Chinese Journal of Pharmaceuticals

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Improved Synthesis of Safinamide Mesilate

HUANG Jian1, BI Guangqing1, XIE Jianshu1, WU Jiajie2

2016, 47(07): 828. https://doi.org/10.16522/j.cnki.cjph.2016.07.001

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An improved synthetic process of safinamide mesilate with an overall yield of 79.6％ was described, which comprised the condensation of 3-fluorobenzyl chloride with 4-hydroxybenzaldehyde in the presence of organicbase, followed by reaction with L-alaninamide hydrochloride via a one-pot imine generation, reduction and salification.The process had the advantages of mild reaction condition and high reaction selectivity with good potential for industrial application.

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Synthesis of Sapropterin Dihydrochloride

WU Mei, QIU Yuehen, ZHENG Yunxiaozhu, DENG Yong*

2016, 47(07): 832. https://doi.org/10.16522/j.cnki.cjph.2016.07.002

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Sapropterin dihydrochloride was synthesized from L-(+)-rhamnose monohydrate via condensation with 1-dodecanethiol, oxidation and MacDonald-Fischer degradation to obtain the key intermediate 5-deoxy-L-arabinose, which was subsequently subjected to condensation with phenylhydrazine and acetylation with acetic anhydride, then cyclization with 2,4,5-triamino-6-hydroxypyrinidine sulfate and deprotection to afford 2-amino-6-[(1R,2S)-1,2-dihydroxypropyl]-4(1H)-pteridinone, followed by catalytic hydrogenation with platinum dioxide, then hydrochloric acid salt formation with an overall yield of about 26.8％.

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Synthesis of Topiroxostat

GAO Rui, WANG Decai, XU Bin, WANG Xin, SU Peng

2016, 47(07): 835. https://doi.org/10.16522/j.cnki.cjph.2016.07.003

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Methyl isonicotinate-N-oxide reacted with dimethylcarbamyl chloride in the presence of cuprous iodide and zinc cyanide to give methyl 2-cyanopyridine-4-carboxylate, followed by hydrazinolysis to obtain 2-cyanoisoniazide, then the latter was condensed with 4-cyanopyridine, followed by reaction with p-toluenesulfonic acid monohydrate and dissociation by potassium carbonate, the anti-hyperuricemia drug topiroxostat was prepared with an overall yield of 41％. This method started from cheap and easily obtained raw materials, with mild reaction conditions, short synthetic route and good potential for industrial application.

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Synthesis of Central Analgesic Succinate Dehydro-tapentadol Ester

TAO Junyu, XU Kui

2016, 47(07): 838. https://doi.org/10.16522/j.cnki.cjph.2016.07.004

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1-Dimethylamino-2-methyl-3-pentanone reacted with m-methoxyphenyl magnesium bromide by Grignard reaction to give 1-dimethylamino-3-(3-methoxyphenyl)-2-methyl-3-pentanol hydrochloride(2), 2 was chlorinated with thionyl chloride, and then demethylated by boron tribromide to give 3-[3-chloro-1-(dimethylamino)-
2-methylpentan-3-yl]phenol hydrochloride(4), 4 reacted with 4-tert-butyl-cyclohexanol sodium in 4-tert-butylcyclohexanol to give dehydro-tapentadol(5) by cis-antichloration, 5 was esterificated with succinic anhydride to give (Z)-3-[1-(dimethylamino)-2-methyl-2-penten-3-yl]phenyl succinic acid monoester(6), followed by esterification, reduction and salinization to give (Z)-3-[1-(dimethylamino)-2-methyl-2-penten-3-yl]phenyl-4-hydroxybutyrate succinate(1) with an overall yield of 31.8％. Compound 1, named as succinate dehydro-tapentadol ester, is a new candidate central analgesic drug in phase II clinical trial.

