Journal of Chinese Pharmaceutical Sciences

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2005, 14(3): 1-01.

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A Benzofuranoid Neolignan from Magnolia biondii Pamp

LU Yan-hua, GAO Yang, WANG Zheng-tao, LIU Jian-qun, WEI Dong-zhi^*

2005, 14(3): 137-139.

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Aim Isolation and structural elucidation of the constituents from the dried flower buds of Magnolia biondii Pamp. Methods Column chromatography and TLC were used to isolate chemical constituents. Spectroscopic methods were employed for structural elucidation. Results One benzofuranoid neolignan (licarin B) and two bisepoxy lignans (magnolin, fargesin) were isolated and identified. Conclusion Licarin B is the first reported benzofuranoid lignan from the family Magnoliaceae.

Herpetin, a New Bioactive Lignan Isolated from Herpetospermum caudigerum

YUAN Hai-long^*, LIU Yi, ZHAO Yan-ling, XIAO Xiao-he

2005, 14(3): 140-143.

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Aim To study the chemical constituents of seeds of Herpetospermum caudigerum. Methods Column chromatography was used in the isolation procedure, and the structure was elucidated by spectral data, whose pharmacologic activity was assayed in vitro. Results A new compound named herpetin was isolated, whose structure was determined to be 3-benzofuran methanol-2,3-dihydro-2-(4-hydroxy-3-methoxyphenyl)-4-methoxy-6-[tetrahydro-2-(3-hydroxy-4-methoxyphenyl)-3-methanol]-2-furanmethyl, showed significant inhibitory effects on HBV-DNA and the replication and expression of HBsAg and HBeAg. Conclusion Herpetin offers wide research and development prospect.

Identification of Stellaria media by PCR

HUANG Wen-zhe, DONG Ting-xia, QI Huan-yang, LU Zhen-qiang, ZHAN Hua-qiang^*

2005, 14(3): 144-148.

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Aim To provide a rapid and reliable method for identifying the fork medicine Stellaria media (Linn.) Cyr. (Herba Stellariae mediae) (Caryophyllaceae) from its adulterant Myosoton aquaticum (L.) Fries (Herba Myosoti aquatici) (Caryophyllaceae) by polymerase chain reaction (PCR) technology. Methods A molecular genetic approach has been developed to identify S.media for the first time. 5S-rRNA spacer domain was amplified by PCR from the isolated genomic DNA, and the PCR pro-ducts were then sequenced. Results The nucleotide sequences of S.media and M.aquaticum were measured to determine their identity. Furthermore, the nucleotide sequences of three Stellaria species, S.vestita, S. longifolia and S.radians, were also measured for the sake of providing the evidence of the biological phylogeny of Stellaria. Diversity between DNA sequence and restriction enzyme mapping among a variety of the species was found in their 5S-rRNA spacer domains. Conclusion The 5S-rRNA spacer domains can be used as a molecular marker for differentiating S.media from M.aquaticum and in phylogenetic studies of Stellaria.

3D-QSAR Analysis of DDPH Derivatives for α₁-Adrenoceptor Antagonist Activity

FANG Hao, LU Jing-fen^*, XIA Lin

2005, 14(3): 149-153.

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Aim and methods The study of three-dimensional quantitative structure-activity relationship (3D-QSAR) of DDPH and its derivatives has been performed using Apex-3D programme. Results The result indicates that substituents of para- and ortho-positions in phenyl ring of aryloxyalkylamine greatly influence the bioactivity. Conclusion The biophore model and 3D-QSAR equation help us not only further understand receptor-ligand interactions, but also design new compounds with better bioactivity.

Population Pharmacokinetics of Propofol Administered by TCI in Chinese Elderly Patients

XU Chuan-ya^*, WU Xin-min, JIANG Jian-yu, LU Wei

2005, 14(3): 154-161.

