2015 Vol. 33, No. 6
Display Method:
2015, 33(6): 481-485,569.
doi: 10.3969/j.issn.1006-0111.2015.06.001
Abstract:
Objective Anthrax is an anthropozoonosis caused by the bacterium Bacillus anthracis. Bacillus anthracis is an aerobic, spore-forming, rod-shaped bacterium, which infects human through ingestion or inhalation of the spores. The exosporium of spores of Bacillus anthracis contains tetrasaccharide antigen with specific chemical structure, which can be used in preparation of glycoconjugates vaccines, inducing an immune response. This paper reviewed articles in the last decade that reported research advances in chemical synthesis of anthrax tetrasaccharide, presented the methods for synthesis, and compared the advantages and limitations among different methods.
Objective Anthrax is an anthropozoonosis caused by the bacterium Bacillus anthracis. Bacillus anthracis is an aerobic, spore-forming, rod-shaped bacterium, which infects human through ingestion or inhalation of the spores. The exosporium of spores of Bacillus anthracis contains tetrasaccharide antigen with specific chemical structure, which can be used in preparation of glycoconjugates vaccines, inducing an immune response. This paper reviewed articles in the last decade that reported research advances in chemical synthesis of anthrax tetrasaccharide, presented the methods for synthesis, and compared the advantages and limitations among different methods.
2015, 33(6): 486-489.
doi: 10.3969/j.issn.1006-0111.2015.06.002
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The rearrangement reaction of benzyl phenyl ethers(BPE) plays an important role in the organic chemistry and drug synthesis. This paper briefly reviewed the rearrangement reaction and its possible mechanism in various catalytic systems, such as trifluoroacetic acid, phosphotungstic acid, cyclodextrin, molten tin and aluminium bromide.
The rearrangement reaction of benzyl phenyl ethers(BPE) plays an important role in the organic chemistry and drug synthesis. This paper briefly reviewed the rearrangement reaction and its possible mechanism in various catalytic systems, such as trifluoroacetic acid, phosphotungstic acid, cyclodextrin, molten tin and aluminium bromide.
2015, 33(6): 490-493,532.
doi: 10.3969/j.issn.1006-0111.2015.06.003
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Aptamers are single stranded oligonucleotides that have high affinity and specificity towards a wide range of target molecules. Owing to the indispensable advantages, aptamers have wildly prospects and have become a research hotspot in targeted drug delivery system (TDDS). In this article, application advantage and progress of aptamers in TDDS were briefly reviewed, the problems and prospects were also discussed.
Aptamers are single stranded oligonucleotides that have high affinity and specificity towards a wide range of target molecules. Owing to the indispensable advantages, aptamers have wildly prospects and have become a research hotspot in targeted drug delivery system (TDDS). In this article, application advantage and progress of aptamers in TDDS were briefly reviewed, the problems and prospects were also discussed.
2015, 33(6): 494-497,512.
doi: 10.3969/j.issn.1006-0111.2015.06.004
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Tumor diseases have attracted great attention of the society because of the increasing morbidity in recent years. To inhibit the P53-MDM2 interaction has become an important target for design of cancer drug, and a lot of peptide and small molecule inhibitors have been found with various kinds of drug screening and research tools. This paper summarized the recent progress of the peptide and peptidomimetic inhibitors of P53-MDM2 at home and abroad lately.
Tumor diseases have attracted great attention of the society because of the increasing morbidity in recent years. To inhibit the P53-MDM2 interaction has become an important target for design of cancer drug, and a lot of peptide and small molecule inhibitors have been found with various kinds of drug screening and research tools. This paper summarized the recent progress of the peptide and peptidomimetic inhibitors of P53-MDM2 at home and abroad lately.