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Improved Synthetic Process of Ganciclovir

LI Ying

2016, 47(07): 841. https://doi.org/10.16522/j.cnki.cjph.2016.07.005

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Ganciclovir, an antiviral drug, was synthesized from 2,9-diacetyl guanine and methyl [(2-acetoxy-1-acetoxymethyl)ethoxy]acetate by condensation to give N2-acetyl-N9-[(1,3-diacetoxy)-2-propyloxymethyl]guanine, and then treatment with methylamine solution with an overall yield of 38.6％ and HPLC purity of 99.6％.

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Novel Synthesis of 8-Chloro-5,6-dihydro-11Hbenzo[5,6]cyclohepten[1,2-b]pyridine-11-one

WANG Hongbo, ZHANG Kehua, ZHOU Houyuan

2016, 47(07): 843. https://doi.org/10.16522/j.cnki.cjph.2016.07.006

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A novel synthetic route of 8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepten[1,2-b]pyridine-11-one(1), an important intermediate of loratadine was described. Diethyl 2-[2-(3-chlorophenyl)ethyl]-2-[2-(1,3-dioxolan-2-yl)ethyl]malonate (6) was synthesized from 1,3-dichlorobenzene and epoxyethane via Grignard reaction and bromination, followed by the nucleophilic substitutions successively with diethyl malonate and 2-(2-bromoethyl)-1,3-dioxolane. Then compound 6 was converted to 2-[2-(1,3-dioxolan-2-yl)ethyl]-4-(3-chlorophenyl)butanic acid (7) by hydrolysis and decarboxylation. 3-[2-(3-Chlorophenyl)ethyl]-2-methylpyridine (9) was obtained by methylation
of 7 with lithium methide, followed by condensation with hydroxylamine hydrochloride and cyclization. Finally, 1 was prepared by oxidation of 9 with SeO2 and Friedel-Craft cyclization. The new route was unprecedentedly reported and showed a potency for manufacture in industrial scale.

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Synthesis of 2-Amino-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide

LIU Changchun, WANG Tianyang, ZHANG Yuqing

2016, 47(07): 848. https://doi.org/10.16522/j.cnki.cjph.2016.07.007

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2-Amino-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide, the key intermediate of dasatinib, was synthesized from 1,1,3,3-tetramethoxypropane via bromination with copper(Ⅱ) bromide to give 2-bromo-1,1,3,3-tetramethoxypropane, followed by condensation and cyclization with thiourea to afford 2-aminothiazole-5-carbaldehyde, which was subjected to oxidative amidation with 2-chloro-6-methylaniline in the presence of cuprous bromide and tertbutylhydroperoxide. The overall yield was 81.3％. This method provides several advantages such as short synthetic route, inexpensive and easily obtained raw materials, high yield and lower production costs, it also avoids using volatile bromine and acyl chloride.

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Transient Expression of rhHER2-mAb and Its Antitumor Activity

LIU Dongchen, HONG Po, ZHAN Xianlong, XIA Qiankun, XIE Qiuling

2016, 47(07): 851. https://doi.org/10.16522/j.cnki.cjph.2016.07.008

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Recombinant humanized anti-HER2 monoclonal antibody (rhHER2-mAb) was expressed through transient transfection into HEK293F cells. The transfection conditions were optimized, and the antitumor activity of the purified antibodies was analyzed. The expression vectors, pCMV-HC and pCMV-LC, which contained heavy and light chains of rhHER2-mAb were constructed respectively, and co-transfected into HEK293F cells using polyethylenimine (PEI) as the tranfectant. The recombinant protein was purified by Protein A affinity chromatography. Its antitumor activity was determined by WST-8 method. Under the optimal transfection conditions as the cell density of 4×106 cells/ml, DNA concentration of 2.0 μg/106 cells, DNA∶PEI of 1∶2, and heavy chain∶light chain of 1∶1, the highest titer of
rhHER2-mAb reached 73.0 mg/L, with a purity over 98％. The inhibitory rates of rhHER2-mAb on the BT-474 cells with HER2 overexpression was up to (72.3±2.0)％, and on the SK-BR-3 cells with moderate HER2 expression was (32.1± 1.2)％, but it showed no inhibitory activity on the MCF-7 cells with low HER2 expression. In addition, the rhHER2-mAb could induce the BT-474 cells apoptosis up to 25％ compared with the control group, while it was only about 15％ to the SK-BR-3 cells.

