Journal of Chinese Pharmaceutical Sciences

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2012, 21(4): 283-286.

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Design and synthesis of cADPR analogues with simplified ribose and nucleobase

Yue Zhou, Pei-Lin Yu, Zhen-Jun Yang, Liang-Ren Zhang^*, Li-He Zhang

2012, 21(4): 287-291. DOI: 10.5246/jcps.2012.04.038

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New cADPR mimic 5 that integrates the simplified nucleobase and ribose was designed and synthesized by using Cu(I)-catalyzed Huisgen [3+2] cycloaddition to build the simplified triazole nucleobase and microwave-assisted reaction to carry out intramolecular pyrophosphorylation. Primary biological investigation showed that the introduction of an ether strand to replace northern and southern riboses could retain calcium inducing activity, but the introduction of a carbon strand to replace the northern ribose could lead to decreased activity.

Improved synthesis of leonurine as cardioprotective agent

Shan-Shan Luo, Xian-Feng Gu^*, Yi-Zhun Zhu^*

2012, 21(4): 292-295. DOI: 10.5246/jcps.2012.04.039

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A new synthetic method of leonurine was developed. Leonurine 1 was synthesized from the key intermediates 4 and 5, two compounds with high solubility in dichloromethane which allowed the synthetic procedure to be performed under mild conditions and afforded 1 with a good yield. Comparing the previous methods, the yield was increased from 30% to 54%, time consumed was significantly reduced as well.

A sensitive LC-MS/MS method to determine the concentrations of erlotinib and its active metabolite OSI-420 in BALB/c nude mice plasma simultaneously and its application to a pharmacokinetic study

Meng-Yao Li, Qiong Wu, Han-Qing Li, Miao-Ran Ning, Ye Chen, Liang Li, Tian-Yan Zhou^*, Wei Lu^*

2012, 21(4): 296-303. DOI: 10.5246/jcps.2012.04.040

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A simple, rapid and sensitive LC-MS/MS method was developed to quantify erlotinib and its active metabolite, OSI-420, simultaneously in BALB/c nude mice plasma. Erlotinib, OSI-420 and propranolol (internal standard) were extracted from nude mice plasma samples by liquid-liquid extraction. Separation was achieved on a reversed phase C18 column with a mobile phase of acetonitrile-water (35:65, v/v) containing 5 mM ammonium formate (pH = 3.0). All compounds were monitored by mass spectrometry with electrospray positive ionization. The lower limit of quantification was 0.5 ng/mL for both erlotinib and OSI-420; accuracy was estimated by relative error, which was in the range from 0.07% to 8.00% for erlotinib and -2.83% to 6.67% for OSI-420; precision was validated by relative standard deviation, which was from 2.28% to 15.12% for erlotinib and from 1.96% to 11.50% for OSI-420. This method was applied to a pharmacokinetic study of BALB/c nude mice following oral administration of erlotinib at 12.5 mg/kg. A 2-compartment model was used to fit the pharmacokinetics of erlotinib and 1-compartment model for the pharmacokinetics of OSI-420. The ratio of the active metabolite to parent drug in mice was greater than previously reported in humans and probably reflects interspecies difference in the rate of conversion of erlotinib to OSI-420.

Determination of paclitaxel in human plasma by LC-ESI-MS and its application in a pharmacokinetic study

Jun Qian, Yi-Xuan Wang, Sheng-Min Su, Yun-Qiu Yu^*

2012, 21(4): 304-310. DOI: 10.5246/jcps.2012.04.041

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A sensitive and selective method has been developed and validated for the quantitation of paclitaxel in human plasma by liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS). Paclitaxel and norethindrone (used as internal standard, I.S.) were extracted from human plasma by a one-step liquid-liquid extraction with t-butyl methyl ether. Separation on a Zorbax SB-C18 column (100 mm×2.1 mm, 3.5 μm, Agilent) was achieved by gradient elution with methanol and 0.2 mmol/L ammonium formate containing 0.1% formic acid. The selected-ion monitoring (SIM) targeted ions of [M+Na]⁺ at m/z 876.5 for paclitaxel and [M+H]⁺ at m/z 299.4 for I.S. The assay was validated in the range of 1.0-400 ng/mL (r>0.998) with LLOQ of 1.0 ng/mL. Intra- and inter-day precisions were all less than 9.0%, with accuracies of ±6.8%. The method was successfully applied to evaluate the pharmacokinetics of paclitaxel liposome for injection in patients.

