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[From the approving of 3D printing tablet to the innovation of drug delivery systems]. 【从3D打印片剂获批到给药系统创新】。
Pub Date : 2016-11-01
Qiang Zhang

A 3D printing tablet of levetiracetam has been approved by FDA on August 3th, 2015, as the first pharmaceutical product based on 3D printing technique. 3D printing tablet indicates the perfect combination of active pharmaceutical ingredient (API), excipient, dosage form, pharmaceutical equipment and techniques including the software design and computer control. As a very vivid instance, the marketing of 3D printing tablet actually demonstrated again that the drug delivery systems (DDS) cannot work without preparation techniques, pharmaceutical excipient, device, manufacture and test equipment, package materials, and so on. This comment, briefly introduces the significance of these areas to DDS, as well as the advances and problems in China, followed by the indication that interdisciplinary study is the most critical feature for the innovation of DDS. It explains the rules of DDS innovation by various examples, and analyzes the challenges that we are facing. Finally, some suggestions are given to the innovation and development of DDS in China: 1 emphasizing the research on DDS with high originality; 2 emphasizing the study on the areas closely related to the DDS, like preparation techniques, pharmaceutical excipient and so on; 3 emphasizing the substantially interdisciplinary research on DDS; 4 emphasizing the combination between the basic and translational study on DDS.

3D打印左乙拉西坦片剂已于2015年8月3日获得FDA批准,成为首个基于3D打印技术的药品。3D打印片剂标志着原料药、赋形剂、剂型、制药设备和工艺的完美结合,包括软件设计和计算机控制。作为一个非常生动的例子,3D打印片剂的营销实际上再次证明了药物传递系统(DDS)的工作离不开制备技术、药用辅料、设备、制造和测试设备、包装材料等。本文简要介绍了这些领域对DDS的意义,以及国内的进展和问题,并指出跨学科研究是DDS创新的最关键特征。通过实例阐述了DDS创新的规律,分析了我们面临的挑战。最后,对国内DDS的创新与发展提出了几点建议:1、重视高独创性的DDS研究;2 .重视与DDS密切相关的制备技术、药用辅料等领域的研究;强调DDS的跨学科研究;4强调DDS的基础研究与转化研究相结合。
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引用次数: 0
[The determination and clinical application of inosine 5’-monophosphate dehydrogenase activity]. 肌苷5′-单磷酸脱氢酶活性的测定及临床应用
Pub Date : 2016-11-01
Fei-yan Liu, Xiao-yan Qiu, Zheng Jiao

Inosine 5’-monophosphate dehydrogenase(IMPDH) is a rate-limiting enzyme in de novo biosynthesis of guanine and plays an important role in cell proliferation. In clinic, IMPDH inhibitors are mainly used in fields of anticancer, antiviral, anti-parasitic, and immunosuppressive chemotherapy. However, since there are usually great inter- and intra-individual variability between drug concentration and clinical effect of IMPDH inhibitors, the enzyme activity of IMPDH may be applied as a specific biomarker and combined with the pharmacokinetics (PK) monitoring to improve efficacy and safety of IMPDH inhibitors. This review aims to discuss the assay of IMPDH activity measurement and its clinical application in recent years and provide valuable insights and theoretical basis for the development of IMPDH inhibitors’ pharmacodynamics monitoring.

肌苷5′-单磷酸脱氢酶(IMPDH)是鸟嘌呤新生生物合成的限速酶,在细胞增殖中起重要作用。临床上,IMPDH抑制剂主要应用于抗癌、抗病毒、抗寄生虫、免疫抑制化疗等领域。然而,由于药物浓度与IMPDH抑制剂的临床效果之间通常存在较大的个体间和个体内差异,因此可以将IMPDH酶活性作为特异性生物标志物,并与药代动力学(PK)监测相结合,以提高IMPDH抑制剂的疗效和安全性。本文综述了近年来IMPDH活性测定方法及其临床应用,为开展IMPDH抑制剂的药效学监测提供有价值的见解和理论依据。
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引用次数: 0
[Molecular cloning and functional characterization of the gene encoding hydroxy-2-methyl-2-(E)-butenyl 4-diphosphate reductase gene from Artemisia annua L.]. [黄花蒿羟基-2-甲基-2-(E)-丁烯基4-二磷酸还原酶基因的克隆及功能表征]。
Pub Date : 2016-11-01
Fang Cao, Jing Xia, Yu-pei Chen, Man Zhang, Li-en Xiang, Jun-lan Zeng, Min Chen, Xiao-zhong Lan, Zhi-hua Liao

