Journal of Chinese Pharmaceutical Sciences

Contents list

2004, 13(4): 1-01.

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Analysis of the Constituents in the Chinese Drug Notoginseng by Liquid Chromatography-Electrospray Mass Spectrometry

LIU Jin-huai, WANG Xuan^*, CAI Shao-qing, KOMATSU Katsuko, NAMBA Tsuneo

2004, 13(4): 225-237.

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Aim To develop a HPLC-UV-MS method for identifying the constituents in the Chinese drug Notoginseng (the root of Panax notoginseng). Methods A Phenomenex Luna C18 column (250 mm×4.6 mm ID, 5 μm) was utilized. Water containing 0.005% formic acid (A) and acetonitrile containing 0.005% formic acid (B) were used as gradient eluents. UV spectra were recorded in range 195-400 nm. Both positive and negative ion ESI modes were used. Results The constituents in Notoginseng were well separated and detected. Fourteen compounds were identified by comparing their retention time and ESI-MS data with those obtained from the reference compounds. Forty-one compounds were deduced by data analysis of MS and literature; among them, yesanchinosides-H and -E, chikusetsusaponin-L5, malonyl-ginsenoside-Rg1, the isomers of notoginsenosides-J, -A, -R1, -G, -R2, and ginsenoside-Rh3 were discovered in Notoginseng for the first time. Conclusion This method gives high sensitivity and good separation, and is suitable for identifying the constituents in Notoginseng. This result is helpful for further phytochemical research on Notoginseng. Based on this result, further quality control can be studied.

Template Synthesis of CPP32 Inhibitors by Ugi Four-Component Condensation Reaction

ZHANG Xin, ZOU Xiao-min, FU Yi-qiu, YANG Xiao-ming, MOU Ke, XU Ping^*

2004, 13(4): 238-241.

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Aim To find a reasonable way to prepare the designed CPP32 inhibitors. Method Ugi four-component condensation reaction was used to synthesize peptide mimic CPP32 inhibitors; Results A key isocyanide component (aspartate-derived isocyanide 3) and one of the designed CPP32 inhibitors 4 (as a template) were synthesized; Conclusion The CPP32 inhibitor 4 was synthesized by the newly developed procedure, which is an Ugi four-component condensation reaction based on aspartate-derived isocyanide 3. This method can be used to build up the CPP32 inhibitor library.

Use of Glucosyl 3,5-Dinitrobenzoate in Synthesis of Glucosides and Related Oligosaccharides

HUANG He-qing, LI Qing, CAI Meng-shen, LI Zhong-jun^*

2004, 13(4): 242-244.

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Aim To investigate a new glycosylation method. Methods In the presence of TMSOTf as catalyst, 1-O-(3, 5-dinitrobenzoyl)-2, 3, 4, 6-tetra-O-benzyl-α-D-glucopyranose 1 reacted with a series of carboxylic acid, phenols, alcohols and saccharides respectively to give the corresponding glycosylation products. The compounds were determined by ¹H NMR and ¹³C NMR spectra. Results The α-gluco-pyranosides and related oligosaccharides were prepared in high yields. Conclusion The 3, 5-dinitrobenzoyl group was found to be a good leaving group at the anomeric position and O-glucopyranosides and oligosaccharides were stereoselectively synthesized in good yield.

Synthesis of a New Series of Chalcone Derivatives and Their Antifungal Activities

LI Zheng-xiang, LI An-liang^*

2004, 13(4): 245-248.

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Aim To study the antifungal effect of chalcone derivatives. Methods Sixteen chalcone derivatives were synthesized and confirmed by ¹H NMR and IR spectra, and tested for antifungal activity against four common pathogenic fungi. Their structure-activity relationship is discussed. Results Among 16 title compounds, there were 5 new compounds, which have not been reported before. The preliminary antifungal test showed that all title compounds exhibited antifungal activities to a certain extent. The activity of compound 8 against Trichophyton rubrum had a potency equal to that of fluconazole, with a MIC of 4 μg·mL^-1. Conclusion Sixteen chalcones were prepared and their antifungal activities against four common pathogenic fungi in vitro were examined. Some of them exhibited antifungal activities to a certain extent.

Pharmacokinetics of Moclobemide Sustained Release Tablets after Multiple Oral Dose Administration in Healthy Volunteers

HU Dao-de^*, MAO Dan-zhuo, PEI Yuan-ying

2004, 13(4): 249-253.

