Journal of Chinese Pharmaceutical Sciences

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2000, 9(4): 1-01.

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Kiridine, A C18-Diterpene Alkaloid from Aconitum kirinense

Feng Feng, Ye Wencai, Liu Jinghan, Zhao Shouxun, Ian D. Williams, Che Chuntao

2000, 9(4): 167-169.

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Kiridine, a new C18-diterpenoid alkaloid, was isolated from the roots of Aconitum kirinense. Its structure was elucidated by MS, 1D- and 2D- NMR, and mono-crystal X-ray analysis. It is the first norditerpene alkaloid containing a 9,14-methylenedioxy group and the substituent at C-14 is β-configuration.

Five Polyoxygenated Cyclohexenes from Uvaria grandiflora

Liao Yonghong, Zou Zhongmei^*, Guo Jian, Xu Lizhen, Zhu Min, Yang Shilin

2000, 9(4): 170-173.

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Five new polyoxygenated cyclohexenes, uvarigranones A (2), B (3), C (6) D (7) and uvarigranol J (5) were isolated from the stems of Uvaria grandiflora. Their structures were established on the basis of spectral data and comparison with known compounds. Among them, the absolute configurations of 2, 5, 6 and 7 were determined from their CD spectra.

Synthesis and Antifungal Activities of 1-[2-(N-methyl-N-substituted-benzyl)amino-2-(2,4-dichlorophenyl)ethyl]-1H-1,2,4-triazoles

Feng Zhixiang, Zhang Wannian^*, Zhou Youjun, Zhu Ju, Lu Jiaguo, Li Ke

2000, 9(4): 174-178.

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Based on the structure-activity relationships and antimycotic mechanism of azole and benzylamine antifungal compounds, twenty-two 1-[2-(N-methyl-N-substituted-benzyl)amino-2-(2,4-dichlorophenyl)ethyl]-1H-1,2,4-triazoles were designed and synthesized. All of them were first reported and their structures were confirmed by elementary analysis, IR and 1H NMR spectra. Results of preliminary antifungal tests in vitro show that all the compounds are active against the nine pathogenic fungi to some extent. Compounds 2, 5, 6, 9, 10, 12, 13, 14 and 18 exhibit great activities against Trichophyton rubrum, and compounds 1, 2, 5, 10, 15 and 18 are very active against Microsporum canis. Their antifungal activities against these two fungi are the same or more potent as compared with econazole; compounds 2 and 5 show great activity against many fungi.

Synthesis of 1-Methylethyl 2-Chloro-5-[[(5,6-dihydro-2-methyl-1,4-oxathiin-3-yl)carbonyl]amino] Benzoate Analogs and Their Antiviral Activity

Ji Xiaoshen, Wang Yulun, Zhang Huafeng, Gao Yan, Liu Zhenye, Wang Jiankang

2000, 9(4): 179-181.

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Methylethyl 2-chloro-5-[[(5,6-dihydro-2-methyl-1,4-oxathiin-3-yl)carbonyl] amino] benzoate (UC84) has strong antiviral activity. UC84 was taken as the leading compound and 11 analogs were synthesized. All these compounds were evaluated and some of them showed the obvious anti-HBV and anti-HSV activities. The results indicated that the analogs of 1-methylethyl 2-chloro-5-[[(5,6-dihydro-2-methyl-1,4-oxathiin-3-yl)carbonyl] amino] benzoate (UC84) might be the potential anti-HSV and anit-HBV drugs.

The Antioxidization Effects of TP-5, Thyα1[Lys²³] and Their Spin Labeled Derivatives

Wang Qin, Wang Fang, Yang Jinbo, Meng Xueqin, Hu Xiaoyu

2000, 9(4): 182-184.

