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• 2012 Volume 43 Issue 5
  Published: 10 May 2012

    

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  Preparation of α-Stereoisomer of Decitabine

  ZHU Zhou-Hai, QI Chuang-Yu*, ZHU Yu-Tong, LI Wen-Hong

  2012, 43(5): 326-328.

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  To perform the quality control of decitabine, the α-stereoisomer was synthesized from 2-deoxy-D-ribose by methylation and acetylation to give 1-O-methyl-2-deoxy-3,5-di-(O-acetyl)-α,β-ribofuranose, which was subjected to glycosylation with 2,4-O,N-bis(trimethylsilyl)-1,3,5-triazine(6) followed by deprotection with NH3. Its configuration was confirmed by X-ray. The compound 6 was prepared from 5-azacytosine(5) by protection with hexamethyl disilylamine.
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  Preparation of β-Artemether

  LUO Chun, HUANG Jian-Jun, YANG Liu*, XIE Xiao-Ling, LIU Chu-Ying

  2012, 43(5): 329-330.

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  β-Artemether was synthesized from artemisinin by reduction with potassium borohydride to give dihydroartemisinin, which was subjected to etherification with methanol in the presence of aluminum perchlorate nonahydrate followed by recrystallization with 50% methanol in 69% overall yield and 98.5% purity.
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  Synthesis of Ethyl 1-Cyclopropyl-6,7-difluoro-1,4-dihydro-8-hydroxy-4-oxo-3-quinolinecarboxylate

  WU Wen-Liang1,2, LU Xiao-Yi2, SONG Qing-Bao1

  2012, 43(5): 331-332.

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  Ethyl 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-hydroxy-4-oxo-3-quinolinecarboxylate(1) was synthesized from ethyl 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylate(2) by hydrolysis with 40％ hydrobromic acid to give 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-hydroxy-4-oxo-3-quinolinecarboxylic acid (4), followed by esterification with ethanol in the presence of trimethyl chlorosilane with an overall yield of about 52.1％. Also compound 1 was hydrolyzed directly from 2 in the presence of anhydrous aluminum chloride in 1,2-dichloroethane with a yield of 66.9％.
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  Preparation and Characterization of Liranaftate Solid Lipid Nanoparticles

  ZHANG Hai-Long, LIU Hai-Le, LAN Tian, DING Jin-Song*

  2012, 43(5): 351-355.

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  Solid lipid nanoparticles (SLN) loaded with liranaftate were prepared by emulsion solvent diffusion method with glyceryl monostearate and cholesterin as matrix material. The formulation was optimized through orthogonal design. The mean particle size of the liranaftate SLN was(145.3±6.1)nm with the entrapment efficiency of (75.8±0.7)％ and drug loading of (4.82±0.03)％. The results of differential scanning calorimetry (DSC) showed that liranaftate was
  entrapped in the SLN as amorphous form. The results of preliminary stability test showed that the liranaftate SLN stored at 4 ℃ for 30 d could maintain stable. The results of in vitro transdermal test showed that the skin deposition ratio of liranaftate SLN gel was about 100 times of the commercial cream(Zefnart).
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  Preparation of Probucol Submicron Emulsions

  QIN Xue1,2, WANG Cheng-Gang2*, REN Xiao-Wen2

  2012, 43(5): 356-359.

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  The probucol submicron emulsions were prepared by high pressure homogenization method. Medium chain triglyceride was used as oil phase, and egg yolk lecithin and poloxamer 188 were used as emulsifiers. The preparation was optimized with mean diameter, polydispersity index ζ potential and stability as indexes. The optimal product was stable, and the average particle size, ζ potential and drug loading were (168.8±1.5)nm, (-50.1±1.7)mV and (4.2±1.6)mg/ml, respectively.
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  Pharmacokinetics of Lorazepam Droplets for Intranasal Delivery in Rabbits

  WU Wen-Zhe, LI Ding, HOU Hui-Min

  2012, 43(5): 360-362.

