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| 1 | Preparation, stability and pharmacokinetics evaluation of lipid microspheres loading a promising antitumor candidate, Timataxel显示文摘Timataxel(13-(N-Boc-3-i-butylisoserinoyl-4,10-β-diacetoxy-2-α-benzoyloxy-5-β-20-epoxy-1,13-α-dihydroxy-9-oxo-19-norcyclopropa[g]tax-11-ene)), used to be called TM-2, is a novel semi-synthetic promising candidate for cancer treatment. However the preformulation study showed that TM-2 was insoluble and chemically instable in water, which would limit its application. This study aimed at the preparation of Timataxel lipid microspheres(TM-2 LMs)and investigated the difference between TM-2 LMs and TM-2 solution in pharmacokinetics. In this work, the final formulation was as follows: 0.10%(w/v) TM-2;10.00%(w/v) oil phase(long chain triglyceride:media chain triglyceride = 2.50%:7.50%);1.40%(w/v) phospholipid;0.02%(w/v) NaH2 PO4;2.25%(w/v) glycerin and water to a total volume of 100 ml.The particle size distribution, content and entrapment efficacy were 205.0 ± 43.3 nm, 101.00% and 99.12%, respectively. TM-2 LMs were stable during storage at 25 °C for 3 months, even under the condition of 60 °C and 4500 lx for 10 d. Phosphatidylethanolamine(PE) in phospholipid may contribute to the stability of TM-2 LMs. The pharmacokinetic parameters for TM-2 LMs were as follows: AUC(0-∞) 3663.71 μg/l h and the clearance 2.26 l/h/kg. As for solution, these parameters were 1712.52 μg/l h and 4.77 l/h/kg, respectively. The t1/2 of TM-2 LMs was similar to TM-2 solution. The pharmacokinetic results indicated that the AUC of TM-2 LMs was larger, the clearance was smaller than that of TM-2 solution. In a word, lipid microspheres were a promising drug delivery system for TM-2. | Yan Li Haibing He Qiao Wang Xing Tang | 2016 | Asian Journal of Pharmaceutical Sciences2016，11，6： | 4 |
| 2 | Supersaturation induced by Itraconazole/Soluplus micelles provided high GI absorption in vivo显示文摘To investigate the effect of supersaturation induced by micelle formation during dissolution on the bioavailability of itraconazole(ITZ)/Soluplus~? solid dispersion. Solid dispersions prepared by hot melt extrusion (HME) were compressed into tablets directly with other excipients. Dissolution behavior of ITZ tablets was studied by dissolution testing and the morphology of micelles in dissolution media was studied using transmission electron microscopy (TEM). Drug transferring from stomach into intestine was simulated to obtain a supersaturated drug solution. Bioavailability studies were performed on the ITZ tablets and Sporanox~? in beagle dogs. The morphology of micelles in the dissolution media was observed to be spherical in shape, with an average size smaller than 100 nm. The supersaturated solutions formed by Soluplus~? micelles were stable and no precipitation took place over a period of 180 min. Compared with Sporanox~?, ITZ tablets exhibited a 2.50-fold increase in the AUC (0–96) of ITZ and a 1.95-fold increase in its active metabolite hydroxyitraconazole (OHITZ) in the plasma of beagle dogs. The results obtained provided clear evidence that not only the increase in the dissolution rate in the stomach, but also the supersaturation produced by micelles in the small intestine may be of great assistance in the successful development of poorly water-soluble drugs. The micelles formed by Soluplus~? enwrapped the molecular ITZ inside the core which promoted the amount of free drug in the intestinal cavity and carried ITZ through the aqueous boundary layer(ABL), resulting in high absorption by passive transportation across biological membranes. The uptake of intact micelles through pinocytosis together with the inhibition of P-glycoprotein-mediated drug efflux in intestinal epithelia contributed to the absorption of ITZ in the gastrointestinal tract. These results indicate that HME with Soluplus~?, which can induce supersaturation by micelleformation, may be of great assistance to the successful development of poorly watersoluble drugs. | Yue Zhong Guanghui Jing Bin Tian Hao Huang Yuanyuan Zhang Jingxin Gou Xing Tang Haibing He Yanjiao Wang | 2016 | Asian Journal of Pharmaceutical Sciences2016，11，2： | 3 |
