Journal of Chinese Pharmaceutical Sciences

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2004, 13(3): 1-01.

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Iridoid Glycosides from Buddleja lindeyana

LU Jiang-hai, PU Xiao-ping, TU Guang-zhong, ZHAO Yu-ying^*

2004, 13(3): 151-154.

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Aim To study the chemical constituents of Buddleja lindeyana. Methods The constituents were separated and purified by different methods of chromatography, and their structures were elucidated by IR, MS and NMR. Results Three iridoid glycosides and two other compounds were isolated from Buddleja lindeyana. Their structures were elucidated to be 6-O-feruloylajugol (1), erythro-6-oxo-4'-(3-methoxyl-4-hydroxyphenylglycol-8'')-feruloylaj-ugol (2), threo-6-oxo-4'-(3-methoxyl-4-hydroxyphenylglycol-8'')-feruloylajugol (3), tetra-cosanoic acid 2,3-dihydroxypropyl ester (4), and galactitol (5). Conclusion All the compounds have been isolated from this plant for the first time. Compounds 1, 2 and 3 have protective effect agains MPP⁺-induced apoptosis.

Chemical Constituents of Euphorbia ebracteolata

SHI Hai-ming, MIN Zhi-da^*

2004, 13(3): 155-157.

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Aim To studythe chemical constituents of Euphorbia ebracteolata Hayata. Methods Column chromatography was used in the isolation procedure, while the structures of isolated compounds were elucidated by spectral data. Results Six compounds were isolated and their structures were identified as baccatin (1), 3-acetyl-β-amyrin (2), 3,3'-diacetyl-4,4'-dimethoxy- 2,2',6,6'-tetrah ydroxy diphenylmethane (3), 2,4- dihydroxy-6- methoxy-3-methyl acetophenone (4), β- sitosterol(5), and daucosterol (6). Conclusion Baccatin was obtained from Euphorbia ebracteolata for the first time.

Effect of Complexation with Hydroxylpropyl-β-Cyclodextrin on Solubility, Dissolution Rate and Chemical Stability of Prostaglandin E₁

GU Fu-gen, CUI Fu-de^*, GAO Yong-liang

2004, 13(3): 158-165.

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Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin (HP-β-CD) on the solubility,dissolution rate and chemical stability of prostaglandin E1 (PGE1), thereby providing a basis for preparing a stable solid or aqueous preparation of PGE1 formulated with HP-β-CD. Methods The effect of HP-β-CD on the solubility of PGE1 was studied by phase solubility method. The formation of inclusion complexes of PGE1 with HP-β-CD in the aqueous solution was confirmed by UV spectra, circular dichroism spectroscopy, and that in the solid state by IR spectra and X-ray diffractometry. An solid inclusion complex of PGE1 with HP-β-CD was prepared by lyophilization. The dissolution rate and stability of the inclusion complex were determined and compared with those of PGE1 alone. Meanwhile, the stability of PGE1 aqueoussolutions in the presence of HP-β-CD was studied under different pH conditions. Results The solubility of PGE1 increased linearly with increasing HP-β-CD concentration in various pH buffered solutions, showing typical AL-type phase solubility diagrams. The stability and dissolution rate of the solid inclusion complex of PGE1 were significantly increased, compared with those of pure PGE1. The stability of PGE1 in HP-β-CD solutions was also obviously improved under acidic and basic conditions, but the stabilizing effect was absent under neutral conditions. Conclusions The solubility,dissolution rate and chemical stability of PGE1 are markedly improved by complexation with HP-β-CD. It is quite possible to prepare a stable PGE1 inclusion complex-containing solid dosage forms, but almost impossible to obtain a stable aqueous preparation of PGE1 formulated with HP-β-CD.

Determination of Clarithromycin in Human Plasma by Liquid Chromatography-Tandem Mass Spectrometry: Validation and Application in Clinical Pharmacokinetic Study

ZHANG Xiang-rong, CHEN Xiao-yan, LI Xiao-yan, ZHONG Da-fang^*

2004, 13(3): 166-170.

