Journal of Chinese Pharmaceutical Sciences

Contents list

2001, 10(3): 1-01.

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Triterpenes and Other Constituents from Rhaponticum uniflorum

Zhang Yonghong, Wang Wen, Wang Tao, Wang Hanqing^*

2001, 10(3): 113-114.

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From the roots of Rhaponticum uniflorum a new triterpene was isolated together with ursolic acid(2), 3-oxo-19a-hydroxyurs-12-en-28-oic acid (3), pomolic acid (4), 2α,3α,19α-trihydroxyurs-12-en-28-oic acid (5), arctic acid (6), catechin (7) and b-sitosterol (8). The structure of the new compound was elucidated as 2α,3α,19α,25-tetrahydroxyurs-12-en-23,28-dioic acid (1) on the basis of spectral and chemical methods.

Microbiological Transformation of Ginsenoside Rg1

Dong Aling, Cui Yajun, Guo Hongzhu, Zheng Junhua, Guo Dean^*

2001, 10(3): 115-118.

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Forty-nine microbial strains were used to screen their ability for the microbiological transforma-tion of ginsenoside Rg1. Aspergillus niger (3.1858) and Absidia coerulea (3.3538) were found to convert ginsenoside Rg1 efficiently to less polar metabolites. Preparative scale transformation with both fungi Absidia coerulea (3.3538) and Aspergillus niger (3.1858) have resulted in the production of one same metabolite (MT1). Its structure was char-acterized as 6-O-β-D-glucopyranosyl-20(S)-protopanaxatriol (Ginsenoside Rh1) on the basis of its TOF-MS and ¹H, ¹³C NMR spectral data. The biotransformation kinetic curves for Ginsenoside Rg1 and MT1 were reported for the first time, and the biotransformation pathway was proposed.

The Syntheses of β-Carboline-3-carboxamides Derivatives and Their Interaction with DNA

Lin Wei, Xiao Sulong, Yang Ming^*

2001, 10(3): 119-123.

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To study the interactions of these compounds with calf thymus DNA(CT-DNA), seven β-carboline-3-carboxamides were designed and synthesized. The interactions of these compounds with CT-DNA were determined by the viscometric titration assay and Tm (melting temperature) value assay. Binding strengths were evaluated by spectrophotometric titration experiment and microcalorimetric measurement. The interactions of these compounds were tested with CT-DNA. It was showed that all of these compounds were able to change the Tm value of CT-DNA. The results of viscometric titration assay indicated that these compounds interacted with CT-DNA by intercalation. Spectrophotometric titration experiment showed that the binding strengths of these compounds with CT-DNA were different, which was well in agreement with the cell culture results. The binding was driven by entropy according to the results of the microcalorimetric measurement. This series of β-carboline-3-carboxamides is DNA targeting compounds. Their obvious antitumor biological effect is based on the intercalation with DNA base-pairs.

The Interaction of Ribavirin and DII-18-2 with RNA

Hao Meirong, Yang Ming^*

2001, 10(3): 124-127.

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The Aim of this study was to investigate the interaction between polymers polyA-polyU (RNA) and two general anti-viral drugs with anti-HIV-1 activities. Tm experiment showed that the compounds had interacted with RNA, and CD spectra also observed the changes of RNA conformation induced by the compounds. Cytometric flow analysis indicated that ribavirin and DII-18-2 could decrease the percentage of hypodiploid cells, especially ribavirin.

The Study of Dipivefrin Hydrochloride Ophthalmic Gel

Wang Liru, Zhang Qiang

2001, 10(3): 128-132.

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Dipivefrin hydrochloride ophthalmic gel was prepared and the release test and the isolated cornea permeation test of the formulation in vitro were investigated. The release test of the formulation was studied by using permeable membrane. The content and the release amount of Dipivefrin hydrochloride from the gel base were measured by high performance liquid chromatography. The cornea permeation test of the formulation was studied by using isolated rabbit corneas. The formulation release behavior in vitro followed the first-order kinetic equation. The release amount of Dipivefrin hydrochloride raised significantly with less polymer in the formulation. The cornea permeation behavior of the drug in vitro followed the first-order kinetic equation. The eye irritancy of Dipivefrin hydrochloride gel is lower than that of eyedrops.

