Journal of Chinese Pharmaceutical Sciences

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2003, 12(2): 1-01.

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Polyphenols from Vitis thunbergii Sieb. et Zucc.

DOU De-qiang^*, REN Jie, Maggie Cooper , HE Yue-hua, PEI Yu-ping, Yoshiaki Takaya, Masatake Niwa, CHEN Ying-jie, YAO Xin-sheng, ZHOU Ren-ping

2003, 12(2): 57-59.

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Aim Isolation and structural elucidation of the constituents from the aerial part of Vitis thunbergii. Methods To isolate chemical constituents, column chromatography and HPLC were used. Physico-chemical characterization and spectroscopic analysis were employed for structural identification. Results Eleven polyphenols were isolated and identified. Conclusion Compound 1 is a new compound and its structure was characterized to be 3,5-dimethoxyl-4-hydroxyl-phenyl-propanol-9-O-β-D-glycopyranoside.

Purification and Characterization of Flammulin,a Basic Protein with Anti-tumor Activities from Flammulina velutipes

CHEN Chang, XUE Jiu-gang, ZHOU Kai-song, LI Yan, ZHANG Han-xing, ZHANG Chang-kai^*

2003, 12(2): 60-65.

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Aim To purify and characterize flammulin, a basic protein with anti-tumor activities. Methods Ammonium sulfate, ethanol fractionation and column chromatography were used for separation and purification. Electrophoretic analysis, amino acid analysis, and MS of flammulin were carried out. Results Flammulin was purified to electrophoretic homogeneity and crystallized. With a molecular mass of 19891.13 Da, pI = 8.9, λmax = 276-278 nm, λmin = 250nm, flammulin was characterized by its lack of methionine. Fingerprint mapping of flammulin was determined by MALDI-MS following in-gel protease digestion; no close matches were identified. Conclusion Flammulin was purified to electrophoretic neity, and its characteristics are discussed for the first time.

Synthesis of PNA Monomer by Ugi Four-Component Condensation Reaction

WANG Wen-hao, ZHANG Ting, XU Ping^*

2003, 12(2): 66-70.

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Aim To improve the physico-chemical and biological properties, original PNAs were derivatized and modified; Methods Ugi four-component condensation reaction (Ugi 4-CC) was used to synthesize PNAs, in which the Fmocprotecting strategy was adopted; Results The Fmoc-protected PNA monomer and the key component isocyanide were synthesized; Conclusion A simple and changeable method for synthesis of PNA monomer has been developed.

Comparative Efficacy and Distribution of Evans Blue Liposome Modified with DSPE-PEG, Tween80, and Brij35

ZHANG Xiao-bin, HOU Xin-pu^*

2003, 12(2): 71-75.

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Aim To improve the stability and optimize the tissue distribution of Evans blue liposome in rats, some surfactants such as DSPE PEG, Tween80, and Brij35 were used to modify the Evans blue liposome. Methods The Evans blue liposome was prepared by the reverse phase evaporation method. The effect of cholesterol on the encapsulation percentage of Evans blue was studied. The effects of DSPE PEG, Tween80, and Brij35 on the encapsulation percentage and tissue distribution of Evans blue liposome in the rat were determined. Results The top encapsulation percentage of Evans blue liposome is 25.30%. After modification by DSPE PEG, Tween80, and Brij35, the encapsulation percentages decreased slightly, but not significantly. After modification, the Evans blue concentrations deceased in the liver, spleen, lung and kidney, but increased in the brain, especially in the EB-L-Tween80 group. Conclusion DSPE-PEG, Tween80, and Brij35 have slight effect on the encapsulation percentage of Evans blue liposome. The effect of Brij35 on the distribution of Evans blue liposome is similar to that of DSPE-PEG because they both is prevent the reticuloendothelial system (RES) from clearing liposome. The Evans blue concentration in the brain is greatly improved when Tween80 is used to modify the EB liposome, which is good information for preparing liposome targeting the brain.

Preparation and Characterization of Solid Dispersions of Silymarin with Polyethylene Glycol 6000

LI Feng-qian^*, HU Jin-hong, JIANG Yuan-ying

2003, 12(2): 76-81.

