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	1. Pharmacokinetics of membrane-moderated granulated pellet-containing tablets in beagles
	LI Lu,LIN Shiqi,HUANG Ying,ZHU Chune,QUAN Guilan,PAN Xin,WU Chuanbin
	Pharmacy 21 May 2016
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	Abstract:Granulated pellet-containing tablets (GPCT) were prepared via a novel granulation technique, which laid the excipients on coated pellets and then compressed into GCPT after mixing with the cushioning fillers. The pharmacokinetics of doxycycline hydrochloride GPCT were evaluated to confirm the integrity of the coating film after compaction, with the coated pellets as a reference, containing equivalent doxycycline hydrochloride in the two formulations. The study was performed on six healthy beagles by a randomized-sequence, open-label, single-dose, two-period, crossover design with a 2-week washout period. Blood samples were collected and analyzed to calculate several pharmacokinetics parameters. The mean maximum plasma concentration (Cmax) for the test formulation and reference formulation were 2.73±0.22 mg/L and 2.94±0.47 mg/L, the mean time to reach Cmax (Tmax) were 6.67±0.47 h and 6.33±0.42 h, the AUC0-t were 68.42±6.94 mgoh/L and 72.87±12.51 mgoh/L, and the mean residence time (MRT) were 15.62±0.53 h and 15.26±0.79 h respectively. The pharmacokinetics analysis suggested that there was no significant difference regarding drug release properties, and the granulated pellet-containing tablets met the regulatory criteria for bioequivalence to the reference formulation of coated pellets in the healthy fasting beagles, from which the novel granulation technique might be proposed as an effective approach to prepare pellet-containing tablets without compromising the integrity of coating films.
	TO cite this article:LI Lu,LIN Shiqi,HUANG Ying, et al. Pharmacokinetics of membrane-moderated granulated pellet-containing tablets in beagles[OL].[21 May 2016] http://en.paper.edu.cn/en_releasepaper/content/4693621


	2. Subcellular Quantification of Doxorubicin and its Metabolite in Cultured Human Leukemia Cells using Liquid Chromatography-Tandem Mass Spectrometry
	Xu Jinhui,Chen Yun
	Pharmacy 03 December 2012
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	Abstract:Doxorubicin (DOX) is widely used in the world as an anti-cancer agent for the treatment of leukemia and solid tumors. However, its clinic use is largely limited by the emergence of cardiotoxicity. One of the most frequently proposed mechanisms for DOX induced cardiotoxicity is the formation of metabolites. However, the enzymatic pathways involved in DOX intracellular metabolism have not been fully elucidated thus far. To provide a more detailed description of DOX metabolism, an assay using liquid chromatography-tandem mass spectrometry (LC/MS/MS) was developed in our lab to simultaneously determine DOX and its primary metabolite doxorubicinol (DOXol) in subcellular compartments. Good accuracy and precision were achieved. Using this assay, the accumulation of DOX and DOXol in whole cells, nuclear enriched fraction (NEF) and organelle-enriched fraction (OEF) were compared between two human T leukemia cell lines (i.e., Jurkat and CCRF-CEM). A time-course analysis was also carried out. The resulting varieties of DOX and DOXol subcellular distributions and concentration-time profiles might be attributed to the differential expression, activities and localization of reductive enzymes within these cell lines. More importantly, this work demonstrated that simultaneous determination of drug and its metabolite in subcellular compartments could be achieved using LC/MS/MS.
	TO cite this article:Xu Jinhui,Chen Yun. Subcellular Quantification of Doxorubicin and its Metabolite in Cultured Human Leukemia Cells using Liquid Chromatography-Tandem Mass Spectrometry[OL].[ 3 December 2012] http://en.paper.edu.cn/en_releasepaper/content/4500290


