Yaoxue Xuebao Pub Date : 2016-11-01

Qiang Zhang

{"title":"[From the approving of 3D printing tablet to the innovation of drug delivery systems].","authors":"Qiang Zhang","doi":"","DOIUrl":"","url":null,"abstract":"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.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1655-8"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36227105","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

[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

Yaoxue Xuebao Pub Date : 2016-11-01

Fei-yan Liu, Xiao-yan Qiu, Zheng Jiao

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]。

Yaoxue Xuebao 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

{"title":"[Molecular cloning and functional characterization of the gene encoding hydroxy-2-methyl-2-(E)-butenyl 4-diphosphate reductase gene from Artemisia annua L.].","authors":"Fang Cao, Jing Xia, Yu-pei Chen, Man Zhang, Li-en Xiang, Jun-lan Zeng, Min Chen, Xiao-zhong Lan, Zhi-hua Liao","doi":"","DOIUrl":"","url":null,"abstract":"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\u0000 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.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1791-8"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36227606","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

[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]。

Yaoxue Xuebao 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

{"title":"[The anti-HIV-1 activities of benzophenones non-nucleoside reverse transcriptase inhibitors in vitro].","authors":"Ping Wang, Gao-hong Zhang, Si-ying Xiang, Liu-meng Yang, Cheng-run Tang, Xiao-dong Ma, Yong-tang Zheng","doi":"","DOIUrl":"","url":null,"abstract":"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.","PeriodicalId":35924,"journal":{"name":"Yaoxue Xuebao","volume":"51 11","pages":"1704-10"},"PeriodicalIF":0.0,"publicationDate":"2016-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"36228011","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

[Flavonoids from leaves of Psidum littorale]. [从苦荞麦叶中提取的类黄酮]。

Yaoxue Xuebao Pub Date : 2016-11-01

Hang-qing Cui, Cai-ying Peng, Ying-zheng Huang, Ying Gao, Jian-qun Liu, Rui Zhang, Ji-cheng Shu

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]。

Yaoxue Xuebao Pub Date : 2016-11-01

Jia-qing Li, Xiao Han

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]。

Yaoxue Xuebao Pub Date : 2016-11-01

Dong-lin He, Fu-guo Han, Zhao Wang, Qing-fei Liu

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]。

Yaoxue Xuebao Pub Date : 2016-11-01

Zi-hua Xia, Yi Liu, Li-ping Yu, An-an Yu, Fan Yang

{"title":"[Based on in vivo fluorescence imaging technology, to extablish a fluorescence modification method for amphipathic block polymers].","authors":"Zi-hua Xia, Yi Liu, Li-ping Yu, An-an Yu, Fan Yang","doi":"","DOIUrl":"","url":null,"abstract":"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.","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]。

Yaoxue Xuebao Pub Date : 2016-11-01

Jia-li Ye, Xin-bo Zhou, Su-xiang Wu, Meng-ying Sun, Jian-ming Gu, Xiu-rong Hu

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。

Yaoxue Xuebao Pub Date : 2016-11-01

Hong-yan Yu, Guo-ru Liu, Yu-jing Cui, Wei Wang, Qing-yan Li

{"title":"[Simultaneous determination of 7 benzodiazepines in human plasma by UHPLC-MS/MS].","authors":"Hong-yan Yu, Guo-ru Liu, Yu-jing Cui, Wei Wang, Qing-yan Li","doi":"","DOIUrl":"","url":null,"abstract":"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.","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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