Journal of Chinese Pharmaceutical Sciences

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2005, 14(1): 1-01.

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Cytochrome P450 Directed Prodrug Activation Therapy in Research of Cancer Enzymology

ZHOU Jiang-quan, TANG Zhi-qiang^*

2005, 14(1): 1-9.

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Selective 3-OH Isomerization of Resibufogenin by Cell Suspension Cultures of Ginkgo biloba

XIN Xiu-lan^*, XIE Xiao-hui

2005, 14(1): 10-12.

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Aim To modify the structure of resibufogenin by using Ginkgo biloba suspension. Methods Young leaves of Ginkgo biloba were dedifferentiated into callus in MS medium with only 2,4-D as plant growth regulator. The callus was then transferred aseptically to liquid MS medium exogenously supplemented with appropriate concentration of 6-BA, NAA and 2,4-D to establish suspension cell culture system. Resibufogenin was administered into the well-grown cell cultures and incubated for 4 d. The products dissolved in the liquid phase of the cultures were extracted and purified by silica gel column chromatography gradiently eluted with petroleum ether and acetone system. Results One transformed product was obtained in 40% yield after 4 d incubation, which was identified as 3-epi-resibufogenin on the basis of FAB MS, ¹H NMR and ¹³C NMR spectroscopic analysis and corresponding data reported in literature. Conclusion G. biloba suspension cultures can be used as an enzyme system to biotransform resibufogenin, an animal-originated bufadienolide, into 3-epi-resibufogenin.

Total Synthesis of Anisodine

WU Yan-fen, LU Qiang, Lü Wen, ZHANG Wen-sheng^*

2005, 14(1): 13-17.

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Aim To design a practical synthetic route of anisodine. Methods Sta rting from 3α-hydroxy-6β-acetyltropine, anisodine was synthesized in 11 steps. Result Anisodine was obtainded with an overall yield of 2.6%. Conclusion Total synthetic route of anisodine was achieved whi ch may afford a possible route for commercial preparation of anisodine.

Characteristics and Transdermal Drug Delivery of Triamcinolone-Acetonide-Acetate-Loaded Solid Lipid Nanoparticles Carbomer Gel

LIU Wei, ZHU Yao-liang, CHEN Hua-bing, YANG Xiang-liang^*

2005, 14(1): 18-24.

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Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipid nanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate their characteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressure homogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology, particle size with polydispersity index (PI) and zeta potential were examined by atomic force microscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability and in vitro drug release were also studied. The transdermal drug delivery through porcine ear skin was evaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with the average size of (95.5-186.2) nm, the zeta potential of (-26.3~-15.7) mV and the entrapment efficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had good stability, the release profile in vitro fitted Higuchi equation. In comparison with conventional hydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition within porcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is prepared with stable physicochemical properties. The release profile and improved drug permeation into skin make it be a promising vehicle for transdermal drug delivery.

Determination of Zolmitriptan in Human Plasma by High-Performance Liquid Chromatography-Electrospray Mass Spectrometry and Study on Its Pharmacokinetics

YAO Jin-cheng, QU Yan-hui, ZHAO Xu-yuan, Hu Ling^*, ZHU Rong-hua, LI Huan-de, DING Jing-song

2005, 14(1): 25-28.

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Aim To establish a new and sensitive HPLC-MS method for the determination of zolmitriptan in human plasma and study the pharmacokinetics of zolmitriptan in healthy volunteers. Methods A single oral dose of 5 mg of zolmitriptan tablet was given to 20 healthy male volunteers. After dosing, blood samples were collected for a period of 24 h, and zolmitriptan concentration in plasma was analyzed by HPLC-MS. Results The plasma concentration-time course fitted well a two-compartment open model with a lag time, giving the following pharmacokinetic parameters: Tmax 1.60±0.24 h, Cmax 9.73±1.43 ng·mL^-1, T1/2α1.72±0.46 h, T1/2β 4.52±0.97 h and AUC0-t 55.59±5.12 ng·mL^-1·h. Conclusion The improved analytical method for zolmitriptan is rapid,sensitive and suitable for application to pharmacokinetic studies and routine determination of numerous samples.

Pharmacokinetics of Oxiracetam in Healthy Volunteers

WEI Chun-min^*, WANG Ben-jie, GUO Rui-chen^**

2005, 14(1): 29-32.

