主办:上海医药工业研究院
   中国药学会
   中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA

Archive

  • 2012 Volume 43 Issue 2
    Published: 10 February 2012
      

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  • ZHANG Yi-Kun, JIA Gui-Peng, LIU Zhi-Ling, ZOU Jiang, YANG Yan
    2012, 43(2): 81-83.
    Abstract ( )   Knowledge map   Save
    Linezolid was synthesized from 3,4-difluoronitrobenzene(4) by reaction with morpholine, reduction and condensation with ethyl chloroformate to give ethyl N-(3-fluoro-4-morpholino-4-ylphenyl)carbamate(7), which was subjected to cyclization with (S)-1-azido-3-chloropropan-2-ol(3), reduction and then acylation with an overall yield of about 40%(based on compound 4). Compound 3 was prepared from (S)-epichlorohydrin(2) by reaction with sodium azide.
  • HE Yong, CHEN Shi-Yun, WU Zong-Hao*
    2012, 43(2): 84-86.
    Abstract ( )   Knowledge map   Save
    Repaglinide was synthesized from 4-ethoxycarbonyl-3-ethoxyphenylacetic acid by reaction with p-toluenesulfonyl chloride in the presence of potassium carbonate and benzyltriethylammonium chloride to give the mixed anhydride, which was subjected to condensation with (S)-3-methyl-1-(2-piperidin-1-ylphenyl)butylamine and then hydrolysis with NaOH with an overall yield of about 74%(based on 4-ethoxycarbonyl-3-ethoxyphenylacetic acid).
  • XIE Yan1, ZHENG Tu-Cai1, ZHOU Wen-Jun1, CHEN Fen-Er2
    2012, 43(2): 87-89.
    Abstract ( )   Knowledge map   Save
    2-(2-Phenylethyl)benzoic acid or 2-(thiophen-2-ylethyl)benzoic acid was synthesized from o-cyanobenzyl chloride via Wittig-Horner reaction with benzaldehyde or 2-thiophene carboxaldehyde, hydrolysis and then hydrogenation with the overall yield of about 64% or 60% .
  • ZHOU Rong-Guang1, WANG Jin2, YANG Zhao-Xiang1, YANG Bo2
    2012, 43(2): 90-91.
    Abstract ( )   Knowledge map   Save
    2,3,4-Trimethoxybenzoic acid was synthesized from pyrogallic acid by methylation with dimethyl carbonate and Blanc chloromethylation to give trimethoxybenzyl chloride, followed by oxidation with KMnO4 in the presence of NaOH and tetrabutyl ammonium bromide with an overall yield of about 63%.
  • RAO Min1,2, JIN Xu1,2, RUAN Li-Jun2, LUO Min-Yu2, SHENG Xia-Fang1*
    2012, 43(2): 92-96.
    Abstract ( )   Knowledge map   Save
    An HPLC method, coupled with MS data analysis and amino acid analysis, was established for the separation and identification of the major metabolites from the fermentation broth of Streptomyces parvus HCCB10043. The obtained three compounds were identified as A21978C1, C2 and C3. The 16S rDNA sequence of S. parvus HCCB10043 showed 99.2% identity to that of S. roseosporus NRRL11379, the known A21978C producer, and phylogenetic analysis revealed that they had very close relationship. Gene cluster for the biosynthesis of A21978C complex in S. parvus HCCB10043 was identified by comparing with the reported one in S. roseosporus NRRL11379 as reference, and validated by gene in-frame deletion. The results showed that the gene clusters were same in both strains.
  • XIAO Pei-Yun, YANG Yong-Shou, LIU Guang-Ming
    2012, 43(2): 97-99.
    Abstract ( )   Knowledge map   Save
    An UV spectroscopy method was established for determination of the total flavonoids from pine needles of Pinus yunnanensis Franch.. The dynamic changes of total flavonoids from the pine needles dried by different methods and collected at different time were investigated. The results showed that the highest content of total flavonoids from pine needles were dried by baking as well as the pine needles collected in July. There was a significant difference of
    total flavonoids content among the pine needles dried by different methods and collected at different time.
  • WANG Jian1, HOU Hui-Min1, XIA Yi-Ran1, SUN Han-Dong2, PU Jian-Xin2
    2012, 43(2): 100-103.
    Abstract ( )   Knowledge map   Save
    The eriocalyxin B nanosuspension was prepared by combined application of wet milling and high pressure homogenization with lecithin and poloxamer as stabilizers. The mean diameter of the product was 98.2 nm with the drug loading of 4.2 mg/ml. The in vivo process of eriocalyxin B in mice after iv administration could be described by two-compartment model. The plasma elimination half-lives of iv group and ip group were 49.8 and 45.1 min, respectively. The apparent volumes of distribution were 4.0 and 5.4 L/kg, respectively.
  • SONG Yi, GONG Shan-Shan
    2012, 43(2): 103-106.
