Journal of Chinese Pharmaceutical Sciences

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2002, 11(1): 1-01.

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Two New Phenolic Carboxylic Acid Esters from Opuntia vulgaris

Jiang Jianqin, Ye Wencai, Chen Zhen, Lou Fengchang, Min Zhida

2002, 11(1): 1-01.

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Two new phenolic carboxylic acid esters n-butyl eucomate(1) and methyl eucomate (2) and six known compounds eucomic acid (3), 3-β-acetyl-taraxerol (4), friedelin (5), lupenone (6), methyl linoleate (7) and methyl oleate (8) were isolated from the stems of Opuntia vulgaris Mill (Cactaceae). Their structures were determined on the basis of spectral methods. Compounds 3,4,6,7,8 were isolated for the first time from this plant.

neo-Lignans and Hemiterpenoid from the Seeds of Artabostrys hexapetalus (Annonaceae)

Yu Jingguang, Li Tongmei, Sun Lan, Luo Xiuzhen, Ding Wei, Li Deyu

2002, 11(1): 4-10.

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Four neo-lignans: isoamericanin A(1), isoamericanol A(2), americanin B(3), artabotrycinol(4), a hemiterpenoid: (R)-artabotriol(5) and other compounds: palmitic acid(6), β-sitosterol(7) and daucosterol(8) were isolated from the seeds of Artabostrys hexapetalus (L.f.) Bhadari (Annonaceae). Artabotrycinol(4) is a new neo-lignan and (R)-artabotriol(5) is a new hemiterpenoid. Their structures were established by IR, UV, MS, 1D and 2D-NMR. Three other neo-lignans 1, 2, 3 were isolated from this plant for the first time.

Exploratory Study of Laser-induced Thymine-thymine Dimer in DNA by RP-HPLC

Zhang Lingxia, Hu Yuzhu

2002, 11(1): 11-15.

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The relationship between the yield of thymime-thymine dimer after laser irradiation and physical parameters, such as intensity and pulse number was studied to explore the function of laser irradiation to induce thymine-thymine dimer. A modified high-performance liquid chromatography (HPLC) method has been developed for the determination of thymine-thymine dimer in DNA for. The thymine-thymine dimer was prepared by a photochemical reaction to be used as the standard substance. The HPLC method we proposed is not interfered by other hydrolysate from DNA. The stability and reproducibility are good, and it can determine as little as 4.42×10^-5μg·mL^-1 thymime-thymine dimer. Three levels of laser intensity to irradiate DNA were selected from calf thymine to test the influence of the pulse number. The mechanism of DNA lesion and repair caused by laser irradiation was studied preliminarily.

Development and Validation of an HPLC Method for the Determination of Bupropion Hydrochloride in Tablets

Qi Meiling, Wang Peng, Geng Yingshu, Gu Junling, Fu Ruonong

2002, 11(1): 16-18.

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A rapid, accurate and sensitive HPLC method for the determination of bupropion hydrochloride in a new tablet formulation is described. Chromatographic separation of bupropion hydrochloride is achieved using a mobile phase consisting of methanol -0.01 mol·L^-1 ammonium dihydrogen phosphate (80:20, v/v, pH 4.8) at a flow rate of 1.0 mL·min^-1 on a Hypersil BDS C18 column. Absorbance is monitored at 251 nm where bupropion hydrochloride has maximum absorption in the mobile phase. The linear range of determination for bupropion hydrochloride is between 2.12 and 21.2 μg·mL^-1. The proposed method was validated with respect to accuracy, precision, limits of detection and quantification and robustness, etc.

Development and Validation of Liquid Chromatographic Method for the Determination of the Related Substances of Rifampicin

Zhu Bin, Hu Changqin^*

2002, 11(1): 19-23.