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Aim To investigate the population pharmacokinetics of propofol administered by TCI in Chinese elderly patients. Methods Thirty-two patients with ASA I-II, 65-82 years old, undergoing selective lower abdominal operation were studied. Propofol was administered by target-controlled infusion with Marsh parameter. The target plasma concentration was 3 μg·mL-1. Radial arterial blood samples were collected and analyzed by reversed phase HPLC with fluorescence detection. Population pharmacokinetic modeling was performed using NONMEM. Inter-individual variability and intra-individual variability of propofol were estimated for clearances and volumes of distribution. The effects of age, body weight, lean body mass, gender, height, hemoglobin, total protein, albumin, creatinine, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) were investigated. The effects of coadministered opioid drugs were also studied. Results The pharmacokinetics of propofol in the Chinese elderly patients was best described by a three-compartment open model. Lean body mass was found to be a covariate for system clearance at significant level (P<0.005). The clearance decreased linearly with age as well (P<0.005). The apparent volume of distribution for deep peripheral compartment (V3) was influenced by gender. Elderly female patients showed a higher value for V3. Conclusion The pharmacokinetics of propofol administered by TCI in Chinese elderly patients can be well described by a three-compartment open model. Inclusion of age, lean body mass and gender as covariates significantly improved the model. To ensure the accuracy and precision of target-controlled infusion, the population pharmacokinetic model applied to the individual patient should be adjusted reasonably.

High Resolution Determination of Ondansetron in Human Plasma by HPLC and Pharmacokinetics of Orally Disintegrating Tablets

CHEN Wei, WU Wei^*, WANG Yang, HUANG Min, QUE Li, HU Tao, SUN Ning-yun

2005, 14(3): 162-168.

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Aim To develop a high resolution HPLC method for the determination of ondansetron in human plasma and to study the pharmacokinetics of ondansetron in orally disintegrating tablets. Methods HPLC determination involved liquid-liquid extraction, separation on a CN column and ultraviolet detection at 310 nm with granisetron as an internal standard. Pharmacokinetics and bioequivalence of ondansetron in orally disintegrating tablets by direct compression and conventional 8 mg tablets were evaluated and compared in 20 healthy human male volunteers after a single oral dose in a randomized cross-over study. Results The limit of quantification was 0.25 ng·mL^-1. The recovery was about 85% or over for ondansetron and about 90% for internal standard. Linearity was good within the concentration range of 0.5-50 ng·mL^-1 with r² ranging from 0.997 1 to 0.999 9. Intra- and inter-assay coefficients of variation ranged from 1.78% to 2.38% and 3.88%-5.19%, respectively. Accuracies for spiked concentrations of 2.0, 10.0, and 30.0 ng·mL^-1 were 104.7%±4.4%, 102.2%±1.1%, and 99.51%±2.34%, respectively. Pharmacokinetic parameters of AUC0-t, AUC0-∞, Cmax, Tmax, and T1/2 were 230.2±78.0 ng·h·mL^-1, 265.2±101.5 ng·h·mL^-1, 35.67±8.94 ng·mL^-1, 1.51±0.79 h, and 5.00±1.41 h for orally disintegrating tablets, respectively. The analysis of variance did not show any significant difference between orally disintegrating tablets and conventional tablets, and 90% confidence intervals fell within the acceptable range for bioequivalence. Conclusion High resolution HPLC method has been set up and applied in pharmacokinetic evaluation of ondansetron in orally disintegrating tablets.

Compound Metformin/Glipizide Bilayer Extended Release Tablets: Development and in Vitro Release

OUYANG De-fang, NIE Shu-fang, MENG Jin, YANG Xing-gang, SONG Zhi-quan, PAN Wei-san^*

2005, 14(3): 169-172.

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Aim In this study, compound metformin/glipizide bilayer extended release tablets were formulated with hydroxypropyl methylcellulose (HPMC) by wet granulation technique in order to tackle the problems associated with the multidrug therapy of non-insulin dependent diabetes mellitus. Methods High-dose metformin is difficult to formulate into a tablet dosage form due to its poor compressibility and compactibility. In this study, the way to overcome the difficulty was to utilize stearic alcohol to prepare the tablet formulation. The influences of viscosity, amount of HPMC, and weight of fillers were investigated. The optimal formulation had acceptable physicochemical properties and released metformin and glipizide over 10 h. Results The data of metformin obtained from in vitro release fitted Higuchi kinetics best, while the release of glipizide in vitro was found to follow zero kinetics. Conclusion Compound metformin/glipizide bilayer extended release tablets have been successfully developed.