Artemisinin is the first choice for malaria treatment. The plastidial MEP pathway provides 5-carbon precursors (IPP and its isomer DMAPP) for the biosynthesis of isoprenoid (including artemisinin). Hydroxy-2-methyl-2-(E)-butenyl 4-diphosphate reductase (HDR) is the last enzyme involved in the MEP pathway, which catalyzes HMBPP to form IPP and DMAPP. In this study, we isolated the full-length cDNA of HDR from Artemisia annua L. (AaHDR2) and performed functional analysis. According to gene expression analysis of AaHDR2 (GenBank: KX058541) and AaHDR1 reported ever (GenBank: ADC84348.1) by qPCR, we found that AaHDR1 and AaHDR2 had much higher expression level in trichomes than that in roots, stems, leaves and flowers. AaHDR2 had much higher expression level in flowers than that in leaves. Further, the plant hormones such as Me JA and ABA respectively up-regulated the expression level of AaHDR1 and AaHDR2 significantly, but GA3 up-regulated the expression level of AaHDR2 only. The gene expression analysis of AaHDR1 and AaHDR2 showed that AaHDR2 had a greater contribution than AaHDR1 to isoprenoid biosynthesis(including artemisinin). We used AaHDR2 for the following experiments. Bioinformatic analysis indicated that AaHDR2 belonged to the HDR family and the functional complementation assay showed that AaHDR2 did have the enzymatic function of HDR, using E. coli mutant MG1655(ara)<>HDR as host cell. The subcellular localization assay showed that AaHDR2 fused with GFP at its N-terminal specifically targeted in chloroplasts. Finally, AaHDR2 was overexpressed in Arabidopsis thaliana. The AaHDR2-overexpressing plants produced the isoprenoids including chlorophyll a, chlorophyll b and carotenoids at significantly higher levels than the wild-type Arabidopsis plants. In summary, AaHDR2 might be a candidate gene for genetic improvement of the isoprenoid biosynthesis.

青蒿素是治疗疟疾的首选药物。质体MEP途径为类异戊二烯(包括青蒿素)的生物合成提供5碳前体(IPP及其异构体DMAPP)。羟基-2-甲基-2-(E)-丁烯基4-二磷酸还原酶(HDR)是MEP途径中参与的最后一个酶,它催化HMBPP形成IPP和DMAPP。本研究从黄花蒿(Artemisia annua L.)中分离出HDR全长cDNA (AaHDR2)并进行功能分析。通过对已有报道的AaHDR2 (GenBank: KX058541)和AaHDR1 (GenBank: ADC84348.1)基因的qPCR表达分析,发现AaHDR1和AaHDR2在毛状体中的表达量远高于根、茎、叶和花中的表达量。AaHDR2在花中的表达量明显高于叶片。此外,Me、JA和ABA等植物激素分别显著上调AaHDR1和AaHDR2的表达水平,而GA3仅上调AaHDR2的表达水平。AaHDR1和AaHDR2的基因表达分析表明,AaHDR2对类异戊二烯类生物合成(包括青蒿素)的贡献大于AaHDR1。我们使用AaHDR2进行下面的实验。生物信息学分析表明AaHDR2属于HDR家族,功能互补实验表明AaHDR2确实具有HDR的酶促功能,以大肠杆菌突变体MG1655(ara)<>HDR为宿主细胞。亚细胞定位分析表明,AaHDR2在其n端与GFP融合,特异性靶向叶绿体。最后,AaHDR2在拟南芥中过表达。过表达aahdr2的植物产生的类异戊二烯包括叶绿素a、叶绿素b和类胡萝卜素的水平显著高于野生型拟南芥。综上所述,AaHDR2可能是类异戊二烯生物合成遗传改良的候选基因。
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引用次数: 0
[The anti-HIV-1 activities of benzophenones non-nucleoside reverse transcriptase inhibitors in vitro]. [二苯甲酮类非核苷类逆转录酶抑制剂的体外抗hiv -1活性]。
Pub Date : 2016-11-01
Ping Wang, Gao-hong Zhang, Si-ying Xiang, Liu-meng Yang, Cheng-run Tang, Xiao-dong Ma, Yong-tang Zheng

