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Mass spectrometry-based metabolomics in biomarker-assisted drug discovery and oxidative stress research 基于质谱的代谢组学在生物标志物辅助药物发现和氧化应激研究中的应用
Pub Date : 2017-01-01 DOI: 10.4103/ddt.DDT_2_16
V. Sivaram, AKiran Kumar, S. Devi
Biomarker-assisted drug discovery is a major step in identification of drug efficacy and disease proliferation of both communicable and noncommunicable diseases. Biomarker-assisted drug discovery using metabolomics approach is now a reliable “path of opportunity” in drug discovery, as it offers precise insight into the efficacy of tested drug in the biological setup. With the advent of recent advances in instrumentation, accuracy and specificity of biomarker-based drug discovery program is improved. A key challenge in biomarker discovery is the choice of detection method, as diverse metabolites present in the physiological system pose varying levels of detection response with different instrumentation platforms. In biomarker-assisted early diagnosis, mass spectrometry-based metabolomics has a major advantage due to its capability of wide metabolite range coverage with great specificity. This review also discusses the advantage of biomarker-assisted discovery using metabolome analysis.
生物标志物辅助药物发现是识别传染性和非传染性疾病药物疗效和疾病扩散的重要步骤。使用代谢组学方法的生物标志物辅助药物发现现在是药物发现的可靠“机会之路”,因为它提供了对生物设置中被测试药物功效的精确洞察。随着仪器技术的进步,基于生物标志物的药物发现程序的准确性和特异性得到了提高。生物标志物发现的一个关键挑战是检测方法的选择,因为生理系统中存在的多种代谢物在不同的仪器平台上产生不同水平的检测响应。在生物标志物辅助的早期诊断中,基于质谱的代谢组学具有很大的优势,因为它具有广泛的代谢物范围覆盖和高特异性的能力。本文还讨论了利用代谢组分析进行生物标志物辅助发现的优势。
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引用次数: 0
Comparative analysis of cost and efficacy for mono and dual therapy of antiepileptics among children 儿童抗癫痫药物单药与双药治疗的成本与疗效比较分析
Pub Date : 2017-01-01 DOI: 10.4103/ddt.DDT_16_16
E. Vigneshwaran, Monica Madineni, K. Saké, K. Alakhali, S. A. Sirajudeen, Noohu Abdullah Khan
Introduction: Developing countries contribute to major number of patients living with epilepsy, around five million people are living with epilepsy in India alone. Most of the epileptic children may require multiple antiepileptic therapy due to the failure of monotherapy. Basic research evidence suggest that sodium valproate and carbamazepine (CBZ) may have synergistic anticonvulsant effects when they are used together. In addition to that, chronic disorders make the patients economically weak and produce more burden. Aim and Objective: Therefore, this study was designed to compare the efficacy of valproate monotherapy with valproate and CBZ dual therapy. Methodology: It is a prospective, comparative study conducted at a secondary care referral hospital and private clinic. A nonprobabilistic convenient sampling was done to recruit the study subjects. A total of fifty subjects were recruited into the present study, and they were divided into two groups, i.e., monotherapy group (CBZ) and dual therapy group (CBZ and valproate). After providing appropriate counseling, subjects were interviewed to estimate the quality of life (QOL) using child version of TNO-AZL Children's Quality of Life questionnaire. Hospital patient records, prescription data from the pharmacy were also used to obtain the direct and indirect cost of treatment. Results: Our study results showed that monotherapy has a potential to produce a higher level of QOL than dual therapy. It also involved with decreased seizure frequency. Although there was no statistically significant difference in terms of cost for both the treatment groups, still dual therapy is associated with higher cost burden. The average costs per QOL and changes in the frequency of seizure are also identified to produce higher economic burden to the patients.Conclusion: Thus, the present study has concluded that monotherapy may be considered as better cost-effective treatment in partial seizures than dual therapy, unless if there is no treatment failure with monotherapy.