The Effect of pH on the Permeation of Lidocaine Hydrochloride Across Excised Rat Skin

Jia Shicong, Ding Pingtian, Zheng Junmin, Wu Cuishuan, Hua Shiyuan

2001, 10(3): 133-135.

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The effect of pH on the permeation of Lidocaine hydrochloride (LH) across excised rat skin was studied, the steady state flux (JSS) at different pH being determined using improved Valia-Chien diffusion cells. JSS increased substantially when pH was close to the pKa of LH. The profile of JSS versus pH showed an 'S'-shaped curve. JSS of Lidocaine free base (LFB) was fourteen times that of LH. The pH of vehicle influences the permeation of LH significantly and should be considered as an important factor when a formulation is developed.

Interaction of Soybean Phospholipids Based Lipo-Vesicle and Surfactants of Bile Salts In Vitro

Li Fengqian, Hu Jinhong, Zhu Quangang

2001, 10(3): 136-139.

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Liposomes were prepared with natural soybean phospholipids by extrusion method after rotating-film evaporating technique. Transmission electron micrography was used to detect the appearances of the prepared liposomes, and the liposome diameter was also measured. The prepared liposomes were sphere in shape with the mean diameter of 217 nm and span of 0.838. The phospholipid bilayer structure, suitable for entrapping various effector molecules, could be seen clearly under transmission electron microscopy. The bile salts of sodium cholate and sodium deoxycholate were used as the surfactants to investigate their interaction with liposomes. The turbidities for the mixture of bile salts and liposomes were evaluated by the visible spectrometry method at the wavelength of 500 nm. And the diameter changes of liposomes were also tested to examine the effect of bile salts on liposomes. At the beginning, the diameters and turbidities of liposomes increased a little as the result of mixed micelles formation during the different stages for the structure changes of surfactant-liposomes micelles. The further added bile salts decreased the diameters and turbidities of liposomes. The liposome suspension underwent several rearrangements before small mixed micelles formed. And the diameter of liposomes changed regularly. The interaction of bile salts and liposomes is important for the further study of the behaviors of liposomes in vivo. The drug loaded and release properties of liposomes can also be well reflected by the interaction of liposomes and surfactants.

Pharmacokinetics of 20(R)-Ginsenoside Rg3 in Human Volunteers

Pang Huan, Wang Hailin, Fu Li, Su Chengye

2001, 10(3): 140-143.

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Objective: To study the pharmacokinetics of 20(R)-Ginsenoside Rg3 in the human body. Methods: High-performance liquid chromatography-ultraviolet detection method was used in this study. Results: The pharmacokinetics of Ginsenoside Rg3 in 14 healthy volunteers were investigated. After a single oral dose of 3.2 mg·kg^-1 Ginsenoside Rg3 in 8 male volunteers, the plasma concentration-time course fitted in well with a two-compartment open model, with the following pharmacokinetic parameters: Tmax 0.66±0.10 h, Cmax 166 ng·mL^-1, T1/2α 0.46±0.12 h, T1/2β 4.9±1.1 h, T1/2(Ka) 0.28±0.04 h, AUC0-∞ 7726 ng·mL^-1·h, respectively. No kinetic analysis was made after an oral dose of 0.8 mg·kg^-1 Rg3 in other 6 volunteers because of the low concentration, but there was a good correlation between Cmax and dosage of the two groups. Conclusion: The absorption of Rg3 was rapid in the human body, and its elimination was rapid too after oral administration of Ginsenoside Rg3. The pharmacokinetic results shows that it exhibited the first-order kinetic characteristics.

pH Stability of Defibrase in Aqueous Solution Determined by En-zyme-linked Immunosorbent Assay

Zhao Huiying, Zheng Junmin^*, Xu Hui, Wei Gang, Zhao Haiqing

2001, 10(3): 144-147.

