Journal of Chinese Pharmaceutical Sciences

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2006, 15(4): 1-01.

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Comparison and Quality Assessment of Cassia Bark (Cortex Cinnamomi) by Thin Layer Chromatography

HE Zhen-dan, QIAO Chun-feng, HAN Quan-bin, SONG Jing-zheng, CHENG Chuen-lung, XU Hong-xi, JIANG Ren-wang, WONG Ka-lok, BUT Paul Pui-hay, SHAW Pang-chui^*

2006, 15(4): 195-199.

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Aim To differentiate the genuine cassia bark from its substitutes and adulterants. Methods Six components, phenylpropyl acetate, cinnamyl acetate, cinnamaldehyde, cinnamyl alcohol, coumarin, and cinnamic acid were used as characteristic markers, and an optimized TLC method was developed. Results The TLC profile of cassia bark is similar to its closely related variety Cinnamomum cassia Presl var. macrophyllum Chu but significantly different from other six Cinnamomum species. High content of phenylpropyl acetate, cinnamaldehyde, and coumarin was found in superior commercial grade debarked cortex. Conclusion The developed TLC method can be used to differentiate the genuine cassia bark from its substitutes and adulterants.

GC-MS Analysis of Essential Oil Constituents from Rhizome and Root of Notopterygium forbesii

YANG Xiu-wei^*, ZHANG Peng, TAO Hai-yan, JIANG Shun-yuan, ZHOU Yi

2006, 15(4): 200-205.

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Aim To analyse the chemical constituents of the essential oil extracted from the rhizome and root of Notopterygium forbesii Boiss. and provide scientific basis for quality control. Methods The total essential oil was extracted by water-steam distillation and separated by capillary gas chromatography (GC). The components were determined by normalization method, and identified by GC-MS. Results GC-MS exhibited 217 peaks and 100 compounds were identified, accounting for 78.3% of the total essential oil. Conclusion In the total essential oil of the rhizome and root of N. forbesii, monoterpenes and sesquiterpenes account for 41.30% and 32.65%, respectively, in which (1R)-α-pinene (3.98%), sabinene (2.51%), (1S)-β-pinene (5.78%), m-cymene (4.05%), limonene (3.55%), 3, 7-dimethyl-1, 3, 7-octatriene (3.98%), γ-terpinene (8.70%), anisole (1.78%) and (1S)-endo-bornyl acetate (2.62%) as the monoterpenes and its derivatives, and (+)-β-elemene (1.17%), α-bulnesene (1.40%), (+)-β-bisabolene (1.21%), (±)-elemol (1.42%), guaiol (1.14%), dehydroxyisocalamendiol (1.13%), (-)-aristolene (1.99%), bulnesol (9.48%), γ-eudesmol (1.77%), guai-1 (10)-en-11-ol (1.12%) and α-bisabolol (5.35 %) as the sesquiterpenes and its derivatives are the main components.

Chemical Constituents of Rheum tanguticum Maxim.ex Balf.

JIN Wei, GE Ri-li, HUANG Zhi-qin, WEI Quan-jia, BAO Tian-you, TU Peng-fei^*

2006, 15(4): 206-210.

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Aim To study the chemical constituents of the root and rhizome of Rheum tanguticum Maxim. ex Balf. Methods Chemical constituents were isolated and purified by many chromatographic methods, and their structures were elucidated by MS, NMR, and others. Results Twenty compounds were isolated and their structures were identified as β-sitosterol, chrysophanol, aloe-emodin, physcion, rhein, emodin, etc. Conclusion Among these compounds, 4-(4'-hydroxyphenyl)-2-butanone, 4-(4'-hydroxyphenyl)-2-butanone-4'-O-β-D-(2''-O-cinnamoyl-6''-O-galloyl)-glucopyranoside and 4-(4'-hydroxyphenyl)-2-butanone-4'-O-β-D-(2''-O-galloyl-6''-O-p-coumaroyl)-glucopyranoside were isolated from the root and rhizome of Rheum tanguticum for the first time.

Chemical Constituents from Ampelopsis grossedentata

ZHANG Yan-song, ZHANG Qing-ying, WANG Bin, LI Li-ying, ZHAO Yu-ying^*

2006, 15(4): 211-214.

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Aim To study chemical constituents from Ampelopsis grossedentata. Methods Separation and purification were performed by using silica gel, polyamide, reverse-phase silica gel, Sephadex LH-20 column chromatographic techniques and silica gel PTLC. Structures were determined by means of physicochemical properties and spectral analysis. Results Four flavonoids were separated and identified from Ampelopsis grossedentata including dihydromyricetin (1), myricetin (2), myricitrin (3), and myricetin-3-O-β-D-galactopyranoside (4). Conclusion Compound 4 was isolated from this genus for the first time, and 2D NMR techniques permitted the correct assignment of ¹H and ¹³C NMR signals of 1.

