Journal of Chinese Pharmaceutical Sciences

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2006, 15(2): 1-01.

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Preparation and Physicochemical Characterization of Quercetin-HP-β-CD Inclusion Complexes

YANG Zhao-gang, Gulisitan Awuti, CAO Yi, ZHU Jing, WU Bo-shen, WANG Jian-cheng, LU Wan-liang, ZHANG Xuan^*, ZHANG Qiang

2006, 15(2): 69-75.

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Aim To prepare and characterize the QURC-HP-β-CD inclusion complexes and investigate the thermodynamic parameters of the process. Methods QURC-HP-β-CD inclusion complexes were prepared by the grinding method. The equilibrium inclusion constants and thermodynamic parameters were determinated by phase solubility analysis. Dissolution tests were performed to study the dissolution rate of inclusion complexes. The formation of inclusion complexes was confirmed by differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffractometry (PXRD) and scanning electron microscopy (SEM). Results The aqueous solubility of quercetin was greatly increased (about 37 folds) by inclusion technique, and the initial dissolution rate was markedly improved (10 folds) in the first 5 min. The results of DSC and SEM photographs showed that quercetin crystal disappeared in inclusion complexes, which indicated the formation of new phase. FT-IR spectra showed that the carbonyl absorption band of quercetin was shifted. PXRD showed that the diffraction peak of quercetin crystal disappeared. Conclusion QURC-HP-β-CD inclusion complexes are produced by the grinding method. The solubility of quercetin is improved by the inclusion technique.

Influence of Electric Field Direction on Enhanced Transdermal Delivery of Caffeine by Electroporation

HU Qiao-hong^*, XU Dong-hang

2006, 15(2): 76-82.

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Aim To study the influence of electric field direction on the in vitro enhanced transdermal delivery of caffeine by electroporation. Methods Using side-by-side compartment diffusion cells method and Ag-Ag/AgCl electrodes, the transport of caffeine through human cadaver skin by electroporation (exponentially decaying pulse, pulse voltage = 350 V, pulse frequency = 4 pulses·min^-1, capacity = 22 μF, pulse length = 7 ms, 25 pulses) with different electric field directions was carried out and compared with passive diffusion and iontophoresis (0.25 mA·cm^-2, lasted for 4 h). Results (i) The cumulative quantity and flux of caffeine through human skin were increased significantly by electroporation or iontophoresis. (ii) The transport of caffeine by positive iontophoresis (with electric field from donor to receptor compartment) was significantly greater than that by negative iontophoresis (with electric field from receptor to donor compartment). (iii) The transport of caffeine by positive electroporation (with electric field from donor to receptor compartment) was similar to that by negative electroporation (with electric field from receptor to donor compartment). (iv) The enhancing effect of positive iontophoresis on the transdermal delivery of caffeine was significantly greater than that of electroporation (positive or negative). Conclusion Electric field direction significantly influences the enhancing effect of iontophoresis on the transdermal delivery of caffeine, but does not influence the enhancing effect of electroporation.

Preparation of Sustained-release Silybin Microspheres by Spherical Crystallization Technique

HU Rong-feng^*, ZHU Jia-bi, MA Feng-yu, XU Xiang-yang, SUN Yu-liang, MEI Kang-kang, LI Shi

2006, 15(2): 83-91.

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Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with solid-dispersing and release-retarding polymers. A differential scanning calorimeter and an X-ray diffractometer were used to investigate the dispersion state of silybin in the microspheres. The shape, surface morphology, and internal structure of the microspheres were observed using a scanning electron microscope. Characterization of the microspheres, such as average diameter, size distribution and bulk density of the microspheres was investigated. Results The particle size of the microspheres was determined mainly by the agitation speed. The dissolution rate of silybin from microspheres was enhanced by increasing the amount of the dispersing agents, and sustained by the retarding agents. The release rate of microspheres was controlled by adjusting the combination ratio of the dispersing agents to the retarding agents. The results of X-ray diffraction and differential scanning calorimetry analysis indicated that silybin was highly dispersed in the microspheres in amorphous state. The release profiles and content did not change after a three-month accelerated stability test at 40 ºC and 75% relative humidity. Conclusion Sustained-release silybin microspheres with a solid dispersion structure were prepared successfully in one step by a spherical crystallization technique combined with solid dispersion technique. The preparation process is simple, reproducible and inexpensive. The method is efficient for designing sustained-release microspheres with water-insoluble drugs.

Mechanism of Drug Release from Compound Metformin/Glipizide Elementary Osmotic Pump Tablets

OUYANG De-fang, MENG Jin, KONG Cui-feng, NIE Shu-fang, PAN Wei-san^*

2006, 15(2): 92-96.

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In previous studies, compound metformin/glipizide elementary osmotic pump tablet was developed. Aim To discover the mechanism of drug release from it. Methods Three rate-limiting factors influencing drug release from dosage form (the semi-permeable membrane, tablet core and delivery orifice) were investigated. Results The influx of water that passed the osmotic pump tablet was almost equal to the metformin release rate, while it was greatly less than the drug dissolution rate from tablet core. The size of orifice from 0.4 mm to 0.8 mm had no influence on drug release. The osmotic pressure of tablet core was mainly caused by metformin. Conclusion From the developed model of osmotic pump systems, it can be seen that only the water influx through the membrane is a rate-limiting step, not tablet core dissolution rate and solution influx, and only when the core dissolution rate is equal to the solution influx, the zero order release is seen in the osmotic pump systems.

