Journal of Chinese Pharmaceutical Sciences

Analysis of the chemical composition of Angelicae Pubescentis Radix by ultra-performance liquid chromatography and quadrupole time-of-flight tandem mass spectrometry

Meiqi Wan, Youbo Zhang, Yanfang Yang, Xiaoyan Liu, Lingyun Jia, Xiuwei Yang

2019, 28(3): 145-159. DOI: 10.5246/jcps.2019.03.014

Asbtract ( 348 )

HTML ( 6)

PDF (1763KB) ( 365 )

References | Related Articles | Metrics

Angelicae Pubescentis Radix(APR, Duhuo) is a commonly used traditional Chinese medicine and usually used for the treatments of rheumatic diseases. To assess the chemical composition of APR extract, a sensitive and reliable UPLC-Q-TOF-MS method was used for qualitative analysis. The separation was achieved on an Agilent SB-C₁₈ column (1.8 μm, 2.1 mm×50 mm) with a gradient elution system consisting of acetonitrile and water containing 0.1% formic acid. An electrospray ionization (ESI) was used for mass spectrometer, and the data were collected in the positive ion mode, which was operated in a full-scan mode at m/z 100–800. A total of 49 compounds including 46 coumarins were identified according to the MS and MS/MS data. Among them, two were new compounds, and isoangenomalin, scoparone, 4-methyl-umbelliferyl acetate, suberenol, trans-dehydroosthol, and oroselone were first reported in APR.

Electrophysiological characterization of furo[3,2-b]pyridine derivatives as negative allosteric modulator of a7 nicotinic acetylcholine receptor

Xintong Wang, Wenxing Zou, Haoran Xiao, Wenjun Xie, Xin Li, Xiling Bian, Qi Sun, Kewei Wang

2019, 28(3): 160-166. DOI: 10.5246/jcps.2019.03.015

Asbtract ( 272 )

HTML ( 1)

PDF (1556KB) ( 178 )

References | Related Articles | Metrics

A series of 1H-pyrrolo[3,2-b]pyridine (3a–3f) and furo[3,2-b]pyridine derivatives (4a–4g) were evaluated on human α7 nicotinic acetylcholine receptors (nAChRs) using two-electrode voltage clamp (TEVC) recording. A representative 2-(2-methoxy-phenyl)-furo[3,2-b]pyridine 4f as negative allosteric modulator (NAM)selectively inhibited alpha7 nAChR over α3β4, α4β2 nAChRs and 5-HT_3A receptor, with a potency of IC₅₀ of 5.51 μM and a maximum inhibition rate of 87.8%. The preliminary analysis ofstructure-activity relationship (SAR) suggested that compound 4fcould serve as a basis for further discovery of potent and selective α7 nAChR NAMs.

Rapid and sensitive HPLC-MS/MS method for quantitative determination of isochlorogenic acid B in rat plasma and its application in pharmacokinetic study

Xin Liu, Bo Zhang, Dan Mei, Kai Huang

2019, 28(3): 167-173. DOI: 10.5246/jcps.2019.03.016

Asbtract ( 262 )

HTML ( 11)

PDF (2472KB) ( 197 )

References | Related Articles | Metrics

Asensitive LC-ESI-MS/MS method for determination of isochlorogenic acid B in rat plasma was developed and validated in the present study. Plasma samples were prepared by a simple protein precipitation with methanol containing resveratrol as internal standard (IS). The chromatographic separation was performed on a Zorbax SB-C₁₈column (3.5 μm, 2.1 mm×100 mm, Agilent, USA) at a flow rate of 0.2 mL/min using methanol/water containing 0.1% formic acid (v/v) as mobile phase. The detectionwas performed on a triple quadrupole tandem mass spectrometer equipped with Electronic Spray Ion by selected reaction monitoring (SRM) of the transitions at m/z 515.3→352.9 for isochlorogenic acid B and m/z 227.1→143.1 for IS, respectively. The calibration curve of the method was linear over the range of 5–2500 ng/mL (r²= 0.9982). The intra- and inter-day precisions (R.S.D.%) were less than 12.46%, and the accuracy (R.E.%) was within ±5.80%. Isochlorogenic acid B was sufficiently stable under all relevant analytical conditions. The validated method was successfully applied to the plasma pharmacokinetic studies of isochlorogenic acid B in rats. It was found that isochlorogenic acid B had non-linear pharmacokinetic characteristics in rats within the dosage ranges from 5 to 20 mg/kg.