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Aim To develop a liquid chromatographic-tandem mass spectrometric (LC-MS-MS) method to determine clarithromycin in human plasma. Methods The analyte and internal standard roxithromycin were extracted from plasma samples by n-nexane-dichloromethane-isopropanol (300:150:15, V/V/V) and chromatographed on a C18 column. The mobile phase consisted of methanol-water-formic acid (80:20:1, V/V/V). Detection was performed on a triple quadrupole tandem mass spectrometer via electrospray ionization source (ESI) in the positive mode. Results The method had a lower (limit) of quantification of 10.0 ng·mL^-1 when 0.2 mL plasma was used. The linear calibration curves were obtained in the concentration range of 10.0-5000 ng·mL^-1. The intra- and inter-run precisions were lower than 3.3% in terms of relative standard deviation (RSD), and the accuracy ranged ±0.7% in terms of relative error (RE). Tmax, Cmax, T1/2 and AUC0-24h values were found to be (3.1±2.7)h, (8750±4734)ng·mL^-1, (5.3±2.2) h, and (5 932±2 449)ng·mL^-1, respectively, after a single oral dose of 250 mg clarithromycin tablet to 18 volunteers. Conclusion This validated method was successful in the evaluation of pharmacokinetic profiles of clarithromycin tablets administered to 18 healthy male volunteers.

Determination of Mirtazapine in Human Plasma by HPLC-MS and Bioavailability of Newly Developed Mirtazapine Tablets in Healthy Volunteers

LI Rong-shan, DING Li^*, JIAN Long-hai, XIAO Hong

2004, 13(3): 171-175.

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Aim To establish a sensitive and specific liquid chromatography-mass spectrometry method for determination of mirtazapine in human plasma and evaluation of its relative bioavailability. Methods After being alkalized by 25% ammonia, mirtazapine in the plasma was extracted with n-hexane. Desloratadine was used as internal standard (IS). Solu-tes were separated on a C18 column with a mobile phase of methanol-ammonium acetate buffer (pH 3.5) (75:25). The flow rate of the mobile phase was 1 mL·min^-1. Detection was performed on an electrospray ionization (ESI) mass spectrometer and operated in selected ion monitoring (SIM) and positive-ionization mode using target ionsat m/z 266.2 for mirtazapine and m/z 311.2 for the IS. The fragmentor voltage was 90 V. A randomized cross-over study was performed in 20 healthy volunteers. In the two study periods, twenty healthy Chinese male subjects received a single oral dose of mirtazapine 30 mg. Results The calibration curve was linear over the range of 0.3-200 ng·mL^-1. The limit of quantitation was 0.1 ng·mL^-1. The parameters for mirtazapine test tablet and reference tablet were as follows: T1/2(24.7±4.1) and (23.6±4.3) h, Tmax(1.6±0.8) and (1.5±0.8) h, Cmax(95.9±29.8) and (91.9±26.7) ng·mL^-1, respectively. Conclusion The established HPLC-MS method is rapid, sensitive and specific for the determination of mirtazapine in human plasma. The relative bioavailability was 100.0%±10.8%.

In Vitro Skin Permeation of Osthol from Hydro-Alcoholic Gel Formulations

YUAN Zhen-ting, DING Ping-tian^*, Lu Bo, CHEN Da-wei

2004, 13(3): 176-179.

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Aim To evaluate the in vitro percutaneous absorption behavior of osthol from a series of hydro-alcoholic gel formulations containing three penetration enhancers through excised human skin (stratum cormeum and epidermis,SCE). Methods Excised human skin was mounted in Franz-type diffusion cells. The samples withdrawn from the receptor cell were analyzed for osthol content by high-performance liquid chromatography (HPLC). Results The enhancers azone, menthol and chenopodium increased the osthol percutaneous steady-state fluxes 3.12, 2.00 and 1.25 times those of the enhancer-free formulations (controls), separately. Conclusions The main enhancement mechanism of the skin penetration enhancers azone, menthol and chenopodium is to destroy the barrier function of stratum corneum, reducing the resistance of drug transport through the skin and increasing the diffusion coefficients of osthol.

Improvement of Similarity Measure: Pearson Product-Moment Correlation Coefficient

LIU Yong-suo, MENG Qing-hua, CHEN Rong, WANG Jian-song, JIANG Shu-min, HU Yu-zhu^*

2004, 13(3): 180-186.