	3. Synthesis and Biological Evaluation of Oleanolic Acid Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B
	Li Hui,Zou-Hui,Gao Lixin,Liu Ting,Yang Fan,Li Jingya,Li Jia,Qiu Wen-Wei,Tang Jie
	Pharmacy 18 January 2012
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	Abstract:A series of oleanolic acid (OA) derivatives have been synthesized and their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Some compounds with five-membered heterocyclic ring fused at C-2, C-3 positions showed a dramatic increase in inhibition, the two most potent PTP1B inhibitors 19 (IC50 = 0.91 μM) and 21 (IC50 = 0.98 μM) showed about 3-fold more potent than lead compound OA. Some compounds with C-ring modified showed high selectivity for PTP1B over TCPTP, among them, 50 possessed the best selectivity of 6.6-fold.
	TO cite this article:Li Hui,Zou-Hui,Gao Lixin, et al. Synthesis and Biological Evaluation of Oleanolic Acid Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B[OL].[18 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4463053


	4. Regioselective glucuronidation of tanshinone IIa following quinone reduction: identification of human UDP-glucuronosyltransferases, species differences, and interaction potentials
	Wang Qiong,Wang Guangji,Zhu Xuanxuan,Yu Guo,Lai Li,Liu Yitong, , ,
	Pharmacy 20 January 2010
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	Abstract:We have previously identified that the NQO1 mediated quinone reduction and subsequent glucuronidation is the predominant metabolic pathway for tanshinone IIa (TSA) in rats. The present study contributes to the further research on its glucuronidation enzyme kinetics, the identification of human UDP-glucuronosyltransferase (UGT) isoforms, and the interaction potentials. A pair of regioisomers of reduced TSA glucuronides was found from human, rats and mice, whereas only M1 was found in dog liver S9 incubations. The overall glucuronidations clearance of TSA in human liver S9 was 11.8±0.8μl/min/mg protein, 0.7, 0.8, and 3 fold of that in the mice, rats and dogs, respectively. Using CLint M2/M1 as a regioselective index, opposite regioselectivity was found between human (0.7) and mice (1.3), whereas no significant regioselectitvity was found in rats. In a sequential metabolism system by applying human liver cytosol as a NQO1 donor in combination with a panel of 12 recombinant human UGTs screen, multiple UGTs were found involved in the M1 formation, whereas only UGT1A9 and to a very minor extent of UGT1A1 and 1A3 contributed to the M2 formation. Further enzyme kinetics, correlation, and chemical inhibition studies confirmed that UGT1A9 played the major role for both M1 and M2 formations. In addition, TSA presented potent inhibitory effect on the glucuronidations of typical UGT1A9 substrates propofol and MPA, with an IC50 value at 8.4±1.8μM and 8.9±1.9μM respectively. This study would be helpful for guiding the future studies on characterizing the NQO1 mediated reduction and subsequent glucuronidations of other quinones.
	TO cite this article:Wang Qiong,Wang Guangji,Zhu Xuanxuan, et al. Regioselective glucuronidation of tanshinone IIa following quinone reduction: identification of human UDP-glucuronosyltransferases, species differences, and interaction potentials[OL].[20 January 2010] http://en.paper.edu.cn/en_releasepaper/content/39224


	5. Modeling the Interaction between Glycogen Synthase Kinase 3β (GSK-3β) and Its Non-ATP Competitive Inhibitors
	Yong Chu,Keng-Chang Tsai,Deyong Ye,Minyong Li
	Pharmacy 27 September 2009
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	Abstract:Glycogen synthase kinase-3 (GSK-3) plays an important role in a diverse number of regulatory pathways. GSK-3 inhibitors, particularly the non-ATP-competitive inhibitors, have been evaluated as promising drug candidates for a lot of unmet pathologies, such as Alzheimer’s disease and diabetes. In this paper, a molecular docking study with the published GSK-3β crystal structure and receptor-based pharmacophore modeling of four highly active non-ATP-competitive GSK-3 inhibitors were performed by DOCK 5.4 and Catalyst 4.11, respectively. The results could provide an exquisite understanding on their mechanism of interaction within the non-ATP-binding pocket of GSK-3β, meanwhile the finding of the common properties shared by these pharmacological inhibitors of GSK-3β could be helpful to further chemical optimization of such potent drug candidates.
	TO cite this article:Yong Chu,Keng-Chang Tsai,Deyong Ye, et al. Modeling the Interaction between Glycogen Synthase Kinase 3β (GSK-3β) and Its Non-ATP Competitive Inhibitors[OL].[27 September 2009] http://en.paper.edu.cn/en_releasepaper/content/35514

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