Absorption mechanism of paeonol nanoemulsion using in vitro intestinal cell models

Yi Ouyang, Jing Zhang, Hongfei Wu, Min Dai

2019, 28(3): 174-185. DOI: 10.5246/jcps.2019.03.017

Asbtract ( 251 )

HTML ( 1)

PDF (2022KB) ( 103 )

References | Related Articles | Metrics

The use of nanoemulsion has improved the bioavailability of paeonol, and that is mainly because of the P-glycoprotein(P-gp)-mediated efflux described in our previous study. However, other mechanisms involved in the intestinal absorption of paeonol nanoemulsion are still unknown. Therefore, we aimed to investigate additional paeonol nanoemulsion absorption mechanisms. By establishing the Caco-2 cells model and the follicle-associated epithelium (FAE) model, uptake studies and bidirectional transport of paeonol nanoemulsion in the presence of different efflux inhibitors were conducted to observe its intake and transport. The paracellular pathway was evaluated by fluorescent staining of Occludin, and the expressions of efflux proteins and tight junction proteins were detected by Western blotting analysis. In this study, we found that nanoemulsion improved the absorption of paeonol by increasing its uptake across the Caco-2 and FAE cells and by reducing the expressions of efflux proteins. In addition, paeonol nanoemulsion had no effect on the opening of tight junctions. The results showed that the absorption of paeonol nanoemulsion occurred by passive diffusion in the Caco-2 cell model and by endocytosis in the FAE model, which was related to multidrug resistance-associated protein 2 (MRP2) and breast cancer resistance protein (BCRP) efflux. Paeonol nanoemulsion significantly increased the absorption of the drug in intestinal cells, which was possibly related to the increase in intestinal cell uptake, inhibited expressions of efflux protein and reduction of drug efflux.

Determination the content of gypsum fibrosum in Xiaokening tablets by powder X ray diffraction method

Jianping Zhang, Xinxin Feng, Dong Wang

2019, 28(3): 186-194. DOI: 10.5246/jcps.2019.03.018

Asbtract ( 287 )

HTML ( 1)

PDF (1698KB) ( 267 )

References | Related Articles | Metrics

The research on the application of X-ray diffraction in the quantitative analysis of Chinese medicines is rare. The main reason is that the technical problems related to the internal standard and the selection of quantitative peaks are not well solved, and the accuracy and precision of the results are not satisfactory. This study employed the concept of mass absorption coefficient based on the internal standard method, and the full spectrum fitting and quantitative methods were used to solve the above technical problems. The sample was blended, the internal standard substance of zinc oxide was fully ground, and tablets were prepared by positive pressure method. Under certain instrumental conditions, the PXRD pattern was obtained by scanning. The percentage of gypsum fibrosum in Xiaokening tablet was obtained by quantitative analysis of full spectrum fitting internal standard by TOPAS software. The method was investigated by methodology. At the same time, the method was compared by ion chromatography, and SPSS software was used to make a significant t test on the results of the two methods. After the investigation, the average standard recovery rate of CaSO₄·2H₂O was 99.06% (RSD=3.02%); and the recovery rate for simulated samples was 96.7%. The method had good specificity. After statistical analysis, there was no significant difference between the new PXRD method and the traditional method of ion chromatography.

Implications for the therapeutic role of Imatinib in systemic sclerosis: a single-arm meta-analysis

Qi Zhang, Bo Zhang, Nengming Lin

2019, 28(3): 195-202. DOI: 10.5246/jcps.2019.03.019

Asbtract ( 273 )

HTML ( 1)

PDF (1345KB) ( 229 )