2015, 33(6): 498-501.
doi: 10.3969/j.issn.1006-0111.2015.06.005
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In the recent years, siRNA has been widely used as effector molecule in the field of gene therapy for cancer. In order to achieve ideal treatment effect, the key factor is to find safe, efficient, stable and controllable gene vectors. The commonly used vectors include viral and non-viral vectors. The non-viral gene vector has superiority of low toxicity, bare immunogenicity, simple to manufacture and high capacity which have been taken as the highlight of the research of carrier of gene drugs. Based on the study of the previous researchers, this study reviewed the prevalence study of the former carriers in the delivery system of siRNA from the point of pharmaceutics.
In the recent years, siRNA has been widely used as effector molecule in the field of gene therapy for cancer. In order to achieve ideal treatment effect, the key factor is to find safe, efficient, stable and controllable gene vectors. The commonly used vectors include viral and non-viral vectors. The non-viral gene vector has superiority of low toxicity, bare immunogenicity, simple to manufacture and high capacity which have been taken as the highlight of the research of carrier of gene drugs. Based on the study of the previous researchers, this study reviewed the prevalence study of the former carriers in the delivery system of siRNA from the point of pharmaceutics.
2015, 33(6): 502-504,517.
doi: 10.3969/j.issn.1006-0111.2015.06.006
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Objective To discuss the antitumor effect of snake venom toxins and its application in medical field. Methods To review the research progress of composition, the antitumor effect and mechanism of snake venom toxins. Results It was demonstrated that the snake venom toxins can stop various tumor cells from growing, and have the functions of killing the tumor cells, inducing cell death, and inhibition of angiogenesis. Conclusion It is an important direction in antitumor drug research and development to deeply research the composition and the mechanisms of action of the snake venom toxins.
Objective To discuss the antitumor effect of snake venom toxins and its application in medical field. Methods To review the research progress of composition, the antitumor effect and mechanism of snake venom toxins. Results It was demonstrated that the snake venom toxins can stop various tumor cells from growing, and have the functions of killing the tumor cells, inducing cell death, and inhibition of angiogenesis. Conclusion It is an important direction in antitumor drug research and development to deeply research the composition and the mechanisms of action of the snake venom toxins.
2015, 33(6): 505-507,543.
doi: 10.3969/j.issn.1006-0111.2015.06.007
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Quinolones are widely used due to the wide antimicrobial spectrum and strong activity. The common adverse reactions of quinolones include gastrointestinal disturbances, central nervous system reaction, skin reaction, etc. These adverse reactions are mild in severity and self-healing. Since some agents were withdrawn from the market due to severe adverse effects, we should pay more attention to quinolones. Both internal and abroad literatures were reviewed, the adverse effects, the high risk factors of the adverse effects and the application in special population were summarized to provide reference for rational clinical drug use.
Quinolones are widely used due to the wide antimicrobial spectrum and strong activity. The common adverse reactions of quinolones include gastrointestinal disturbances, central nervous system reaction, skin reaction, etc. These adverse reactions are mild in severity and self-healing. Since some agents were withdrawn from the market due to severe adverse effects, we should pay more attention to quinolones. Both internal and abroad literatures were reviewed, the adverse effects, the high risk factors of the adverse effects and the application in special population were summarized to provide reference for rational clinical drug use.
2015, 33(6): 508-512.
doi: 10.3969/j.issn.1006-0111.2015.06.008
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Drug metabolism and drug-drug interactions were associated with the single nucleotide polymorphisms of CYP. The relationship between CYP2C19 polymorphisms and metabolism as well as interactions of proton pump inhibitors, voriconazole and clopidogrel were reviewed to provide evidence for personalized medication.
Drug metabolism and drug-drug interactions were associated with the single nucleotide polymorphisms of CYP. The relationship between CYP2C19 polymorphisms and metabolism as well as interactions of proton pump inhibitors, voriconazole and clopidogrel were reviewed to provide evidence for personalized medication.