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Aim To study the reason of the insensitiveness of Pearson product-moment correlation coefficient as a similarity measure and the method to improve its sensitivity. Methods Experimental and simulated data sets were used. Results The distribution range of the data sets influences the sensitivity of Pearson product-moment correlation coefficient. Weighted Pearson product-moment correlation coefficient is more sensitive when the range of the data set is large. Conclusion Weighted Pearson product-moment correlation coefficient is necessary when the range of the data set is large.

Enantiomeric Separation of Meptazinol Hydrochloride by Capillary Electrophoresis

YU Yun-qiu, CHEN Yan, LI Ni, QIU Zhui-bai^*

2004, 13(3): 187-189.

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Aim To establish a capillary electrophoresis method for enantiomeric separation of meptazinol hydrochloride. Methods The separation conditions such as cyclodextrin (CD) type, buffer pH, concentration of 2,3,6-O-trimethyl-β-cyclodextrin and organic additives were optimized. An optimum concentration was 30 mmol·L^-1 phosphate (pH 7.02) with 10% (W/V) TM-β-CD and 2% acetonitrile. Results Baseline resolution of the enantiomer was readily achieved using 2, 3, 6-O-trimethyl-β-cyclodextrin. Conclusion This is a convenient method for fast enantiomeric resolution of meptazinol hydrochloride.

High-Performance Liquid Chromatographic Method for Determination of Germacrone in Rat Plasma

HE Hai-bing, TANG Xing^*, CUI Fu-de

2004, 13(3): 190-192.

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Aim A reliable high-performance liquid chromatographic (HPLC) method was developed for determination of germacrone in rat plasma. Methods The plasma samples were treated with acetonitrile and analyzed by HPLC with UV detection at 244 nm. Results The limit of detection was 100 ng·mL^-1 for germacrone in plasma and the linear range was 0.100 4-15.06 μg·mL^-1 in plasma. The RSD of intra-day and inter-day assay was 1.87%-4.29% and 1.29%-5.15%, respectively. The recoveries of germacrone were over 95%. The endogenous substances in plasma did not show any interference in the analysis. Conclusion The method is accurate and convenient, and suitable for pharmacokinetic studies of germacrone in rats.

Effects of Matrine on Aconitine-Induced Electrophysiological Changes in Rat Ventricular Myocytes

SHAN Hong-li, YANG Bao-feng^*, ZHOU Yu-hong, WANG He, LI Bao-xin

2004, 13(3): 193-198.

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Aim To explore the reason that the antiarrhythmic effect of the extract of traditional Chinese medicinal herb, matrine, is weaker than quinidine and verapamil by comparision of the effect and efficacy of matrine on various kinds of transmembrane ionic currents with those of quinidine and verapamil; and to demonstrate the best targets for antiarrhythmic drugs. Methods Whole-cell patch-clamp techniques were used to record the action potential and ionic currents in single cells of rat ventricular myocytes. Aconitine was used to induce the changes of ionic currents, then study the effects of matrine and quinidine, verapamil on aconitine-induced imbalanced channel currents and action potential. Results Aconitine 1 μmol·L^-1 induced significant changes in transmembrane currents and action potential in single cells of rat ventricular myocytes. APD was significantly prolonged by aconitine. Simultaneously, aconitine increased sodium, L-type calcium and inward rectifier potassium currents. Matrine 100 μmol·L^-1 reversed the aconitine-induced changes of sodium current (INa) from (-70.2±10.5) pA/pF to (-39.6±4.0) pA/pF (n=5, P<0.05 vs aconitine); L-type calcium current (ICa-L) from (20.4±3.8) pA/pF to (-12.9±2.9) pA/pF (n=6, P<0.01); the inward rectifier potassium current (Ik1) from (-32.2±1.08) pA/pF to (-24.0±3.4) pA/pF (n=6, P<0.01), and action potential duration. The reversal effects of quinidine and verapamil on aconitine-induced changes of APD and ionic currents were more marked than matrine. Conclusion Aco-nitine significantly disturbs the normal equilibrium of ion channels in ventricular myocytes. It induces changes of INa, ICa-L, Ik1 and prolongation of action potential duration. Matrine at concentration 50 or 100 μmol·L-1 statistically significantly suppresses aconitine-induced changes of APD and ionic currents. The potency and efficacy of inhibitory effect of matrine are markedly weaker than those of commonly used verapamil and quinidine.