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A number of HPLC methods have been approved for the determination of rifampicin, but no references involved the assay of related substances of rifampicin. In the present paper, a reversed-phase liquid chromatographic method for the determination of related substances of rifampicin is developed and validated. Rifampicin and its related substances, including rifamycin SV, rifampicin N-oxide and 3-formylrifamycin SV were separated using a Zorbax Eclipse C8, 250×4.6 mm (i.d), 5 μm column by isocratic elution at a flow rate of 1 mL·min^-1. The detector was set at 254 nm. The mobile phase is a mixture of methanol-acetonitrile -0.075 mol·L^-1 monopotassium phosphate -1.0 mol·L^-1 citric acid (31:31:35:3, v/v). The method validation included accuracy, precision, linearity, sensitivity and stability. All results are shown to be acceptable.

Determination of Ciprofloxacin Lactate by Sodium Tetraphenylboron Method

Zhao Yansheng, Li Yanwei^*, Wei Wenlong, Wang Jinhui

2002, 11(1): 24-27.

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This paper describes an effective method for determining ciprofloxacin lactate. An excess of sodium tetraphenylboron was added to precipitate ciprofloxacin lactate in HAc-NaAc buffer solution (pH = 4.0). After filtering off the precipitate, the excessive sodium tetraphenylboron in the filtrate was titrated with cetyltrimethylammonium bromide standard solution, with bromophenol blue as indicator. The method is simple and rapid, it has been applied to the determination of ciprofloxacin lactate raw material with satisfactory results. The recovery was between 99.66% and 100.2%, the relative error was less than ±0.40%. Experiments showed that the method gave the same results as the approach using nonaqueous titration (ChP).

Effect of Enzymes in Buccal Mucous Membrane on Buccal Absorption of Insulin

Yang Tianzhi, Chen Dabing, Chen Qilong, Zhang Qiang^*

2002, 11(1): 28-33.

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Promoting Effect of the Ultradeformable Liposomes on Transdermal Delivery

Hu Xin, Liu Yan, Lu Jihua, Cui Xiaofeng

2002, 11(1): 34-37.

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In this article different types of ultradeformable liposomes were designed and the properties of transdermal delivery were studied with sodium salicylate as model drug. These results showed that liposomes with strong hydrophilic surfactant added is a new type of penetration enhancer.

Effect of Experimental Parameters on the Encapsulation of Insulin-loaded Poly(lactide-co-glycolide) Nanoparticles Prepared by a Double Emulsion Method

Pan Yan^*, Zhao Huiying, Xu Hui, Wei Gang, Hao Jinsong, Zheng Junming

2002, 11(1): 38-41.

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Insulin-loaded poly(lactide-co-glycolide) nanoparticles (INS-PLGA-NPs) were prepared by a double emulsion method (w/o/w), using ethyl acetate as organic solvent and poloxamer188 as emulsifier. Experimental parameters such as the emulsifier and PLGA concentrations, the pH and concentration of the insulin solution, the solvent evaporation method and PVA in the internal phase were investigated for the encapsulation efficiency. The results indicated that higher emulsifier concentration, relatively less amount of PLGA and lower insulin concentration would increase the entrapment of insulin. Furthermore, pH of insulin solution approaching to pI (5.3), adding some PVA to the internal phase and a shorter evaporation time helped to enhance the incorporation efficiency of insulin. Optimized preparation parameters led to nanoparticles with well-defined characteristics such as an average size around 149.6 nm, a polydispersity lower than 0.1 and high encapsulation efficiency up to 42.8%.

Protective Effects of Sodium Magnesium Fructose Diphosphate on Brain Damage of Rats Subjected to Focal Cerebral Ischemia and Reperfusion

Dong Zhi, Zeng Fanxin, Zhou Qixin, Fu Jieming, Xue Chunsheng

2002, 11(1): 42-45.