| 3 | The study of the adductor muscle-shell interface structure in three Mollusc species显示文摘The adductor muscle scar(AMS) is the fixation point of adductor muscle to the shell. It is an important organicinorganic interface and stress distribution area. Despite recent advances, our understanding of the structure and composition of the AMS remain limited. Here, we report study on the AMS of three bivalves: Mytilus coruscus,Chlamys farreri and Ruditapes philippinarum. Results showed that there were significant differences among their AMS structures. Both M. coruscus and C. farreri were found to have a columnar layer above the nacreous platelet shell structure at the AMS and this layer was more organized in M. coruscus. There was no distinguishable twolayer structure in R. philippinarum. Atomic force microscopy(AFM) and Fourier transform infrared spectroscopy(FT-IR) results showed that the AMS was much smoother than the nacreous inner shell in all the three species and the AMS had minor different compositions from the nacreous shell layer. SDS-PAGE(sodium dodecyl-sulfate polyacrylamide gel electophoresis) study of the proteins isolated from the interface indicated that there was a 70 k Da protein which seemed to be specifically located to the highly organized columnar AMS structure in Mytilus coruscus. Further analysis of this protein showed it contained high level of Asx(Asp+Asn), Glx(Glu+Gln) and Gly.The special structure and composition of the AMS might play important roles in the stability, adhesion and function at this stress distribution site. | ZHU Yaoyao SUN Chengjun SONG Yingfei JIANG Fenghua YIN Xiaofei TANG Min DING Haibing | 2016 | Acta Oceanologica Sinica2016，35，8： | 1 |
| 4 | Tablets of paliperidone using compression-coated technology for controlled ascending release显示文摘The aim of this work was to prepare ascending release compression-coated(CC) tablets with paliperidone(PAL) using a simple manufacturing technique and short manufacturing process.The release behavior and mechanisms in vitro of the final tablets was investigated and evaluated. The PAL CC tablets were comprised of a core layer of high viscosity hydroxypropyl cellulose(HPC-H) and a coating layer of high viscosity hydroxypropyl methylcellulose(HPMCK100 M). Several factors such as materials and core tablet compositions were studied for their influence in the formulation procedure. The drug release mechanism was studied using gravimetric analysis. The data could be fitted to the Peppas model. The ascending drug release results were expressed in terms of the slope of the release curve at different time points.Results showed that the formulation could achieve a good ascending drug release when the weight ratio of PAL was 5:1(core:layer). The fraction of HPC and HPMC was 33 %, and the combination of Eudragit RL-PO was 10%. The ascending release mechanism was due to solvent penetration into the PAL CC tablets, and subsequent drug dissolution from the gelatinous HPC and HPMC matrix erosion. The release mechanism was therefore a combination of diffusion and erosion. This work demonstrated that the compression-coated tablets could achieve controlled ascending release over 24 h for the oral administration systems. | Yingying Tang Huan Teng Yanan Shi Haibing He Yu Zhang Tian Yin Cuifang Cai Xing Tang | 2018 | Asian Journal of Pharmaceutical Sciences2018，13，2： | 1 |
| 5 | Exhumation structure and mechanism of the Sulu ultrahigh-pressure metamorphic belt central China显示文摘 | Xu Zhiqin Zhang Zemin Liu Fulai Yang Jingsui Li Haibing Yang Tiannan Qiu Haijun Li Tianfu Meng Fanchong Chen Shizhong Tang Zemin and Chen Fangyuan | | ACTA GEOLOGICA SINICA(CHINESE EDITION)0，，： | 1 |