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TP-5 and Thyα1, synthesized by solid phase synthesis, have the effect to restrain the formation of superoxide anion in xanthine oxidase system in vitro. The formations of lipid peroxide in several organs (such as liver, brain and thymus) of the mice treated with TP-5, TP-5-R, active fragment of Thyα1 and active fragment of Thyα1-R of 10 μg·kg·d^-1 for 10 d were decreased. That means these peptides possess the capability of antioxidezation.

Study of Sustained Release Phenylpropanolamine Hydrochloride Hydrophilic Matrix Tablets Containing Hydroxypropylmethylcellulose K100M and Carbopol 971P

Lu Dan, Pei Yuanying^*

2000, 9(4): 185-190.

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In this study sustained release Phenylpropanolamine Hydrochloride (PPA(HCl) hydrophilic matrix tablets containing HPMC K100M and Carbopol 971P were prepared by direct compression method, and the release tests were performed. In all cases the plot of cumulative drug release percentage against t1/2 produced a straight line (r>0.98, P<0.01). The composition of polymers was selected employing orthogonal design. The chosen formulation showed consistent performance. The release profiles of the test and reference preparation were similar in 0.1 mol·L^-1 HCl, distilled water, phosphate buffer pH 5.0, 6.8, 7.4 and in 0.1 mol·L^-1 HCl for 2 h followed by release in phosphate buffer pH 6.8 for 10 h, for in these cases, the values of "similarity factor, f2" varied within the range of 63~74. The rate of PPA(HCl released in 0.1 mol·L^-1 HCl was significantly higher than in other four media (P<0.05). It was found that in the ranges examined, the rate of PPA(HCl released in distilled water decreased with the content of HPMC K100M or Carbopol 971P increased (P<0.05), but variations of the polymers ratio (using the same total content of polymers), the content of magnesium stearate or hardness of matrices appeared to insignificantly affect release rates (P>0.05).

Doxorubicin Stealth Liposomes Prepared with PEG-Distearoyl Phosphatidylethanolamine and Distribution as well as Antitumor Activity in Mice

Lu Wanliang, Wei Shuli, Zhang Qiang, Qi Xianrong, Sun Huadong

2000, 9(4): 191-195.

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The stealth liposomal doxorubicin and regular liposomal doxorubicin were prepared with and without polyethylene glycol-distearoylphosphatidylethanolamine (PEG2000-DSPE) by the method of ammonium sulfate gradient, respectively. A reversed HPLC-UV method was established to determine the concentrations of doxorubicin in mice tissues after administration. The tissue distribution of stealth liposomal, regular liposomal and free doxorubicin (doxorubicin hydrochloride solution) in mice and pharmacokinetics were investigated. The results showed that the distribution and pharmacokinetics of stealth liposomal doxorubicin in mice were pronouncedly changed as compared with regular liposomal doxorubicin and free doxorubicin. The levels of liposomal doxorubincin in the heart tissues were reduced and those of in the blood increased, especially of stealth liposomal doxorubicin. In evaluation of antitumor activity, the differences between stealth liposomal doxorubicin and regular liposomal doxorubicin were that the inhibition rate of solid tumor weight for stealth liposomal doxorubicin was higher than that of regular liposomal doxorubicin. It is concluded that the PEG ylation of liposomes can pronouncedly prolong the circulation time of doxorubicin in mice blood and increase the antitumor activity.

Effects of Several Transmucosal Absorption Promoters on Buccally Administered Insulin in Rats

Zhang Dawei, Shen Zancong, Zhou Tianyan, Wei Shuli, Zhang Qiang^*

2000, 9(4): 196-199.

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Effects of several transmucosal and transdermal absorption promoters on buccal insulin delivery in rats were evaluated. Insulin absorption has been assessed from cumulative response of serum glucose concentrations and by comparison with a s.c. insulin dose/response curve. In the absence of absorption promoters, buccal insulin was less than 7% as effective as s.c. insulin. The non-ionic surfactant, Brij78, obviously improved buccal insulin absorption, using phosphate buffer solution at pH 7.4 containing 5% adjuvant. One steroidal detergent, sodium deoxycholate, tested as absorption promoter was also effective. Another effective absorption promoter was sodium lauryl sulfate. In the presence of the most effective absorption-promoting systems, the pharmacological availability (PA) of buccal insulin was about one third as effective as s.c. insulin.