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Synthesis of Guanine Arabinoside from 2,6-Diaminopurine Arabinoside by Pseudomonas aeruginosa TX16

LIU Guosheng, XU Hang, CAO Qian, XING Shantao, LI Meng

2016, 47(07): 857. https://doi.org/10.16522/j.cnki.cjph.2016.07.009

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Guanine arabinoside were synthesized from 2,6-diaminopurine arabinoside with Pseudomonas aeruginosa TX16 cells as catalytic agent. Through optimization experiments, the optimal reaction conditions were obtained as follows: adding 13％ Pseudomonas aeruginosa TX16 bacterial cells and 30 mmol/L 2,6-diaminopurine arabinoside into the 160 mmol/L phosphate buffer solution (pH 7.5), at the reaction temperature of 60 ℃ and reacting for 120 h. Under the above conditions, the conversion rate of purine nucleoside was 90.0％.

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Study on Chemical Constituents from Viscum coloratum (Komar.)Nakai

CAO Duo, CHENG Liang, LI Jianqi, HE Quanquan, YANG Peiming

2016, 47(07): 861. https://doi.org/10.16522/j.cnki.cjph.2016.07.010

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The chemical constituents from the dry stems and leaves of Viscum coloratum (Komar.)Nakai were isolated and purified by various chromatographic methods and their structures were elucidated on the basis of detailed spectroscopic analysis. The dry stems and leaves of Viscum coloratum (Komar.)Nakai was extracted by 95％ ethanol, followed by concentration and extraction by water and chloroform. Then the water part was eluted in D101- type macroporous resin by the gradient elution of water∶ethanol (100∶0—0∶100) to obtain water and 10％—95％ ethanol six parts. Three compounds were isolated from the 95％ ethanol part and identified as rhamnazin-3-O-β-D-[5''- (3-hydroxy-3-methylglutaryl)]-api-(1→2)-[6''-(3-hydroxy-3-methylglutaryl)]-O-β-D-glucoside(1), rhamnazin-3-O- β-D-[6''-(3-hydroxy-3-methylglutaryl)]-O-β-D-glucoside (2) and rhamnazin-3-O-β-D-api-(1→2)-[6''-(3-hydroxy-3- methylglutaryl)]-O-β-D-glucoside (3). Compound 1 is a new flavonoid glycoside, named as viscumneoside Ⅷ.

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Accumulation of Main Active Ingredients in the Leaves of Three Gentianaceous Medicinal Plants

HAN Duo, ZHAO Zhilian, LIU Weihong, LI Yuehua, LI Haifeng

2016, 47(07): 865. https://doi.org/10.16522/j.cnki.cjph.2016.07.011

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An HPLC method was applied for the determination of the active ingredients such as gentiopicroside (1), swertiamarin (2), sweroside (3) and amarogentin (4) in the leaves of Gentiana rigescens Franch., G. cephalantha Franch., and G. delavayi Franch., from the same origin. Their HPLC fingerprints were compared with those of the roots and rhizomes of G. rigescens Franch.. The accumulation of the main active ingredients in the leaves were evaluated by one-way ANOVA analysis. The results showed that the accumulations of compounds 1 and 2 in the leaves of G. rigescens Franch. and G. cephalantha Franch. were significantly higher than those in G. delavayi Franch. (P<0.01), while the accumulations of compounds 3 and 4 in the leaves of G. delavayi Franch. were significantly higher than those in G. rigescens Franch. and G. cephalantha Franch. (P<0.01). The fingerprint similarities between the leaves of G. rigescens Franch., G. cephalantha Franch. and the roots and rhizomes of G. rigescens Franch. were high (0.999 and 0.991). Their main active ingredients were also similar. However, the fingerprint similarity of G. delavayi Franch. (leaves) was low, and their main active ingredients were quite different.