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Aim To study the pharmacokinetics of oxiracetam after single and multiple intravenous administrations in healthy volunteers. Method A HPLC method was used to determine the serum concentration of oxiracetam after intravenous single dose and daily dose of 2 000 mg for 7 d in ten Chinese healthy volunteers. Pharmacokinetic analysis was carried out using Drug And Statistic software. Results The AUC0~12, AUC0~∞, Ke, t1/2, MRT after a single dose of 2 000 mg oxiracetam were 256.26±16.84 μg·mL^-1·h^-1, 276.74±18.11 μg·mL^-1·h^-1, 0.18±0.03 h^-1, 3.84±0.64 h, and 4.39±0.39 h, and after multiple doses of oxiracetam were 259.36±25.43 μg·mL^-1·h^-1, 285.59±27.38 μg·mL^-1·h^-1, 0.17±0.04 h^-1, 4.14±0.82 h, and 4.87±0.69 h, respectively. Conclusion The pharmacokinetic parameters of oxiracetam do not differ remarkably after single and multiple intravenous administration and there is accumulation in serum after 2000 mg multiple intravenous administration once a day for 7 d.

Interaction Between Gatifloxacin and Bovine Serum Albumin

YAN Zheng-yu^*, SHAO Xiu-fen, YAN Lin, HU Yu-zhu

2005, 14(1): 33-37.

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Aim To study the reaction mechanism between gati fl oxacin and bovine serum albumin (BSA) at different pHs. Methods Fluorescence spectra and UV absorbance spectra were used. Results The binding constants were determined from a double reciprocal Lineweaver- Burk curves at different pHs. The binding distance r under normal physiologi cal condition was obtained according to Foster theory of non-radiative energy transfer. The binding force between gatifloxacin and BSA was inferred by thermody namical coordination. Conclusion The interaction between gatifl oxacin and BSA seems to be strong and the main binding force is electrostatic fo rce.

Determination of Scutellarin in Rabbit Plasma after Oral Administration by HPLC-MS with Solid-Phase Extraction

LI Ni, HUANG Jian-ming, WENG Wei-yu, HUANG Zhao-chang, CAI Jia, YU Yun-qiu^*

2005, 14(1): 38-42.

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Aim To establish a sensitive and specific liquid chromatography-mass s pectrometry method for determination of scutellarin in rabbit plasma after oral administration. Methods For the quantitative analysis, rutin was used as an internal standard and solid-phase extraction (SPE) was performe d by using a Phenomenex C8 cartridge. HPLC was carried out using a Zorbax Exte nd-C18 column (150 mm×2.1 mm ID, 5 μm) with a guard cartridge (Phenomenex). Gradient elution was selected with the mobile phase of methanol 10 mmol·L^-1 ammonium acetate solution (pH adjusted to 8.0 with ammonia soluti on). The flow rate of mobile phase was 0.4 mL·min^-1 and the column temperatur e was 35 ºC. Both scutellarin a nd the internal standard rutin in rabbit plasma extracts were detected by mass s pectrometry using an ESI interface in the negative ion mode. Results The linear range was from 2 to 200 ng·mL^-1, with acceptable accuracy and precision (RSD). Conclusion A sensitive, reliable and accurate method for the quantitati on of scutellarin in rabbit plasma has been established.

Study and Application of Fingerprints of Ginkgo biloba Leaves Preparations

XU Ya-ping, YAO Tong-wei^*

2005, 14(1): 43-50.

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Aim To establish a method for determination of Ginkgo biloba L, its extract and preparations with HPLC fingerprints, so as to c ontrol the quality of the preparations. Methods HPLC-DAD method was used to determine the constituents in preparations. Diamonsil^TM C18(200 mm×4.6 mm, 5 μm) was used as analytical column, and acetonitrile/KH2PO4 was used as mobile phase with gradient elution. The column temperatu re was at 24 ºC. The HPLC profile of chemical constituents of control sample and preparations were analyzed using similarity software. Results The fingerprints of different preparations from different companies were slightl y different because of the different preparing procedures. Mean while, the finge rprints of different batches of the same preparation from the same company were similar to each other and the technology of each preparation was stable. Conclusion This method is accurate, reproducible, simple, and can be used as an analytical method for the routine quality control of Ginkgo biloba preparations.

Determination of Eleutheroside B and E in Acanthopanax Preparations by High-Performance Liquid Chromatography with Solid-Phase Extraction

HU Fang-di, FENG Shi-lan^*, ZHAO Jian-xiong, CHEN Li-ren, XU Jing-wen

2005, 14(1): 51-55.

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Aim An HPLC method for analyzing eleutheroside B (ELU B) and eleutheroside E (ELU E), two of the main active substances of Acanthopanax preparations were studied. Methods The samples were analyzed on a kromasil ODS column with water-acetonitrile as a gradient mobile phase. The flow rate was 0.8 mL·min-1 and detecting wavelengths were 206 nm for ELU B, 220 nm for ELU E, solid phase extraction (SPE) and internal standard-salicin were selected. Results The recoveries of Acanthopanax tablets and injection were 90.4%-96.8% and 96.4%-99.8% for ELU B, 87.7%-93.3% and 95.7%-98.5% for ELU E, respectively. The linear ranges were 4.45-22.25 μg·mL^-1(r = 0.9998) and 5.11-25.55 μg·mL^-1(r = 0.9997) respectively. Conclusion This method can save the time for cleaning the chromatographic system and improve sensitivity for Acanthopanax preparations, thus providing a way to evaluate the quality of Acanthopanax preparations.