    Abstract ( )   Knowledge map   Save
    The in vitro release rates of carbamazepine from three batches of sustained-release tablets of a domestic factory (test preparation) and Tegretol (reference preparation) in different pH mediums (water, pH 4.5 acetate buffer and pH 6.8 phosphate buffer) were compared. The determination was carried out in 900 ml medium by paddle method with 75 r/min stirring rate. The results showed that there was a significant difference in the release rates of the three batches, even the same batch, of test preparation in the above mediums. The quality of the test preparation was inferior to the reference preparation.
  • LUO Jing1, ZHANG Tao2,3, HUANG Hua1*, DING Yan-Ji2,3, LIU Ze-Rong2,3
    2012, 43(2): 107-111.
    Abstract ( )   Knowledge map   Save
    The loxoprofen sodium cataplasm was prepared with water-soluble polymer material partially neutralized polyacrylate (NP700) as matrix, polyvinylpyrrolidone K90 and carboxymethylcellulose sodium as viscosityenhancing agents and gelatin as film forming material. The formulation was optimized by orthogonal design. The product could completely release in 2 h. The transdermal behavior through excised Bama miniature pig skin fitted to zero-order kinetics equation. The cumulative transdermal amount of cataplasm containing combined permeation enhancers was significantly higher than that of the blank group (containing no permeation enhancer) and other groups (containing a single permeation enhancer). The results of preliminary stability study showed that the adhesion, content, in vitro release and transdermal property of the product stored at 30 ℃ and 60% relative humidity for 6 months had no significant
    change.
  • WANG Feng-Juan1, HU Shi-Gao2, BAO Yong-Chu1, CHEN Qing-Hua1*
    2012, 43(2): 112-115.
    Abstract ( )   Knowledge map   Save
    The intestinal absorption of gabapentin in rats was investigated by means of in situ single pass perfusion. The results showed that gabapentin could be absorbed in the whole small intestine (duodenum, jejunum and ileum) and colon. The drug absorption constant (Ka) and effective absorption coefficient (Peff) of small intestine were higher than those of colon in low and middle concentration (1 and 10 mmol/L) groups (P<0.05). The drug absorption in duodenum was significantly higher than colon in high concentration (50 mmol/L) group (P<0.05). The gabapentin concentration had a significant effect on absorption in small intestine. The Ka and Peff of small intestine in low concentration group were significantly higher than those of high concentration group (P<0.05). However, drug concentration had no effect on absorption in colon.
  • ZHU Zhuang-Zhi1, WU Yu-Bo1, LUO Hua-Fei1, WANG Hao1, GAO Fan2*
    2012, 43(2): 116-119.
    Abstract ( )   Knowledge map   Save
    An UPLC-MS/MS method was established for the simultaneous determination of oxybutynin and its main metabolite N-desethyloxybutynin in rat plasma with oxybutynin-D11 hydrochloride as the internal standard. The plasma samples were treated by liquid-liquid extraction. A tandem mass spectrometric detection was conducted under positive ionization mode with an electrospray ionization (ESI) interface. A multiple reaction monitoring (MRM) mode was chosen for the detection of m/z 358.2→124.1 (oxybutynin), m/z 330.2→96.1 (N-desethyloxybutynin) and m/z 369.3→142.1 (oxybutynin-D11). The calibration curves were linear in the concentration range of 0.5 - 100 ng/ml for oxybutynin and 0.2 - 40 ng/ml for N-desethyloxybutynin, respectively. The intra- and inter-day RSDs were less than 8% .
  • WANG Lin-Bo1, YANG Mei-Cheng1, WANG Hao2, CHEN Gui-Liang1, HAN Peng3
    2012, 43(2): 120-122.
    Abstract ( )   Knowledge map   Save
    Polyethylene glycol(PEG) 1000 is a representative Newtonian fluid pharmaceutical excipient. However its viscosity determination methods in pharmacopoeias are different. A method was established for the determination of the kinematic viscosity of 50% PEG 1000 solution at (20±0.1)℃ with a U-tube viscometer, whose fluid time was more than 200 seconds. Then the method was validated by a rheometer method. The results demonstrated that
    the U-tube viscometer method was simple, accurate and reproducible.
  • AN Jing1, ZHANG Jun-Zhen2, LU Yan-Fang1, NI Mei-Ping1, JIANG Ye1*
    2012, 43(2): 123-125.
    Abstract ( )   Knowledge map   Save
    A flow injection chemiluminescence method was established for the determination of ibandronate monosodium. Ibandronate monosodium was demolished and converted to inorganic phosphate which could react with ammonium molybdate to form heteropoly molybdophosphoric acid, further reacted with luminol to generate chemiluminescence. The calibration curve was linear in the concentration range of 5 - 25 μg/ml. The recoveries were over 97.6% , with RSDs less than 2.0% .
  • 吕Shan-Shan , CHEN Jing, LIU Xiao, AN Yi-Qiang, JIANG Xiang-Lan*
    2012, 43(2): 126-129.