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Preparation and Antitumor Activity of pH-Responsive Drug Carriers Based on K5 Polysaccharide

ZHANG Yirang, PENG Huanhuan, YE Baotong, CHEN Jingxiao, CHEN Jinghua

2016, 47(07): 870. https://doi.org/10.16522/j.cnki.cjph.2016.07.012

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In this study, K5 polysaccharide was modified with histidine to obtain a series of amphiphilic conjugates (KH1, KH2, KH3) with degrees of substitution (DS) of 20％, 28％ and 39％, respectively. These conjugates could self-assemble into nanoparticles in water and encapsulate doxorubicin (DOX). The particle size of drug-loaded or unloaded nanoparticles decreased with the increasing of DS values. Among them, the drug-loaded KH3 (DKH3) nanoparticles dispersed well in aqueous solution with the average particle size of 207.7 nm, ζ potential of -22.1 mV, drug loading of (10.25±0.05)％ and encapsulation efficiency of (51.26±0.27)％. In accordance with the results of in vitro release test, DKH3 nanoparticles exhibited a fast and complete drug release behavior in the acidic milieus compared with that in neutral medium. Cytotoxicity assay indicated that KH3 nanoparticles had no obvious toxicity against B16 cells and COS7 cells. The half maximal inhibitory concentration (IC50) of DKH3 nanoparticles against B16 cells and COS7 cells were 1.97 and 13.3 μg/ml, meanwhile, the IC50 values of DOX were 0.66 and 0.86 μg/ml correspondingly. Combining with the results of cellular uptake experiments, DKH3 nanoparticles could significantly improve the selectivity in cancer chemotherapy.

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A Comparison of Dissolution Curves between Self-prepared Eslicarbazepine Acetate Tablets and Reference Listed Drug

HAN Song, RUAN Jianshan, DING Zhongjie, CHEN Xiangwei

2016, 47(07): 877. https://doi.org/10.16522/j.cnki.cjph.2016.07.013

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A similarity evaluation experiment was conducted to compare the dissolution curves of self-prepared eslicarbazepine acetate tablets and reference listed drug in four media. The in vitro dissolution test was carried out at (37.0±0.5)℃ and rotation rate of 50 r/min with the paddle apparatus method in 900 ml of four media [pH 1.2 hydrochloric acid solution, pH 4.5 acetate buffer, pH 6.8 phosphate buffer and water]. An HPLC method was used to determine drug concentration in four media. The dissolution data were analyzed with difference factor (f1) and similarity factor (f2) method. The results indicated that the dissolution curves of self-prepared tablets and reference listed drug were similar in four media.

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Preparation and in vitro Evaluation of Isradipine Extended-release Tablets

TAN Yongjin, CHEN Zhi

2016, 47(07): 881. https://doi.org/10.16522/j.cnki.cjph.2016.07.014

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The solid dispersions (SDs) loaded-with isradipine were prepared with polyethylene glycol (PEG) 6000 as carriers. The effect of the drug-carrier ratio on drug dissolution rate from the SDs was investigated. Then the extended-release hydrophilic matrix tablets based on the SDs with a drug-carrier ratio of 1∶4 were prepared. The formulation of the self-made extended-release tablets was optimized with the similarity factor (f2) between the release curves of the self-made tablets and the reference preparation (DynaCirc CR) in 0.2％ sodium dodecyl dimethyl amine oxide solution as an index. A similarity evaluation was conducted to compare the release curves of the optimal extendedrelease tablets and the reference preparation in pH 1.2 hydrochloric acid solution, pH 4.5 phosphate buffer, pH 6.8 phosphate buffer and water, respectively. The calculated f2 values were all above 50, indicating the similarity of two preparations in four media. Moreover, the in vitro release behaviors of three batches of optimal extended-release tablets had a good reproducibility.

