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Asian Journal of Pharmaceutical Sciences 2016年第6期11卷 771-779页

作者： Yan Li haibing he Qiao Wang Xing Tang Shenyang Pharmaceutical University

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 *** 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.

关键词： Timataxel Lipid microspheres Stability assessment Pharmacokinetics

Titanium-promoted Intramolecular Photoenolization/Diels-Alder Reaction to Construct Polycyclic Terpenoids: Formal Synthesis of Mycoleptodiscin A

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Chinese Journal of Chemistry 2019年第2期37卷 135-139页

作者： Dongsheng Xue Mengmeng Xu Chaoying Zheng Baochao Yang Min Hou haibing he Shuanhu Gao Shanghai Key Laboratory of Green Chemistry and Chemical Processes School of Chemistry and Molecular EngineeringEast China Normal University3663N Zhongshan RoadShanghai 200062China Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development East China Normal University3663N Zhongshan RoadShanghai 200062China

Summary of main observation and conclusion A titanium-promoted intramolecular photoenolization/Diels-Alder (PEDA) reaction was developed to construct the core skeleton of aromatic polycyclic terpenoids bearing an all-carbon quaternary center on the benzylic position. Titanium(Ⅳ) isopropoxide [Ti(Oi-Pr)4] plays a key role during the photo cycloaddition, which may help to accelerate the in teraction between dienophile and the stereo-hi ndered diene species as well as control the diastereoselectivity. This photolysis provides a new solution for the stereospecific formation core structures of aromatic abietane diterpenoids and sesquiterpenoids, which have multiple functional groups for the further transformations. As a synthetic application, it was successfully used in the synthesis of indolosesquiterpenoid mycoleptodiscin A.

关键词： Titanium-promoted Intramolecular Photoenolization Construct Polycyclic Terpenoids

Hot-melt sub-and outercoating combined with enteric aqueous coating to improve the stability of aspirin tablets

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Asian Journal of Pharmaceutical Sciences 2017年第3期12卷 266-278页

作者： Xiuzhi Wang Puxiu Wang Chenglong Huang Xiaoyang Lin Haoyu Gong haibing he Cuifang Cai Department of Pharmaceutics Science Shenyang Pharmaceutical University

Aspirin is apt to hydrolyze. In order to improve its stability, a new method has been developed involving the application of hot-melt sub-and outercoating combined with enteric aqueous coating. The main aim was to investigate the influence of these factors on the stability of ASA and understand how they work. Satisfactory storage stability were obtained when the aspirin tablet core coated with Eudragit L30D55 film was combined with glycerin monostearate(GMS) as an outercoat. Hygroscopicity testing indicated that the moisture penetrating into the tablet may result in a significant change in the physical properties of the coating film observed by scanning electron microscopy. Investigation of the compatibility between the drug and film excipients shows that the talc and methacrylic acid had a significant catalytic effect on ASA. A hypothesis was proposed that the hydrolysis of ASA enteric coated tablets(ASA-ECT) was mostly concentrated in the internal film and the interfaces between the film and tablet core. In conclusion, hot-melt coating technology is an alternative to subcoating or outercoating. Also, GMS sub-coating was a better choice for forming a stable barrier between the tablet core and the polymer coating layer, and increases the structure and chemical stability.

关键词： Acetylsalicylic acid Hot-melt coating Glycerin monostearate Storage stability Drug/excipient compatibility

A numerical study on Rayleigh-Taylor instability of aluminum plates driven by detonation

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Science China(Physics,Mechanics & Astronomy) 2010年第2期53卷 195-198页

作者： he ChangJiang,ZHOU haibing & HANG YiHong Institute of Applied Physics and Computational Mathematics,Laboratory of Computational Physics,Beijing 100088,China 1. Institute of Applied Physics and Computational Mathematics Laboratory of Computational Physics Beijing 100088 China

The authors,using elastic-plastic hydrodynamic code,present the Rayleigh-Taylor (RT) instability of Al plates driven by high-explosive detonation. Our numerical study assumes the material is fluid,or it is an elastic-plastic solid,and we compare the results of these simulations with the experimental data. For the numerical simulation of Rayleigh-Taylor instability of the metal driven by high-explosive detonation,the elastic-plastic effect must be assumed. The result of the simulation is different from the experiment,using only equation of state. However,the growth of perturbation agrees well with the measured growth under the second assumption. There is a cutoff wavelength for RT instability of the metal. The growth of perturbation is stable for short wavelength. The growth increases rapidly as the wavelength increases.

关键词： interface instability elastic-plastic numerical simulation

Glucocorticoids-based prodrug design:Current strategies and research progress

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Asian Journal of Pharmaceutical Sciences 2024年第3期19卷 41-78页

作者： Hongbing Liu Muse Ji Peifu Xiao Jingxin Gou Tian Yin haibing he Xing Tang Yu Zhang Department of Pharmaceutics Shenyang Pharmaceutical UniversityShenyang 110016China School of Chinese Materia Medica Shenyang Pharmaceutical UniversityShenyang 110016China

Attributing to their broad pharmacological effects encompassing anti-inflammation,antitoxin,and immunosuppression,glucocorticoids(GCs)are extensively utilized in the clinic for the treatment of diverse diseases such as lupus erythematosus,nephritis,arthritis,ulcerative colitis,asthma,keratitis,macular edema,and ***,longterm use often causes undesirable side effects,including metabolic disorders-induced Cushing's syndrome(buffalo back,full moon face,hyperglycemia,etc.),osteoporosis,aggravated infection,psychosis,glaucoma,and *** notorious side effects seriously compromise patients'quality of life,especially in patients with chronic ***,glucocorticoid-based advanced drug delivery systems for reducing adverse effects have received extensive *** them,prodrugs have the advantages of low investment,low risk,and high success rate,making them a promising *** this review,we propose the strategies for the design and summarize current research progress of glucocorticoid-based prodrugs in recent decades,including polymer-based prodrugs,dendrimer-based prodrugs,antibody-drug conjugates,peptide-drug conjugates,carbohydrate-based prodrugs,aliphatic acid-based prodrugs and so ***,we also raise issues that need to be focused on during the development of glucocorticoid-based *** review is expected to be helpful for the research and development of novel GCs and prodrugs.