| 6 | An intravenous clarithromycin lipid emulsion with a high drug loading, H-bonding and a hydrogen-bonded ion pair complex exhibiting excellent antibacterial activity显示文摘The aim of this study was to develop an intravenous clarithromycin lipid emulsion(CLE)with good stability and excellent antibacterial activity. The CLE was prepared by the thinfilm dispersed homogenization method. The interaction between clarithromycin(CLA) and cholesteryl hemisuccinate(CHEMS) was confirmed by DSC, FT-IR and^1H NMR analysis. The interfacial drug loading, thermal sterilization, freeze–thaw stability, and in vitro and in vivo antibacterial activity were investigated systematically. DSC, FT-IR and^1H NMR spectra showed that CHEMS(CLA: CHEMS, M ratio 1:2) could interact with CLA through H-bonding and a hydrogen-bonded ion pair. The CHEMS was found necessary to maintain the stability of CLE.Ultracentrifugation showed that almost 88% CLA could be loaded into the interfacial layer.The optimized CLE formulation could withstand autoclaving at 121 °C for 10 min and remain stable after three freeze–thaw cycles. The in vitro susceptibility test revealed that the CLA–CHEMS ion-pair and CLE have similar activity to the parent drug against many different bacterial strains. The in vivo antibacterial activity showed that the ED50 of intravenous CLE was markedly lower than that of CLA solution administrated orally. CLE exhibited pronounced antibacterial activity and might be a candidate for a new nanocarrier for CLA with potential advantages over the current commercial formulation. | Haoyu Gong Sicong Geng Qi Zheng Puxiu Wang Lifeng Luo Xiuzhi Wang Yan Zhang Yu Zhang Haibing He Xing Tang | 2016 | Asian Journal of Pharmaceutical Sciences2016，11，5： | 1 |
| 7 | Clarithromycin-loaded liposomes offering high drug loading and less irritation显示文摘 | Xiaona Liu Wei Sun Bo Zhang Bin Tian Xing Tang Na Qi Haibing He Huifang Li Xiangqun Jin | 2013 | International Journal of Pharmaceutics . 2013 (1-2)2013，，： | 1 |
| 8 | Single-cell RNA Sequencing Reveals Thoracolumbar Vertebra Heterogeneity and Rib-genesis in Pigs显示文摘Development of thoracolumbar vertebra(TLV)and rib primordium(RP)is a common evolutionary feature across vertebrates,although whole-organism analysis of the expression dynamics of TLV-and RP-related genes has been lacking.Here,we investigated the single-cell transcriptome landscape of thoracic vertebra(TV),lumbar vertebra(LV),and RP cells from a pig embryo at 27 days post-fertilization(dpf)and identified six cell types with distinct gene expression signatures.In-depth dissection of the gene expression dynamics and RNA velocity revealed a coupled process of osteogenesis and angiogenesis during TLV and RP development.Further analysis of cell type-specific and strand-specific expression uncovered the extremely high level of HOXA103′-UTR sequence specific to osteoblasts of LV cells,which may function as anti-HOXA10-antisense by counteracting the HOXA10-antisense effect to determine TLV transition.Thus,this work provides a valuable resource for understanding embryonic osteogenesis and angiogenesis underlying vertebrate TLV and RP development at the cell type-specific resolution,which serves as a comprehensive view on the transcriptional profile of animal embryo development. | Jianbo Li Ligang Wang Dawei Yu Junfeng Hao Longchao Zhang Adeniyi C.Adeola Bingyu Mao Yun Gao Shifang Wu Chunling Zhu Yongqing Zhang Jilong Ren Changgai Mu David M.Irwin Lixian Wang Tang Hai Haibing Xie Yaping Zhang | 2021 | Genomics, Proteomics & Bioinformatics2021，19，3： | 1 |
| 9 | Removal of arsenic by pilot-scale vertical flow constructed wetland显示文摘Four pilot-scale Vertical Flow Constructed Wetlands(VFCWs)filled with gravel and planted with Phragmites australis were operated for seven months in the field to study the efficiency of arsenic removal in contaminated wastewater.The average arsenic removal efficiency by the VFCWs was 52.0%±20.2%,52.9%±21.3%,and 40.3%±19.4%at the theoretical concentrations of 50µg/L(CW50),100µg/L(CW100),and 500µg/L(CW500)arsenic in the wastewater,respectively.The results also showed no significant differences in the removal efficiency for conventional contaminants(nitrogen,phosphorus,or chemical oxygen demand)between wastewater treatments that did or did not contain arsenic(P>0.05),except for phosphorus in CW500.The highest average monthly removal rate of arsenic occurred in August(55.9%–74.5%)and the lowest in November(7.8%–15.5%).The arsenic removal efficiency of each VFCW was positively correlated with temperature(P<0.05).Arsenic accumulated in both substrates and plants,with greater accumulation associated with increased arsenic concentrations in the influent.The maximum accumulated arsenic concentrations in the substrates and plants at the end of the experiment were 4.47 mg/kg and 281.9 mg/kg,respectively,both present in CW500.The translocation factor(TF)of arsenic in the reeds was less than 1,with most of the arsenic accumulating in the roots.The arsenic mass balance indicated that substrate accumulation contributed most to arsenic removal(19.9%–30.4%),with lower levels in plants(3.8%–9.5%).In summary,VFCWs are effective for the treatment of arsenic-containing wastewater. | Yaocheng Fan Tiancui Li Deshou Cun Haibing Tang Yanran Dai Feihua Wang Wei Liang | 2021 | Frontiers of Environmental Science & Engineering2021，15，4： | 0 |