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Preparation and Characterization of Cordycepin-loaded Carboxymethyl Chitosan Nanoparticles

LÜ Dan, GU Xinxia, ZHU Di, CHEN Qin, GE Xiaoqun

2016, 47(07): 885. https://doi.org/10.16522/j.cnki.cjph.2016.07.015

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Emulsion and ionic crosslinking method was adopted to prepare cordycepin-loaded carboxymethyl chitosan nanoparticles (1-CMC-NPs). The formulation was optimized by single-factor test and orthogonal design with particle size and entrapment efficiency as indexes. The results showed that the entrapment efficiency and drug loading of the optimal product were about 70％ and 9％. The mean diameter and ζ potential of the optimal 1-CMC-NPs with spherical appearance were about 148 nm and -25 mV. The results of differential scanning calorimetry (DSC) and X ray diffraction (XRD) showed that the drug might exist in an amorphous form in carriers. The results of in vitro release test showed that the cumulative release from the 1-CMC-NPs at 48 h in phosphate buffer without or with serum were 68.1％ and 80.4％, respectively. Compared with the cordycepin solution, the drug release from the 1-CMC-NPs exhibited a good sustained-release behavior.

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Bi-directional Regulation of Glycyrrhizic Acid on Transdermal Permeation of Podophyllotoxin Tincture and Preliminary Investigation on Attenuation of Adverse Effects

WANG Yatian, ZHAO Boxin, WANG Shengqi, LIANG Qianying, LI Guofeng

2016, 47(07): 891.

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The skin permeation profile of podophyllotoxin (1) from the tincture was evaluated by Franz diffusion cells with excised rat skin as a barrier. The concentration of 1 was determined by HPLC. The effect of glycyrrhizic acid (2) on the transdermal permeation of 1 and its side effect on skin was preliminary investigated. The 1 tinctures containing different concentrations (0.1, 1, 5, 10, 20 and 40 mg/ml) of 2 were prepared. The results of transdermal test showed that there was a bi-directional regulation of 2 on transdermal permeation of 1. It demonstrated a promotion effect on 1 when the concentration of 2 was in the range of 0.1—1 mg/ml; while in the range of 5—40 mg/ml, the transdermal permeation amounts of 1 were inhibited. The permeation amount and permeation rate of 1 from the tincture containing 1 mg/ml of 2 were significantly improved (P<0.001). The results of particle size determination showed that the drug loaded micelles formed in the tincture with particle size of about 265 nm, which changed the drug release process and limited permeation of 1. However, when 1 tincture was given on the rat skin with pretreatment of 2, the skin permeability and the permeation rate of 1 were increased in a concentration-dependent manner. HE staining and immunohistochemical assays were used to observe the morphology of the skin tissue. It indicated that 2 could reduce the secretion of skin inflammation factors caused by 1 tincture.

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Determination of Mono-ester Alkaloids in Aconitum Plants by ELISA

YUAN Shuai, XU Yu, HUANG Lei, XU Yunhui, HUA Moli

2016, 47(07): 897. https://doi.org/10.16522/j.cnki.cjph.2016.07.017

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The hapten, mono benzoylmesaconine-3-yl glutarate (BM-GA), was synthesized by introduction of a glutaryl group to benzoylmesaconine (BM). The derivative was then conjugated with bovine serum albumin (BSA) by the active ester method to form the artificial antigen (BM-GA-BSA). A polyclonal antibody (PAb) was produced from immunized New Zealand rabbits. It had been proved that the PAb had high specificity with mono-ester alkaloids. An enzyme-linked immunosorbent assay (ELISA) method was established for the determination of mono-ester alkaloids in Aconitum plants. The linear range of mono-ester alkaloids was 0.005—5 μg/ml. The limit of detection (LOD) was 139 pg, the limit of quantity (LOQ) was 575 pg, and the average recovery rate was 97.31％, with RSDs no more than 1.68％. The sensitivity of ELISA was approximately 112 times higher than that of HPLC.

