Journal of Chinese Pharmaceutical Sciences

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2003, 12(1): 1-01.

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New Constituents from the Fresh Stems of Opuntia Dillenii

QIU Ying-kun^*, CHEN Ying-jie, PEI Yu-pin, Matsuda Hisashi, Yoshikawa Masayuki

2003, 12(1): 1-01.

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Aim To study the chemical composition of Opuntia dillenii Haw. Methods Many kinds of chromatography methods were used in the isolation procedure, while the structures of isolated compounds were determined on the aids of NMR and MS spectral analysis. Result Three new compounds, together with 14 known compounds, were isolated form the80% ethanolic extract of its stems. Conclusion The three new compounds, opuntioside I (2), 4-ethoxyl-6-hydroxymethyl-α-pyrone (3) and kaempferol 7-O-β-D-glucopyranosyl (1→4)-β-D-glucopyranoside (4), were characterized.

Qualitative and Quantitative Evaluation of Epimedium and Ginseng Contained Combinations Using HPLC

MA Yuan-chun, LUO Mai, Sarah Wittenberg, Clive Barwell, ZHOU Yu-xin^*, WEI Lu-xue

2003, 12(1): 6-10.

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Aim To develop a rapid, effective method for the determination of flavonoids and ginsenosides in one injection and evaluate the flavonoids and ginsenosides content to control the ratio of Epimedium and Ginseng herbs in botanicalcombinations. Methods The quality evaluation was determinatted using reversed-phase high performance liquid chromatog raphy (HPLC), referred by the major flavonoids from Epimedium, epimedin A, epimedin B, epimedin C, and icariin as thestandards, and the major ginsenosides Rg1 , Re, Rf, Rb1 , Rb2, and Rd as the standards, included Epimedium brevicornum Maxim., E. sagittatum (Sieb. et Zucc) Maxim., E. koreanum NaKai, P. ginseng C. A. Meyer, P. quinquefolium L., P. notoginseng and some products containing the above herbs. Results The main flavonoids and ginsenosides couldbe clearly resolved in the single analysis. Conclusion The results can be effectively used in evaluating qualitatively andquantitatively the ration of Epimedium and Ginseng contained products.

FTIR Characterization of the Secondary Structure of Insulin Encapsulated within Liposome

ZHANG Xuan, HUANG Li-xin, NIE Song-qing, QI Xian-rong, ZHANG Qiang^*

2003, 12(1): 11-14.

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Aim To determine the secondary structure of insulin encapsulated within liposome. Methods The secondary structure of native insulin, mixture of insulin with liposome (sample I) and insulin encapsulated within liposome (sample II) were determined by FTIR (Fourier Transform Infrared) spectroscopy. Results The secondary structure of insulin encapsulated within liposome (II) are similar with the secondary structure of native insulin. The difference existed in the amount of α-helices (from 36% of insulin to 31% of sample II) and β-sheet (from 48% of insulin to 51% of sample II). The content of α-helices and β-sheet of insulin in sample I was found to be very close to that of sample II. The results revealed that the insulin encapsulated within liposome possibly spread on the surface of liposome, without inserting into the liposome membrane. Conclusion The secondary structure of insulin encapsulated within liposome is similar with the native insulin.

The Binding Ability and Inclusion Complexation Behavior of Curcumin with Natural α-, β-, γ-Cyclodextrins and Organoselenium-Bridged Bis(β-cyclodextrin)s

QI Ai-di, LI Li, LIU Yu^*

2003, 12(1): 15-20.

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Aim To investigate quantitatively the binding ability and inclusion complexation behavior of curcumin with natural α-, β-, γ-cyclodextrins (1-3) and a series of organoselenium-bridged bis (β-cyclodextrin) s with simple spacer (4-6). Methods The spectrophotometric titrations have been performed in KCl-HC1 buffer solution (pH = 2.0) at 25 °C to calculate the complex stability constants (Ks) and Gibbs free energy changes (ΔG°) for the stoichiometric 1: 1 inclusion complexation of 1-6 with curcumin. Results The binding ability of β-cyclodextrin for inclusion complexation with guestcurcumin is higher than that of a-and γ-cyclodextrins. As compared with parent β-cyclodextrin, the organoselenium bridged bis (β-cyclodextrin) s tethered by some functional groups can further enhance the original molecular binding ability through cooperative binding of one curcumin molecule in the closely located two cyclodextrin cavities, showing the enhanced binding abilities of parent β-cyclodextrin by a factor 2.8-17.1. Conclusion Size/shape fit and hydrophobic interaction between host cyclodextrins and guest curcumin molecule are the important factors affecting the binding ability and inclusion complexation behavior of these cyclodextrins 1- 6.

Preparation of PLA or PLGA Microspheres with Estradiol the Effects of THF-adding on the Properties of MS

ZHOU Xin-teng^*, ZHU Feng, PAN Wei-san, ZHANG Ru-hua

2003, 12(1): 21-25.

