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??OBJECTIVE To explore the determination of pethidine hydrochloride injection by using Raman spectroscopy to realize in-site non-invasive inspection. METHODS CLS algorithm was used to eliminate the interference of the ampoule, correlation coefficient was used for identification, and PLS algorithm was used to establish the quantitative model. Moreover, the transfer performance of the models was investigated when used on different portable Raman instruments. RESULTS Nineteen samples of four different batches were used to verify the method. The RESULTS showed a good coincidence with reference RESULTS on both identification and quantification, and the relative deviation from HPLC method was within 5%. Meanwhile, the Raman method showed good accuracy and repeatability with relative deviation of mean and RSD value within 1% for samples from the same batch. The differences between instruments were controlled by the key index, and quantitative analysisRESULTS of 51 samples measured on three instruments all fell in the range of 90% to 110%, among which 96% fell in a more narrow range of 95% to 105%. CONCLUSION The Raman method established in this study could be used for the in-situ non-invasive determination of pethidine hydrochloride injection.     

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??OBJECTIVE To investigate the impacts of particle size and preferred orientation on relative peak intensity, number of peaks and order of peak intensity in powder X-ray diffraction (PXRD) analysis of organic and inorganic pharmaceutical crystalline materials and evaluate the phase identification methods in various pharmaceutical compendiums.METHODS The PXRD patterns of organic and inorganic materials with different particle sizes obtained by sieving or grinding were acquired and the number of diffraction peaks, peak position and intensity of diffraction peaks were compared across different samples. RESULTS Due to preferred orientation effects, the diffraction patterns of samples with different particle sizes were apparently different, including the number of peaks, relative peak intensity and the order of the peak intensity. CONCLUSION Scientists may get different CONCLUSION s from the RESULTS of same tests performed according to the related guiding principles of current Chinese Pharmacopeia and USP39, EP8.0, JP16 ???? pharmacopoeia for identifying the crystalline forms.The phase identification by PXRD method in current Chinese Pharmacopeia neglects the effects of preferred orientation on diffraction peaks and relative peak intensity. This guideline needs to be updated to better reflect the scientific observation in industry and align with other well accepted compendiums such as USP, EP and JP.     

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??OBJECTIVE To study the chemical constituents of Erigeron annuus (L.) Pers.. METHODS The compounds were isolated and purified by Diaion HP-20, Toyopearl HW-40, Sephadex LH-20, MCI Gel CHP-20, silica gel column chromatography, and preparative HPLC, and their structures were elucidated on the basis of spectral data and physiochemical properties. RESULTS Twenty compounds were elucidated as vanillic acid(1), ferulic acid(2), 4-hydroxyacetophenone(3), dihydroconiferylalcohol(4), loliolide(5), 4-hydroxy-3-methoxyphenylprop-8-ene 4-O-??-D-xylopyraosyl-(1??6)-??-D-glucopyranoside(6), 1H-indole-3-carbaldehyde(7), 5,7-dihydroxychromone(8), pyromeconic acid(9), erigeside D(10), methyl syringate 4-O-??-D-glucopyranoside(11),(7S,8R)-urolignoside(12), homoeriodictyol(13), pinobaksin(14), chrysin(15), hispidulin(16), chryseriol(17), cyclomorusin(18), cirsimaritin(19), and naringenin(20), respectively. CONCLUSION Compounds 1-8 and 11-19 is isolated from this plant for the first time.     