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A Comparison of Dynamic Flowability Evaluations of Lactose Powder by Two Analyzers

HUANG Lin, CHEN Lan, LU Xiangyun

2016, 47(07): 902. https://doi.org/10.16522/j.cnki.cjph.2016.07.018

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Five kinds of lactose carrier for dry powder inhalation (DPI) were prepared by mixing Inhalac® 120 with Inhalac® 400 in weight ratios of 100∶0, 95∶5, 90∶10, 85∶15 and 80∶20. The dynamic flowabilities of these lactose carriers were evaluated by two analyzers, FT4 Powder Rheometer and Powder Flow Analyzer (PFA). The indexes measured by FT4 analyzer were as follows: stability index (SI), basic flowability energy (BFE), flow rate index (FRI) and specific energy (SE). The indexes measured by PFA were as follows: flow stability (FS), compaction coefficient at rate of 100 mm/s (CC100), ratio of compaction coefficients at rate of 10 and 100 mm/s (CC10/100) and cohesion index (CI). The comparisons of the methods based on two analyzers were carried out. The differences of SE and CI, the repeatabilities of BFE and CC100, the sensitivities of FRI and CC10/100 were compared. This paper also summarized the applications of two instruments to DPI flowability evaluation. In conclusion, both two analyzers provided similar results of flow stability with good repeatability, while FT4 analyzer was more suitable for flow energy test and PFA showed a better performance on cohesion measurement. In addition, the CC10/100 values obtained by PFA were similar to FRI values by FT4, which indicated that both analyzers were suitable for dynamic flowability evaluation.

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Determination of Catechin and Gaultheroside A in Dianbaizhu Syrup by HPLC

SUN Jia, SUN Xu, WANG Xia, CHEN Qingfeng, LI Yongjun,

2016, 47(07): 907. https://doi.org/10.16522/j.cnki.cjph.2016.07.019

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An HPLC method was established for the determination of catechin (1) and gaultheroside A (2) in Dianbaizhu syrup. An Aglient Eclipse XDB-C18 column was used, with the mobile phase of methanol∶0.1％ phosphoric acid by gradient elution, at the detection wavelength of 230 nm. The linear ranges for 1 and 2 were 0.01—0.20 μg and 0.09—1.80 μg. Their average recoveries were 98.86％ and 95.98％, with RSDs of 1.8％ and 1.6％, respectively.

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Determination of 20 NSAIDs Added Illegally in Chinese Patent Drugs and Health Products by Solid Phase Extraction-HPLC-DAD

HOU Xiaomei, FENG Anyong, YUAN Ping, CHEN Zhiqiong

2016, 47(07): 910. https://doi.org/10.16522/j.cnki.cjph.2016.07.020

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A solid phase extraction-high performance liquid chromatography with diode array detector (SPEHPLC- DAD) method was established for the determination of 20 nonsteroidal anti-inflammatory drugs (NSAIDs) probably added illegally in Chinese patent drugs and health products. Samples were extracted with methanol by ultrasound, and the extract was cleaned up by an Oasis HLB SPE column. A Waters XBridge Shield RP C18 column was used, with the mobile phase of 0.02 mol/L ammonium acetate solution (pH 5.0)∶acetonitrile by gradient elution, at the detection wavelengths of 230 nm and 280 nm. The results showed that the interference of the matrix was low. It was linear for 20 NSAIDs in the range of 1—50 μg/ml. Their limits of detection were 0.03—0.80 mg/kg.

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Determination of Six Constituents in Zhaqu Pingwei Mixture by HPLC

ZHANG Li, LIU Jinying, MA Lingzhen

2016, 47(07): 915. https://doi.org/10.16522/j.cnki.cjph.2016.07.021

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An HPLC method was established for the determination of honokiol, magnolol, glucosylvitexin, vitexin-2-O-rhamnoside, vitexin and hyperoside in Zhaqu Pingwei mixture. A Kromasil C18 column was used, with the mobile phase A of 25％ acetonitrile methanol solution and the mobile phase B of 0.5％ formic acid by gradient elution, at the detection wavelengths of 294 nm (for the detection of honokiol and magnolol) and 340 nm (for the detection of glucosylvitexin, vitexin-2-O-rhamnoside, vitexin and hyperoside). The linear ranges for the above six components were 4.75—95.0, 5.00—100.0, 2.50—50.0, 6.50—130.0, 2.00—40.0 and 3.25—65.0 μg/ml, respectively. Their average recoveries were 98.9％, 97.8％, 99.3％, 98.5％, 97.9％ and 97.2％, with RSDs of 1.44％, 1.08％, 1.21％, 0.98％, 1.30％ and 1.52％, respectively.