2015, 33(6): 513-517.
doi: 10.3969/j.issn.1006-0111.2015.06.009
Abstract:
Objective To study the influence on common logarithm of partition-coefficient (log P) value of insoluble drugs on nano-lipid emulsion properties, including drug-loading amount, in vitro release, and phase distribution etc. Methods 6 insoluble drugs, nimodipine (NIM), docetaxel (DTX), curcumin (CUR), paclitaxel (PTX), teniposide (TEN), silybin (SLB), were selected as the model drugs, to investigate the relationship between log P value and nano-lipid emulsion of the dissolubility in PEG400, the amount of drug-loading, particle diameter, Zeta potential, in vitro release, and phase distribution respectively. Results With the increase of log P value, drug solubility in PEG400 first increased and then decreased, drug-loading in nano-lipid emulsion increased, release rate in vitro of drug slowed down, drug distribution in oil phase increased while in emulsion layer decreased. Log P value has no correlation with particle diameter and Zeta potential. Conclusion The properties of drug-loading nano-lipid emulsion can be preliminarily judged by log P values and the solubility in PEG400 of drugs.
Objective To study the influence on common logarithm of partition-coefficient (log P) value of insoluble drugs on nano-lipid emulsion properties, including drug-loading amount, in vitro release, and phase distribution etc. Methods 6 insoluble drugs, nimodipine (NIM), docetaxel (DTX), curcumin (CUR), paclitaxel (PTX), teniposide (TEN), silybin (SLB), were selected as the model drugs, to investigate the relationship between log P value and nano-lipid emulsion of the dissolubility in PEG400, the amount of drug-loading, particle diameter, Zeta potential, in vitro release, and phase distribution respectively. Results With the increase of log P value, drug solubility in PEG400 first increased and then decreased, drug-loading in nano-lipid emulsion increased, release rate in vitro of drug slowed down, drug distribution in oil phase increased while in emulsion layer decreased. Log P value has no correlation with particle diameter and Zeta potential. Conclusion The properties of drug-loading nano-lipid emulsion can be preliminarily judged by log P values and the solubility in PEG400 of drugs.
2015, 33(6): 518-521,575.
doi: 10.3969/j.issn.1006-0111.2015.06.010
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Objective To observe the dynamic characteristics of protein kinase, casein kinase II α (CK2α), expression during hepatic fibrogenesis in rats;and the effects of a matrine derivative, 13-methylamino-18-thione-matrine (MASM), on CK2α expression when it is used for anti-fibrotic treatment. Methods Hepatic fibrosis model was established in SD rats by dimethylnitrosamine (DMN) injection or by bile duct ligation (BDL). The established fibrotic rats were given 50 mg/kg MASM or saline as a control by gavage for three weeks. The level of hepatic fibrosis was evaluated by histopathology examination using hematoxylin-eosin staining, and using the sirius red and Masson's trichrome staining for collagen determination in fibrosis. The expressions of CK2α and α-smooth muscle actin (α-SMA) in hepatic tissues were detected by immunohistochemisry. Results CK2α is mainly expressed in the stellate cells of fibrotic livers induced by DMN or BDL comparing the control group. Along with the development of hepatic fibrosis as evidenced by α-SMA expression, increased CK2α-positive cells in liver were detected while injecting DMN in the rats for one to four weeks. MASM treatment significantly inhibited the hepatic fibrosis and suppressed the expression of CK2α comparing the model group. Conclusion The expression level of CK2α, and hepatic fibrosis formation are positively correlated. The matrine derivative, MASM, can significantly inhibit hepatic fibrosis and suppress the CK2α expression. These Results suggest CK2α may be a potential target for hepatic fibrosis therapy.
