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• 2013 Volume 44 Issue 8
  Published: 10 August 2013

    

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  Synthesis of of Phosphocreatine Disodium

  MI Chenggen1, TANG Xuemei1, LIU Junqiang1, CHENG Du2, HUANG Wencai1*

  2013, 44(8): 741-743.

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  Phosphocreatine disodium was synthesized from dibenzyl phosphate by chlorination with oxalyl chloride and cyclization with creatine ethyl ester hydrochloride in the presence of Et3N to give dibenzyloxyphosphoryl creatinine, which was subjected to hydrogenolysis and alkaline hydrolysis with an overall yield of about 34％, and purity of above 99.0％.
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  Synthesis of Esomeprazole Magnesium

  SONG Weiguo1,2, CHU Yafei2, SONG Chenggang2, ZHANG Xiaopan2, XU Wenfang1*

  2013, 44(8): 744-746.

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  Esomeprazole magnesium, a proton pump inhibitor, was synthesized from 2-hydroxymethyl-3,5-dimethyl-4-nitropyridine by chlorination, condensation, asymmetric oxidation, methoxylation and then reacted with magnesium chloride. The overall yield was 73.6％(based on 2-hydroxymethyl-3,5-dimethyl-4-nitropyridine).
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  Synthesis of Stiripentol

  ZHAO Jie1, ZHANG Kai1*, HUA Yuan1, CHENG Cheng2, DU Yumin1

  2013, 44(8): 747-748.

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  Stiripentol, an anti-epileptic drug, was synthesized from piperonal and 3,3-dimethylbutan-2-one by Claisen-Schmidt reaction in the presence of phase transfer catalyst benzyltributylammonium chloride to give 4,4-dimethyl-1-[(3,4-methylenedioxy)phenyl]-1-pentene-3-one, which was subjected to reduction using NaBH4 with an overall yield of about 85％.
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  Synthesis of (R,S)-N-(1-Ethoxycarbonyl)-3-phenylpropyl-L-alanine

  FANG Yingquan

  2013, 44(8): 749-751.

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  (R,S)-N-(1-Ethoxycarbonyl)-3-phenylpropyl-L-alanine was synthesized from (S)-malic acid by hydroxyl protection and dehydration to give (S)-2-acetoxysuccinic anhydride, which was subjected to Friedel-Crafts acylation reaction, reduction, esterification, substitution and then debenzylation with an overall yield of about 30％.
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  Preparation of D-Tryptophan from L-Tryptophan

  WEI Pinghe1, PENG Jiaping1, ZHOU Xiliang2

  2013, 44(8): 752-753.

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  Started from L-tryptophan, DL-tryptophan was obtained by racemization in the basic condition. Then DL-tryptophan was resoluted to D-tryptophan camphorsulfonate using D-camphorsulphonic acid as resolving agent. After the hydrolysis reaction, D-tryptophan could be afforded with an overall yield of about 40％.
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  Separation of Mangrove Endophytic Fungus Fusarium proliferatum's secondary metabolite 1403B Using Adsorption Chromatography

  YANG Xiaojing1, ZHAO Bo1, NA Ke1, ZHAO Wenjie2*, ZHU Baoquan1

  2013, 44(8): 754-760.

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  1403B is the major impurity from fermentation process of 1403C which is marine bioactive substance with antitumor effect. This research established a method for preparation of 1403B coarse crystal and separation of 1403B from 1403B coarse crystal on the carrier of PS30-300, respectively. Quick  Screenings of desorption ratio and pH were carried out by high performance liquid chromatography. The isolate process of 1403B was as follows: 30％ ethanol with 1％ acetic acid was used to dissolve 1403B coarse crystal and 55％ ethanol with 1％ HOAc was for desorption at a flow rate of 0.8 ml/min. The chromatographic purity of 1403B was above 96％ and the yield was above 95％.
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  Preliminary Studies on the Minor Antibacterial Factors in the Nystatin Fermentation Broth Filtrate by the Chinese Producer: Streptomyces aureus A94 Strain S-7

  YU Kui, ZHU Hongjuan , ZHANG Dongmei, BAO Xuefen, XU Yongshou, GONG Baiyan, LUO Yuanhui, SHEN Guo

  2013, 44(8): 761-763.

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  It was reported long ago that the Chinese nystatin producer didn’t produce the antibacterical substances. We studied on the antibacterial substances produced by Streptomyces aureus A94 strain S-7 during nystatin fermentation, and suggested to as the beginning for further study its applied values and theoretical significances. Multiple minor antibacterial components active against super sensitive E. coli(E. coliSS), S. lutea and Staph. aureus were coproduced in the nystatin fermentation broth filtrate by the Chinese nystatin producer: Streptomyces aureus A94 strain S-7. The components which were co-produced during nystatin fermentation and resulted in the blurred (bacteriostatic) or clear zone (bacterial lytic) to Sarcina lutea were preliminarily separated to each other. During UV spectrum absorption scanning tests, the results appeared that the curde preparation YZ8157 A(leads to clear inhibition zone) having λmax 267.5 and 268.5 nm, crude preparation YZ8157 B caused to blurred inhibition zone having λmax 199.9 nm.
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  HPLC Fingerprint of Gardenia Jasminoides from Jiangxi Based on Principle Component Analysis Coupled with Cluster Analysis

  QU Xiaosheng1,2, YANG Yifang1*, YANG Yuewen1,2, HU Xiao2, LUO Yongming2

  2013, 44(8): 764-769.