To evaluate the anti-HIV-1 activities of 5 benzophenones non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as DY1203, DY1204, DY1119, DY1208 and DY1209 in vitro, the cytotoxicity of 5 compounds were tested on C8166, MT-4, H9 and PBMC with the MTT assay. The anti-HIV-1 activities of compounds were evaluated on laboratory-adapted strain, drug-resistant strains and primary isolated strains by p24 antigen expression ELISA. The inhibition of HIV-1 recombinant reverse transcriptase activity was assessed by ELISA assay. Among 5 compounds, DY1203 and DY1204 showed low cytotoxicities with CC(50) greater than 200 μg·m L(-1). DY1119, DY1208 and DY1209 showed strong anti-HIV-1 activities against HIV-1(IIIB,) HIV-1(74V,) HIV-1(RF/V82F/184V,) HIV-1(NL4-3) (gp41(36G)N42S,) HIV-1(KM018,) HIV-1(TC-1) and HIV-1(Wan.) However, NNRTIs drug-resistant strain HIV-1(A17) showed different resistance to these compounds. The 5 compounds proved active against HIV-1 recombinant reverse transcriptase. DY1208 is expected to become a new lead compound for its high therapeutic index. The results can provide new information for HIV-1 drug research and promote the development of new HIV-1 drugs.

为了评价5种二苯甲酮类非核苷类逆转录酶抑制剂(NNRTIs) DY1203、DY1204、DY1119、DY1208和DY1209的体外抗hiv -1活性,采用MTT法检测了5种化合物对C8166、MT-4、H9和PBMC的细胞毒性。采用p24抗原表达ELISA法对实验室适应株、耐药株和原代分离株进行抗hiv -1活性评价。ELISA法检测其对HIV-1重组逆转录酶活性的抑制作用。5个化合物中DY1203和DY1204具有较低的细胞毒性,CC(50)均大于200 μg·m L(-1)。DY1119、DY1208和DY1209对HIV-1(IIIB)、HIV-1(74V)、HIV-1(RF/V82F/184V)、HIV-1(NL4-3)、gp41(36G)N42S、HIV-1(KM018)、HIV-1(TC-1)和HIV-1(Wan)具有较强的抗HIV-1活性。然而,NNRTIs耐药菌株HIV-1(A17)对这些化合物表现出不同的耐药性。这5种化合物被证明对HIV-1重组逆转录酶有活性。DY1208具有较高的治疗指数,有望成为新的先导化合物。研究结果可为HIV-1药物研究提供新的信息,促进HIV-1新药的开发。
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引用次数: 0
[Flavonoids from leaves of Psidum littorale]. [从苦荞麦叶中提取的类黄酮]。
Pub Date : 2016-11-01
Hang-qing Cui, Cai-ying Peng, Ying-zheng Huang, Ying Gao, Jian-qun Liu, Rui Zhang, Ji-cheng Shu

We investigated the chemical constituents of the leaves of Psidum littorale, which include 16 flavonoids, including seven flavonols, six flavonoid glycosides and three flavonones. The compounds were isolated by silica gel column chromatography. Their structures were elucidated on the basis of spectral analysis and by comparison with published data. Seven flavonols were kaempferol (1), isorhamnetin (2), myricetin- 3,7,3’-trimethyl ether(3), laricitrin (4), quercetin (5), myricetin (6) and quercein-3,4’-dimethyl ether (7), six flavonoid glycosides were guaijaverin (8), hyperoside (9), 5,4’-dyhydroxy-3,7,5’-methoxyflavone-3’-O-β-D- glucoside (10), laricitrin-3-O-xyloside (11), myricetin-3-O-α-L-rhamnopyranoside (12) and myricetin-3-O-β-D- xyloside (13). Three flavonones were 4’-O-methyldihydroquercetin (14), dihydroapigenin (15) and ampelopsin 4’-O-β-D-glucopyranoside (16). Compound 10 is a new chemical, compounds 2-4, 7, 10-16 were first isolated from this plant. (1)H NMR and (13)C NMR data of compound 11 were not reported in literature.