Objective To observe the dynamic characteristics of protein kinase, casein kinase II α (CK2α), expression during hepatic fibrogenesis in rats;and the effects of a matrine derivative, 13-methylamino-18-thione-matrine (MASM), on CK2α expression when it is used for anti-fibrotic treatment. Methods Hepatic fibrosis model was established in SD rats by dimethylnitrosamine (DMN) injection or by bile duct ligation (BDL). The established fibrotic rats were given 50 mg/kg MASM or saline as a control by gavage for three weeks. The level of hepatic fibrosis was evaluated by histopathology examination using hematoxylin-eosin staining, and using the sirius red and Masson's trichrome staining for collagen determination in fibrosis. The expressions of CK2α and α-smooth muscle actin (α-SMA) in hepatic tissues were detected by immunohistochemisry. Results CK2α is mainly expressed in the stellate cells of fibrotic livers induced by DMN or BDL comparing the control group. Along with the development of hepatic fibrosis as evidenced by α-SMA expression, increased CK2α-positive cells in liver were detected while injecting DMN in the rats for one to four weeks. MASM treatment significantly inhibited the hepatic fibrosis and suppressed the expression of CK2α comparing the model group. Conclusion The expression level of CK2α, and hepatic fibrosis formation are positively correlated. The matrine derivative, MASM, can significantly inhibit hepatic fibrosis and suppress the CK2α expression. These Results suggest CK2α may be a potential target for hepatic fibrosis therapy.
2015, 33(6): 522-524.
doi: 10.3969/j.issn.1006-0111.2015.06.011
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Objective To study the anti-fatigue effect of methylphenidate hydrochloride oral fast dissolving films (MPH-OFDF) and its mechanism. Methods 60 mice were randomly divided into 6 groups as: normal control group (physiological saline), model group (physiological saline), Yiqiyangxue oral liquids positive group (7.00 mg/kg), MPH-OFDF high-dose group (5.20 mg/kg), MPH-OFDF middle-dose group (2.60 mg/kg) and MPH-OFDF low-dose group (1.30 mg/kg). Besides the normal control group,model group and positive group were orally administered, the other groups are administered with the drug once daily sublingually daily for consecutive 15 days. The mice were put in the load-weighted swimming test 30 min after the last oral administration, then the anti-fatigue effect was assessed based on recording exhausting swimming time and detecting the levels of serum lactale dehydrogenase (LDH), creatine kinase (CK), triglycerides (TG) in mice. Results Compared with control group, the middle-dose and the high-dose MPH could prolong the exhausting swimming time (P<0.05,P<0.01) and decrease the activity of LDH and CK significantly (P<0.05,P<0.01);in addition the middle-dose MPH could decrease the content of TG (P<0.05). Conclusion The MPH had marked anti-fatigue effect that may be associated with reduced serum LDH, CK and TG.
Objective To study the anti-fatigue effect of methylphenidate hydrochloride oral fast dissolving films (MPH-OFDF) and its mechanism. Methods 60 mice were randomly divided into 6 groups as: normal control group (physiological saline), model group (physiological saline), Yiqiyangxue oral liquids positive group (7.00 mg/kg), MPH-OFDF high-dose group (5.20 mg/kg), MPH-OFDF middle-dose group (2.60 mg/kg) and MPH-OFDF low-dose group (1.30 mg/kg). Besides the normal control group,model group and positive group were orally administered, the other groups are administered with the drug once daily sublingually daily for consecutive 15 days. The mice were put in the load-weighted swimming test 30 min after the last oral administration, then the anti-fatigue effect was assessed based on recording exhausting swimming time and detecting the levels of serum lactale dehydrogenase (LDH), creatine kinase (CK), triglycerides (TG) in mice. Results Compared with control group, the middle-dose and the high-dose MPH could prolong the exhausting swimming time (P<0.05,P<0.01) and decrease the activity of LDH and CK significantly (P<0.05,P<0.01);in addition the middle-dose MPH could decrease the content of TG (P<0.05). Conclusion The MPH had marked anti-fatigue effect that may be associated with reduced serum LDH, CK and TG.