Synthesis and Antibacterial Activities of Erythromycin Derivatives

FENG Run-liang^*, GONG Ping, ZHAO Yan-fang

2006, 15(4): 215-222.

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Aim To synthesize 4''-carbamate derivatives of erythromycin and test their antibacterial activities in vitro. Methods New erythromycin antibacterial agents containing 4''-carbamate group were designed and synthesized from azithromycin via protection, aminoformylation, amination and deprotection. Their antibacterial activities against Staphylococcus aureus strains were tested. Results Nine compounds were synthesized. Their structures were confirmed by MS, IR, ¹H NMR and ¹³C NMR, and the synthetic condition (reagent ratios) was exploited. Among them, compounds F-3 and F-4 showed strong antibacterial activities against Staphylococcus aureus. But, all compounds did not show bactericidal activity. Discussion The test results showed that piperidinyl or pyrrolidinyl group may be of benefit to enhancing antibacterial activities.

Use of Solid SMEDDS in Delivery of Carvedilol

WEI Lan-lan, SUN Pei-nan, TIAN Lei, TANG Xin, YAO Ting-ting, PAN Wei-san^*

2006, 15(4): 223-227.

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Aim A new solid SMEDDS (self-microemulsifying drug delivery system) capsule has been developed to increase the solubility and dissolution rate. Methods The solubilities of carvedilol in various bases were investigated. Ternary phase diagrams were used to evaluate the self-emulsification and self-microemulsfication domains. The particle size distribution and ζ-potential were determined. The mean diameter of the three formulae decreased with an increase of Lutrol F68. Results The in vitro dissolution rate of carvedilol from solid SMEDDS capsule was significantly increased, compared with that from commercially available tablets. Conclusion The solid self-microemulsifying capsule showed the potential of improving the bioavailability of carvedilol.

Exchange Reaction Characteristics of Anion Exchange Resin for Diclofenac Sodium

WU Jing, YANG Li, LIU Hong-fei, WANG Chao, CAO Guo-liang, PAN Wei-san^*

2006, 15(4): 228-232.

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Aim To study the exchange reaction characteristics of anion exchange resin for diclofenac sodium. Methods The drug-resin complexes were prepared by a batch method with diclofenac sodium as the model drug and the strong anion exchange resin (201 × 7) as the carrier. The effects of different forms (OH^-and Cl^-) of the strong anion exchange resin, the particle size of the resin, and the reaction temperature on the exchange behavior were described. The exchange kinetic profiles were fitted. The related exchange reaction rate constants, exchange activation energy, and selectivity coefficients were determined. The exchange thermodynamic parameters, such as Δ_rG^θ_m, Δ_rH^θ_m andΔ_rS^θ_m, were evaluated. Results The anion exchange resin in the Cl^- and OH^- form had the same exchange capacity of diclofenac sodium. When the size of resin particle decreased or the temperature increased, the rate of exchange reaction increased. The exchange reaction between the drug and resin was accorded with first order kinetics. The exchange activation energy was about 60.68 kJ·mol^-1. The exchange thermodynamics parameters achieved at 303K, 313K and 323K were all satisfied with the following results: Δ_rG^θ_m<0, Δ_rH^θ_m>0 and Δ_rS^θ_m>0. Conclusion The exchange process of drug-resin complexes was mainly influenced by the size of the resin and the reaction temperature. The exchange reaction was an endothermic and spontaneous reaction as the temperature increased.

Determination of Lovastatin Level in Human Plasma and Lovastatin Capsules Bioavailability in Healthy Volunteers Using HPLC-MS

XIAO Hong^*, SHEN Hong, CHEN Jian-fang, XIAO Da-wei

2006, 15(4): 233-237.

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Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was extracted with acetoacetate. Simvastatin was added as internal standard (IS). Samples were separated on a C₁₈ column with a mobile phase consisting of methanol and 50 mmol·L^-1 sodium acetate (88:12). The flow rate was 1 mL·min^-1. Sample was detected using an electrospray ionization (ESI) mass spectrometer with selected ion monitoring (SIM) and positive-ionization mode. The target ionsat for lovastatin was m/z 427.3, while that for simvastatin was m/z 441.3. The fragmentor voltage was 150 V. A randomized crossover study was performed in 20 healthy Chinese male volunteers. In the two study periods, each subject was given orally two capsules at a single dose 40 mg of lovastatin. Results The calibration curve was linear in the range of 0.5 - 30 ng·mL^-1. The limit of quantification was 0.5 ng·mL^-1. The parameters for lovastatin test capsule and reference capsule were as follows: T_1/2(6.02 ± 1.67) and (5.63 ± 1.00) h, Tmax (2.8 ± 0.5) and (2.7 ± 0.4) h, C_max (14.58 ± 4.55) and (14.38 ± 4.51) ng·mL^-1, respectively. The relative bioavailability was 95.9% ± 14.4%. Conclusion The established HPLC-MS method is rapid, sensitive and specific for determination of lovastatin level in human plasma.