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Aim To prepare and characterize solid dispersions of silymarin with the intention of improving their dissolution properties. Methods The solid dispersions were prepared by the fusion method with polyethylene glycol 6000 (PEG 6000) as the carrier. Evaluation of the properties of the dispersions was performed using dissolution studies, X-ray powder diffraction and Fourier-transform infrared (FT-IR) spectroscopy. Results The rate of dissolution of silymarin was considerably improved as compared with pure silymarin when formulated in solid dispersions with PEG 6000. The data of the X-ray diffraction showed some changes in the parameters of lattice spacing [d], peak position and relative intensities. FT-IR together with those from X-ray diffraction showed the absence of well-defined drug-polymer interactions. Conclusion The dissolution improvement of poorly soluble silymarin could be illuminated by the changes of the lattice parameters of PEG 6000 and the drug.

Preparation and Pharmacokinetic Characterization of Sustained Release Melatonin Tablet

HE Zhong-gui^*, ZHANG Tian-hong, TANG Xing, ZHANG Ru-hua

2003, 12(2): 82-86.

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Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of the size of melatonin, type and amount of HPMC, drug loading, type and amount of additives, and compressing pressure were investigated. Plasma concentration of melatonin in dogs after intravenous injection of two doses and oral administration of sustained release tablets and unmodified release capsules was detected by HPLC using fluorescence detector. Results The drug release from sustained release tablets was influenced by the size of melatonin, type and amount of HPMC, drug loading, and type and amount of additives. Melatonin was found to fit two compartment model after intravenous injection, AUC was proportional to doses, and t1/2β of two doses has no significant difference. Relative bioavailability of melatonin sustained release tablet to normal capsule was 83.8%, and absolute bioavailability was 3.75% for sustained release tablet and 4.49% for capsule. Conclusion The melatonin sustained release tablet was well formulated. The absolute bioavilability for oral administration of either sustained release tablet or unmodified release capsule of melatonin was less than 5%. The bioavailability of melatonin sustained release tablet was lower than that of unmodified release capsule, but MRT of sustained release tablet was significantly longer than that of capsule.

Preparation and in Vitro Evaluation of Polylactic Acid (PLA) or Polylactic-co-Glycolic Acid (PLGA) Microcapsules Loaded with Estradiol

ZHOU Xin-teng^*, ZHU Feng, PAN Wei-san, WANG Lei, ZHANG Ru-hua

2003, 12(2): 87-92.

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Aim PLA/PLGA was used as biodegradable and biocompatible carriers to achieve sustained release of estradiol (E2). Methods Microcapsules (MC) were prepared by an emulsification-solvent extraction method, and then the properties and in vitro drug release behavior of MC were examined. An analysis of variance (ANOVA) was used to test the statistical significance. Then, multiple comparisons were made with a T-method between levels to examine the significance of difference further. For all the results a P value>0.05 was considered statistically insignificant. Results Under the same conditions, the water-adding speed and the particle size had significant effects (P<0.01) on the entrapment efficiency of MC; the water-adding speed and the concentration of PLA in the oil phase had significant effects (P<0.01) on the diameter MC in medium. Release of E2 from MC was influenced significantly (P<0.01) by the water-adding speed and the type and molecule weight of the polymers. But the differences between levels of the variates were not all significant. Conclusion E2-PLA/PLGA-MC with various properties can be formed when the formulation and the technology were changed accordingly.

Determination of 2-Amino-6-Cyclopropylamino-9-(2,3-Dideoxy-β-D-glyceropent-2-enofuranosyl)purine in Rat Plasma, Urine and Liver Homogenates by High Performance Liquid Chromatography

LIU Yi, YANG Zhen-jun^*, Boudinot F Douglas, CHU Chang kuang, ZHANG Li-he

2003, 12(2): 93-97.