Determination of Naftopidil in Dog Plasma by High Performance Liquid Chromatography and Study on Its Pharmacokinetics

Ding Jinsong, Jiang Xuehua, Zhu Hao

2000, 9(4): 200-203.

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A simple, sensitive, accurate and rapid HPLC method for naftopidil determination in dog plasma or serum has been developed. Naftopidil was extracted from alkalinized plasma or serum with diethyl ether. The mobile phase consists acetonitrile and 0.05 mol·L^-1 phosphate buffer (pH 6.5) (60:40). Verapamil was used as the internal standard and the eluate was monitored at 230 nm. The calibration curve of naftopidil was linear within the range of 10 ng·mL^-1(1200 ng·mL^-1. The recovery of this method is 100.23%±3.00%, within-day RSD and between-day RSD were no more than 3.30%, 5.56% respectively. The plasma drug concentration-time course in dogs after an oral single dose of 200 mg conformed to the one-compartment model. Mean T1/2Ke, Tmax, Cmax value were 3.19±1.27 h, 1.15±0.49 h, and 697.48±94.22 ng·mL^-1 respectively.

A Comparative Study on the Stability of Roxithromycin in Different pH Solutions by Colorimetry, TLC and HPLC

Wei Zhenping, Bi Dianzhou

2000, 9(4): 204-207.

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In the present study, roxithromycin solutions of different pH values were prepared with water, simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). Stability of roxithromycin in the above solutions were determined separately by colorimetry, TLC and HPLC. All the three methods achieved an identical conclusion that this drug was stable in water and SIF. However, for the stability test of roxithromycin in SGF, the results obtained by colorimetry were contrary to those by TLC and HPLC. According to the results by colorimetry, this drug was stable in SGF for as long as 168 hours. However, when tested by TLC and HPLC, decomposition of this drug was found within 2 h and 10 min separately. According to the determination by HPLC, 8.15 % and 62.02 % of roxithromycin were decomposed in 10 min and 2 h in SGF, which can be explained like this: the decomposition products reacted with H2SO4 to form a solution with the same photo-absorptivity range as that of the original drug. Accordingly, colorimetry is not suitable for the assay and stability test of roxithromycin in acidic solution like SGF. Similarly, we also have reason to predict that microbacterial assay is not suitable for roxithromycin in acidic solution if the decomposition product still has antibacterial activities.

Susceptibility of 30 Antimicrobial Agents in 200 Strains of Campylobacters

Hou Fengqin, Shen Baoquan, Sun Xinting

2000, 9(4): 208-210.

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To access the variance of antibiotic-resistance, we investigated the susceptibility of 30 antimicrobial agents in Campylobacters isolated from 1994 to 1998 using the agar dilution method. All Campylobacter was susceptible to aminoglycoside, imipenem, polymycin B, clarithromycin, josamycin and medemycin. Of the 200 strains of Campylobacters, 3% were resistant to erythromycin; 44.5% to fluoroquinolones. Complete cross-resistance among the fluoroquinolones was observed. The rate of resistance to erythromycin and gentamycin remained relatively lower and stable over the past five years, so these two drugs remain to be the choice for the treatment of Campylobacter infections. The rate of drug resistance to fluoroquinolones of Campylobacters in Beijing area is so high that the application of these drugs should be modulated strictly.

Quantitative Analysis of Gadopentetate Dimeglumine Liposomes by Fluorescent Method

Wang Xianglin, Liu Qian, Chen Chen

2000, 9(4): 211-213.

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A fluorescent method has been developed for the assay of gadopentetate dimeglumine liposomes. The optimal conditions for its determination were investigated. The sample was analyzed at Ex = 275 nm and Em = 313 nm, pH 6.0~8.0. The linear range was between 9.4 μg·ml^-1 and 9.4 mg·ml^-1 and the average recovery was 100.2%. By this method, gadopentetate dimeglumine liposomes has been determined with satisfactory results.