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??OBJECTIVE To investigate the Polygonum capitatum's influences on the related indicators in db/db mice which is the obesity model of type 2 diabetes mellitus. METHODS Randomly dividing the mice into 5 groups:model group, rosiglitazone hydrochloride group, low-, moderate- and high-dose groups of Polygonum capitatum (5, 10, 20 g??kg^-1), make the db/m mice as blank control. Give the medicine for four weeks. The body weight, blood sugar were determined every week.At the end of fourth week, measuring the glucose tolerance and INS, IL-6 in serum. After all the mice were killed, testing the cholesterol and triglyceride in liver and skeletal muscle and then collecting the liver tissue for HE staining. At the meantime, the expression level of AMPK and GLUT4 in liver were detected by Q-PCR. RESULTS Polygonum capitatum can improve the body weight, blood sugar and glucose tolerance of db/db mice as well as the content of INS and IL-6 in serum, but increase the content of SOD and decrease the content of MDA in mice, furthermore, the cholesterol and triglyceride levels in the liver and skeletal muscle were also declined. HE staining showed that Polygonum capitatum could reduce the number of vacuoles in the liver of db/db mice, and make its shape more complete and ordered. What's more, raising the expression of AMPK and GLUT4 in the liver. CONCLUSION Polygonum capitatum can improve the condition of insulin resistance state, alleviate inflammation and advance the ability of db/db mice, which can also reduce the number of vacuoles in liver, and relieve the tissue lipid metabolic disorder. Meanwhile, Polygonum capitatum can promote the uptake of glucose in liver tissues, which is resulted from up-regulation of expression in hepatic AMPK and GLUT4 gene.     

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??OBJECTIVE To synthesize the impurity A of sitagliptin which is a highly selective DPP-4 inhibitor used for treatment of type 2 diabetes. METHODS 1-{3-Trifluoromethyl-5,6-dihydro-1,2,4-triazo[4,3-a]piperazin-7(8H)-yl}-4-(2,4,5-trifluorophenyl)butane-1,3-dione was prepared from 2,4,5-triflurophenylacetic acid, meldrum's acid and 3-trifluromethyl-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazine hydrochloride with one-pot reaction, followed by reduction with sodium borohydride to yield the impurity A of sitagliptin. RESULTS The structure of the impurity A of sitagliptin was characterized by IR, MS, and ¹H-NMR. CONCLUSION The established synthetic route of the impurity A in this study has not been reported in the literature, and has the advantages of low-cost, easy operation, mild reaction, and high overall yield.     

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??OBJECTIVE To probe into the operation and management of quality control of chemotherapy in cancer hospital, so as to improve the efficacy and standardization of chemotherapy. METHODS By summarizing management practice of clinical chemotherapy of pharmacist inrapy drugs, and analyzing the pharmacists?? work and problems in cancer hospital, combining with domestic and foreign literature reports of pharmacists in quality control of chemotherapy, the concept and scope of chemothe sting in quality control of chemotherapy were formulated. RESULTS The scope of quality control of chemotherapy should include standardization of all drugs in the process of chemotherapy; pharmacists' work about quality control mainly includes two aspects: the quality control of pharmaceutical affairs management and clinical pharmaceutical care; the barriers of quality control are the lack of clinical knowledge and pharmaceutical guidelines, and the records of patients' chemotherapy.CONCLUSION With the pharmacist participating in clinical chemotherapy, pharmacists have the ability to become the interdisciplinary and multidisciplinary cooperation in tumor chemotherapy of participants, so as to guarantee the specification of the chemotherapy.     

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??Quercetin could affect both the in vivo and in vitro transport of a variety of commonly used drugs by modulating the uptake transporter organic anion transporter polypeptides (OATPs), organic anion transporters (OATs), efflux transporter P-glycoprotein (P-gp), multidrug resistance-related protein (MRP) and breast cancer resistance protein (BCRP), respectively. Quercetin can regulate various drug transporters, thereby affecting other drugs in vivo process.     

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??OBJECTIVE To investigate the contents of oligosaccharides in 37 batches of Morinda officinalis How samples from different habitats and germplasm resources at various ages. METHODS HPLC-ELSD method was used to determine the contents of four oligosaccharides, i.e sucrose, 1-kestose, nystose and 1^F-fructofuranosylnystose in Morinda officinalis How at different ages from different habitats and germplasm resources. The relationships among the several factors were analyzed. RESULTS The samples from Guangdong Province had larger amounts of sucrose, 1-kestose and 1^F-fructofuranosylnystose than those from Fujian, Guangxi and Hainan Provinces. The content of nystose in the samples from Guangdong Province was similar with those from Fujian Province. The contents of sucrose and 1-kestose were the highest in the samples of 2.5 years old, while the contents of nystose and 1^F-fructofuranosylnystose were the highest in the samples of 4 years old. The germplasm resources of small leaf had higher content of oligosaccharides than the large leaf germplasm in Guangdong Province, and different germplasm resources of Morinda officinalis How also had different morphological characteristics. CONCLUSION The contents of four Morinda officinalis How oligosaccharides vary with habitat, germplasm and age. This research may provide references for the quality control of Morinda officinalis How.     