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Aim To investigate the pharmacokinetic characteristics of moclobemide sustained release tablets after multiple oral dose administration in healthy Chinese volunteers. Methods Moclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg once daily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide in plasma were determined by reversed-phase high performance liquid chromatography. The partial pharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results The concentration-time profile fitted an one-compartment model best. The steady-state pharmacokinetic parameters of moclobemide sustained release tablets after multiple oral doses were as follows: Cmax was (1 950±156)μg·L^-1, Tmax was (6.00±1.55) h, T1/2(kel) was (3.14±0.12) h, AUCss0-24 was (22836±1842) μg·h·L^-1, MRT was (7.68±0.36) h, CL/F(s) was (20.2±2.1) L·h^-1, and V/F(c) was (91.4±9.4) L, respectively. No marked adverse events were noted during this study. Conclusion The formulation has a sustained-release effect and good tolerance in the healthy volunteers, which provides useful information for clinical practice.

Dissolution Improvement of Cisapride by Solid Dispersion with HPMC

WEI Zhen-ping, MAO Shi-rui, BI Dian-zhou, LI Yong*

2004, 13(4): 254-258.

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Aim To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose (HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means of improving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) were used to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in the carrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporation method. Powder X-ray diffraction (XRD) was used to measure the diffraction peaks of pure carrier, pure cisapride, physical mixture of HPMC with cisapride (4:1), and HPMC-cisapride solid dispersion (4:1) to confirm the crystal existence. The solubility of pure drug and HPMC-cisapride solid dispersion was measured with water, SGF and simulated intestinal fluid (SIF). The in vitro drug releases of the sustained release tablet prepared with pure cisapride or HPMC-cisapride solid dispersion were investigated with water and SGF as media, respectively. Results No diffraction peaks were found by X-ray diffraction in the HPMC-cisapride solid dispersion (4:1), indicating that the drug existed in an amorphous form at that drug-carrier ratio. Compared with the pure drug, the solubilities of HPMC-cisapride solid dispersion are increased by 239.4% in SGF, 132.6% in water, and 117.9% in SIF. According to the in vitro drug release, the sustained release tablet prepared with HPMC-cisapride solid dispersion had a faster drug release than did that prepared with pure drug. The in vitro drug release profiles were found to comply with Higuchi's rule. Conclusion The in vitro drug release of the sustained release tablet made by HPMC-cisapride solid dispersion is improved owing to the increased drug solubility.

Determination of Lycopene Concentration in Dog Plasma by RP-HPLC

WANG Hui-juan, LI Xin-ru, Huang Yan-qing, LIU Yan^*

2004, 13(4): 259-261.

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Aim A method for determination of lycopene concentration in dog plasma was established. Methods RP-HPLC was used; the mobile phase wavelength of detection was 472 nm, the column temperature was ambient temperature, and the flow rate was 1.0 mL·min^-1. Results The standard curve was linear in the range from 0.012 4 to 0.496 μg·mL^-1 with r = 0.9992. The average extraction recovery was 97.6%±4.2%. The intra-day and inter-day RSD were 1.52%-4.95% and 2.31%-7.38%, respectively. Conclusion This method is sensitive, rapid, reproducible, and of good selectivity for the analysis of lycopene in dog plasma.

Gel Filtration Chromatography Combined with Bradford Method for Determination of Total Residual Protein in Ferment Antibiotics

XU Ming-Zhe, MA Shi-Hong, HU Chang-Qin^*

2004, 13(4): 262-266.

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Aim A novel method has been developed for evaluation of the levels of total residual protein in antibiotics produced by fermentation using gel filtration chromatography (GFC) combined with Bradford assay based on determination of residual protein in lincomycin hydrochloride. Methods The chromatographic conditions were Superdex^TM peptide column, 0.01 mol·L^-1 phosphate buffer solution as mobile phase, and flow rate of 1 mL·min^-1. Five hundred microliters of lincomycin hydrochloride solution (3 g of lincomycin hydrochloride dissolved in 10 mL of mobile phase) was injected into the chromatograph and the eluted solution was collected between 6 min and 14.5 min (protein eluted from column within this period), and the residual content of total protein in the eluted solution was assayed using Bradford assay method. Results The average recovery was more than 90% for bovine serum albumin, the calibration equation for the range of 0-12 μg·mL^-1 of protein was y = -0.0024x² + 0.0642x + 0.0029, r²＝0.9999, RSD = 0.1%-0.9%, and the LOD and LOQ were 3 and 10 ng·mL^-1 of protein, respectively. Conclusion The novel method for determining the residual protein in ferment antibio-tics is simple, rapid, and precise.