研究了苦麻黄叶的化学成分,其中含有16种黄酮,包括7种黄酮醇、6种黄酮苷和3种黄酮。通过硅胶柱层析分离得到化合物。通过光谱分析和与已发表数据的比较,对它们的结构进行了鉴定。7种黄酮醇分别为山奈酚(1)、异鼠李素(2)、杨梅素- 3,7,3′-三甲基醚(3)、杨梅素(4)、槲皮素(5)、杨梅素(6)和槲皮素-3,4′-二甲醚(7);6种类黄酮苷分别为木桂木苷(8)、金丝桃苷(9)、5,4′-二羟基-3,7,5′-甲氧基黄酮-3′- o -β- d -葡萄糖苷(10)、杨梅素-3- o -α- l -鼠李糖苷(11)、杨梅素-3- o -α- l -鼠李糖苷(12)和杨梅素-3- o -β- d -木糖苷(13)。3种黄酮分别为4′-O-甲基二氢槲皮素(14)、二氢芹菜素(15)和葡萄素4′-O-β- d -葡萄糖苷(16)。化合物10为新化合物,化合物2 ~ 4、7、10 ~ 16为首次从该植物中分离得到。(1)化合物11的H NMR和(13)C NMR数据未见文献报道。
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引用次数: 0
[Synthesis and anti-tumor activity of novel histone deacetylase inhibitors based on dihydropyridin-2-one scaffold]. [基于二氢吡啶-2- 1支架的新型组蛋白去乙酰化酶抑制剂的合成及抗肿瘤活性]。
Pub Date : 2016-11-01
Jia-qing Li, Xiao Han

To discover novel dihydropyridin-2-one derivatives with higher HDAC inhibitory activity and subtype selectivity, twenty-seven dihydropyridin-2-one derivatives containing triazole unit were synthesized via click chemistry. The structures of these compounds have been confirmed by IR, 1H NMR and HR-MS spectra. Preliminary in vitro pharmacological tests showed that these compounds potently inhibited HDAC1 and HDAC6, which also displayed significant antiproliferative effect on five cancer cells, and most of them were better than that of the parent compound 1A and drug SAHA. Specifically, compound 18g exhibited most potent anti-HDAC1 activity, and also showed the greatest potency against PC-3 and Hep G2. Additionally, all compounds were nontoxic to health RWPE-1 and VERO cells, while SAHA showed essential toxicity.

为寻找具有较高HDAC抑制活性和亚型选择性的新型二氢吡啶-2- 1衍生物,采用click化学方法合成了27个含三唑单元的二氢吡啶-2- 1衍生物。这些化合物的结构经IR、1H NMR和HR-MS确证。初步体外药理实验表明,这些化合物对HDAC1和HDAC6均有较强的抑制作用,对5种肿瘤细胞均有明显的抗增殖作用,且多数优于母体化合物1A和药物SAHA。具体而言,化合物18g表现出最有效的抗hdac1活性,并且对PC-3和Hep G2也表现出最大的效力。此外,所有化合物都对健康的RWPE-1和VERO细胞无毒,而SAHA显示出必要的毒性。
{"title":"[Synthesis and anti-tumor activity of novel histone deacetylase inhibitors based on dihydropyridin-2-one scaffold].","authors":"Jia-qing Li,&nbsp;Xiao Han","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>To discover novel dihydropyridin-2-one derivatives with higher HDAC inhibitory activity and subtype selectivity, twenty-seven dihydropyridin-2-one derivatives containing triazole unit were synthesized via click chemistry. The structures of these compounds have been confirmed by IR, 1H NMR and HR-MS spectra. Preliminary in vitro pharmacological tests showed that these compounds potently inhibited HDAC1 and HDAC6, which also displayed significant antiproliferative effect on five cancer cells, and most of them were better than that of the parent compound 1A and drug SAHA. Specifically, compound 18g exhibited most potent anti-HDAC1 activity, and also showed the greatest potency against PC-3 and Hep G2. Additionally, all compounds were nontoxic to health RWPE-1 and VERO cells, while SAHA showed essential toxicity.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1734-44"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36228015","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
[A review of 3D printing via fused deposition modeling in pharmaceutics]. [通过熔融沉积建模在制药领域的3D打印综述]。
Pub Date : 2016-11-01
Dong-lin He, Fu-guo Han, Zhao Wang, Qing-fei Liu

Three dimensional printing (3D printing) has been known as additive manufacturing technique based on digitally-controlled deposition of materials. Fused deposition modeling (FDM) is one of techniques commonly used in 3D printing, in which materials are soften or melt by heat to create objects during printing. This paper is prepared to review the research and application of 3D printing via FDM in the pharmaceutical sciences, including its advantages and limitations.

