Chinese Journal of Pharmaceuticals

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Synthesis of Safinamide

XING Rui-Juan1, LV Tao1, LIU Lei-Na1, ZHU Meng-Chu2, DU Yu-Min1*

2012, 43(3): 161-163.

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Safinamide, an antiparkinson drug, was synthesized from 3-fluorobenzyl chloride by substitution with 4-hydroxybenzaldehyde to give 4-(3-fluorobenzyloxy)benzaldehyde, which was subjected to condensation and reduction to give (S)-2-[4-(3-fluorobenzyloxy)benzylamino]propionamide, followed by salification with methanesulfonic acid. The overall yield was about 76％.

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Synthesis of Alverine Citrate

YANG Dan1, ZHANG Yu-Bin1, WANG Lan-Zhou2, JI Qing-Gang1*

2012, 43(3): 164-166.

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Alverine citrate, a spasmolytic agent, was synthesized from 3-phenyl-1-propanol by bromination and reaction with ethylamine to produce N-ethyl phenylpropylamine(4) , which was reacted with 1-bromo-3- phenylpropane in the presence of sodium hydroxide and tetraethyl ammonium bromide to obtain N-ethyl-N-(3- phenylpropyl)benzenepropanamine(5), followed by salification with citric acid with an overall yield of about 58％ .

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Synthesis of Tesuofovir Circularproxil fumarate

LIU Li1, XU Kui2

2012, 43(3): 166-169.

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Tesuofovir circularproxil fumarate was synthesized from from (R)-1,2-propanediol by condensation, reaction with adenine, condensation, hydrolysis, protection and chlorination to give (R)-9-[2- (dichlorothiophosphorylmethoxy)propyl]adenine, which was subjected to reaction with (S)-(-)-(3-chlorophenyl)-
1,3-propanediol in the presence of TiCl4 and then salification with an overall yield of about 13％(based on (R)-1,2- propanediol).

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Synthesis of Mitotane

DENG Li-Ping, TAO Wei-Feng, WANG Wei, ZHANG Yong, WU Chun-Lei

2012, 43(3): 170-171.

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Mitotane, an antineoplastic agent, was synthesized from 2-chlorobenzaldehyde by reaction with chloroform in KOH/CH3OH and DMF to give 2,2,2-trichloro-1-(2-chlorophenyl)ethanol, which was subjected to reduction followed by reaction with chlorobenzene in the present of sulfuric acid with an overall yield of about 27％.

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Synthesis of Methyl (3S)-3-(tert-Butoxycarbonylamino)-4-oxobutanoate

GUO Jin-Cai1, ZHANG Yong-Jun2, ZHANG Xing-Xian1*

2012, 43(3): 172-174.

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Methyl (3S)-3-(tert-butoxycarbonylamino)-4-oxobutanoate, an important chiral intermediate of sitagliptin, was synthesized from L-aspartic acid by selective methylation in the presence of SOCl2 to give 4-methyl L-aspartate hydrochloride, which was subjected to Boc-protection, acylation with ethyl chloroformate and reduction by NaBH4, followed by oxidization by NaClO/TEMPO with an overall yield of about 41％.

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Virus Inactivation Process of Sodium Hyaluronate from Animal Source

FAN Su-Jun, KONG Shu-Jing, HOU Yong-Tai

2012, 43(3): 175-177.

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In order to ensure the safety of sodium hyaluronate from animal source, selection of effective virus inactivation process was necessary. The crest was used as the source of hyaluronic acid. Theiler's mouse encephalomyelitis virus (TMEV), vesicular stomatitis virus (VSV), simian virus 40 (SV40) and pseudo-rabies virus (PRV) were chosen as indicators for the virus inactivation. The results showed that enzymolysis was an effective method. The efficiency of virus inactivation was verified. The average logarithm inactivation value (LIV) of TMEV, VSV, SV40 and PRV were 6.125, 5.438, 5.792 and 5.250 lgTCID50/0.1 ml, respectively.

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Component Analysis of SFE-CO2 Extracts of Callicarpa kwangtungensis Chun. by GC-MS and Antimicrobial Activity

JIA An, YANG Yi-Fang*, KONG De-Yun, ZHU Xue-Gui△

2012, 43(3): 178-181.