Simultaneous Determination of Clonidine Hydrochloride,Hydrochlorothiazide, and Rutin in Zhenju Jiangya Tablet by Capillary Electrophoresis

SU Sheng-min, YU Yun-qiu^*

2005, 14(3): 173-175.

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Aim To develop a method for the determination of three drug components: clonidine hydrochloride, hydrochlorothiazide and rutin in Zhenju Jiangya tablet. Methods An uncoated capillary tube was used to analyze under 20 kV voltage at 20 ºC. The samples were introduced into the capillary tube by hydrodynamic mode applying 50 kPa for 5 s and detected at 210 nm. Results The linear ranges of clonidine hydrochloride,hydrochlorothiazide, and rutin were 10 μg·mL^-1-100 μg·mL^-1, 30 μg·mL^-1-300 μg·mL^-1, and 30 μg·mL^-1-300 μg·mL^-1, respectively. Inter-day and intra-day RSD were all below 10.5%. The recoveries were 94.96% for clonidine hydrochloride, 84.45% for hydrochlorothiazide, and 89.88% for rutin. Conclusion Clonidine hydrochloride,hydrochlorothiazide, and rutin are baseline separated. The method is simple and rapid for simultaneous determination of the three drug components in Zhenju Jiangya tablet.

Primary Comments on Chemotaxonomy of Paris spp. Based on Saponins Analysis

HUANG Yun, WANG Qiang^*, CUI Li-jian

2005, 14(3): 176-180.

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Aim The several species of the genus Paris called “Chonglou” are famous traditional Chinese herbal medicines. We established the quantitative analysis method of the steroidal saponins in some species of the genus Paris and discussed their relations. Methods We detected the contents of 11 steroidal saponins in Paris samples with a Kromasel C18 (150 mm×4.6 mm ID, 5 μm) column which was subjected to gradient elution with acetonitrile-water (30:70-60:40, V/V) at a flow rate of 1 mL·min^-1 by HPLC-ELSD and established chemical cluster tree using SPSS 11 software. Results All the samples could be separated and calibration curves of 11 saponins were prepared. We successfully detected the contents of 11 steroidal saponins in 14 Paris spp. in 30 min. The recovery for the assay of saponins was between 95% and 97%. The RSD of precision of 11 saponins and stability of samples were below 3%. Chemical phylogenetic tree based on saponin contents indicated that 17 samples of Paris spp. clustered separately. Conclusion The established method is accurate and convenient, and suitable for the quantitative analysis of these 11 steroidal saponins in Paris spp.. The chemical phylogenetic tree is in accordance with Takhtajian classical taxonomy.

Hydroxysafflor Yellow A Promotes Vascular Endothelial Cell Proliferation via VEGF/VEGF Receptor

SONG Yan, ZHANG Ling, QU Kai, LI Chang-ling, ZHU Hai-bo^*

2005, 14(3): 181-185.

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Aim To study the proliferative effect of hydroxysafflor yellow A (HSYA) on cultured canine aortic endothelial cell (VEC) in normoxic (21% O2) or hypoxic (10% O2) culture and the underlying mechanism. Methods The endothelial cells were scratched from trypsined canine aorta endothelium. HSYA was added to the cells at final concentrations of 1×10^-3, 1×10^-4 and 1×10^-5 mol·L^-1, respectively. VEGF (2.6×10^-7 mol·L^-1)-treated cells were used as the positive control. The proliferative effect of HSYA on VEC was determined at 48, 72, 96, and 120 h in normoxic culture by MTT assay. Similarly, the proliferation of VEC was determined at 12, 24, 48, and 72 h in hypoxic culture by MTT assay. The effects of HSYA on VEC proliferation and VEGF secretion were investigated by MTT and ELISA assays at the presence of the antibodies to VEGF and VEGF receptors. Results Pretreatment with HSYA at concentrations of 1×10^-3 and 1×10^-4 mol·L^-1 enhanced VEC proliferation in normoxic culture. The most significant enhancing effect of HSYA on VEC proliferation was achieved at 24, 48, and 72 h in hypoxic culture in concentration-dependent and time-dependent manner. HSYA at 1×10^-3 mol·L^-1 showed a potency similar to VEGF at 2.6×10^-7 mol·L^-1. Pretreatment with the antibodies of Flt-1, KDR or VEGF blocked the proliferative effect of HSYA with similar potencies. Antibodies of Flt-1 or VEGF antagonized the promoting effect of HSYA on VEGF secretion. Conclusion HSYA promotes VEC proliferation either in normoxic or hypoxic culture, especially in the latter condition. This effect of HSYA is at least partly mediated by VEGF and VEGF receptor.