Preparation and characterization of nanosized ethosomes loaded with tetrandrine and their in vivo efficacy in arthritis treatment

Chao Fan, Xin-Ru Li, Yan-Xia Zhou, Yong Zhao, Wen-Jing Li, Shu-Jin Ma, Yan Liu^*, Gui-Ling Li, Mei Li

2012, 21(4): 311-320. DOI: 10.5246/jcps.2012.04.042

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The purpose of this work was to explore the feasibility of ethosomes for improving the anti-arthritic efficacy of topically administered tetrandrine, a bisbenzylisoquinoline alkaloid. Ethosomes were prepared by using the transmembrane pH-gradient loading method and characterized by mean diameter, morphology and entrapment efficiency. The prepared tetrandrine-loaded ethosomes exhibited spherical shape with about 78 nm of average diameter and entrapment efficiency of (52.87±3.81)%, whereas the liposomes had bigger size (99 nm) and higher entrapment efficiency (98.80±0.01)%. In addition, ethosomes exhibited favorable and enhanced penetration behavior as compared with liposomes. More importantly, tetrandrine-loaded ethosomes had a significantly better anti-adjuvant arthritis efficacy in rats compared to liposomes formulation, but no significant difference in the anti-arthritic efficacy between tetrandrine-loaded ethosomes and commercial dexamethasone ointment was observed. These results suggest that ethosomes would be a promising nanocarrier for topical delivery of tetrandrine across skin.

Development of an HPLC-UV method for the determination of ethaselen in its injection formulation

Su Chen, Ping Song, Ying Wang, Qi-Zhi Hu, Xuan Zhang^*, Qiang Zhang

2012, 21(4): 321-326. DOI: 10.5246/jcps.2012.04.043

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A novel ethaselen injection formulation has been developed in our laboratory. The objective of the present study was to establish and validate a high performance liquid chromatography (HPLC) method for the determination of ethaselen in its injection formulation. Analysis was performed on an ODS column with isocratic elution at 40 °C. Mobile phase was consisted of 0.01% phosphoric acid and methanol (60:40, v/v). The detection wavelength was set at 320 nm and the flow rate was 1.0 mL/min. The results showed that the calibration curves of ethaselen were linear in the range of 10-50 µg/mL (r² = 0.9999). The limit of detection for ethaselen was 100 ng/mL. The average recovery of ethaselen was 100.14%. The labeled content of ethaselen in its injection formulation was in the range of 102%-103% of the measured content. In conclusion, this method was stable and reproducible, thus providing a useful tool for the routine analysis of this novel ethaselen injection formulation.

A pharmacokinetic study of puerarin formulated in mixed micelles in Beagle dogs by HPLC

Yan-Jiao Li, Hui-Min Liu, Xiao-Fang Dang, Shuo-Feng Zhang, Jin-Ying Wu, Zhan-Hong Jia, Li-Wei Han^*

2012, 21(4): 327-332. DOI: 10.5246/jcps.2012.04.044

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We developed an HPLC method to study the pharmacokinetics of puerarin in Beagle dogs after oral administration of puerarin or puerarin mixed micelles (PMMS). Beagle dogs were divided into two groups randomly, and the blood samples were collected at fixed time intervals after single oral administration of puerarin or PMMS at a dosage of 120 mg/kg. Following sample preparation, analytes were separated on a C18 column (DIKMA, 150 mm×4.6 mm, 5 μm) with a guard column (DIKMA, 8 mm×4 mm) and eluted with methanol-water (25:75, v/v). Theophylline was used as the internal standard. WinNonlin 6.1 (Pharsight, USA) was used to calculate the pharmacokinetic parameters. The pharmacokinetic parameters for puerarin and PMMS in Beagle dogs were as follows: AUC, 515.96 and 2796.43 min·µg/mL; Tmax, 61.48 and 202.91 min; CL/F, 232.58 and 42.91 mL/min/kg, respectively. The relative bioavailability of PMMS to puerarin was 542.0%. Our results showed that the mixed micelle preparation significantly improved the bioavailability of puerarin by delaying absorption and reducing clearance.

Determination of luteolin and acteoside in Siphonostegiae Herba by
high-performance liquid chromatography

Ming-Bo Zhao, He-Lin Wei, Jun Li, Peng-Fei Tu^*

2012, 21(4): 333-337. DOI: 10.5246/jcps.2012.04.045

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A sensitive RP-HPLC-DAD method has been developed and validated for the determination of luteolin and acteoside in the herb of Siphonostegia chinensis Benth. (Siphonostegiae Herba). Separation was achieved on an Agilent Zorbax SB-Aq C18 column (250 mm×4.6 mm, 5 μm) using a gradient elution with mobile phases of 0.05% phosphoric acid aqueous solution (A) and methanol (B). The assay was carried out at a flow rate of 1.0 mL/min with detection at 310 nm and 350 nm. Luteolin and acteoside showed good linearity in the ranges of 0.0341-0.8172 mg/mL (r² = 0.9999) and 0.0708-2.832 mg/mL (r² = 0.9999) with average recoveries of 102.7% and 98.3%, respectively. The contents of luteolin and acteoside varied greatly in 15 samples from different habitats. This is the first report on the quantitative determination of acteoside in Siphonostegiae Herba.