导言:发展中国家是癫痫患者的主要来源,仅在印度就有约500万人患有癫痫。大多数癫痫患儿由于单药治疗失败,可能需要多次抗癫痫治疗。基础研究证据表明,丙戊酸钠和卡马西平(CBZ)一起使用时可能具有协同抗惊厥作用。此外,慢性疾病使患者经济能力较弱,负担更重。目的:因此,本研究旨在比较丙戊酸单药治疗与丙戊酸与CBZ双药治疗的疗效。方法:这是一项前瞻性的比较研究,在二级保健转诊医院和私人诊所进行。采用非概率方便抽样方法招募研究对象。本研究共招募50名受试者,将其分为两组,即单药治疗组(CBZ)和双药治疗组(CBZ和丙戊酸)。在给予适当的心理辅导后,使用儿童版TNO-AZL儿童生活质量问卷对被试进行访谈,评估其生活质量(QOL)。医院患者记录、药房处方数据也被用于获取治疗的直接和间接费用。结果:我们的研究结果表明,单药治疗比双药治疗有可能产生更高水平的生活质量。它还与癫痫发作频率降低有关。虽然两种治疗组在费用方面没有统计学上的显著差异,但双重治疗仍与较高的费用负担相关。每个生活质量的平均成本和癫痫发作频率的变化也会给患者带来更高的经济负担。结论:因此,本研究得出结论,除非单药治疗没有治疗失败,否则单药治疗可能被认为是部分性癫痫发作比双药治疗更具成本效益的治疗方法。
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引用次数: 0
Development and validation of a liquid chromatography/tandem mass spectrometric method for determination of ethinyl estradiol in human plasma 液相色谱/串联质谱法测定人血浆中乙炔雌二醇的建立与验证
Pub Date : 2017-01-01 DOI: 10.4103/ddt.DDT_5_16
Vijay Kotra, Nageswara Rao Ramisetti, R. Surapaneni, Dr. Sathish Kumar Konidala
Introduction: A simple and rapid bioanalytical liquid chromatography-tandem mass spectrometry (LC-MS/MS) method based on solid phase extraction (SPE) followed by liquid-liquid extraction (LLE) has been developed and validated for quantification of Ethinyl Estradiol in human plasma. Methods: API 5500 LC-MS/MS system with turbo ion-spray interface equipped with pumps (Shimadzu LC-20ADVP), an auto Sampler (Shimadzu SIL-HTC), analytical column SB C18 HT (50 x 3.0 mm, 1.8 μ) and data acquisition system and quantitation program (Applied Biosystems Analyst Software version 1.5, Thermo scientific) was used. The Positive ions were measured in MRM mode for the analyte and Ethinyl Estradiol-d4 used as an internal standard. A composition of 2 mM ammonium formate buffer: acetonitrile (20: 80 v/v) was used as mobile phase. The total run time was 4.0 min. The proposed method has been validated with in the linear range of 5.000–308.560 pg/ml for Ethinyl Estradiol. Results: The retention times of Ethinyl Estradiol and Ethinyl estradiol-d4 were 3.42 min ± 0.30 min and 3.45 min ± 0.30 min respectively. The intraday and interday precision values were within 1.58% to 10.86% and 4.62% to 19.74% respectively for Ethinyl estradiol. The overall recovery for Ethinyl estradiol was found to be 86.91%-103.15%. Conclusion: The method was validated as per ICH guidelines and it would be useful for bioequivalence and pharmacokinetic studies of Ethinyl Estradiol in human plasma.
建立了一种基于固相萃取(SPE) -液-液萃取(LLE)的高效液相色谱-串联质谱(LC-MS/MS)测定人血浆中乙炔雌二醇的方法,并进行了验证。方法:采用API 5500 LC-MS/MS系统,配备涡轮喷雾接口,泵(Shimadzu LC-20ADVP),自动进样器(Shimadzu SIL-HTC),分析柱SB C18 HT (50 x 3.0 mm, 1.8 μ),数据采集系统和定量程序(Applied Biosystems Analyst Software version 1.5, Thermo scientific)。用MRM模式测定分析物的正离子,用Estradiol-d4作为内标。以2 mM甲酸铵缓冲液:乙腈(20:80 v/v)为流动相。总运行时间为4.0 min。所提出的方法在5.000-308.560 pg/ml的线性范围内被验证。结果:雌二醇和雌二醇-d4的保留时间分别为3.42 min±0.30 min和3.45 min±0.30 min。雌二醇日内精密度在1.58% ~ 10.86%之间,日内精密度在4.62% ~ 19.74%之间。乙烯基雌二醇的总回收率为86.91% ~ 103.15%。结论:该方法符合ICH标准,可用于乙炔雌二醇在人血浆中的生物等效性和药代动力学研究。
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引用次数: 1
An ayurvedic formulation Sankat Mochan: A potent anthelmintic medicine 阿育吠陀配方Sankat Mochan:一种有效的驱虫药
Pub Date : 2017-01-01 DOI: 10.4103/ddt.DDT_84_15
K. Sarwa, P. Vishwakarma, V. Suryawanshi, Tilotma Sahu, L. Kumar, Jaya Shree
Aim and Object: Sankat Mochan is an ayurvedic formulation used in the urban and rural area of India. This polyherbal formulation is used for general stomach problems including abdominal cramping and diarrhea. The present investigation evaluated the anthelmintic activity of an aqueous solution of an ayurvedic medicine Sankat Mochan. Materials and Method: Various concentrations (1%, 5%, and 10%) of medicine were used for anthelmintic activity on Pheretima posthuma. Piperazine citrate (10 mg/ml) was used as a reference standard and distilled water as a control. Result and Conclusion: The result showed that the Sankat Mochan possess anthelmintic activity more potent than that of piperazine citrate. Thus, Sankat Mochan may be used as a potent anthelmintic agent against helminthiasis.