Selenium Distribution Pattern, Antineoplastic and Immunostimulatory Activities of a Novel Organoselenium Compound Eb

YAN Jun, DENG Sheng-ju, KUANG Bin, HE Fei, LIU Tao, ZENG Hui-hui^*

2004, 13(3): 199-204.

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Aim To study the distribution pattern, antineoplastic activity and immunocompetence of a novel organoselenium compound Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming mice (dosage, 0.1 g·kg^-1·d^-1) intragastrically for 7 successive days. The contents of selenium in heart, liver, spleen, kidneys, lungs, stomach, brain, muscle, and bone were determined by fluorometric method on the eighth day. MTT assay was used to study tumor growth inhibition of Eb in vitro, and lymphocyte transformation, hemolysin formation and phagocytosis assay were used to study its immunocompetence. Results After 7 days, administration of Eb, the tissue contents of sele-(nium) in liver, spleen, lungs, kidneys, and bone of mice increased, especially those in liver and spleen increased significan-tly, compared with controls; but no significant changes of such contents were found in muscle, heart, brain, and stomach. Eb demonstrated inhibitory effects on human Bel-7402, BGC-823, and Calu-3 cancer cell lines in vitro. Eb also showed ability to enhance lymphocyte transformation and serum hemolysin formation in vitro and increase the phagocytosis of macrophages. Conclusion The validated antitumor and immunostimulatory activities of Eb suggest a hypothesis that Eb may behave as a biological response modifier when used as an antitumor agent. Eb is worthy of further study in developing a new antineoplastic and immunity enhancing agent in the light of its antitumor activity, immunocompetence and specific distribution in liver, lungs, kidneys, bone, and spleen.

Effects of Glucose on Transmembrane Ionic Current of Ventricular Myocytes in Guinea Pig

AI Jing, JIAO Jun-dong, WANG He, DU Zhi-min, YANG Bao-feng^*

2004, 13(3): 205-211.

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Aim To determine the effects of glucose on APD, IK1, IK, ICa-L of ventricular myocytes in guinea pigs. Methods Whole-cell patch-clamp technique was used to record the changed action potential ionic current induced by glucose of single cell in guinea pig ventricular myocytes, to compare the action of 0, 10 and 20 mmol·L^-1 glucoses on transmembrane ionic current. Results (1) Compared with 10 mmol·L^-1 glucose concentrations, 0 and 20 mmol·L^-1 glucose both shortened APD of ventricular myocytes (P<0.05). (2) The inward components of IK1 density were maximal when the glucose concentration was at 10 mmol·L^-1. Normalized I-V relationships showed that both 0 and 20 mmol·L^-1 glucose produced a left-shift of I-V curve. The reverse potential changed from -72.4 mV to -64.6 mV. (3) Compared with 10 mmol·L^-1, both 0 and 20 mmol·L^-1 glucose markedly increased the ICa-L amplitude and density. The ICa-L current density was (-8.035±0.82) pA/pF (n=8) at a test potential of 10 mV when the glucose concentration was 10 mmol·L^-1. But its current density decreased to (-5.45±0.67) pA/pF and (-6.50±0.56) pA/pF when glucose concentrations were 0 and 20 mmol·L^-1, respectively. (4) The current densities of IK were (18.96±2.86) pA/pF, (8.66±1.87) pA/pF, and (15.32±3.12) pA/pF, at +70 mV for 0, 10 and 20 mmol·L^-1 glucoses, respectively. Conclusion Glucose in different concentrations has different effects on APD, IK1, IK, and ICa-L of single ventricular myocyte in guinea pigs. There are similar actions of 0 and 20 mmol·L-1 glucoses on the transmembrane ionic current of ventricular myocytes in guinea pigs.

Flavones Isolated from Codonopsis xundianensis

HE Qing, ZHU En-yuan, WANG Zheng-tao^*, XU Luo-shan, HU Zhi-bi,

2004, 13(3): 212-213.

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Flavonoids from Leaves of Heritiera littoralis D.

TIAN Yan, WU Jun, ZHANG Si*

2004, 13(3): 214-216.

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Synthesis and Neuroprotective Activity of Novel C4, C7 Derivatives in Tetracycline Series

ZHOU Zhan-yun, WANG Hong-tao, WANG Xiao-wei, WANG Rui-ping, DU Yan-sheng, LIU Jun-yi^*

2004, 13(3): 217-220.

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