Simultaneous Determination of Ceftazidime and Tazobactam in Injectable Powder by Reversed-Phase High Performance Liquid Chromatography

MENG Xiang-ming, MENG Zhi-yun, ZHANG Liang, DOU Gui-fang^*

2004, 13(4): 267-270.

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Aim A reversed-phase high performance liquid chromatographic (RP-HPLC) method was developed and validated for the simultaneous determination of ceftazidime and tazobactam in injectable powder. Methods Chromatography was carried out on Zorbax 300SB-C18 column using a mixture of methanol and aqueous solution of phosphate buffer (pH = 5.6) as mobile phase. The UV detection wavelength was 220 nm. Results The linear ranges of ceftazidime and tazobactam were 0.62-631.8 μg·mL^-1 and 0.66-677.50μg·mL^-1, respectively. The average recoveries were 98.8%-101.4% for ceftazidime, and 99.1%-100.2% for tazobactam. The RSD values of inter-day and intra-day assays were lower than 1.5% for ceftazidime and 2.6% for tazobactam. Conclusion This method is reproducible, simple, precise, and rapid for the quality control of ceftazidime and tazobactam in injectable powder.

Wavy Distribution of Trace Elements in Phytolacca Samples from Different Areas

DU Ying, OUYANG Li, LIU Ya-qiong, WANG Jing-yu^*

2004, 13(4): 271-275.

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Aim To study the distribution of 25 elements, i.e. Be, Cd, Ce, Cr, Cu, Dy, Er, Eu, Gd, Ge, Ho, La, Lu, Mo, Nd, Pb, Pr, Sm, Sr, Tb, Tl, Tm, Y, Yb and Zn in Phytolacca, a traditional Chinese medicinal herb, collected from nine areas of P.R. China. Methods Twenty-five elements in Phytolacca including essential elements, toxic elements and rare earth elements in traditional Chinese medicinal herbs from different areas were analyzed by ICP-MS. Results The 25 elements in Phytolacca were determined by ICP-MS under optimized conditions. The detection limits were 0.003-0.71 ng·mL^-1. The recoveries were 88%-118%. The relative standard deviations of the measurements were 1.7%-13.3%. Conclusion The determined concentrations of elements in Phytolacca acinosa Roxb vary from one area to another; however, the distribution tendency of elements in all the samples is similar. The distribution tendency of rare earth elements in Phytolacca acinosa Roxb is consistent with that in nature.

Preparation of BCEC-Astrocyte Co-culturing Membrane Plate Insert

ZHAO Kang-feng, WANG Qi, PU Xiao-ping^*, YANG Xiu-wei, ZHU Yu-zhen

2004, 13(4): 276-281.

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Aim To prepare a hand-made micropore membrane culture plate insert for co-culture. Methods The plate insert was made using plastic centrifuge tube and micropore membrane. After seeding brain capillary endothelial cells (BCECs) on it (under the effect of astrocyte-conditioned medium), the plate insert was assessed by analysis of trans-endothelial electrical resistance (TEER). Results The plate insert has a stability of at least 15 d under culture condition. TEER increased significantly under co-culture condition from (66.1±13.3) Ωcm² to (182.2±6.7) Ωcm². Conclusion This micropore membrane culture plate insert can be easily made, on which BCEC culture can be successfully performed. Moreover, it is adjustable and recyclable. It follows that the plate insert is a useful tool for co-culture and the related research fields.

Unbalance of the Physiological System May Cause Trouble —The Other Side of the Story from the Very Successful Drug, VIOXX

SUN Hong-shuo, FENG Zhong-ping^*

2004, 13(4): 282-284.

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A Bioactive Diterpene from the Chinese Herb Aster souliei

ZHANG Yong-hong^*, WANG Yan-lin, CAI Ai-hua, WANG Qin, CHENG Dong-liang

2004, 13(4): 285-287.

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