目的和用途:Sankat Mochan是印度城市和农村地区使用的阿育吠陀配方。这种多草药配方用于一般胃病,包括腹部痉挛和腹泻。本研究评价了阿育吠陀药Sankat Mochan水溶液的驱虫活性。材料与方法:采用不同浓度(1%、5%、10%)的药物对假金银花进行驱虫活性测定。以柠檬酸哌嗪(10 mg/ml)为标准品,蒸馏水为对照。结果与结论:山茱萸的驱虫活性明显高于枸橼酸哌嗪。因此,Sankat Mochan可作为一种有效的驱虫剂用于治疗寄生虫病。
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引用次数: 4
Efficacy and safety of hepano tablet in liver disorder patients with abnormal liver function test: A randomized active controlled prospective clinical study 肝肽片治疗肝功能异常患者的疗效和安全性:一项随机主动对照前瞻性临床研究
Pub Date : 2017-01-01 DOI: 10.4103/ddt.DDT_12_16
Satyendra Kumar, Arun Gupta, Meenakshi Revadekar, S. More, A. Kulkarni, S. Borkar
Objective: Hepano Tablet is an Ayurvedic herbal formulation studied in pre-clinical models for safety and hepatoprotective efficacy. The current study was a randomized, active controlled, multicentre, prospective clinical study that aimed to evaluate hepatoprotective efficacy and safety of Hepano Tablets. Materials and Methods: Male and female liver diseases patients (18-65 years) with abnormal liver function tests were randomized to receive two tablets twice daily orally of either Hepano or a marketed comparator for 8 weeks with follow up at day 7, 14, 28 & 56 during treatment period and thereafter at day 84. Results were assessed from baseline to end of treatment basis changes in liver function tests and improvement in clinical symptoms of icterus in both the groups. Safety was assessed at all the visits basis changes in laboratory parameters and adverse event reporting for all cases who took at least one dose of the study drug. Results: Hepano Tablet and marketed comparator showed significant improvement in Liver functions - Serum Aspartate transaminase (AST), Alanine transaminase (ALT) and Total, Direct and Indirect Bilirubin Levels and a significant reduction in clinical symptoms of icterus that was comparable at all the visits. Conclusion: Hepano Tablets can significantly improve Liver Function Tests and clinical symptoms in liver disease patients and could be consumed safely.
目的:通过临床前模型研究阿育吠陀草药制剂肝帕诺片的安全性和肝保护作用。目前的研究是一项随机、主动对照、多中心、前瞻性临床研究,旨在评估Hepano片的肝保护功效和安全性。材料与方法:将肝功能检查异常的男性和女性肝病患者(18-65岁)随机分为两组,每天口服2片Hepano或一种市售比较药,疗程为8周,治疗期间第7、14、28和56天随访,随访时间为第84天。结果评估从基线到治疗结束的基础上肝功能检查的变化和黄疸临床症状的改善。在所有访问中,根据实验室参数的变化和所有服用至少一剂研究药物的病例的不良事件报告,对安全性进行评估。结果:肝素片和上市比较药在肝功能、血清谷草转氨酶(AST)、丙氨酸转氨酶(ALT)、总胆红素、直接胆红素和间接胆红素水平上均有显著改善,黄疸临床症状显著减轻,在所有就诊时均具有可比性。结论:肝肽片能明显改善肝病患者的肝功能检查和临床症状,可安全食用。
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引用次数: 2
Development and detection efficiency of sequence characterized amplified region markers for authentication of medicinal plant Ruta graveolens and its adulterant Euphorbia dracunculoides 药用植物石竹及其掺假大戟序列扩增区标记的开发及检测效率
Pub Date : 2016-07-01 DOI: 10.4103/2394-6555.191172
Irum Gul, Athar Ali, K. J. Mirza, M. Abdin
Background: With the increase in demand of herbal medicines, adulteration in these drugs is also gaining momentum and remains an indispensable problem in domestic and export markets. Correct identification is the first step toward assuring quality, safety, and efficacy of indigenous herbal medicines. Materials and Methods: In this study, sequence characterized amplified region (SCAR) markers were developed to discriminate Ruta graveolens from its adulterant Euphorbia dracunculoides. Random amplified polymorphic DNA (RAPD) was performed and subsequently converted into SCAR markers. Results: After performing RAPD, SCAR primers were designed from the selected unique RAPD amplicons of the genuine drug as well as its adulterant. These primers produced 670 bp and 750 bp SCAR markers with genomic DNA sample of R. graveolens and E. dracunculoides, respectively. Conclusion: Development of these markers will help in the quality control of herbal drugs and monitoring widespread adulteration of these drugs by pharmaceutical industries and government agencies.
