相关化合物的液相色谱定量方法的建立与验证
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000595
S. Islam, Murugan, P. Kumari, N. Shabbhag
A simple reverse- phase high performance liquid chromatographic method (RP-HPLC) was developed for quantification of the related compounds in Cyclophosphamide. The chromatographic separation was achieved with C18 column (250 × 4.6 mm, 5 µm particle size) with gradient elution composed of 0.02 M Potassium dihydrogen phosphate (pH-7.0) as mobile phase-A and 60:40% v/v Acetonitrile / Water as mobile phase-B at a flow rate of 0.8 mL /min and column compartment maintained at 40° C for separation. Detection was carried out at 195 nm. The correlation coefficient (≥0.99) shows the linearity response against concentration over the range of Limit of Quantification (LOQ). Precision studies showed the Relative Standard Deviation (RSD) values less than 5% for Cyclophosphamide and its related compounds. The method was substantiated with respect to specificity, precision, linearity, accuracy, limit of quantification, and robustness. The proposed method could be used for routine analysis of Cyclophosphamide formulations.
建立了一种简便的反相高效液相色谱法(RP-HPLC)定量测定环磷酰胺中有关化合物的方法。色谱柱为C18 (250 × 4.6 mm,粒径为5µm),流动相为0.02 m磷酸二氢钾(pH-7.0),流动相为60:40% v/v乙腈/水,梯度洗脱,流速为0.8 mL /min,柱室保持在40°C进行分离。在195 nm处进行检测。相关系数≥0.99,在定量限(LOQ)范围内与浓度呈线性关系。精密度研究表明,环磷酰胺及其相关化合物的相对标准偏差(RSD)小于5%。方法在特异性、精密度、线性度、准确度、定量限和稳健性等方面进行了验证。该方法可用于环磷酰胺制剂的常规分析。
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引用次数: 0
Extractable and Leachable Testing in Pharmaceutical Analysis 药物分析中的可萃取和可浸出试验
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000E193
M. Zhong
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引用次数: 1
Validated Reversed-Phase Liquid Chromatographic Method for Simultaneous Determination of Dextromethorphan and Chlorpheniramine in Non-biological and Biological Matrices Using PDA Detector PDA反相液相色谱法同时测定非生物和生物基质中的右美沙芬和氯苯那敏
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000590
H. Shafi, N. Din, Muhammad Imran, M. Sarwar, M. Tahir, S. Khursheed
A simple, precise and sensitive reversed-phase HPLC method using Photo-diode array detector for simultaneous determination of dextromethorphan (DXM) and chlorpheniramine (CLP) in various matrices had been developed and validated. The separation was achieved within 8 minutes on a C-18 column (15 cm x 4.6 mm x 5 μm) using methanol/ pH 3.0 potassium dihydrogen phosphate buffer (60:40, v/v) mobile phase in an isocratic elution mode with flow rate 0.8 mL/min and UV-detection at 230 nm. External standard was employed for quantification. The current method demonstrated good linearity ranged 1-200 μg/mL for CLP (retention time 3.83 ± 0.10 min) with r2 of 0.9994 and 2-1000 μg/mL for DXM (retention time 5.02 ± 0.10 min) with R2 of 0.9993. The limits of detection and quantification were 0.25 μg/mL and 1.0 μg/mL for CLP and 0.50 μg/mL and 1.5 μg/mL for DXM. No interference from matrices was observed and samples remained stable in the HPLC injector for 12 h. The developed method was accurate that employed a simple liquid/liquid extraction procedure with recovery ranged 90.0%-101.9% for both analytes. Intra and inter-day precision were less than 2.5%. The method was proved robust and reproducible that is applicable to pharmaceutical (active raw materials, syrups) and biological (blood) matrices.