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??OBJECTIVE To identify Dalbergiae Odoriferae Lignum and its adulterants using DNA barcoding. METHODS ITS2 is one of the popular DNA barcoding in the identification of traditional Chinese medicine. In this paper,the ITS2 regions of Dalbergiae Odoriferae Lignum and its adulterants were amplified and sequenced bi-directional.The length and GC content of ITS2 sequence were analyzed through MEGA5.0 software. The genetic distances were computed by kimura 2-parameter (K2P) model. Dalbergiae Odoriferae Lignum and its adulterants have been identified through the species identification system for traditional Chinese medicine and neighbor-joining (NJ) phylogenetic tree. RESULTS The sequence lengths of ITS2 of Dalbergiae Odoriferae Lignum were 216 bp, and the GC content was 68.5%. The minimum K2P interspecific genetic distances of Dalbergiae Odoriferae Lignum and its adulterants were 0.009, which was larger than that of the intraspecific genetic distances of Dalbergiae Odoriferae Lignum.The Dalbergiae Odoriferae Lignum and its adulterants can be obviously identified using the Species identification System and NJ phylogenetic trees.CONCLUSION ITS2 Regions as DNA barcode can identify Dalbergiae Odoriferae Lignum and its adulterants accurately.     

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??Topical ocular medication is commonly used for eye diseases treatment.In view of low bioavailability and poor efficacy of traditional ocular preparations,the development of novel ocular drug delivery systems has become a great challenge in pharmaceutics.In recent years, nano preparations have been widely used for ocular drug delivery systems. At present, several nanocarriers, such as polymeric micelles, nanoparticles, nanosuspension, liposomes, emulsion, and dendritic polymers have been developed for ocular drug delivery.There are some other new dosage forms, such as in-situ gelling systems, implants, contact lenses, and microneedles are also under continuous research. The aim of development of these new dosage forms is to improve the drugs' ocular bioavailability and therapeutic effects.In this paper,the development in these areas in recent years are reviewed in order to provide reference for the development of new ocular drug delivery systems.     

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??OBJECTIVE To explore the accumulation rules of the effective constituents in Ophiopogonis Radix to provide theoretical support for its production and quality control. METHODS Ophiopogonis Radix samples in different growth phases were harvested, and the total polysaccharides, total flavones, and total saponins in the sampleswere measured by ultraviolet spectrophotometry. Methylophiopogonanone A, ophiopogonin C, ophiopogonin D, and ophiopogonin D?? were determined by HPLC. RESULTS The contents of total polysaccharides, total flavones, and total saponins in Ophiopogonis Radix were positively correlated with root growth time. The contents of three categories of constituents increased with the prolongation of root growth time, but the accumulative rate was inconsistent in different growth phases, which had a slight decrease after reaching the maximum at the end of March. The accumulation trend of six single components were basically the same to the three categories of constituents. For samples with same harvest time, the content of the main constituents was higher in the samples treated by paclobutrazol than those without paclobutrazol treatment. CONCLUSION The variation trend of the main chemical components in Ophiopogonis Radix is basically the same to that of the root growth. Methylophiopogonanone A and phiopogonin D are the most representative, and they could be taken as evaluation index to guide production and quality control of Ophiopogonis Radix.     

道地药材川麦冬和浙麦冬的生态遗传分化

目的:探讨川麦冬和浙麦冬的生态型差异,为道地药材生物学实质的深入研究提供参考。方法:选择传统道地药材麦冬为模型,收集75份实验样本,通过分子鉴定技术和生态因子分析研究川麦冬和浙麦冬的生态型差异。结果:川麦冬和浙麦冬的psbA-trnH序列在49位点处存在变异,川麦冬为碱基腺嘌呤(A),浙麦冬为碱基鸟嘌呤(G),此为两者序列的差异化特征;生态因子分析显示四川、浙江两大产区呈现不同的地理生态型。其中,浙江产区在年均日照强度、年均降水量、年均相对湿度、最热季平均温度、生长期平均温度等因子上高于四川,而四川产区的最冷季平均温度高于浙江。结论:川麦冬和浙麦冬的基因型和生态因子均存在明显差异。     