背景:随着草药需求的增加,这些药物的掺假也愈演愈烈,在国内和出口市场上仍然是一个不可缺少的问题。正确鉴别是保证本土草药质量、安全性和有效性的第一步。材料与方法:建立了序列特征扩增区(SCAR)标记,对芦笋及其伪品大戟进行鉴别。随机扩增多态性DNA (RAPD)随后转化为SCAR标记。结果:进行RAPD后,根据所选择的真药和假药的RAPD特异扩增子设计SCAR引物。这些引物分别产生了670 bp和750 bp的SCAR标记。结论:这些标志物的开发将有助于中药质量控制和监测制药行业和政府机构普遍存在的掺假现象。
{"title":"Development and detection efficiency of sequence characterized amplified region markers for authentication of medicinal plant Ruta graveolens and its adulterant Euphorbia dracunculoides","authors":"Irum Gul, Athar Ali, K. J. Mirza, M. Abdin","doi":"10.4103/2394-6555.191172","DOIUrl":"https://doi.org/10.4103/2394-6555.191172","url":null,"abstract":"Background: With the increase in demand of herbal medicines, adulteration in these drugs is also gaining momentum and remains an indispensable problem in domestic and export markets. Correct identification is the first step toward assuring quality, safety, and efficacy of indigenous herbal medicines. Materials and Methods: In this study, sequence characterized amplified region (SCAR) markers were developed to discriminate Ruta graveolens from its adulterant Euphorbia dracunculoides. Random amplified polymorphic DNA (RAPD) was performed and subsequently converted into SCAR markers. Results: After performing RAPD, SCAR primers were designed from the selected unique RAPD amplicons of the genuine drug as well as its adulterant. These primers produced 670 bp and 750 bp SCAR markers with genomic DNA sample of R. graveolens and E. dracunculoides, respectively. Conclusion: Development of these markers will help in the quality control of herbal drugs and monitoring widespread adulteration of these drugs by pharmaceutical industries and government agencies.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":"79 1","pages":"117 - 121"},"PeriodicalIF":0.0,"publicationDate":"2016-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83770917","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
Is depression an independent risk factor for the onset of Type 2 diabetes mellitus? 抑郁是2型糖尿病发病的独立危险因素吗?
Pub Date : 2016-07-01 DOI: 10.4103/2394-6555.191148
H. Parihar, Harivansh Thakar, H. Yin, Shari N. Allen
Depression is one of the most common mental illnesses characterized by loss of pleasure, whereas diabetes is a metabolic disorder which leads to high serum glucose levels. Current literature supports the development of depressive symptoms in patients with chronic illnesses including diabetes. However, depression as a potential risk factor for diabetes has attracted a lot of attention for clinicians and researchers. It has been hypothesized that both diabetes and depression may be bidirectional in nature, and each may exacerbate the symptoms or play an important role in the development of the other. The most common association between them is the diagnosis of depression in Type 1 or Type 2 diabetes. As the matter of fact, diabetes has been reported to double the risk of depression. In this review article, we have summarized various scientific studies to evaluate the potential of depression as a risk factor for diabetes. MEDLINE search identified various articles assessing this hypothesis. Our review of literature indicate some support for depression as a risk factor for Type 2 diabetes however more clinical studies need to be performed to clarify the contribution of depression as an independent risk factor for diabetes and to check the diabetes epidemic from escalating at a higher rate.