关键词： Glucocorticoids Prodrug design Targeted drug delivery Research progress

Tablets of paliperidone using compression-coated technology for controlled ascending release

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Asian Journal of Pharmaceutical Sciences 2018年第2期13卷 143-154页

作者： Yingying Tang Huan Teng Yanan Shi haibing he Yu Zhang Tian Yin Cuifang Cai Xing Tang School of Pharmacy Shenyang Pharmaceutical University

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 *** 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 *** 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.

关键词： Paliperidone Compression-coated tablet Ascending release Controlled release

Effects of mixed fertilizers formed by the compounding of two targeted controlled-release nitrogen fertilizers on yield,nitrogen use efficiency,and ammonia volatilization in double-cropping rice

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The Crop Journal 2023年第2期11卷 628-637页

作者： Jian Ke Jie Sun Tingting Chen Shibao Tao Tiezhong Zhu Chuanjun Yin haibing he Cuicui You Liquan Wu Shuangshuang Guo College of Agronomy Anhui Agricultural UniversityHefei 230031AnhuiChina Zoomlion Intelligent Agriculture Co. Ltd.Wuhu 241000AnhuiChina

One-time application of mixed fertilizer formed by the compounding of two controlled-release nitrogen fertilizers(CRUs)with targeted N supply during the periods from transplantation(TS)to panicle initiation(PI)and from PI to heading(HS)is expected to synchronize the double-peak N demand of ***,its effects on the yield and N use efficiency(NUE)of labor-intensive double-cropping rice were *** targeted CRU(CRU_(A)and CRU_(B))were compounded in five ratios(CRU_(A):CRU_(B)=10:0,7:3,5:5,3:7,and 0:10)to form five mixed fertilizers(BBFs):BBF1-5.A field experiment was performed to investigate the characteristics of N supply in early and late seasons under different BBFs and their effects on N uptake,yield,and ammonia volatilization(AV)loss from paddy fields of double-cropping *** high-yield fertilization(CK,three split applications of urea)and zero-N treatments were established as *** N supply dropped significantly with the increased compound ratio of CRU_(B)during the period from TS to PI,but increased during the period from PI to *** the exception of the period from TS to PI in the late rice season,the N uptake of early and late rice maintained close synchronicity with the N supply of BBFs during the double-peak *** N supply(BBF1 and BBF2)in the late rice season during the period from TS to PI increased N loss by *** effect of BBF on grain yield increase varied widely between seasons,irrespective of *** the BBFs,the BBF2 treatment of early rice not only stabilized the spikelets per panicle but also ensured a high number of effective panicles by promoting N uptake during the period from TS to PI and a high grain-filling percentage by appropriately reducing the N supply at the later PI stage,resulting in the highest rice *** stabilizing the effective panicle number,the BBF4 treatment of late rice increased the number of spikelets per panicle by promoting N uptake during the period from PI to HS,resul

关键词： Targeted controlled-release fertilizer Mixed fertilizer Double-cropping rice N uptake Yield

Oral delivery of polyester nanoparticles for brain-targeting: Challenges and opportunities

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Chinese Chemical Letters 2023年第4期34卷 99-109页

作者： Ping Wang Yue Wang Ping Li Chen Chen Siman Ma Linxuan Zhao haibing he Tian Yin Yu Zhang Xing Tang Jingxin Gou Department of Pharmaceutics Shenyang Pharmaceutical UniversityShenyang 110016China School of Pharmacy Jilin UniversityChangchun 130021China School of Functional Food and Wine Shenyang Pharmaceutical UniversityShenyang 110016China

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.

关键词： Polyester nanoparticles Oral brain drugs Brain-targeted delivery Physiological barrier Absorption enhancement

Supersaturation induced by Itraconazole/Soluplus micelles provided high GI absorption in vivo

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Asian Journal of Pharmaceutical Sciences 2016年第2期11卷 255-264页

作者： Yue Zhong Guanghui Jing Bin Tian Hao Huang Yuanyuan Zhang Jingxin Gou Xing Tang haibing he Yanjiao Wang Department of Pharmaceutics Shenyang Pharmaceutical University

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 gre

关键词： Solid dispersion Itraconazole tablets Hot melt extrusion Supersaturation Micelles Bioavailability

An intravenous clarithromycin lipid emulsion with a high drug loading, H-bonding and a hydrogen-bonded ion pair complex exhibiting excellent antibacterial activity

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Asian Journal of Pharmaceutical Sciences 2016年第5期11卷 618-630页

作者： Haoyu Gong Sicong Geng Qi Zheng Puxiu Wang Lifeng Luo Xiuzhi Wang Yan Zhang Yu Zhang haibing he Xing Tang Shenyang Pharmaceutical University

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 *** showed that almost 88% CLA could be loaded into the interfacial *** 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.

关键词： Clarithromycin Cholesteryl hemisuccinate H-bonding and hydrogen-bonded ion pair complex Antibacterial activity Thin-film dispersed homogenization