Determination of Diphenytriazol (DL111-IT) in Rabbit Plasma by High-Performance Liquid Chromatography with Fluorescence Detection

HE Min, YAO Tong-wei^*

2005, 14(1): 56-60.

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Aim To develop an HPLC method with fluorescence detection for the assay of DL111-IT in rabbit plasma. Methods DL111-IT and internal standard glybenzcyclamide in rabbit plasma were extracted with chloroform. The determination was performed on a Diamonsil ODS-C18 column (150 mm×4.6 mm, 5 μm) with a mobile phase of acetonitrile and 0.025 mol·L^-1 diammonium hydrogen phosphate buffer (pH 5.0, adjusted by phosphoric acid) (60:40, V/V) at a flow-rate of 1.0 mL·min^-1. Fluorescence detector was operated at excitation wavelength of 250 nm and emission wavelength of 332 nm. Results The calibration curve in plasma was linear from 1.00-20.00 ng·mL^-1 (r = 0.9996, n = 5).The method afforded average extracting recoveries of 85.3%±1.3%, 84.9%±2.7% and 85.8%±1.8%, and the average method recoveries were 99.5%±0.4%, 102.1%±1.8% and 101.3%±2.4% for the high (20.00 ng·mL-1), middle (10.00 ng·mL^-1) and low (1.00 ng·mL^-1) check samples, respectively. The intra-day (n = 5) and inter-day (n = 5) precisions (RSD) were less than 3.0% and 7.0%, respectively. The limit of detection and quantitation for the method were 0.3 ng·mL^-1 (S/N = 3) and 1 ng·mL^-1 (S/N = 10, RSD<7.0%) plasma sample, respectively. Conclusion The developed method was accurate, sensitive, simple and could be used for pharmacokinetic study of DL111-IT.

Current Issues and Development Strategies of Building the Discipline of Pharmacy Administration at Pharmacy Schools in China

JIANG Bin*, SUN Yuan, CHEN Jing, SHI Lu-wen

2005, 14(1): 61-64.

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The history and current status of Pharmacy Adminis tration discipline at pharmacy schools in China are illustrated. Several current issues are explored including: (1) insufficient teaching organizations and curr iculum, (2) faculty deficiency both in quantity and quality, and (3) much improv ement needed in the scope, methodology, and sophistication of research. Several development strategies are formulated such as (1) integrating native education resources in order to better foster quality professionals, (2) accelerating int er-university cooperation both in teaching and research, and (3) studying the regularites of discipline development and enhancing international exchange.

Current Status and Development Strategies of TCMM Exportation in China

YU Zhong, JIANG Bin^*, WANG Yi-tiao, SHI Lu-wen

2005, 14(1): 65-68.

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Low market share, small scale, inappropriate product structure, relati vely high market concentration, and heavy dependence on Asian markets such as Ja pan and Korea are some of the characteristics of the current exportation status of traditional Chinese medicinal materials (TCMM). The profound reasons for the se problems lie in the cultural, technological and informative barriers between TCMM and the international market as well as the underdevelopment of TCMM modern ization. Therefore, measures should be taken to enhance the cultural exchange an d strategic cooperation in TCMM marketing with international organizations, impl ement a standardization of TCMM, establish information sharing and other support ing mechanisms, and accelerate TCMM modernization and innovation.

Current Regulatory Status and Development Trend of Drug Inserts in China

GAO Song, YANG Yue-min, SUN Yuan, SHI Lu-wen^*

2005, 14(1): 69-71.

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Regulatory status of drug inserts in China is described in terms of it s legal system, administrative ramifications and existing problems. Lack of go vernment regulatory enforcement, industry self-control mechanisms and academic research are blamed to be the root of these problems. The trend of regulatory policies on the issue is outlined and suggestions on several important issues are made.

Current Status and Development Strategies of Chinese Cosmetic Industry

LI Xiao-zhu, JIANG Bin^*, WANG Yi-tao, SHI Lu-wen

2005, 14(1): 72-74.

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Current status and existing problems in the Chine secosmetic industry are analyzed from the aspects of industry scale, technology and management level, R & D investment and human resources. Strategies to promote t he industry are also put forward, such as increasing entry barrier to optimize industry structure, tightening regulatory controls to improve quality assurance, fostering innovation and actively exploring modes of collaboration, and training more technical and managing professionals.

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