三维打印(3D打印)被称为基于数字控制的材料沉积的增材制造技术。熔融沉积建模(FDM)是3D打印中常用的技术之一,其中材料在打印过程中被加热软化或熔化以创建物体。本文综述了FDM技术在制药领域的研究和应用,包括其优势和局限性。
{"title":"[A review of 3D printing via fused deposition modeling in pharmaceutics].","authors":"Dong-lin He,&nbsp;Fu-guo Han,&nbsp;Zhao Wang,&nbsp;Qing-fei Liu","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Three dimensional printing (3D printing) has been known as additive manufacturing technique based on digitally-controlled deposition of materials. Fused deposition modeling (FDM) is one of techniques commonly used in 3D printing, in which materials are soften or melt by heat to create objects during printing. This paper is prepared to review the research and application of 3D printing via FDM in the pharmaceutical sciences, including its advantages and limitations.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1659-65"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36227106","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
[Based on in vivo fluorescence imaging technology, to extablish a fluorescence modification method for amphipathic block polymers]. [基于体内荧光成像技术,建立两亲嵌段聚合物的荧光修饰方法]。
Pub Date : 2016-11-01
Zi-hua Xia, Yi Liu, Li-ping Yu, An-an Yu, Fan Yang

Rhodamine B (Rh B) was used to decorate an amphipathic block polymers (β-CD-[P(AA- co-MMA)-b-PVP](4)) in this study. First, after activated by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, rhodamine B was marked with hydroxyethyl methacrylate (HEMA) through ester exchange reaction. Second, the labeled amphipathic block polymers (β-CD-[P(AA-(HEMA-RhB)-MMA)-b-PVP](4)) were synthesized after polymerization reaction of double bones between Rh B-HEMA and other reactants. Finally, the structure of product was measured by FT-IR spectra and fluorospectro photometer (FLUORO). The critical micelle concentration of Rh B-labeled and unlabeled amphipathic block polymers were 4.96×10(-3), 5.09×10(-3)mg·L(-1), respectively, indicating no change of their micellization behavior. In vivo tissue distribution and whole- body fluorescent imaging were studied by vinpocetine (VP)-loaded polymeric micelles which were prepared through a solvent evaporation method. Compared to the result of in vivo tissue distribution and whole-body fluorescence imaging, a similar bio-distribution behavior of VP-loaded polymeric micelles was found. Those proved the successful fluorescence modification with a labeling yield of 4.13%. With in vivo fluorescence imaging technology, we established a fluorescence method for modification of amphipathic block polymers.