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Stability of Defibrase^® in various pH buffer solutions was investigated. Enzyme-linked immuno-sorbent assay (ELISA) and coagulating time method were used to assess antigenic stability and coagulating stability, respectively. The change of antigenic activities and coagulating activities of Defibrase^® in the same buffer solutions (pH 6, 7 and 8, with the exception of pH 3.6) showed similar tendency to decline with the time. Concentrated Defibrase^® was relatively stable at neutral pH 6~7, more than 95% of its initial activities (100 BU·mL^-1) was kept after a 10-day storage at 40 °C, whereas in pH 3.6 and pH 9 buffer solutions, diluted Defibrase^® was very labile. Addition of Triton X-100 or bovine serum albumin could effectively prevent loss of Defibrase^® by minimizing adsorption of Defibrase^® to plastic surface (P<0.005). Concentration of Defibrase^® could also affect its stability in aqueous solutions.

HPLC Determination of Harpagoside and Cinnamic Acid in Radix Scrophulariae

Xie Lihua, Liu Hongyu, Xu Bingjiu, Wang Xuan, Wang Jianhua, Xu Feng, Cai Shaoqing

2001, 10(3): 148-151.

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A gradient HPLC method was established for the determination of harpagoside and cinnamic acid in Radix Scrophulariae (Xuanshen) and a proposition was put forward for the lowest content of the characteristic and active constituent (harpagoside) for qualified Radix Scrophulariae. The experimental conditions were as follows: Ultrasphere ODS column (250 mm×4.6 mm, 5 mm), mobile phase: acetonitrile-water (containing 1.0% acetic acid) (20:80→50:50) (20 min), flow-rate 1 mL·min^-1, room temperature, detection wavelength 278 nm. Twenty-eight samples of Xuan-shen (Radix Scrophulariae) from different districts of China were analyzed and the contents of harpagoside and cinnamic acid in Xuan-shen were 0.041~0.244% and 0.012~0.068% respectively. The recoveries (±RSD)% were 97.13(±0.80)% for harpagoside and 99.38(±0.51)% for cinnamic acid. The method is simple and accurate. It can be used for the quality control of Radix Scrophulariae. We propose that the content of harpagoside in qualified Radix Scrophularia should be no less than 0.05%.

HPLC Determination of Captopril in Human Plasma with Pre-column Derivation and Solid-phase Extraction and Studies on Its Pharmacokinetic and Relative Bioavailability

Ding Jinsong, Zhang Bikui, Li Huande, Liu Yizhao, Deng Hang

2001, 10(3): 152-156.

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A new pre-column derivation HPLC method with solid-phase extraction to determine captopril in human plasma was established. Derivation products were extracted by a solid-phase extraction method after the reagent, p-α-dibromoacetophenone (p-BPB), was added in the plasma samples. The samples were analyzed in a VP-ODS column with UV-detector. The calibration curve of captopril was linear within the range of 5~1000 g·mL^-1 with r = 0.9987, the recovery of this method was 98.65±2.04%, within day and between day RSD were no more than 3.4% and 8.4% respectively. To study the pharmacokinetics and the relative bioavailability of captopril tablets, two formulations of captopril tablets were given to 18 healthy male volunteers according to a randomized 2-way cross-over design with a 1-week washout period. The respective AUC0~6, Cmax and Tmax values of the two formulations were 424.5±125.7 and 439.4±113.3 μg·h·L^-1; 505.9±244.6 and 504.8±172.2 μg·L^-1; 0.662±0.181 and 0.528±0.176 h. Results from statistics analysis showed that there were no significant difference between the AUC0~6, Cmax and Tmax values of the two formulations, The relative bioavailability of tablets I with respect to II was 96.1±14.6% from AUC0~6

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