| 10 | Closed-Form Solution for a Circular Nanohole with Surface Effects Under Uniform Heat Flux显示文摘This paper investigates the steady-state thermoelastic problem of a circular nanohole embedded in an infinitely large elastic plane subjected to a uniform far-field heat flux.A lowly conductive surface model is used to account for the effects of surface phonon scattering,while the complete Gurtin–Murdoch model is utilized to characterize the effects of surface tension and surface elasticity.The closed-form solution to the temperature and stress field surrounding the hole is derived in the context of complex variable methods.Several numerical examples are presented to analyze the influence of surface effects on thermal stress fields.It is shown that surface effects induce notable increases in normal and shear stresses around the hole.Specifically,all three stress components(hoop,normal,and shear)in the vicinity of the hole exhibit substantial augmentation with increasing surface tension and surface modulus.In particular,it is found that the presence of surface effects amplifies the variation in stress gradients and intensifies stress concentration around the hole. | Jieyao Tang Jieyan Zhao Haibing Yang Cunfa Gao | 2024 | Acta Mechanica Solida Sinica2024，37，1： | 0 |
| 11 | Crisis Public Diplomacy in China显示文摘Due to the current domestic situation and trend of development, China should strive to promote internal harmony and progress, and improve strategic coordination with all major powers and the peripheral countries. It should study seriously the theories and practices of crisis public diplomacy, consolidate fundamental strategic capabilities, and enhance its ability to execute relevant programs. | Huang Zhong Tang Xiaosong Xing Haibing | 2014 | Contemporary International Relations2014，24，3： | 0 |
| 12 | Oral delivery of polyester nanoparticles for brain-targeting: Challenges and opportunities显示文摘Efficient oral delivery of drugs treating brain diseases has long been a challenging topic faced by the drug delivery community. Fortunately, polyester nanoparticles offer certain solutions to this problem. This review article firstly describes the main obstacles faced by oral administered brain targeting, including:(1)instability in the gastrointestinal tract;(2) poor penetration of the intestinal mucosa and epithelium;(3)blood clearance;and(4) restriction by the BBB. Then the key factors influencing brain-targeting efficiency of orally administered polyester nanoparticles are also discussed, such as size, shape and surface properties. Finally, recent brain-targeting delivery strategies using oral polyester nanoparticles as carriers and their effects on brain drugs transport are reviewed, and the delivery ‘as a whole’ strategy of polyester nanoparticles will provide new insight for oral brain-targeting delivery. And by combination of multiple strategies, both the stability and permeability of polyester nanoparticles can be greatly improved for oral brain drug delivery. | Ping Wang Yue Wang Ping Li Chen Chen Siman Ma Linxuan Zhao Haibing He Tian Yin Yu Zhang Xing Tang Jingxin Gou | 2023 | Chinese Chemical Letters2023，34，4： | 0 |
| 13 | Geographical Boundaries of the Ryukyu Islands: An Analysis显示文摘Three authors from the Institute of Japanese Studies, CICIR have analyzed geographical boundaries of the Ryukyu Islands from different perspectives to respond to Japan's view on this issue. | Sun Jianhong Tang Qi Xu Yongzhi Xing Haibing | 2013 | Contemporary International Relations2013，23，3： | 0 |
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