本研究采用罗丹明B (Rh B)修饰两亲嵌段聚合物β-CD-[P(AA- co-MMA)- B - pvp](4)。首先,罗丹明B被1-(3-二甲氨基丙基)-3-乙基碳二亚胺盐酸盐活化后,通过酯交换反应被甲基丙烯酸羟乙酯(HEMA)标记。其次,将Rh B-HEMA与其他反应物进行双骨聚合反应,合成标记的两亲嵌段聚合物(β-CD-[P(AA-(HEMA-RhB)- mma)-b- pvp](4)。最后用FT-IR光谱和荧光光度计(FLUORO)测定产物的结构。Rh b标记和未标记的两亲嵌段聚合物的临界胶束浓度分别为4.96×10(-3)和5.09×10(-3)mg·L(-1),表明它们的胶束行为没有改变。采用溶剂蒸发法制备长春西汀聚合物胶束,研究了长春西汀在体内的组织分布和全身荧光成像。与体内组织分布和全身荧光成像结果相比,发现负载vp的聚合物胶束具有相似的生物分布行为。结果表明,荧光修饰成功,标记率为4.13%。利用体内荧光成像技术,建立了两亲嵌段聚合物的荧光修饰方法。
{"title":"[Based on in vivo fluorescence imaging technology, to extablish a fluorescence modification method for amphipathic block polymers].","authors":"Zi-hua Xia,&nbsp;Yi Liu,&nbsp;Li-ping Yu,&nbsp;An-an Yu,&nbsp;Fan Yang","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Rhodamine B (Rh B) was used to decorate an amphipathic block polymers (β-CD-[P(AA- co-MMA)-b-PVP](4)) in this study. First, after activated by \u00001-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, rhodamine B was marked with hydroxyethyl methacrylate (HEMA) through ester exchange reaction. Second, the labeled amphipathic block polymers (β-CD-[P(AA-(HEMA-RhB)-MMA)-b-PVP](4)) were synthesized after polymerization reaction of double bones between Rh B-HEMA and other reactants. Finally, the structure of product was measured by FT-IR spectra and fluorospectro photometer (FLUORO). The critical micelle concentration of Rh B-labeled and unlabeled amphipathic block polymers were 4.96×10(-3), 5.09×10(-3)mg·L(-1), respectively, indicating no change of their micellization behavior. In vivo tissue distribution and whole- body fluorescent imaging were studied by vinpocetine (VP)-loaded polymeric micelles which were prepared through a solvent evaporation method. Compared to the result of in vivo tissue distribution and whole-body fluorescence imaging, a similar bio-distribution behavior of VP-loaded polymeric micelles was found. Those proved the successful fluorescence modification with a labeling yield of 4.13%. With in vivo fluorescence imaging technology, we established a fluorescence method for modification of amphipathic block polymers.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1777-83"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36227642","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
[Crystal structure and crystal form stability of trelagliptin succinate]. [琥珀酸trelagliptin的晶体结构和晶型稳定性]。
Pub Date : 2016-11-01
Jia-li Ye, Xin-bo Zhou, Su-xiang Wu, Meng-ying Sun, Jian-ming Gu, Xiu-rong Hu

In order to investigate trelagliptin succinate’s stability in solution, recrystallization and suspension methods in polar solvent (mainly in water and 95% alcohol) were used to study the crystal form transformation of trelagliptin succinate. Single crystal X-ray diffraction, powder X-ray diffraction and thermalgravimetric analysis, and differential scanning calorimetry were used to characterize the structure of the solid state form before and after transformation. The results showed that trelagliptin succinate can easily convert to trelagliptin hemi-succinate mediated by solvent, especially by polar solvent, namely trelagliptin hemi-succinate is more stable than trelagliptin succinate in solution.

为了考察琥珀酸trelag列汀在溶液中的稳定性,采用极性溶剂(主要是水和95%酒精)重结晶和悬浮法研究琥珀酸trelag列汀的晶型转变。采用单晶x射线衍射、粉末x射线衍射和热重分析、差示扫描量热法对相变前后固态形态的结构进行表征。结果表明,在溶剂,尤其是极性溶剂的介导下,曲列列汀易转化为曲列列汀半琥珀酸盐,即曲列列汀半琥珀酸盐比曲列列汀在溶液中更稳定。
{"title":"[Crystal structure and crystal form stability of trelagliptin succinate].","authors":"Jia-li Ye,&nbsp;Xin-bo Zhou,&nbsp;Su-xiang Wu,&nbsp;Meng-ying Sun,&nbsp;Jian-ming Gu,&nbsp;Xiu-rong Hu","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In order to investigate trelagliptin succinate’s stability in solution, recrystallization and suspension methods in polar solvent (mainly in water and 95% alcohol) were used to study the crystal form transformation of trelagliptin succinate. Single crystal X-ray diffraction, powder X-ray diffraction and thermalgravimetric analysis, and differential scanning calorimetry were used to characterize the structure of the solid state form before and after transformation. The results showed that trelagliptin succinate can easily convert to trelagliptin hemi-succinate mediated by solvent, especially by polar solvent, namely trelagliptin hemi-succinate is more stable than trelagliptin succinate in solution.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1759-64"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36227840","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
[Simultaneous determination of 7 benzodiazepines in human plasma by UHPLC-MS/MS]. UHPLC-MS/MS同时测定人血浆中7种苯二氮卓类药物。
Pub Date : 2016-11-01
Hong-yan Yu, Guo-ru Liu, Yu-jing Cui, Wei Wang, Qing-yan Li