References | Related Articles | Metrics

Sclerotic chronic graft-versus-host disease (ScGVHD) or systemic sclerosis (SSc) is one of the most severe manifestations of chronic graft-versus-host disease (cGVHD) since the involvement of major organs significantly affects the mortality and morbidity of SSc patients. Currently, there are no effective therapeutic approaches or standard “second-line” therapy for SSc. Imatinib, a clinical tyrosine kinase inhibitor used to treat chronic myeloid leukemia and gastrointestinal tumor, has shown potential therapeutic effects in treating ScGVHD or SSc. Due to the current limitations of clinical trials using Imatinib in the treatment of SSc, the results vary among different studies, and the applications of Imatinib in SSc is still in vagueness. Here we conducted a single-arm meta-analysis to quantitatively and systematically interpret the results of previous studies, as to evaluate the potential therapeutic effect of Imatinib in SSc. The pooled clinical response rate (CRR) showed that Imatinib had higher CRR in SScpatients with longer disease duration (CRR = 0.550) and lung involvement (CRR = 0.601) than those without (P<0.001). Therefore, it was encouraging to conduct future clinical studies regarding Imatinib therapy in SSc patients, since the global response rate of Imatinib was higher than expected in specific subgroup patients.

Brief introduction for application of the USA national drug code

Dongsheng Yang, Lingyun Ma, Jianzhao Niu, Mingdi Xu

2019, 28(3): 203-208. DOI: 10.5246/jcps.2019.03.020

Asbtract ( 386 )

HTML ( 4)

PDF (1152KB) ( 181 )

References | Related Articles | Metrics

The reference listed drug (RLD) adopted in the USA orange book is the important source of the Chinese comparator product directories of generic medicinal products. Therefore, its availability has the vital significance for pharmaceutical enterprise to carry out the re-evaluation of generic medicinal products and study of generic medicinal products. The national drug code (NDC) is the unique, 3-segment number for each drug product in USA, and it serves as a universal product identifier for drugs. While the NDC directory adopts the information of drug products in the current commercial distribution, including all of the prescription drug and over the counter (OTC) drug products. The composition and configuration of the NDC number are systemically elaborated in this paper, as well as the data source, development history and supporting measures of the NDC directory. At the same time, by taking drugs, which are adopted in the Chinese comparator product directory of generic medicinal product (first batch) and sourced from USA orange book, as example, it introduces the application of the NDC directory in the availability aspect of the Chinese comparator products to facilitate the Chinese or foreign pharmaceutical manufacturers to search, identify and purchase the suitable RLD sourced from USA orange book. Moreover, it can provide reference for Chinese drug regulatory to prepare the Chinese comparator product directories of generic medicinal products.

Teaching and practice of pharmaceutical comprehensive study in China

Chao Wang, Xu Wang, Guoying Zhao, Guiling Wang, Jianguo Zhang, Xin Hu, Min Ye, Ping Xu

2019, 28(3): 209-215. DOI: 10.5246/jcps.2019.03.021

Asbtract ( 245 )

HTML ( 5)

PDF (1229KB) ( 126 )

References | Related Articles | Metrics

Pharmaceutical comprehensive study (PCS) is a new system of experimental teaching in China, which integrates multidisciplinary pharmaceutical knowledge and covers the basic process of new drug discovery. To explore the feasibility of this experiment teaching system and mode, we developed PCS as an elective course. The PCS is designed with two sections: pharmaceutical comprehensive design (PCD) and pharmaceutical comprehensive experiment (PCE). The PCD section includes literature review, comprehensive project design and oral examination. PCE can be divided into four parts: synthesis, quantitative determination, pharmacodynamic evaluation, and formulation and quality determination. Course grade was determined by experimental performance, written report, literature review, new project design and oral examination. The learning interest, experimental ability, theoretical level and literature retrieval ability, team spirit and interpersonal skills have been all significantly improved among students taking this course. A survey was administered at the end of the semester to the enrolled students. The responses were reported as percentages, and the feedback was positive. The course was highly recommended by the teaching inspection committee. This new course plays an important role in developing students’ creativity and comprehensive ability. It could help students understand the focus and features of every secondary discipline, as well as establish scientific and reasonable knowledge system. Most students can better understand the process of drug research after this course.

Innovative progress “Structural optimization and additional target identification of antisense Oligonucleotide G3139 encapsulated in a neutral cytidinyl-lipid combined with a cationic lipid in vitro and in vivo, Biomaterials” by professor Zhenjun Yang’s group

School of Pharmaceutical Sciences, Peking University Health Science Center

2019, 28(3): 216-216.

Asbtract ( 243 )

HTML ( 3)

PDF (1169KB) ( 125 )

Table of Content