Analgesic Effects of Tetrodotoxin Combined with Acetylsalicylic Acid on Acetic Acid-induced Abdominal Constriction and Formalin Test in Mice

XU Ying^*, KU Bao-shan, GENG Xing-chao, YAO Hai-yan, ZHANG Yong-he, HAN Ji-sheng, QI Shi-quan

2005, 14(3): 186-192.

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Aim To study the effects of tetrodotoxin (TTX) combined with acetylsalicylic acid (ASA) on nociceptive stimulus in mice. Methods To assess the antinociceptive effects of TTX, ASA or TTX plus ASA, the acetic acid-induced abdominal constriction test and formalin pain test were used. Results TTX (0.5-4.0 μg·kg^-1 ) or ASA (25-200 mg·kg^-1) im produced a significant inhibition of acetic acid-induced abdominal constriction. The median inhibitory doses (ID50s) were 2.1 μg·kg^-1 for TTX and 64 mg·kg^-1 for ASA. TTX and ASA also showed a dose-dependent inhibition of the second phase response in the formalin pain model, the ID50s being 2.3 μg·kg^-1 and 74.2 mg·kg^-1, respectively. The interaction between TTX and ASA was synergistic, as evidenced by the fact that (1) when ASA alone compared with the combination of TTX (0.79 μg·kg^-1 or 0.39 μg·kg^-1) and ASA, the ID50s of ASA reduced from 64.0 mg·kg^-1 to 5.8 mg·kg^-1 or 12.6 mg·kg^-1, and from 74.2 mg·kg^-1 to 7.4 mg·kg^-1 or 13.0 mg·kg^-1 on the two models of nociceptive tests, respectively; and that (2) synergism in the analgesic effects was shown by isobiolographic analysis. Conclusion TTX, ASA and the combination of the two drugs produce analgesic effects in acetic acid-induced abdominal constriction test and formalin-induced pain test. The interactions between TTX and ASA may be useful in developing novel analgesic agents.

Primary Study of Egg Yolk Antibody for Detection of king cobra Venom Antigens

WANG Gui-ping, LIU Xin-yan, ZHU Liu, QIN Yuan, HUANG Shao, YU Qing-sheng^*

2005, 14(3): 193-197.

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Aim To study whether antivenom from laying hens can be used for the detection of venom antigens. Methods Chickens (white Leghorn) were immunized with detoxicated king cobra venom by formaldehyde and egg yolk immunoglobulin (IgY) isolated from yolk; IgY was labelled with the horseradish peroxidase (HRP). Experimental condition and parameters were determined by chessboard test. The specificity, sensitivity, precision, and stability of this method were assayed in the experiment. Results This method could detect as low as 32 μg·L^-1 of the king cobra antigens. A good linear relation was found within 32 - 750 μg·L^-1of king cobra venom concentrations (r = 0.963). There was no cross reactivity for the reagents with Agkistrodon acutus Guenther venom or Vipera russelli siamensis Smith venom; slight cross reactivity with Bungarus multicinctus Blyth venom or Bungarus fasciatus Chmeider venom; and notable cross reactivity with cobra venom. The average intra-assay relative standard deviation (RSD) was 1%-3%, and the inter-assay RSD was less than 8%. The reagents (including IgY and HRP-IgY) were stable; no differences (P>0.05) were observed for the detection of venom antigens when the reagents were stored at 37 ºC up to 6 d. Conclusion IgY is a good reagent for diagnosis of snakebite after eliminating the genus cross reactivity.

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