The study was designed to develop the method for determination of 7 benzodiazepines concentration in human plasma. UHPLC-MS/MS was adopted to analyze plasma with protein precipitated by acetonitrile. Citalopram was used as an internal standard. Plasma samples were separated on CORTECS UHPLC C18 column with the mobile phase of aqueous solution (0.01% formic acid) - methanol (0.01% formic acid) at a flow rate of 0.3 m L·min(-1). Multiple reaction monitoring (MRM) mode was performed in combiation with electrospray ionization source operating in the positive ionization mode. The liner calibration curve of midazolam, nitrazepam, estazolam, clonazepam, lorazepam, triazolam and diazepam were obtained in the concentration range of 1.05-840 (r = 0.999 4), 2.06-824 (r = 0.998 1), 2.02-1 616 (r = 0.994 7), 6.18-2 472 (r = 0.997 9), 6.12-2 448 (r = 0.997 4), 3.02-2 416 (r = 0.990 2), 1.02-816 (r = 0.998 8) ng·m L(-1), respectively. The lowest detection limit were 0.02, 0.52, 0.51, 1.55, 0.77, 0.76, 0.02 ng·m L(-1), respectively. The RSD of inter-day and intra-day were less than 10.81%. The relative recovery was 81.46%-106.53%. The method was successfully applied to clinical analysis of blood samples from patients.

本研究旨在建立测定人血浆中7种苯二氮卓类药物浓度的方法。采用UHPLC-MS/MS对血浆进行乙腈沉淀蛋白分析。以西酞普兰为内标。血浆样品在CORTECS UHPLC C18柱上分离,流动相为水溶液(0.01%甲酸)-甲醇(0.01%甲酸),流速为0.3 m L·min(-1)。多反应监测(MRM)模式结合电喷雾电离源在正电离模式下工作。分别在1.05-840 (r = 0.999 4)、2.06-824 (r = 0.998 1)、2.02-1 616 (r = 0.994 7)、6.18-2 472 (r = 0.997 9)、6.12-2 448 (r = 0.997 4)、3.02-2 416 (r = 0.990 2)、1.02-816 (r = 0.998 8) ng·m L(-1)的浓度范围内建立咪达唑仑、硝西泮、依司唑仑、氯硝西泮、劳拉西泮、三唑仑和地西泮的线性校准曲线。最低检出限分别为0.02、0.52、0.51、1.55、0.77、0.76、0.02 ng·m L(-1)。日间和日间的RSD均小于10.81%。相对回收率为81.46% ~ 106.53%。该方法已成功应用于临床对患者血样的分析。
{"title":"[Simultaneous determination of 7 benzodiazepines in human plasma by UHPLC-MS/MS].","authors":"Hong-yan Yu,&nbsp;Guo-ru Liu,&nbsp;Yu-jing Cui,&nbsp;Wei Wang,&nbsp;Qing-yan Li","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The study was designed to develop the method for determination of 7 benzodiazepines concentration in human plasma. UHPLC-MS/MS was adopted to analyze plasma with protein precipitated by acetonitrile. Citalopram was used as an internal standard. Plasma samples were separated on CORTECS UHPLC C18 column with the mobile phase of aqueous solution (0.01% formic acid) - methanol (0.01% formic acid) at a flow rate of 0.3 m L·min(-1). Multiple reaction monitoring (MRM) mode was performed in combiation with electrospray ionization source operating in the positive ionization mode. The liner calibration curve of midazolam, nitrazepam, estazolam, clonazepam, lorazepam, triazolam and diazepam were obtained in the concentration range of 1.05-840 (r = 0.999 4), 2.06-824 (r = 0.998 1), 2.02-1 616 (r = 0.994 7), 6.18-2 472 (r = 0.997 9), 6.12-2 448 (r = 0.997 4), 3.02-2 416 (r = 0.990 2), 1.02-816 (r = 0.998 8) ng·m L(-1), respectively. The lowest detection limit were 0.02, 0.52, 0.51, 1.55, 0.77, 0.76, 0.02 ng·m L(-1), respectively. The RSD of inter-day and intra-day were less than 10.81%. The relative recovery was 81.46%-106.53%. The method was successfully applied to clinical analysis of blood samples from patients.</p>","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1765-9"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36227841","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
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