建立了一种简便、精确、灵敏的光电二极管阵列反相高效液相色谱法同时测定各种基质中右美沙芬(DXM)和氯苯那敏(CLP)的方法,并进行了验证。色谱柱为C-18 (15 cm × 4.6 mm × 5 μm),流动相为甲醇/ pH 3.0磷酸二氢钾缓冲液(60:40,v/v),流速为0.8 mL/min,流速为230 nm,等密度洗脱,分离时间为8 min。采用外标法定量。本方法对CLP(保留时间3.83±0.10 min)的线性范围为1 ~ 200 μg/mL, r2为0.9994;对DXM(保留时间5.02±0.10 min)的线性范围为2 ~ 1000 μg/mL, r2为0.9993。CLP的检测限和定量限分别为0.25、1.0 μg/mL和0.50、1.5 μg/mL。样品在高效液相色谱进样器中保持稳定12 h,无基质干扰。该方法准确,采用简单的液/液萃取工艺,两种分析物的回收率为90.0% ~ 101.9%。日内和日内精度均小于2.5%。结果表明,该方法稳健性好,重复性好,适用于药物(活性原料、糖浆)和生物(血液)基质。
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引用次数: 6
Effect of a Dietary Supplement Containing Raspberry Ketone on CYP3A Activity in Healthy Women 含覆盆子酮膳食补充剂对健康女性CYP3A活性的影响
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000587
T. Aomori, J. Qi, Y. Okada, Katsunori Nakamura, H. Hiraoka, T. Araki, Tomonori Nakamura, R. Horiuchi, Koujirou Yamamoto
Objective: Raspberry ketone (RK) is available as a supplement with effect on weight gain suppression. Recent studies have found that various herbal products can affect the activities of drug metabolizing enzymes and drug efflux proteins, and provoke clinically relevant drug-drug interactions. Capsaicin, a molecule having a similar chemical structure to RK, is another well-known cytochrome P450 (CYP) inhibitor. On the other hand, it is totally unclear whether RK has any effect on human CYP activities. In this study, we evaluated the effect of orally administered RK on CYP3A activity by measuring 6beta-hydroxycortisol/cortisol ratio in urine samples. Methods: This clinical study was conducted with approval by the Institutional Review Board at Gunma University Hospital. A total of 7 healthy women aged between 20 and 35 years were included and all of them provided written informed consent. Urine samples were collected from all subjects on the morning of day 5 (± 1 day) of menstrual cycle. In the subsequent RK phase, subjects took 3 tablets (16.7 mg/tab) of RK 3 times daily for 7 days, followed by urine sampling on the morning of day 8. In the control phase, the second morning urine sampling was performed 8 days after the first sampling. Urine 6 beta-hydroxycortisol and cortisol concentrations were measured by HPLC UV method and the 6 beta-hydroxycortisol to cortisol ratio was compared between the two phases. Results: The mean basal and assessment ratios in the RK phase were 7.49 ± 4.76 and 9.20 ± 8.05, respectively, while the corresponding ratios in the control phase were 5.36 ± 3.17 and 5.19 ± 4.61, showing no significant difference in either phase. Conclusion: RK does not affect CYP3A activity.
目的:树莓酮(RK)作为一种具有抑制体重增加作用的补充剂。最近的研究发现,各种草药产品可以影响药物代谢酶和药物外排蛋白的活性,并引起临床相关的药物-药物相互作用。辣椒素是另一种众所周知的细胞色素P450 (CYP)抑制剂,与RK具有相似的化学结构。另一方面,RK是否对人类CYP活性有影响尚不清楚。在这项研究中,我们通过测量尿液样本中的6 -羟基皮质醇/皮质醇比值来评估口服RK对CYP3A活性的影响。方法:本临床研究经群马大学附属医院机构审查委员会批准进行。共有7名年龄在20至35岁之间的健康妇女被纳入研究,她们都提供了书面知情同意。所有受试者于月经周期第5天(±1天)上午采集尿样。在随后的RK阶段,受试者每天服用3次RK 3片(16.7 mg/片),连续7天,然后在第8天早上进行尿液采样。在对照阶段,第一次尿样8天后进行第二次晨尿取样。采用高效液相色谱-紫外分光光度法测定尿液中6 -羟基皮质醇和皮质醇的浓度,比较两相间6 -羟基皮质醇与皮质醇的比值。结果:RK期的平均基础比和评估比分别为7.49±4.76和9.20±8.05,对照期的平均基础比和评估比分别为5.36±3.17和5.19±4.61,两期差异均无统计学意义。结论:RK不影响CYP3A活性。
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引用次数: 0
Development and Validation of Mefenamic Acid, Dicyclomine HCl and Pamabrom in Marketed Formulation by HPLC 甲氧胺酸、盐酸双环胺和帕玛溴的高效液相色谱法开发与验证
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000594
Ajay Kumar, P. Chawla, P. Porwal, R. Rawal, D. Anghore
Method has been validated by using spectrophotometric and chromatographic techniques for Mefenamic acid (MEF), Dicyclomine Hydrochloride (DCL) and Pamabrom (PABr) in bulk powder and in pharmaceutical formulations, with a high degree of specificity, selectivity and assurances, method for the drug combination has been not reported. The objectives were to develop and validate a simple, precise and accurate UV and RPHPLC method for simultaneous estimation of mefenamic acid, dicyclomine hydrochloride and pamabrom from multicomponent tablet dosage form. The first Vierdot’s method was performed and absorption maxima of MEF, DCL and PABr at 285, 218 and 278 nm, respectively. Calibration graphs were established in the range of 2-24 μg/mL. The retention time were found to be 5.789, 2.522 and 4.284 min. respectively. UV and HPLC methods were developed and validated for pharmaceutical dosages forms.