基于性状特征的浙产麦冬和川产麦冬的主成分和聚类比较分析

目的比较浙产麦冬Ophiopogonjaponicus和川产麦冬的性状特征,为其快速鉴定提供科学依据。方法实地考察并收集不同产地的浙产麦冬和川产麦冬药材,测量其长度、宽度和颜色等13个性状特征参数,采用Simca14.1和IBM SPSS Statistics26软件进行数据分析。结果浙产麦冬与川产麦冬的种植及采收加工技术有所不同;主成分分析获得了实验室加工样品8个符合变量重要性投影(VIP)值>1的条件性状变量数据,产地加工样品9个符合VIP值>1的条件性状变量数据。聚类分析结果显示,道地主产区的浙产麦冬与川产麦冬在性状上可明显区分,但实验室加工的道地主产区的浙产麦冬与道地非主产区的川产麦冬则有一定的混淆。浙产麦冬外表面颜色深、中柱明显,气味清香,具粘牙性;川产麦冬外表面颜色较浅、中柱不明显,气味淡,无黏牙性。结论浙产麦冬和川产麦冬的性状特征存在显著的差异,其表面颜色、中柱大小、气味和黏性可为作为浙产麦冬和川产麦冬鉴别的依据。     

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??OBJECTIVE To provide a theoretical basis for scientific and rational use of paclobutrazol in the production of Ophiopogonis Radix. METHODS Different concentrations of paclobutrazol were applied to Ophiopogonis Radix plants, and medicinal samples were colleted. The efficacy of Ophiopogonis Radix were comprehensively analyzed from the appearance of the herb and the contents of three kinds of effective components: flavonoids, saponins, and polysaccharides. Residues of paclobutrazol were detected. The effect of paclobutrazol use on the safety of Ophiopogonis Radix was evaluated according to the acceptable daily intake (ADI) of paclobutrazol in the GB2763-2014 and the amount of usage of paclobutrazol required by Chinese Pharmacopoeia. RESULTS Paclobutrazol had no significant effects on the Ophiopogonis Radix appearance; and the contents of polysaccharides and flavonoid were increased in varying degrees, and saponins content were decreased. The daily intake of paclobutrazol was far less than the ADI (0.1 mg??kg^-1?? body weight) when calculated using the maximum residue of paclobutrazol at the usage of 3 kg??acres^-1 and the maximum usage amount of Ophiopogonis Radix in Chinese Pharmacopoeia. CONCLUSION Paclobutrazol can be used within limits according to the actual situation in Ophiopogonis Radix production.     

基于化学组分特征评价不同干燥方法对麦冬品质的影响

目的通过化学组分测定和特征图谱分析,评价不同干燥方式对麦冬品质的影响。方法总皂苷、总黄酮和总多糖量采用紫外分光光度法进行测定,麦冬皂苷D和麦冬甲基黄烷酮A的量采用HPLC法进行测定;特征图谱采用HPLC法建立。结果不同干燥方法对麦冬化学组分量的影响差异显著,变异系数在6.9%~20.8%,其中,阴干、晒干、冷藏干燥和晒半干后烘干对麦冬化学组分破坏程度均较小,远红外干燥和微波干燥对麦冬化学组分破坏最大;麦冬样品有18个HPLC特征峰,聚类分析可将14种干燥方法分为3类,聚为一类的干燥方法干燥条件相近。结论通过化学组分量变化和HPLC图谱特征能够有效地反映干燥方法的差异,可作为麦冬产地干燥方法筛选的技术指标,在麦冬产地加工过程中建议晒干和空气源热泵烘干机烘干相结合应用。     