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Determination of the Related Substances in Cefetamet Pivoxil Hydrochloride and Its Preparations by HPLC

LI Danfeng, HUANG Lili, LIU Zhuangwei, ZHU Jianping

2016, 47(07): 918. https://doi.org/10.16522/j.cnki.cjph.2016.07.022

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An HPLC method was established for the determination of the related substances in cefetamet pivoxil hydrochloride and its tablets, capsules, dry suspensions and dispersible tablets. A Capcell PAK C18 column was used, with the mobile phase A of 5 mmol/L tetrabutylammonium hydroxide solution (adjusted to pH 4.5 with phosphoric acid) and the mobile phase B of acetonitrile by gradient elution, at the detection wavelength of 232 nm. Cefetamet pivoxil hydrochloride and its related substances were separated well. It was linear for cefetamet pivoxil hydrochloride in the range of 5—100 μg/ml, and its average recovery was 99.8％, with RSD of 1.2％.

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Preparation, Mechanism and Application of Discoid Micro/nano-particles

SHI Ye, HE Fen

2016, 47(07): 924. https://doi.org/10.16522/j.cnki.cjph.2016.07.023

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Spherical micro/nano-particles as drug delivery systems have been studied extensively. However, the shape of micro/nano-particles does matter in circulation time in vivo, cellular uptake and biodistribution, according to recent studies. The advantages of discoid micro/nano-particles become even more prominent, such as more susceptible to mammalian cell absorption, longer circulation time and less cytotoxicity. In this paper, preparation method and mechanism of micro/nano-particles in cell phagocytosis are reviewed and the application to delivery of peptides are particularly focused on.

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Research Advances in Effects of Formulation and Process Parameters on Quality of Multivesicular Liposomes

ZHANG Ranran, SUN Yandong, ZHAO Yuan, LU Weigen

2016, 47(07): 929. https://doi.org/10.16522/j.cnki.cjph.2016.07.024

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A novel type of liposomes, multivesicular liposomes (MVLs) in which one vesicle contains one or more non-concentric aqueous chambers surrounded by a network of lipid membranes, is developed by DepoFoam technology. MVLs can provide a high encapsulation efficiency of water-soluble drugs compared to conventional liposomes, so it is suitable for delivery of these drugs. Moreover, the drug release from MVLs usually exhibits a sustainedrelease property. The advances of enhancing encapsulation efficiency, modulating drug release rate and improving stability of MVLs by adjusting the formulation and process parameters are reviewed in this paper.

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Progress of Antioxidant Effects of Inorganic Nanomaterials and Their Use as Nanocarriers for Drug Delivery

HUANG Yike, WAN Jingyuan

2016, 47(07): 933. https://doi.org/10.16522/j.cnki.cjph.2016.07.025

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Oxidative stress response of the body is a source of many chronic diseases. Taking antioxidants is the currently main methods for treatment of the oxidative stress-related diseases. The classification of various inorganic nanomaterials and their applications to delivery of antioxidants are reviewed in this paper. Antioxidant mechanism of the inorganic nanomaterial itself is also introduced. Inorganic nanocarriers show good prospects in delivery of poorly soluble antioxidants because of the abilities of targeting delivery, sustained-release delivery and improvements of solubility and stability, which are useful to improve the efficacy of antioxidant drugs.

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Graphical Synthetic Routes of Olaparib

ZHANG Guangxia, ZHU Qihua, XU Yungen

2016, 47(07): 940. https://doi.org/10.16522/j.cnki.cjph.2016.07.026

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Graphical Synthetic Routes of Bepotastine

XIA Jun, WANG Haiping, XU Guanyu

2016, 47(07): 943. https://doi.org/10.16522/j.cnki.cjph.2016.07.027

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