Determination of Piperazine Ferulate in Human Plasma by HPLC and Its Pharmacokinetic Study

YUAN Gui-yan*, WANG Ben-jie, WEI Chun-min, LIU Huan-jun, GUO Rui-chen**

2006, 15(4): 238-242.

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Aim To establish a sensitive HPLC method for determination of piperazine ferulate and to study its pharmacokinetics in healthy volunteers. Methods Piperazine ferulate was separated on a Shimadzu C₁₈ column with acetic acid (0.1%)-methanol (60:40, V/V) as mobile phase after liquid-liquid extraction, and detection was performed at 310 nm. Piperazine ferulate pharmacokinetic parameters after a single oral dose of 200 mg of piperazine ferulate dispersible tablets in 20 healthy male volunteers were calculated and evaluated using DAS 2.0. Results The linear range of the calibration curve for piperazine ferulate was 5 - 3 000 ng·mL^-1, and the absolute recovery was about 70%. Intra-day RSD and inter-day RSD were less than 8.9% and 10.1%, respectively. The pharmacokinetic parameters, as Cmax, Tmax , t_1/2, AUC_{0 -4}, and AUC_0-∞, after a single oral dose of piperazine ferulate dispersible tablets were 1144.487 ± 599.839 ng·mL^-1, 0.373 ± 0.08 h, 0.805 ± 0.298 h, 604.01 ± 232.874 ng·mL^-1·h, and 611.778 ± 234.147 ng·mL^-1 ·h, respectively. Conclusion The HPLC method for determining piperazine ferulate concentration in plasma is rapid, sensitive and suitable for pharmacokinetic studies and routine determination of large samples.

Pharmacokinetics and Bioequivalence of Cefprozil Granules and Cefprozil Tablets in Healthy Chinese Volunteers

LI Xiao-li, NI Mei-yuan, WANG Ben-jie, GUO Rui-chen^*

2006, 15(4): 243-247.

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Aim To develop a rapid, simple, and sensitive high-performance liquid chromatographic (HPLC) method for the determination of cefprozil in human plasma and to study its pharmacokinetics and bioequivalence after 0.5 g oral doses of cefprozil granules and tablets. Methods The blood concentration of cefprozil was analyzed after extracted with 6% trichloroacetic acid, using tinidazole as internal standard (I.S.). A C₁₈ column was used to separate cefprozil with mobile phase of methanol, purified water and glacial acetic acid (30:70:1, V/V/V) at flow rate of 1.0 mL·min^-1, and the detection occurred at 280 nm. Pharmacokinetics parameters of cefprozil were calculated and bioequivalence of cefprozil granules and tablets was evaluated. Results The lower detection and quantification limit was 0.05 μg·mL^-1, and the calibration curves were linear over a concentration range of 0.05 − 12 μg·mL^-1 of cefprozil in plasma. The pharmacokinetic parameters after oral administration of 0.5 g cefprozil granules and tablets were as follows, t_1/2 1.970 ± 0.388 h and 2.046 ± 0.449 h; T_max 1.600 ± 0.348 h and 1.675 ± 0.335 h; C_max 6.643 ± 1.104 μg·mL^-1 and 6.637 ± 1.320 μg·mL^-1 ; AUC_0-12 21.586 ± 4.154 μg·mL^-1·h and 21.121 ± 4.255 μg·mL^-1·h; AUC_0-∞ 21.814 ± 4.164 μg·mL^-1·h and 21.388 ± 4.308 μg·mL^-1·h, respectively. The bioavailability of cefprozil granules to tablets was 103.138 ± 12.042%. Conclusion High resolution HPLC method has been set up and succesfully applied to cefprozil pharmacokinetic studies and bioequivalence evaluation of cefprozil granules and tablets. Cefprozil granules and tablets are bioequivalent.

Chemical Constituents from Pueraria lobata

SI Jian-yong, CHANG Qi , SHEN Lian-gang, CHEN Di-hua^*

2006, 15(4): 248-250.

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Chemical Constituents from Roots of Semiaquilegia adoxoides

NIU Feng, XIE Guang-bo, CUI Zheng, CHEN Fa-kui, TU Peng-fei*

2006, 15(4): 251-254.

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CONTENTS OF VOLUME 15
AUTHOR INDEX

2006, 15(4): 255-262.

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