采用分光光度和色谱技术对散粉和制剂中的甲芬那酸(MEF)、盐酸二环胺(DCL)和帕玛溴龙(PABr)进行了验证,具有高度的特异性、选择性和保证性,联合用药方法尚未见报道。目的:建立一种简便、精确、准确的紫外分光光度法和高效液相色谱法同时测定多组分片剂中甲氧胺、盐酸二环明和帕玛溴的方法。采用第一种Vierdot法,MEF、DCL和PABr分别在285、218和278 nm处达到最大吸光度。在2 ~ 24 μg/mL范围内建立校准图。停留时间分别为5.789、2.522和4.284 min。建立并验证了紫外分光光度法和高效液相色谱法测定药物剂型的方法。
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引用次数: 4
The chemical and pharmacological variability of key bio-actives present in commercially available Angelica sinensis, Glycyrrhiza uralensis and Rhodiola rosea samples 市售当归、乌拉尔甘草和红景天样品中主要生物活性成分的化学和药理学差异
Pub Date : 2018-01-01 DOI: 10.4172/2153-2435.1000596
H. Suresh, M. Low, Mariam Jarouche, Gang Zheng, Lin Zhang, Samiuela Lee, Jarryd L Pearson, D. Power, Swastika Singh, C. G. Li, C. Khoo
There is global demand for better quality control (QC) of medicinal herbs including standardisation of bioactive chemical components and pharmacological testing. The quantitative variability of key chemical markers in A. sinensis, G. uralensis and R. rosea from several sources and the pharmacological activity was determined to confirm that the chemical markers’ variability is linked to the biological activity. To quantify the chemical variation, three novel, simple and rapid UPLC-PDA-ESI-MS/MS methods were developed and validated. The qualitative chemical variability of the bio-actives was further studied using 1H NMR metabolomics and principal component analysis (PCA). The pharmacological anti-inflammatory activity of the commercials extracts and marker compounds was assessed using the Griess reagent NO scavenging assay. The A. sinensis samples exhibited the greatest chemical fold-variation while G. uralensis showed the least chemical variability. R. rosea samples indicate the presence of other Rhodiola sub-species. The PCA clustering was consistent with observed trends and identified adulteration. The bioactivity of the selected marker compounds was linked to the extracts activity. The use of PCA analysis and in vitro anti-inflammatory testing improve and provide rationale for better QC of herbal extracts.
全球需要更好的药材质量控制(QC),包括生物活性化学成分和药理学测试的标准化。通过对不同来源中华沙棘、乌拉尔沙棘和玫瑰沙棘关键化学标记的数量变异和药理活性的测定,证实了化学标记的变异与生物活性有关。为了定量测定其化学变化,建立了三种新颖、简单、快速的UPLC-PDA-ESI-MS/MS方法,并进行了验证。利用1H NMR代谢组学和主成分分析(PCA)进一步研究了生物活性成分的定性化学变异。采用Griess试剂NO清除法对商业提取物和标记化合物的药理抗炎活性进行评估。中华沙棘的化学折叠变异最大,乌拉尔沙棘的化学折叠变异最小。红景天样品表明存在其他红景天亚种。PCA聚类与观察到的趋势一致,并确定了掺假。所选标记化合物的生物活性与提取物的活性有关。主成分分析和体外抗炎试验的使用改善了草药提取物的质量控制,并为草药提取物的质量控制提供了依据。
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引用次数: 0
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Pharmaceutica Analytica Acta
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