Simultaneous determination of seven alkaloids and two flavonoid glycosides in Wuzhuyu decoction by RP-HPLC-DAD

Chuan-Qin Hu, Xiu-Wei Yang^*

2012, 21(4): 338-344. DOI: 10.5246/jcps.2012.04.046

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A reversed-phase high-performance liquid chromatography (RP-HPLC) method with diode array detector was established to simultaneously determine nine bioactive compounds in Wuzhuyu decoction, namely dehydroevodiamine, isorhamnetin-7-O-rutinoside, 10-hydroxyrutaecarpine, diosmetin-7-O-β-D-glucopyranoside, evodiamine, rutaecarpine, 1-methyl-2-n-nonyl-4(1H)quinolone, evocarpine, and dihydroevocarpine. The RP-HPLC assay was performed on a reversed-phase C18 column with a gradient elution. The mobile phases consisted of methanol and water containing 1% (v/v) acetic acid. The flow rate was 1.0 mL/min and the detection wavelength was set at 300 nm. All calibration curves showed good linearity (r²>0.9941) within test ranges. The results of intra-day precision, inter-day precision, and accuracy were satisfactory. The overall recoveries were in the range of 90.13%-102.48%. The method was successfully applied to quantify nine bioactive compounds in six samples. Baseline resolution for all nine major compounds was achieved. This method could be used as a suitable quality control assay for Wuzhuyu decoction.

Shenfu injection protects against myelosuppression from chemotherapy

Yan Lu, Li-Na Liu, Hong-Gang Lou, Xiang Xu^*

2012, 21(4): 345-349. DOI: 10.5246/jcps.2012.04.047

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Cyclophosphamide is used to treat a variety of tumors. However, the success of the treatment is limited due to severe myelosuppression caused by cyclophosphamide. Administration of cyclophosphamide could significantly decrease white blood cells (WBCs), platelets, red blood cells (RBCs), as well as hemoglobin level. The aim of this research is to investigate the protective role of Shenfu injection against cyclophosphamide induced myelosuppression. The results showed that Shenfu injection can markedly enhance the level of WBCs, platelets, RBCs, and hemoglobin of myelosuppressed rat. The level of WBCs, platelets, RBCs, and hemoglobin were increased by 70%-100%, 80%-90%, 10%-20% and 10%-20%, respectively. Furthermore, the protective role of Shenfu injection against myelosuppression was confirmed by the microscopic observation of bone marrow sections. In conclusion, Shenfu injection has a potential protective effect against cyclophosphamide-induced myelotoxicity.

Effect of calcium and soy isoflavone supplementation on bone mineral
density of women with different menstrual status

Asma Rashid, Rukhshan Khurshid, Asif Hanif, Mahjabeen Saleem^*, Latif Aftab

2012, 21(4): 350-354. DOI: 10.5246/jcps.2012.04.048

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In order to find out the effective alternative treatments in peri- and post-menopausal women, we carried out the research. Study design was observational experimental study with duration of 6 mon. A total of 250 female subjects were included in the study. Results showed that the bone mass density or T-score in menstruating women was increased after the use of calcium and showed a highly significant difference (P<0.001). In both peri- and post-menopausal women, the values of bone mass density or T-score was non significantly increased after the use of calcium. Values of bone mass density in peri- and post-menopausal women were significantly increased (P<0.001) after the use of phytoestrogen. It is concluded that phytoestrogen is a better treatment therapy of osteopenia/osteoporosis as compared to calcium treatment. However further research is needed in large number of women to meet a better conclusion.

Identification of dimethylamphetamine in a suspect exhibit

Peng Xu, Wen-Si Lin, Chuan-Jun Zhu, Ke-Lin Liu, Ying Chang, Yu-Xin Cui, Xiao-Mei Ling^*, Wei Lu

2012, 21(4): 355-359. DOI: 10.5246/jcps.2012.04.049

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N,N-Dimethylamphetamine (DMA) is a methamphetamine (MA) analog and considered as an amphetamine-derived designer drug. In this study, a method of gas chromatography-mass spectrometry (GC-MS) combined with nuclear magnetic resonance spectroscopy (¹H and ¹³C NMR) was developed for the identification of dimethylamphetamine in a suspect exhibit. The results showed that purity of this sample was above 99% by GC-MS area normalization. Therefore, it could be used as a dimethylamphetamine reference substance in drug FTIR analysis, which was successfully applied to identify samples in other similar cases.

Nine lignans from Artemisia absinthium L.

Abulajiang·Tulake, Yong Jiang, Peng-Fei Tu^*

2012, 21(4): 360-364. DOI: 10.5246/jcps.2012.04.050

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Nine lignans were isolated and purified by silica gel, ODS, Sephadex LH-20 column chromatographies, preparative HPLC and recrystallization from the aerial parts of Artemisia absinthium L., and identified as follows: diayangambin (1), sesartemin (2), epiyangambin (3), (+)arborone (4), (-)syringaresinol (5), epiashchantin (6), caruilignan C (7), 7β-caruilignan C (8), yangambin (9). Compounds 4, 5, 7, 8 were isolated from this plant for the first time.

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