    Abstract ( )   Knowledge map   Save
    An HPLC method was established for the simultaneous determination of nine chemical componentschlorogenic acid, caffeic acid, rutin, forsythoside, scutellarin, baicalin, forsythin, baicalein and wogonin, in the Shuanghuanglian soft capsules. A C18 column was used with the mobile phase of acetonitrile-0.1% formic acid by gradient elution at the detection wavelength of 278 nm. The nine compounds showed good linearity within test ranges. Their recoveries were 97.5% - 101.5% , with RSDs of 1.2% - 4.6% .
  • ZHAO Na1, YAN Zheng-Yu1,2*, JIANG Xin-Min2
    2012, 43(2): 129-131.
    Abstract ( )   Knowledge map   Save
    An HPLC method was established for the determination of dasatinib and its related substances. A C18 column was used with the mobile phase of acetonitrile-0.01 mol/L potassium dihydrogen phosphate solution (adjusted to pH 5 with sodium hydroxide solution) by gradient elution, at the detection wavelength of 230 nm. The calibration curve of dasatinib was linear in the concentration range of 5 - 50 μg/ml, with the low limit of detection of 0.01 μg/ml.
  • HAN Ru, JIA You-Zhi
    2012, 43(2): 132-134.
    Abstract ( )   Knowledge map   Save
    A headspace capillary gas chromatography method was established for the determination of nine residual organic solvents: methanol, acetone, acetonitrile, dichloromethane, ethyl acetate, trichloromethane, benzene, toluene and pyridine in fosinopril sodium. A HP-624(6% cyanopropylphenyl-94% dimethylpolysiloxane) capillary column was used with the application of FID detector. Their average recoveries were 100.7%, 101.7%, 102.2%, 101.6%,
    99.5% , 100.7% , 101.5% , 101.8% and 102.1% , with RSDs less than 2.5% .
  • TIAN Yong, TANG Su-Fang
    2012, 43(2): 134-136.
    Abstract ( )   Knowledge map   Save
    A headspace capillary gas chromatography method was established for the determination of methanol, acetone, isopropanol, dichlormethane, isopropyl ether and ethyl acetate in clopidogrel hydrogen sulfate. The samples were pre-treated with magnesium oxide. A DB-624 capillary column was used with temperature program and FID detector, at injection temperature of 70 ℃ and equilibrium time of 30 min. The calibration curves of these solvents
    were linear in the concentration ranges of 7.5 - 750, 5 - 500, 12.5 - 1 250, 1.5 - 150, 12.5 - 1 250 and 12.5 - 1 250 μg/ml, respectively. The recoveries were 100.4%, 101.2%, 100.5%, 98.2%, 99.2% and 99.6%, with RSDs less than 2.0%.
  • WANG Shuang1, LI Qi-Lu2, DI Guang-Xi1*
    2012, 43(2): 137-142.
    Abstract ( )   Knowledge map   Save
    Many therapeutic drugs can not successfully enter brain due to blood-brain barrier, which is a challenge for the treatment of central nervous system diseases. Research progress in drug delivery system for brain targeting, including active targeting system induced by receptor (such as apoprotein receptor, transferrin receptor), passive targeting system (such as nanoparticles, carbon nanotubes) and other targeting system (such as magnetic particles, cationic preparation), is summarized in this paper.
  • LIU Li-Li1,2 , WANG Cheng-Gang2*, GONG Li2, WANG Ping-Bao2
    2012, 43(2): 143-147.
    Abstract ( )   Knowledge map   Save
    Liquid drug prefilled syringe system develops quickly for its safety and efficacy. The key point of this system is to improve the compatibility of drug and injection device and ensure the safety use. The advantage, disadvantage and applicability of the components of prefilled syringe and manufacturing process should be taken into account in the preparation of prefilled syringe system loaded with different drugs. Based on the domestic and foreign literatures in recent years, the development and application of liquid drug prefilled syringe system are analyzed and summarized in this paper.
  • XU Qing1, HUANG Qin-Qin1, WANG Yong-Lu1, LI Xue-Ming1,2*
    2012, 43(2): 148-152.
    Abstract ( )   Knowledge map   Save
    Nanosuspensions in pharmaceutical field have been increasingly concerned with the rapid development of nanotechnology. Nanosuspensions are colloid dispersion system composed of pure drug sub-micron particles, which depend on surfactants to remain stability. The physical stabilities of  nanosuspensions, including sedimentation, agglomeration, crystal growth and crystal transition are summarized in this paper. The mechanism of stability and main solutions of the problems are briefly reviewed.
  • YUAN You-Zhi, TANG Jia-Deng, CEN Jun-Da*
    2012, 43(2): 153-156.
    Abstract ( )   Knowledge map   Save
  • WANG Guan2, GUO Ye-Kun2, ZHONG Jing-Fen2*, SHI Hui-Lin2
    2012, 43(2): 157-159.
    Abstract ( )   Knowledge map   Save
  • LIANG Yin-Xing, YE Hua
    2012, 43(2): 160-A15.
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