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  An HPLC method was established for the determination of lorazepam in rabbit plasma. The pharmacokinetics of lorazepam in rabbits after intranasal and iv administration were investigated. The calibration curve was linear in the concentration range of 1 - 75 ng/ml. The results of precision and recovery test met the requirements of bioanalysis. After intranasal and iv administration, tmax were (9.2±10.2) and (6.7±4.1)min, AUC0→∞ were (3 386.2± 520.5) and (1 693.2±818.8)ng·ml-1·min, respectively. The absolute bioavailability of nasal droplets was 62.8％.
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  Pharmacokinetics and Tissue Distribution of Epothilone B in Rats

  XU Zhi-Ru1, XIAO Lin1, LIAO Jian-Wei2, DAI Chang-Liang2, QIN Yan1*

  2012, 43(5): 363-367.

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  The validated LC-MS and HPLC method were developed for the determination of epothilone B in rat plasma and tissue, respectively. The pharmacokinetic properties of epothilone B were examined after a single iv injection of 0.5, 1 and 2 mg/kg to rats, respectively. The results suggested that the pharmacokinetic properties of epothilone B fitted well into a two-compartment open model with t1/2β of (7.17±0.68), (7.65±1.40) and (6.68±0.36)h, and AUC0→t of (60.4±6.5), (160.4±37.8) and (428.8±67.1)ng·ml-1·h according to the single dose of 0.5, 1 and 2 mg/kg, respectively. A single dose (1 mg/ml) of epothilone B to tumor bearing Wistar rats resulted in a very rapid wide distribution from plasma to tissue. Plasma elimination was very rapid, while the elimination in tumor was rather slow.
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  Dissolution Determination of Guaifenesin and Dextromethorphan Hydrobromide Tablets

  YIN Guo1, ZHONG Ling2, QIN Bin1, LI Jun1, ZHOU Jie1

  2012, 43(5): 374-376.

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  An HPLC method was established for the determination of the dissolution of guaifenesin and dextromethorphan hydrobromide tablets. The paddle method was used with 900 ml water as dissolution medium at the rotation speed of 50 r/min. A C18 column was used with the mobile phase of 0.5％ triethylamine (adjusted to pH 3.5 with phosphoric acid)-acetonitrile (65︰35) at the detection wavelength of 278 nm. The results showed that the inherent quality of the product could be objectively reflected in the above conditions. Furthermore, it had a significant distinction of the same agents from different sources.
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  Determination of 5-Aminolevulinic Acid by Pre-column Derivatization HPLC-FD

  SHI Lei1, ZHAO Feng2, LUAN Han-Sen2, WANG Hao2, WANG Hong-Wei1*

  2012, 43(5): 377-380.

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  A pre-column derivatization HPLC-FD method was established for the determination of 5-aminolevulinic acid. Fluorescamine was used as the derivatizing agent. A C18 column was used with the mobile phase of acetonitrile-0.1％ trifluoroacetic acid solution (30︰70). The excitation and emission wavelengths were 398 and 480 nm. The calibration curve of 5-aminolevulinic acid was linear in the concentration range of 0.047 5 - 47.5 μg/ml. The average recovery was 99.2％, with RSD of 1.46％.
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  Progress in Enzymatic Synthesis of β-Lactam Antibiotics with α-Amino Acid Ester Hydrolase

  QU Feng1, LI Duan-Hua1,2, WANG Lu1,2, YI Ba-Xian3*

  2012, 43(5): 381-385.

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  β-Lactam antibiotics are one of the most widely used clinical anti-infective agents, and occupy an important position in domestic pharmaceutical industry. Because enzymatic synthesis of β-lactam antibiotics is more friendly to environment and economical than chemical synthesis, it has been applied on a pilot-scale production in foreign enterprises. Therefore, it is important to enhance the research on enzymatic synthesis of β-lactam antibiotics. The research
  progress of α-amino acid ester hydrolase is introduced in this review, and the future application to enzymatic synthesis is prospected.
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  Graphical Synthetic Routes of Midazolam

  GUO Jun-Feng, DAN Xiao-Yan*, SHI Hui-Lin

  2012, 43(5): 396-398.

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