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Aim Polylactic acid (PLA) or polylactide co glycolide (PLGA) was used as biodegradable and biocompatible carriers to achieve sustained release of estradial PLGA/PLA Microspheres (E2 PLGA/PLA MS). THF was added in the organic phase to study its effects on the properties of MS. Methods MS were formed by an emulsification solvent extraction method with mixture of ethyl acetate (EtoAc) and tetrahydrofuran (THF) as the organic solvents, and then the properties and in vitro drug release behavior were examined. Results The results indicated that the drug loading efficiency decreased when THF added, but when the ratio of EtoAc was more than 50%, there was no obvious effect of THF ratio, but the particle size increased accordingly. The carriers' properties and the drug contents were the main factors influencing the in vitro drug release. Conclusions By controlling the technology and formulation, we can get sustained release E2 biodegradable microsperes with proper particle size, drug content and low burst release, although THF with readily solubility in water was used in the organic phase.

Interactions Mode of Amphoteric Molecules with Ordered Phospholipid Membrane

SUN Jin^*, CHENG Gang, HE Zhong-gui, WANG Shu-jun, CHEN Ji-min

2003, 12(1): 26-30.

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Aim To explore interaction mode between amphoteric molecules with the ordered phospholipid membrane. Methods Membrane interactions were determined by immobilized artificial membrane (IAM) chromatography and solutes'hydrophobicity was measured by n-octanol/buffer system. Results The ampholytes, similar to bases, generally exhibitedhigher membrane affinity than expected from their hydrophobicity, resulting from the attractive polar interaction with phospholipid membrane. Furthermore, the strength of additional polar interaction with membrane (△lg kIAM) was then calculated. The △lg kIAM values were far greater for bases and ampholytes ranging from 0.50-1.39, than those for acids and neutrals with the scope from -0.55-0.44. Conclusion Considering the microspecies distribution of amphoteric molecules, itwas assumed that not only neutral and positive but also zwitterionic microspecies are capable of partitioning into ordered amphoteric lipid membrane with complementarily conformational and energetically favorable interactions.

Determination of Captopril in Human Plasma by High-Performance Liquid Chromatography and Study on the Pharmacokinetics after a Single Oral Dose

YANG Li^*, XU Ai-xia, ZHAO Rong-sheng, YAN Bao-xia

2003, 12(1): 31-35.

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Aim To establish a simple high-performance liquid chromatography method for the determination of captopril in human plasma and study the pharmacokinetics of captopril in healthy volunteers. Methods Captopril was stabilizedby forming an adduct with p-bromophenacyl bromide and this adduct in plasma was measured by high-performance liquidchromatography with UV detection following a single oral dose 50 mg of captopril test and reference preparations respectivelygiven to 18 healthy volunteers. Results The standard curve was liner over a range of 25-1200 ng·mL^-1. The quantitativelimit of detection was 25 ng·mL^-1. The RSD of inter- and intra- assay were below 8%. On the basis of elaborated method,single-dose pharmacokinetics in 18 healthy volunteers have been investigated. The comparison of the pharmacokinetic parameters was performed. The pharmacokinetic parameters of test and reference tablets were calculated as follows: tmax were(0.64± 0.18)h and (0.82±0.41)h; Cmax were(600.2+194.3)ng·mL^-1 and (582.7+175.3)ng·mL^-1; AUC0→8h were (1448.5+483.7)ng·h·mL^-1 and (1389.9±392.5)ng·h·mL^-1; AUC0→∞ were (1869.4+701.6)ng·h·mL^-1 and (1781.8 +615.5)ng·h·mL^-1, respectively. Conclusion The improved analytical method for captopril was found to be sensitive,simple and rapid, suitable for application in pharmacokinetic studies and routine determination of numerous samples.

Interaction of Puerarin with Phospholipid in Solid Dispersion

ZHAI Guang-xi^*, LOU Hong-xiang, BI Dian-zhou, ZOU Li-jia

2003, 12(1): 36-40.

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Aim To study the interaction of puerarin (PU) with phospholipid (PL) in solid dispersion. Methods PU/PL solid dispersion was prepared with solvent evaporation and the interaction between PU and PL was studied by analysis of their ultraviolet spectra, infrared spectra, ¹H NMR spectra and thin layer chromatogram. Results In chloroform the maximum absorption peak of PU in PU/PL mixture was located at 243 nm, but 251 nm for that of PU in solid dispersion. However in methanol, QU in mixture or solid dispersion had the same maximum absorption peak location in ultraviolet spectra. Compared with the infrared spectra of mixture, that of solid dispersion showed the specific absorption peak location of benzene ring framework in PU molecule was markedly changed, the stretching vibration peak of P=O in PL molecule was shifted to high wave numbers and the stretching vibration peak of C=C in PL molecule was disappeared. In 1H NMR spectra, most of the signals from PU in solid dispersion were weaken markedly or disappeared and the signals from the polar partof PL molecule were significantly changed. PU and PL in solid dispersion could be separated on silica gel plate with the mixed solvent of chloroform, methanol and water (65:25:5) or ethyl acetate and methanol (10:1). Conclusion In soliddispersion the benzene ring framework of PU molecule could act with the polar part and unsaturated part of PL moleculethrough charges fransfer, and the interacted part could be surrounded by fat chains of PL molecule.