Xuezhikang in Treating Primary Hyperlipidemia

Kou Wenrong, Lu Zongliang, Guo Jingxuan, Li Haiyan, Xue Shiwen, Lin Yuzhen, Wu Xuesi, Chen Hong

2000, 9(4): 214-217.

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Objective: To compare the effects of Xuezhikang and Simvastain in patients with primary hyperlipidemia. Methods: One hundred eight patients with primary hyperlipidemia were randomly divided into two groups. Group 1, 53 patients, took 4 Xuezhikang capsules per day (1.2 g/d) for 8 weeks and Group 2, 55 patients took Simvastain 10 mg per day for 8 weeks. At the end of 8 weeks, the lipid levels were compared with those of the baseline in each group. Results: In Group 1, the serum levels of total cholesterol (TC), low-density lipoprotein (LDL) cholesterol and triglycerides (TG) decreased by 23.0%, 28.0% and 28.1% (P<0.001), and in Group 2 reduced by 23.3%, 29.5% and 29.5% (P<0.001) respectively. The serum levels of high-density lipoprotein (HDL) cholesterol after taking Xuezhikang increased by 5.0% (P>0.05) and after taking Simvastatin increased by 14.3% (P<0.01). No significant differences, however, were found between the two groups in TC, LDL cholesterol, TG and HDL cholesterol. The side effects of Xuezhikang were less than those of Simvastatin. Conclusion: Xuezhikang made in China is a safe, effective and well toleraled lipid modulator.

Comparative Study of Relatively Long-term Therapy for Dyslipidemia with Low-dose Xuezhikang or Pravastatin in Chinese Patients

Xu Chengbin, Hu Dayi, Kang Liping, Tian Yawen, Gao Mingming, Xu Zhimin, Jin Sanyou, Ma Fengyun, Ma Min, Shi Xiang yun, Zhang Baohe, Long Nanzhan, Li Lin, Xue Lin, Zhang Junhua, Chen Xiuli, Dai ChengXiang

2000, 9(4): 218-221.

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Objective To compare the effects of low-dose Xuezhikang with that of Pravastatin for long-term therapy on Chinese patients with dyslipidemia. Methods One hundred and ninety-five cases from six hospitals in Beijing were studied by being randomly divided into two groups and given Xuezhikang 2 capsules QN and Pravastatin 5 mg QN respectively for 6 months. The levels of TC, TG, LDL-C and HDL-C in pre- and post-treatment for each group were analyzed. The differences between the two groups were compared using ANOVA. The efficacy-rates for lowering TC, TG and increasing HDL-C of each group were calculated according to "The Guidline to Clinical Drug Research" and the differences between the two groups were compared with X² test. Results Comparing with pre-treatment the TC decreased 16% and 17%, TG decreased 13% and 15%, LDL-C decreased 23% and 21%, HDL-C increased 2% and 10% after administering for 6 months in Xuezhikang and Pravastatin groups respectively. Both of the drugs could decrease LDL/HDL effectively as well. The decreases of TC, TG, LDL-C, and LDL/HDL were statistically significant in both groups comparing with pre-treatment, however, no significant differences were found between the two groups. But there was significant difference in the increases of HDL-C between two groups. The efficacy-rates of Xuezhikang and Pravastatin were 54.6% and 68.4% for TC, 49.1% and 53.9% for HDL-C, 46.2% and 40.8% for TG respectively. There were no significant differences between the two groups. No severe side effects were observed in the two groups. Conclusion Low-dose statin drugs (such as Xuezhikang and Pravastatin) administrated in relatively long-term are effective and safe for Chinese patients with dyslipidemia.

CONTENTS OF VOLUME 9
AUTHOR INDEX

2000, 9(4): 223-228.

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