抑郁症是最常见的精神疾病之一,其特征是失去快乐,而糖尿病是一种导致高血糖水平的代谢紊乱。目前的文献支持慢性疾病包括糖尿病患者抑郁症状的发展。然而,抑郁症作为糖尿病的潜在危险因素引起了临床医生和研究人员的广泛关注。据推测,糖尿病和抑郁症在本质上可能是双向的,每一方都可能加剧症状或在另一方的发展中发挥重要作用。它们之间最常见的联系是1型或2型糖尿病中抑郁症的诊断。事实上,据报道,糖尿病会使患抑郁症的风险增加一倍。在这篇综述文章中,我们总结了各种科学研究来评估抑郁症作为糖尿病危险因素的潜力。MEDLINE搜索发现了许多评估这一假设的文章。我们对文献的回顾表明,抑郁症是2型糖尿病的一个危险因素,但需要进行更多的临床研究来阐明抑郁症作为糖尿病的一个独立危险因素的作用,并防止糖尿病的流行以更高的速度升级。
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引用次数: 3
Characterization of Arachis hypogaea L. oil obtained from different extraction techniques and in vitro antioxidant potential of supercritical fluid extraction extract 不同提取工艺下花生油的表征及超临界流体提取提取物的体外抗氧化潜力
Pub Date : 2016-07-01 DOI: 10.4103/2394-6555.191150
Rishika Chauhan, I. Ahmad, Y. Khan, E. Tamboli, Sayeed Ahmad
Aim: The present investigation was aimed to characterize the fixed oil of Arachis hypogaea L. using five different extraction methods: Supercritical fluid extraction (SFE), ultrasound assistance extraction, soxhlet extraction, solvent extraction, and three phase partitioning method. Materials and Methods: The SFE conditions (temperature, pressure, and volume of CO 2) were optimized prior for better yield. The extracted oils were analyzed and compared for their physiochemical parameters, high-performance thin layer chromatography (HPTLC), gas chromatography-mass spectrometry (GC-MS), and Fourier transform infrared spectrometry (FT-IR) fingerprinting. Anti-oxidant activity was also determined using DPPH and superoxide scavenging method. Results: The main fatty acids were oleic, linoleic, palmitic, and stearic acids as obtained by GC-MS. HPTLC analysis revealed the presence of similar major components in chromatograms. Similarly, the pattern of peaks as obtained in FT-IR and GC-MS spectra of same oils by different extraction methods was superimposable. Conclusion: Analysis reported that the fixed oil of A. hypogaea L. is a good source of unsaturated fatty acid, mainly n-6 and n-9 fatty acid with a significant antioxidant activity of oil obtained from SFE extraction method.
目的:采用超临界流体萃取法、超声辅助萃取法、索氏萃取法、溶剂萃取法、三相分馏法等5种不同的提取方法对山核桃固定油进行表征。材料和方法:为了获得更好的收率,对SFE条件(温度、压力和co2体积)进行了优化。采用高效薄层色谱(HPTLC)、气相色谱-质谱(GC-MS)和傅里叶变换红外光谱(FT-IR)指纹图谱对提取的油进行理化参数分析和比较。采用DPPH和超氧化物清除法测定其抗氧化活性。结果:气相色谱-质谱法测定的主要脂肪酸为油酸、亚油酸、棕榈酸和硬脂酸。HPTLC分析显示色谱中存在相似的主要成分。同样,不同提取方法得到的同一种油的FT-IR和GC-MS谱的峰型也具有重叠性。结论:分析报道,山楂固定油是不饱和脂肪酸的良好来源,主要为n-6和n-9脂肪酸,且SFE法提取的山楂固定油具有显著的抗氧化活性。
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引用次数: 1
Significance of molecular markers in pharmacognosy: A modern tool for authentication of herbal drugs 分子标记在生药学中的意义:中药鉴定的现代工具
Pub Date : 2016-07-01 DOI: 10.4103/2394-6555.191164
K. Chester, E. Tamboli, S. Paliwal, Sayeed Ahmad
Quality evaluation of herbal preparation is an elementary requirement of industry and other association dealing with Ayurvedic and herbal products. The growing use of botanical products now a days is forcing to assess these agents and to develop standards of quality and produce. An attempt has been made through this article to highlight the use of molecular markers for botanicals with special reference to Indian herbal medicine. As the desire for herbal-based products becomes ingrained in our society but standardization of botanicals offers many obstacles like the controversial identity of various plants, deliberated adulteration of plant material, ensuring quality is much more than discovery, specification, and process control. It also includes awareness of every aspect of a manufacturing process from research to shipping. Extensive research on DNA-based molecular markers is in progress for its great utility in the herbal drug analysis and widely used for the authentification of plant species of medicinal importance. DNA markers are reliable for information as the genetic composition is unique for each species and is not affected by age, physiological conditions, as well as environmental factors. DNA markers offer several advantages over conventional phenotypic markers, as they provide data that can be analyzed objectively.