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??OBJECTIVE To evaluate the feasibility of relay intercropping Ophiopogonis Radix and vegetables by measuring the yield and contents of effective components and fingerprint analysis. METHODS The field capacity when relay intercropping Ophiopogonis Radix and vegetables was evaluated, taking Ophiopogonis Radix monoculture as control. The contents of major compound of Ophiopogonis Radix were measured by ultraviolet spectrophotometry and high performance liquid chromatography, and the HPLC fingerprint of Ophiopogonis Radix was established. RESULTS Relay intercropping vegetables reduced the yield of Ophiopogonis Radix to some extent, but the land equivalent ratios were all more than 1, indicating that it is advantageous to intercrop Ophiopogonis Radix and vegetables.Relay intercropping vegetables did not reduce the contents of chemical constituents in Ophiopogonis Radix significantly. The similarities of all the HPLC fingerprint chromatograms were greater than 0.990. CONCLUSION Relay intercropping Ophiopogonis Radix and vegetables is a feasible pattern to solve the contention for land between Ophiopogonis Radix and vegetables in the main producing areas of Ophiopogonis Radix, and can be applied and generalized.     

生脉注射液中高异黄酮类成分研究

 目的 探讨生脉注射液中高异黄酮类成分物质基础。方法 以麦冬萃取物化学成分研究为基础,采用液相色谱-质谱联用技术对8家生产企业的生脉注射液样品进行化学成分指认。结果 麦冬萃取物中8个主要化学成分中8家生产企业多数共有成分为麦冬黄酮B,麦冬黄烷酮B,麦冬黄烷酮A,甲基麦冬黄烷酮A,甲基麦冬黄烷酮B。结论 建立了生脉注射液中高异黄酮类成分的检查方法,为研究注射剂高异黄酮类成分及统一制法提供实验依据。     

HPLC同时测定麦冬药材中3种黄酮类成分的含量

 目的 测定麦冬药材中甲基麦冬黄烷酮A、甲基麦冬黄烷酮B和6-醛基异麦冬黄烷酮A的含量,为麦冬药材的质量控制提供科学依据。方法 采用Waters Symmetry C₁₈柱(4.6 mm×250 mm, 5 μm),乙腈-0.05%磷酸梯度洗脱,流速为1.0 mL·min-1,检测波长296 nm,柱温30 ℃。结果 甲基麦冬黄烷酮A、甲基麦冬黄烷酮B和6-醛基异麦冬黄烷酮A分别在9.68~96.8、4.96~49.6、4.18~41.8 μg·mL-1内具有良好的线性关系,平均回收率(n=6)分别为100.1% (RSD 1.03%),99.5%（RSD 1.35%）和100.2%（RSD 1.16%）。结论 该方法快速、准确,可用于麦冬药材中甲基麦冬黄烷酮A、甲基麦冬黄烷酮B和6-醛基异麦冬黄烷酮A的含量测定。     

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??OBJECTIVE To establish an HPLC method for simultaneous determination of methylophiopogonone A, methylophiopogonanone A, and methylophiopogonanone B. METHODS Comatex C₁₈ column (4.6 mm??250 mm, 5 ??m)was used for the HPLC analysis. The mobile phase consisted of acetonitrile and water (58??42) and was eluted at the flow rate of 1 mL??min^-1. The column temperature was maitained at 30 ??. The detection wavelength was set at 280 nm. The injection volume was 15.0 ??L. RESULTS The linear regression equations of methylophiopogonone A, methylophiopogonanone A and methylophiopogonanone B were Y=493 321??+31 262(r=0.999 9), Y=605 744??+40 941(r=0.999 9), and Y=586 672??+39 657(r=0.999 9), respectively. The average recovery rates of the three flavones respectively were 100.59%(RSD=1.51%), 99.27%(RSD=1.28%), and 100.04%(RSD=1.33%). CONCLUSION The established method for simultaneous determination of flavone constituents in Ophiopogonis Radix is accurate and sensitive, with good repeatability. It can be applied to the quality evaluation of Ophiopogonis Radix.     

不同产地猫爪草中多糖含量的比较

目的 比较不同产地猫爪草中多糖的含量。方法 采用苯酚-硫酸法。结果 河南信阳、河南驻马店、安徽、浙江、江苏、湖北、山东等地猫爪草中多糖含量分别为:12.65%、12.05%、10.46%、9.78%、8.49 %、8.73%、9.47%。结论 不同产地猫爪草中多糖的含量差异明显,其中以河南产猫爪草中多糖含量最高。