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Objective: To study the effects of sodium magnesiusm fructose diphosphate (FDPM) on brain damage of rats after ischemia-reperfusion. Methods: Rats were subjected to cerebral ischemia-reperfusion induced by inserting a nylon thread into internal carotid artery to block the origin of middle cerebral artery and removing the thread later. FDPM (400 mg·kg^-1), fructose-1,6-diphosphate (FDP, 400 mg·kg^-1)and magnesium sulfate (MgSO4, 30 mg·kg^-1) were administrated 10 min after the onset of ischemia. Neurological scale, brain infarct area, Malondialdehyde (MDA) content and histopathological changes of brain tissue were studied. Results: FDPM decreased neurological scale, diminished brain infarct area, reduced MDA content and relieved histopathological change of rat brain tissue subjected to ischemia-reperfusion. These effects were more powerful than that of FDP or MgSO4. Conclusions: It is suggested that FDPM markedly prevented rats against brain damage after cerebral ischemia-reperfusion, and its effect was better than that of FDP or MgSO4.

Electrophysiologic-electropharmacologic Method for Evaluating the Effects of Antagonizing Ventricular Tachyarrhythmic Drugs

Guo Zhibin, Li Qing, Cao Hongyu, Xu Zhi

2002, 11(1): 46-50.

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Objective To establish a canine model of electrophysiologic-electropharmacology as assessed by programmed electrical stimulation (PES), and to observe the electrophysiologic effects of Procainamide(PA) on normal and ischemic myocardium in case of ischemic ventricular tachyarrhythmia in this model. Methods A ishemic ventricular tachyarrhythmias canine model was established in open-chest dogs subjected to programmed electrical stimulation(PES)for 5-8 days after acute myocardial infarction. The electrophysiologic effects of procainamide were observed in this model. With routine methods of PES,ventricular tachycardia(VT) and ventricular fibrillation (VF) could be reproducibly initiated. Results Procainamide distinctly lengthened the QTc interval (P<0.01) and effective refractory period (ERP) of normal and ischemic ventricular myocardium (NERP and IERP) respectively (P<0.01), decreased the dispersion of ERP in ischemic myocardium and the dispersion of ERP in left ventricle (P<0.01), and increased the diastolic excitability threshold of normal and ischemic ventricular myocardium remarkably (P<0.01). Procainamide effectively prevented the PES-induced VT or VF (P<0.05) and ischemia-induced VF (P<0.05). Conclusion The results indicated that PES-induced VT/VF were highly reproducible and reliable, this canine model is a worthy and reliable one, procainamide may be effective in preventing the onset of VT and VF after myocardial ischemic damage, and deserves further attention as an antifibrillatory agent.

Trends of Antibiotic Resistance in Strains of Shigella Isolated in Beijing Over 8 Years

Hou Fengqin, Sun Xinting, Shen Baoquan, Yu Yanyan

2002, 11(1): 51-54.

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To investigate the trends of antibiotic resistance in strains of Shigella isolated in Beijing, the susceptibility of 30 antimicrobial agents was observed in 327 Shigella strains isolated from 1994 to 2001. The resistance rates of fluoroquinolones increased gradually over the eight years, and the resistance rates of norfloxacin and ciprofloxacin (11.6% and 16.3% respectively) during 1997-1998 were significantly higher than that in 1994 (P<0.001). Meanwhile intermediately susceptible strains of fluoroquinolones also increased gradually from 1994 to 1998,and increased rapidly during 1999-2001, which suggests that the resistance rate of fluoroquinolones may increase rapidly in the coming years. In addition there was partial cross-resistance among fluoroquinolones, and the rate of resistance to 5 species of fluoroquinolones had been increasing from 1995 to 2001. It increased to 8.5% during 1999-2001. The resistance rates of Aminoglycoside and the first-generation cephalosporins remained relatively stable over the eight years, which can be used as the first-line agents for the treatment of dysentery, but intermediately susceptible strains of amikacin and almost all of cephalosporins have increased, which should be noticed.

Novel Synthesis of N,N-dimethylamino-methylne-aniline by Vilsmeier Reaction Procedure

Xu Ping^*, Zhang Ting, Wang Wenhao, Zou Xiaomin, Zhang Xin

2002, 11(1): 55-56.

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