草药制剂的质量评价是行业和其他协会处理阿育吠陀和草药产品的基本要求。如今,植物产品的使用越来越多,这迫使人们对这些制剂进行评估,并制定质量和生产标准。本文着重介绍了分子标记在植物药中的应用,特别是印度草药的应用。随着对草药产品的渴望在我们的社会中变得根深蒂固,但植物药的标准化提供了许多障碍,如各种植物的有争议的身份,故意掺假的植物材料,确保质量远远超过发现,规范和过程控制。它还包括从研究到运输制造过程的各个方面的意识。基于dna的分子标记因其在草药分析和药用植物鉴定中的广泛应用而得到广泛的研究。DNA标记是可靠的信息,因为每个物种的遗传组成是独特的,不受年龄、生理条件和环境因素的影响。与传统的表型标记相比,DNA标记提供了几个优势,因为它们提供了可以客观分析的数据。
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引用次数: 2
Solubility and stability enhancement of curcumin: Improving drug properties of natural pigment 姜黄素的溶解度和稳定性增强:改善天然色素的药物性能
Pub Date : 2016-07-01 DOI: 10.4103/2394-6555.191166
MJ Ansari, R. Parveen
Aim: Water insolubility, low potency, and instability are inherent problems of several herbal medicines. Identity, strength, quality, and purity of herbal products are further compromised during manufacturing and storage. The aim of present work was to evaluate solubility and stability of curcumin, a pigment obtained from dried rhizomes of plant Cucrcuma longa. Materials and Methods: The stoichiometric ratios for inclusion complexation of curcumin with various cyclodextrins (CDs) were determined by phase solubility analysis. Grinding, kneading, and freeze-drying were employed to determine optimum complexation. Complexes were evaluated for drug inclusion, solubility, and stability. Results: Stability constants were 11200 M−1 , 1557 M−1 , 2858 M−1 , and 2206 M−1 for α-, β-, γ-CD, and dimethyl β-CD (DIMEB), respectively, thus indicating good complex formation. Theoretical amounts of curcumin in binary products were between 80% and 97% with a maximum of 96.8% in curcumin-β-CD freeze-dried product. The complexation resulted in a marked improvement in the solubility of curcumin up to 60, 55, 56, and 1500 folds by α-, β-, γ-CD, and DIMEB, respectively. Inclusion complexation protected the drug from hydrolytic degradations as only 20-40% degradation was observed at the end of 8 h as opposed to >70% for pure curcumin. Conclusion: A significant improvement in the solubility and stability was observed with curcumin-CD complex as compared to pure curcumin.
目的:中药不溶于水、效力低、不稳定是中药的固有问题。草药产品的特性、强度、质量和纯度在生产和储存过程中进一步受到损害。本文研究了姜黄素的溶解度和稳定性。姜黄素是一种从蓖麻干根茎中提取的色素。材料与方法:采用相溶解度法测定了姜黄素与不同环糊精包合的化学计量比。研磨、揉捏和冷冻干燥是确定最佳配位的方法。评估配合物的药物包裹性、溶解度和稳定性。结果:α-、β-、γ-CD和二甲基β- cd (DIMEB)的稳定常数分别为11200 M−1、1557 M−1、2858 M−1和2206 M−1,表明配合物形成良好。姜黄素-β-CD冻干产品中姜黄素理论含量在80% ~ 97%之间,最高可达96.8%。通过α-、β-、γ-CD和DIMEB络合,姜黄素的溶解度分别提高了60倍、55倍、56倍和1500倍。包合物保护药物免于水解降解,因为在8小时结束时仅观察到20-40%的降解,而纯姜黄素的降解率>70%。结论:与纯姜黄素相比,姜黄素- cd复合物在溶解度和稳定性方面有显著改善。
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引用次数: 6
期刊
Drug Development and Therapeutics
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