Determination of Erythromycin Ethylsuccinate and its Related Substances by Ion Suppression Chromatography

YU Jian-qing, LEI Jia-chuan^*, LUO Shun-de, ZOU Guo-lin

2003, 12(1): 41-44.

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Aim Method for the determination of erythromycin ethylsuccinate(EES) by ion suppression chromatography (ISC) was developed and the influenc factors on ISC were investigated. Methods A Zorbax SB-C18 column was used with 0.02 mol·L^-1 potassium dihydrogen phosphate acetonitrile (45:55) as mobile phase. The pH and proportion of the mobile phase showed the greatest influences on retention and selectivity. Therefore, the pH of mobile was adjusted to 6.8, the best acetonitrile proportion was 55%. The column temperature was maintained at (30±0.5) °C. Acetonitrile was used as solvent for the sample preparation because EES is more stable in it. The flow rate was 1.2 mL·min^-1and UV detection was performed at 210 nm. Results Under these chromatographic conditions, the main component (erythromycin A ethylsuccinate) and its related substances were separated. The calibration curve showed good linearity over the range of 0.1-1.0 mg·mL^-1, and its correlation coefficient was 0.9998. Conclusion The method is very suitable for the analysis of erythromycin ethylsuccinate.

Effect of Recombinant Prothymosin α on Secretion of IFN-γ IFN-α and TNF-α in vitro

QIU Lei, GUO Bao-yu^*, MIAO Hong, DAO Shu-yan, ZHANG Ran, YUAN Peng-qun, YANG Xu

2003, 12(1): 45-48.

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Aim To study the effect of prothymosin α(Pro %) as a fusion protein on the secretion of IFN-γ, IFN-αand TNF-α in vitro. Methods The in vitro study was carried out on the cultured of splenocytes, splenic and peritonealmacrophages isolated from Balb/c mice. Splenocytes were incubated with various concentrations of Pro Tα(1×10^-7-1×l0^-10 mol·L^-1) with or without Con A(5 μg·mL^-1) for 72 h. Splenic and peritoneal macrophages were respectively treatedwith Pro Tα(1×10^-7-1×l0^-10 mol·L^-1) in the presence of LPS(10 μg·mL^-1) for 24 h. Then IFN-y's, IFN-α's andTNF-α's levels in the supematant were deteced by ELISA. Results Pro Tα (1×10^-7 mol·L^-1) was found to obviously increase IFN-γ level (P<0.05) in the supematant of splenocytes compared with the control group. Moreover, Pro Tα(1×10^-7 mol·L^-1) significantly induced the secretion of IFN-α (P<0.01)and TNF-α(P<0.01) in splenic and peritonealmacrophages. Conclusion In vitro, Pro Tα could increase the secretion of IFN-γ, IFN-α and TNF-α.

Percutaneous Absorption and Metabolism of Ketoprofen Isopropyl Ester via Excised Nude Mouse's and Monkey's Skin

ZHU Quan-gang^*, HU Jin-hong

2003, 12(1): 49-53.

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Aim To study percutaneous absorption and metabolism of ketoprofen isopropyl ester (KPE) via excised nude mouse’s and monkey’s skin. Methods Excised skin was prepared by surgical excision and enzyme digestion. Side-by-side diffusion cells were used for in vitro permeation studies. The concentrations of KPE and its metabolite in samples were assayed by HPLC. Results All KPE penetration through whole thickness skin and stripped skin was metabolized to ketoprofen (KP), the concentration of which in the receiver solution increased linearly with time. As to the nude mouse skin, the steady state flux of KP through whole thickness skin was 2-5 times that of KPE through the whole thickness skin, but the KP and KPE remaining in the whole thickness skin after the finishing of KPE penetration was 22-2 times in compared with the KP remaining in the whole thickness skin after the finishing of KP penetration. The rate of formation of the steady state KP from KPE through dermis was significantly lower than that of KPE through the whole thickness skin. In the monkey skin, the rate of formation of the steady-state KP from KPE through the whole thickness skin was 0-7 times that from KPE through stripped skin. The KP and KPE remaining in the whole thickness skin after the finishing of KPE penetration was 2-0 times that in the stripped skin after the finishing of KPE penetration. The rate of formation of the steady state KP from KPE through dermis was lower than that from KPE through the whole thickness skin and the stripped skin, the KP remaining in dermis after the finishing of KPE penetration was also significantly lower than the KP remaining in the whole thickness skin and the stripped skin after the finishing of KPE penetration. Conclusion KP esters are of benefit to improve the local action of KP, and skin esterase metabolism mainly develops in the epidermis.

Study on Metabolites of Aconitum Alkaloids in Human Urine

SUN Ying, ZHANG Hong-gui, ZHONG Da-fang^*, ZHANG Han-qi

2003, 12(1): 54-55.

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