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Aim To develop a simple and specific high-performance liquid chromatographic (HPLC) method, suitable for the pharmacokinetic studies in Vivo, to determine the concentrations of 2-amino-6-cyclopropylamino-9-(2,3-dideoxy-β-D-glyceropent-2-enofuranosyl) purine (Cyclo-D4G, D4G prodrug) in rat plasma, urine and liver homogenates. Methods Chromatography was performed with C-18 Hypersil ODS column and a mobile phase of 7% (v/v) acetonitrile in phosphate buffer, pH7.40, with UV detection at 283 nm. Results The average extraction recovery of Cyclo-D4G in rat plasma and urine was 100.1% over its linear range of 0.5-80 μg·mL^-1. The accuracy of the assay was 99.4%. The intra-and interday RSDs were less than 9.0%. Conclusion The analytical method was found to be applicable, reliable and suitable for pharmacokinetic studies.

¹H and ¹³C NMR Assignments for Mosapride

SUN Jing, LI Qin, QIAO Liang, CUI Yu-xin^*

2003, 12(2): 98-100.

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¹H and ¹³C NMR spectra for mosapride were assigned by 1D and 2D NMR techniques (gCOSY, gNOESY, gHMQC, gHMBC). The molecular modeling result was used to prove the predominant conformations of the morpholine ring that the authors predicted.

Determination of Sulphonylurea Glimepiride in Dog Serum by RP-HPLC with Pre-column Derivatization

LU Lai-chun, JIANG Xue-hua^*, ZHOU Jing, YANG Jun-yi

2003, 12(2): 101-105.

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Aim A simple, sensitive and rapid RP-HPLC method with pre-column derivatization has been developed for the determination of sulphonylurea glimepiride in dog serum. Methods The sulphonylurea glimepiride was extracted from the dog serun using dichlromethane followed by derivatization with DNBF for 20 min at 100 °C. The solvent was then evaporated at 60 °C under nitrogen, and the residue was taken up in 100 μL of mobile phase consisting of acetonitrile-water (75:30, v/v). The separation was performed on a Hypersil BDS C18 column with a flow rate of 0.8 mL·min^-1, and the ultraviolet detector wavelength was set at 350nm. Results Extraction recovery ranged from 75.9% to83.2%, and methodological recovery was between 96.5% and 109.3%. Within-day RSD ranged from 1.5% to 6.3%, and inter-day RSD was between 2.9% and 14.8%. The method showed good linearity (R = 0.9998). Conclusion The method was simple, convenient and sensitive. reaction of derivatization was reproducible.

Secondary Structure and Neurotrophic Effect of a 33.1 kDa Specific Protein (SSP-33.1) in Spinal Sensory Ganglia

SHEN Jian-ying, YU Qing-sheng, WANG Qi, LI Quan, PU Xiao-ping^*

2003, 12(2): 106-111.

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Aim To analyze the secondary structure and neurotrophic effect of a specific protein in sensory neurons. Methods Comparison of the proteins expressed in the rat spinal sensory neurons and motor neurons was made by two-dimensional electrophoresis. One specific protein in sensory neurons was isolated and purified by DEAE-Sephacel ion exchange chromatography and high performance liquid chromatography. A primary analysis of its secondary structure by circular dichroism, and its neurotrophic effects were investigated using the model of dorsal root ganglia (DRG) cultured in vitro. Results The molecular weight and isoelectric point of the protein were 33.1 kDa and 5.52, respectively. Its circular dichroism showed that there were 20.8% α-helix, 54.8% β-sheet, 7.3% turn, and 17.1% random coil in its secondary structure. Biological experiments showed that the protein could promote the neurite outgrowth of DRG. Conclusion A specific protein in spinal sensory tissue with molecular weight of 33.1 kDa has been purified. There is mainly β-sheet in the secondary structure of the protein. And the protein has neurotrophic effects in the model of DRG.

Three Anthraquinones Isolated from Aster tataricus L.f

LU Yan-hua, WANG Zheng-tao^*, XU Luo-shan, WU Zi-bin

2003, 12(2): 112-113.

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A HPLC Method for the Determination of Salmon Calcitonin in Injection by Gradient Elution

CHEN Xiao-ping, GUO Qing-dong, ZHANG Qiang^*

2003, 12(2): 114-116.

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