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The chemical constituents of SFE-CO2 extracts of Callicarpa kwangtungensis Chun. were separated and analyzed by GC-MS. Their relative percentages were calculated with peak area normalization method. Twenty-seven compounds were identified in the SFE-CO2 extracts I accounting for 81.12％ of the peak area of the total ion-current chromatogram. Twenty compounds were identified in the SFE-CO2 extracts II accounting for 74.60％ of the peak area of the total ion-current chromatogram. The main constituents of SFE-CO2 extracts I, extracts II and their mixture (1︰1) had some activities against Staphylococcus aureus, Escherichia coli and Candida albicans.

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Preparation and Evaluation of Blended Membrane Consisted of Chitosan and Polylactide or Poly(R)-3-Hydroxybutyric Acid Methyl Ester

LIU Yi-Lu, TAN Yan-Ling, LIANG Qiu-Zhi

2012, 43(3): 182-185.

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The blended membrane consisted of chitosan and polylactide (PLA) or poly(R)-3-hydroxybutyric acid methyl ester (PHB) was prepared by the tape casting process. The tensile strength of chitosan-PLA (1∶1, w/w) and chitosan-PHB (1∶1, w/w) blended membrane were (25.39±1.63) and (23.49±0.43)MPa with the water absorption rate of (32.65±2.41)％ and (33.72±3.11)％, respectively. The degrading rate of the chitosan-PLA blended membrane immersed in the artificial tissue fluid for 45 d was (32.26±0.56)％. It indicated that the membrane could induce the new tissue to regenerate.

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Application of Dissolution-precipitation to Reduction in the Diameter of Slightly Soluble Drugs in Solid Preparation

ZHENG Si-Ji, TAN Bo, LIU Xiao-Yi, FU Lin-Yong, YUAN Shao-Qing

2012, 43(3): 186-190.

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The solubility of alkalescent and weakly acidic drugs can be affected by pH of the solution. So by adding appropriate acidulant (or alkalizer) to dissolve the drugs, then adding the carrier and alkalizer (or acidulant), the solid preparation of the slightly soluble drug with small particle size can be prepared by wet granulation method. The granules and tablets of slightly soluble drug (risperidone, indapamide or glipizide) were prepared by this method as well
as the preparations with pre-pulverized bulk drugs. The results showed that the diameter of the granule prepared by this method was significantly reduced as well as the dissolution rate of the tablets was significantly increased.

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Preparation of Indapamide Orally Disintegrating Tablets

XU Zhi, PENG Hong*, CHEN Wen-Jie

2012, 43(3): 191-193.

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The formulation of orally disintegrating tablets without indapamide were screened with compressibility, disintegration time and taste as indexes. The tablets loaded with indapamide were prepared by wet granulation, and the disintegration time and dissolution were determined. The results showed that the average disintegration time of optimal tablets was within 30 s. Compared with common tablets, the product could completely release within 10 min.

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Eriocalyxin B Nanosuspension. Ⅱ. Inhibitory Effects on H22 Hepatoma-bearing Mice

WANG Jian1, HOU Hui-Min1, XIA Yi-Ran1, SUN Han-Dong2, PU Jian-Xin2

2012, 43(3): 194-197.

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The antitumor effect and toxicity of eriocalyxin B nanosuspension on H22 hepatoma-bearing mice were investigated under different administration routes and dosages. The inhibition effect could be achieved by all three routes (iv, ip and ig administration) with the appropriate dose, and a clear dose-effect relationship was observed. Meanwhile, the toxicity was significantly increased with the increasing of dose. The inhibition of ip administration was higher than that of iv at the dose of 10 mg/kg, and the toxicity of ip route was higher. The antitumor effect of ig administration was the weakest, and the serious gastrointestinal adverse reactions were observed in the high-dose group.

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Bioequivalence of Levonorgestrel Tablets in Human

JIANG Meng-Yin1,2, MIAO De-Yu1, CHEN Jun2, CAO Lin3, LI Wei1*

2012, 43(3): 197-200.

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Twenty healthy female volunteers were given a single oral dose of levonorgestrel tablets in a randomized crossover study. Serum levels of the drug were determined by radioimmunoassay method. The pharmacokinetics of test and reference preparation were as follows: tmax (1.9±0.2) and (2.0±0.1) h, cmax (6.34±1.16) and (6.86±1.07 ) ng/ml, MRT (30.48±4.85) and (29.26±4.71) h, t1/2 (24.60±4.28) and (24.12±4.61) h, AUC0→72 h (92.43± 24.24) and (101.09±31.21) h·ng·ml-1, AUC0→∞ (104.41±29.25) and (113.06±36.07) h·ng·ml-1, respectively. The relative bioavailability of the test preparation was (93.5±16.2)％.