Synthesis and Antibacterial Activity of (S)-5-(Heterocycle Methylene) -3-(3-Fluoro-4-morpholin-4-yl-phenyl)-Oxazolidin-2-one Derivatives

LI Rong-po, ZHOU Wei-cheng^*, GUO Yue-fang

2006, 15(2): 97-100.

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Aim To study the structure-activity relationship of antibacterial oxazolidinone derivatives. Methods Seven (S)-5-(heterocycle methylene)-3-(3-fluoro-4-morpholin-4-yl-phenyl)-oxazolidin-2-ones were synthesized by the substitution of (S)-[3-(3-fluoro-4-morpholin-4-yl-phenyl)-oxazolidin-2-one-5-yl]-methanol mesylate with some secondary amines and the structures of the product were confirmed by ¹H NMR and elemental analyses or MS. Results None of the seven compounds showed potent activity against the tested 20 strains of bacteria in vitro. Conclusion The replacement of 5-acetylaminometyl of Linezolid by 5-(heterocycle methylene) lost the antibacterial activity.

Synthesis of Hydroxyethylene-based β-Secretase Inhibitors

YANG Xiao-ming, ZOU Xiao-min, FU Yi-qiu, MOU Ke, XU Ping^*

2006, 15(2): 101-108.

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Aim To discuss in depth the synthesis of hydroxyethylene dipeptide-based β-secretase inhibitors; Methods Organic reactions such as nucleophilic addition and substitution assisted by organometallic agents, catalytic hydrogenation, and classic peptide coupling were used to synthesize peptidomimetic β-secretase inhibitors. Results Ideal reaction conditions and potential problems were investigated, and one of the designed β-secretase inhibitors 13 (as a model) was synthesized successfully; Conclusion This approach might be used to build up the β-secretase inhibitor library and to search for new molecular candidates.

Application of L-Cys-Capped CdS Nanoparticles in Determination of Nucleic Acid by Resonance Light-Scattering Technique

DAI Mei-ling, YAN Zheng-yu^*, QU Ping, SHAO Xiu-fen

2006, 15(2): 109-114.

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Aim To determine nucleic acid (DNA) using Nanometer-sized L-cysteine-capped CdS particles by resonance light scattering (RLS) method. Methods The nano-particles synthesized by a colloidal aqueous method were water-soluble, stable, and highly luminescent. The RLS of L-Cys-CdS particles were greatly quenched by DNA in Tris-HCl solutions. The intensity of RLS at 344 nm was proportional to the concentration of DNA. Results The linearity range of the calibration curve was 0.01-1.0 μg·mL^-1 for calf thymus DNA and 0.04-1.5 μg·mL^-1 for salmon sperm DNA. The detection limits (3 δ) were 8 ng·mL^-1 for calf thymus DNA and 10 ng·mL^-1 for salmon sperm DNA. Conclusion This method is simple, sensitive, and capable of avoiding the use of toxic dyes.

Trichostatin A Induces Apoptosis by Inhibiting Telomerase Activity and Expression of Telomerase Reverse Transcriptase in HL-60 Cells

ZHOU Yong-ming, GUO Wei, ZHOU Hao, LI Hui-yu, LIU Li-qiong, YAO Jun-xia, ZHENG Jin-e, GUO Tian-nan, HUANG Shi-ang^*

2006, 15(2): 115-120.

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Aim To investigate the effects of trichostatin A (TSA) on telomerase activity and the expression of human telomerase reverse transcriptase (hTERT) during apoptosis in vitro and the mechanisms in HL-60 cells. Methods The proliferative activity of HL-60 cells was assessed by MTT assay. Cell apoptosis was analyzed by flow cytometry. Telomerase activity was examined by TRAP-ELISA. The expression of telomerase subunits was analyzed by RT-PCR. Results A time- and dose-dependent inhibition was detected in HL-60 cells treated with TSA. After treatment with 600 nmol·L^-1 TSA for 48 h, the apoptosis rate in HL-60 cells was 42.6% and telomerase activity decreased 1.95±0.25, 1.73±0.12 and 1.52±0.09 for 12, 24 and 48 h, respectively. The expression of hTERTmRNA decreased. No significant changes were observed in the expression of hTRmRNA and hTP1mRNA. Conclusion TSA inhibits telomerase activity and induces apoptosis in HL-60 cells. The underlying mechanism may be related to the down-regulation of hTERT transcription.

Optimization of Preparative Separation and Purification of Total Flavonoids from Radix Puerariae by Macroporous Resin Method

LIU Huo-an, WANG Bo-chu, DAI Chuan-yun^*, SHAO Zhi-yong, HE Cong-lin, JIA Yun

2006, 15(2): 121-126.

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Aim To screen the optimum macroporous resin and conditions for the isolation and purification of flavonoids from Radix Puerariae. Methods The static and dynamic adsorption/desorption methods were used, and the separation and purification process was evaluated by measuring the concentration of total flavonoid in the fractions with UV spectrophotometer. Results The SP70 macroporous resin was the most effective compared with other macroporous resins. The optimum conditions were screened, which were 0.5 g·mL^-1 corresponding to crude drug for concentration of extract, pH 5-6 , and appended 60 times the volume of the resin bed (BV) with the adsorption speed 2 BV·h^-1, and the volume of aq. 70% (V/V) ethanol as eluant was 5 BV with desorption speed 2 BV·h^-1. By this method, the final contents of total flavonoids exceeded 80%. Conclusion The SP70 macroporous resin is the most effective one for large-scale isolation and purification of flavonoids from Radix Pueraria, which meets industrial needs.

Chemical Constituents of Roots of Ranuncalus ternatus Thunb.

HU Xiao-yan, DOU De-qiang^*, PEI Yu-ping, FU Wen-wei

2006, 15(2): 127-129.

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