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  Forty-nine batches of gardenia from different regions of Jiangxi were investigated. The fingerprint chromatography of their ultrasonic aqueous extract was established by HPLC dual wavelength method. The fingerprint similarity evaluation was combined with cluster analysis and principal component analysis. The HPLC method had good precision, stability and reproducibility. The results of similarity evaluation, cluster analysis and principal component analysis were consistent, which proved that the fingerprint could be effective for gardenia and suspected goods identification.
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  Preparation of Amoxicillin PLGA Microcapsules by Digital Micro-jetting Technology

  SUN Huaiyuan1,2, SUN Chenjie1, ZHENG Gang1, LIAO Yuehua2, CUI Lijun2

  2013, 44(8): 770-773.

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  The amoxicillin PLGA microcapsules were prepared by digital micro-jetting technology with a sprinkler with the inner diameter of 40 μm. The optimal preparation obtained by orthogonal test were as follows: PLGA concentration was 3％, driving voltage was 80 V, jet frequency was 10 kHz and agitator rotational speed was 750 r/min. The particle size, encapsulation efficiency and drug loading of the product were (60.25±1.08)μm, 62.4％ and 2.1％, respectively. The in vitro cumulative amount at 30 d was 85.4％.
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  Preparation and Quality Evaluation of Epinastine Hydrochloride Capsules

  ZENG Rui1, LIU Haiping1, LI Qiong1, ZHANG Haixian1, QU Yan2*

  2013, 44(8): 774-777.

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  The epinastine hydrochloride, pregelatinized starch and microcrystalline cellulose were mixed and then filled into capsules. The drug-excipient compatibility, powder properties of the mixture of drug-excipient with different weight ratio and in vitro dissolution of the product were investigated. The results of preliminary stability test showed that after storage at (40±2)℃ and relative humidity of (75±5)％ for 6 months or at room temperature for 12 months, the content and dissolution did not have significant changes but the amount of related substances had a slight increase.
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  Optimization of Freeze-drying Process of Mirtazapine for Injection Based on the Concept of Quality by Design

  ZHANG Xiaofei1, GUO Qiuting2, YANG Jiao3

  2013, 44(8): 778-780.

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  The design space (DS) of the operation parameters of primary drying for mirtazapine injection was obtained based on the concept of quality by design (QbD). The effects of shelf temperature and chamber pressure on the product temperature and primary drying time were investigated with factorial design. The DS of the above two parameters was obtained by Design Expert 8.0.6 software. The results showed that the parameters randomly selected in DS would not affect the lyophilized effect of mirtazapine for injection.
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  Enhanced Oral Absorption of Teniposide Cationic Nanoemulsions

  NIU Baohua1, MA Li2, LIU Zeying2, WANG Yixin1, CHEN Dawei1*

  2013, 44(8): 781-785.

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  The teniposide cationic nanoemulsions (TCN) were prepared by a self-assembly technique with D-α-tocopherol polyethylene glycol 1000 succinate (TPGS), 12-hydroxystearic acid-polyethylene glycol copolymer (HS-15), octadecylamine and medium chain triglyceride. The product was nanometer-sized with the mean diameter of (61.9±4.5)nm and the ζ potential of (+8.38±3.34)mV. The MTT assay showed that the in vitro antitumor activity of teniposide in A549 cells was significantly increased by TCN. The distributions of teniposide from TCN in the intestinal tract and tissues such as heart, liver, spleen, lung and kidney of mice were obviously enhanced compared with teniposide solution. Moreover, the results of in vivo pharmacokinetic test in rats indicated that the cmax and AUC of teniposide from TCN were significantly enhanced. Compared with teniposide solution, the oral bioavailability of TCN was 380％.
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  Determination of Benzalkonium Chloride in Besifloxacin Hydrochloride Eye Drops by HPLC

  CHEN Zaixin, ZHU Feng, WANG Yongjun

  2013, 44(8): 786-788.

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  An HPLC method was established for the determination of benzalkonium chloride in besifloxacin hydrochloride eye drops. A Kromasil C18 column was used, with the mobile phase of 5 mmol/L ammonium acetate (containing 1％ triethylamine, adjust pH to 5.2±0.5 with glacial acetic acid)-acetonitrile (29∶71), at the detection wavelength of 215 nm. The flow rate was 1.0 ml/min. The calibration curve of benzalkonium chloride was linear in the concentration range of 5 - 15 μg/ml (R2=0.998 3). The average recovery was 99.4％ with RSD of 0.42％.
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  Assessing Baizi Yangxin Pills Quality by Merging Chromatographic Fingerprints, Spectrum Fingerprints and Combustion Heat

  SUN Guoxiang, YIN Ruijuan, LI Xiaowen

  2013, 44(8): 789-795.