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Determination of Related Substances in Remifentanil Hydrochloride by HPLC

MA Yu-Jie1, YANG Hong1*, RONG Xiao-Juan2, CAO Jun-Han3

2012, 43(3): 204-207.

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An HPLC method was established for the determination of related substances in remifentanil hydrochloride. By means of stereospecific synthesis, the structure of main related substance was confirmed to be 4-methoxycarbonyl- 4-[(N-1-oxopropyl)phenylamino]-1-piperidinepropionic acid. A Kromasil-CN column was used, with the mobile phase of 0.03 mol/L potassium dihydrogen phosphate solution-methanol-acetonitrile (80 ︰ 16 ︰ 4) at the detection wavelength of 225 nm. The calibration curves for remifentanil hydrochloride and its main related sabstance were linear in the range of 1-15 mg/ml.

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Determination of the Related Substances of Antituberculosis Fixed-dose Combination

LI Bing, YAO Lan, SUN Xiao-Jun

2012, 43(3): 208-211.

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An HPLC method was established for the determination of the related substances of antituberculosis fixed-dose combination (FDC)of rifampin, isoniazid and pyrazinamide. A C18 column was used with the mobile phase of 0.01 mol/L phosphate buffer-methanol(40︰60) at the detection wavelength of 254 nm. The results of specificity test, system suitability test, durability test and solution stability test showed that the proposed method was feasible. The determination of related substances is beneficial to the quality control of compound drugs.

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Determination of Residual Organic Solvents in Olprinone Hydrochloride by Capillary Gas Chromatography

LI Zhi-Wei1, QI Jian-Min1, HE Qing-Guo2, ZHANG Yun-Sheng2, ZHAO Yun-Chao1

2012, 43(3): 212-213.

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A capillary gas chromatography method was established for the determination of seven residual organic solvents: acetone, tetrahydrofuran, ethyl acetate, methanol, ethanol, n-butanol and N,N-dimethylformamide in olprinone hydrochloride. An INNOWax capillary column was used with FID detector and temperature programmed control. The calibration curves were linear in the measured concentration ranges. The recoveries were 95％ - 103％ , with
RSDs less than 2％ .

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Research and Development of Biodegradable Long-action Injectable Drug Delivery System

LI Kun, Liu-Xiao-Jun, Chen-Qing-Hua*

2012, 43(3): 214-221.

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Due to the distinctive advantage of drug sustained-release for several days to months after local injection, biodegradable long-action injectable drug delivery system (DDS) has got more and more attention either in the life science or in the clinic. The purpose of this paper is to review the procedure in R&D of the DDS, the styles and specific properties of biodegradable polymers as well as the application of the DDS in clinic. The prospect and the problems in application are evaluated.

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Progress in Evaluation of Venous Irritation for Injection Screening

WU Shuang, CAI Wei-Hui, JIN Fang*

2012, 43(3): 222-226.

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Screening proper injection preparations of strong irritant drugs with reasonable evaluation methods to decrease the venous irritation has an important effect on improving drug security and patient compliance. In this paper, the mechanism of venous irritation is introduced and different evaluation systems on venous irritation for injection are summarized. The aim of this paper is to provide references for preparing injection with low irritation and good compliance.

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Application of HPLC-Charged Aerosol Detection

LIU Lu1,2, GAO Xuan2, YANG Yong-Jian2*

2012, 43(3): 227-231.

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Charged aerosol detection (CAD) is a novel generic HPLC detector. CAD system has some advantages such as broad dynamic response range, good precision and sensitivity, response independent of chemical properties, widespread application and simple and reliable operation. CAD has been applied for the analysis of neutral, acidic, basic and zwitterionic compounds without volatility and ultraviolet activity. This review introduces its operation principle and selected applications.

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Rational Design of Low Temperature Points of Use in the Distribution System of Water for Injection

YU Fan

2012, 43(3): 232-234.

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In the field of pharmaceutical industry, water for injection has a direct effect on the quality of the final product. The design of low temperature (<70 ℃) points of use in the distribution system of water for injection is a key point of the whole pharmaceutical water system construction. Through the analysis of designs of common low temperature points of use, several optimal designs with parallel structure are suggested in this paper.

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Graphical Synthetic Routes of Azacitidine

YU Juan, CHEN Guo-Hua*

2012, 43(3): 235-238.

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Preparation of Periodic Safety Update Report in Manufacturer

DONG Duo1,2, SUN Li-Hua1*, LIU Wei2

2012, 43(3): 239-A23.

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