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  The HPLC fingerprints, ultraviolet spectrum fingerprints, infrared spectrum fingerprints and the combustion heat of Baizi Yangxin Pills were developed. Based on the principle of complementary advantages, five models were integrated and the systematic qualified fingerprint method was used to evaluate the quality of the medicine. Finally, the results showed that one batch (the grade≥5) was worse. The quality grade of one batch was different in different analytical methods, and the others (the grade≤3) were better. All the chemical constituents were comprehensively monitored by merging the spectrum fingerprints, chromatograph fingerprints and combustion heat, which showed it could be a novel media for the quality control of traditional Chinese medicine.
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  Determination of Naringin in Kanggu Zengsheng Capsules by HPLC

  ZHU Jing, YANG Qingqing*

  2013, 44(8): 795-797.

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  An HPLC method was established for the determination of naringin in Kanggu Zengsheng capsules. A Diamonsil C18 column was used, with the mobile phase of methanol-2％ glacial acetic acid(37∶63) at the detection wavelength of 283 nm. The flow rate was 1.0 ml/min and the column temperature was 30 ℃.The calibration curve of naringin was linear in the concentration range of 40 - 200 μg/ml (r=0.999 6). The average recovery was 100.17％ with RSD of 0.94％．
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  Determination of Dehydroabietic Acid in Pine Cones of Pinus yunnanensis Franch at Different Collection Time by HPLC

  YAN Wenjing1, LI Chunyan2, YANG Yongshou2, LIU Guangming2, XIAO Peiyun2*

  2013, 44(8): 798-801.

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  An HPLC method was established for the determination of dehydroabietic acid in pine cones of Pinus yunnanensis Franch. A Phenomenex Gemini-NX C18 column was used with the mobile phase of acetonitrile-0.3％ phosphoric acid (58︰42) at the detection wavelength of 214 nm. The results showed that the content of dehydroabietic acid from pine cones of Pinus yunnanensis Franch was varied with different collection time and the highest appeared in May.
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  Determination of BHT in Butyl Rubber Closures by GC-MS/MS

  ZHOU Jie, YIN Guo, LIU Hongwei, LIU Yao, WANG Xiaowei

  2013, 44(8): 801-803.

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  A GC-MS/MS method was established for the determination of 2,6-di-tert-butyl-4-methylphenol (BHT) in butyl rubber closures. An Agilent HP-5 column was used, with temperature programming, headspace sampling, and MRM mode. It was linear in the concentration range of 1 - 80 μg/ml. The average recovery was 98.2％.
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  Determination of Ephedrine Hydrochloride in Kechuanning Tablets by HPLC

  LOU Zhaoxuan

  2013, 44(8): 804-806.

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  An HPLC method was established for the determination of ephedrine hydrochloride in Kechuanning tablets. A Diamonds C18 column was used, with the mobile phase of acetonitrile-0.1% phosphoric acid (10∶90), at the detection wavelength of 207 nm. The calibration curve of ephedrine hydrochloride was linear in the concentration range of 10 - 100 μg/ml. The average recovery was 98.92% with RSD of 1.18%.
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  Optimization of Crystallization Technology of Saccharification Liquid from Broken Rice for Preparing Glucose Injection by Central Composite Design and Response Surface Methodology

  SHI Jilian, YANG Yantao, QIU Yun, TANG Yu, HE Fuyuan*

  2013, 44(8): 807-810.

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  The crystallization technology of saccharification liquid from broken rice for preparing glucose injection was optimized by central composite design and response surface methodology (RSM) with the concentration of saccharification liquid, amount of inoculating seed and crystallizing time as independent variables and the yield of glucose crystal as dependent variable. The results showed that the binomial regress equation fit the data well (r=0.916 0). The optimal technology was as follows: the saccharification liquid was condensed to the concentration of 100％ - 150％, amount of inoculating seed was 2％ - 3％ (based on the original glucose concentration), and crystallizing time was 50 - 60 h at room temperature.
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  Application of Soxhlet Extraction and Concentration Units to Production of Traditional Chinese Medicine Extract

  LI Guoming, ZHENG Yanhui, QIAO Sainan

  2013, 44(8): 810-813.

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  To solve the problems of thermal reflux method in the production of traditional Chinese medicine extract, the Soxhlet units of setting extraction and condensation function were designed and proposed. The working principle and operation method of Soxhlet units were elaborated in this paper. The units had the advantages of leaching with simultaneous enrichment, high equipment utilization, high extraction rate and particularly low energy consumption.
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  Progress in Hyaluronic Acid-based Targeted Nano-drug Delivery Systems

  WANG Jing, HUO Meirong, ZHANG Xuyuan, ZHOU Jianping*

  2013, 44(8): 828-835.

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  Hyaluronic acid (HA) possesses lots of advantages such as non-toxicity, low immunogenicity and biodegradability. The active targeting effect can be achieved through the interaction between HA and its receptors, especially CD 44. The purpose of this paper is to review the formulations, physicochemical and biological properties of HA-based targeted nano-drug delivery systems, such as HA-drug conjugates, nanogels, nanomicelles and nanoparticles. Trends and prospects of developments and applications of HA are introduced.