2015, 33(6): 525-528,535.
doi: 10.3969/j.issn.1006-0111.2015.06.012
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Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia. Methods Novel Danshensu derivatives were synthesized chiefly via esterification,methoxy phenol hydroxyl protection,nitration and amine solution reaction. All the target compounds were evaluated their biological effects on anti-myocardial ischemia with H9c2 cells in vitro. Results 15 compounds were synthesized and further confirmed by 1H NMR and MS. Pharmacological studies showed that few synthetic derivatives at 5 μmol/L performed a higher biological effect than Danshensu. Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done.
Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia. Methods Novel Danshensu derivatives were synthesized chiefly via esterification,methoxy phenol hydroxyl protection,nitration and amine solution reaction. All the target compounds were evaluated their biological effects on anti-myocardial ischemia with H9c2 cells in vitro. Results 15 compounds were synthesized and further confirmed by 1H NMR and MS. Pharmacological studies showed that few synthetic derivatives at 5 μmol/L performed a higher biological effect than Danshensu. Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done.
2015, 33(6): 529-532.
doi: 10.3969/j.issn.1006-0111.2015.06.013
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Objective To optimize the synthesis route of substituted quinazolinone and investigate the influence of temperature and time in the synthesis of key intermediates. Methods A parallel test was carried out to compare temperature, time and the ester bond ammonolysis of condensing agent, including the total analysis of experimental result. And orthogonal experimental design was used and the influence of temperature and time on the yield were investigated. Results and Conclusion The structure of the compound was confirmed by 1H NMR, MS and 13C NMR. When the reaction temperature was 30 ℃, the reaction time was 24 h with the condensing agent (DCC) and the reactant ratio of 1.5:1, the yield of ester bond ammonolysis was higher. The optimal preparation procedure of quinazolinone compounds was more available for industrial production. In vitro antifungal activity test Results showed that the lead compounds measured on five clinical pathogenic fungi have the potential antifungal activity, and are worth for further study.
Objective To optimize the synthesis route of substituted quinazolinone and investigate the influence of temperature and time in the synthesis of key intermediates. Methods A parallel test was carried out to compare temperature, time and the ester bond ammonolysis of condensing agent, including the total analysis of experimental result. And orthogonal experimental design was used and the influence of temperature and time on the yield were investigated. Results and Conclusion The structure of the compound was confirmed by 1H NMR, MS and 13C NMR. When the reaction temperature was 30 ℃, the reaction time was 24 h with the condensing agent (DCC) and the reactant ratio of 1.5:1, the yield of ester bond ammonolysis was higher. The optimal preparation procedure of quinazolinone compounds was more available for industrial production. In vitro antifungal activity test Results showed that the lead compounds measured on five clinical pathogenic fungi have the potential antifungal activity, and are worth for further study.
2015, 33(6): 533-535.
doi: 10.3969/j.issn.1006-0111.2015.06.014
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Objective To analyze the chemical components of the liposoluble constituent of Holotrichia diomphalia larvae. Methods Essential liposoluble compounds were extracted from H.diomphalia through ethylacetate. GC-MS analysis was used to identify its main components. Results 33 peaks were separated and 33 compounds were identified from ethylacetate-extracted H.diomphalia. The main compounds were pentadecylic acid, Z-11-Hexadecenoic acid, hexadecanoic acid, heptadecanoic acid, oleic acid and octadecanoic acid. Conclusion This work will contribute to the study of medicinal animals and confirmation of active compounds in H.diomphalia.
Objective To analyze the chemical components of the liposoluble constituent of Holotrichia diomphalia larvae. Methods Essential liposoluble compounds were extracted from H.diomphalia through ethylacetate. GC-MS analysis was used to identify its main components. Results 33 peaks were separated and 33 compounds were identified from ethylacetate-extracted H.diomphalia. The main compounds were pentadecylic acid, Z-11-Hexadecenoic acid, hexadecanoic acid, heptadecanoic acid, oleic acid and octadecanoic acid. Conclusion This work will contribute to the study of medicinal animals and confirmation of active compounds in H.diomphalia.
2015, 33(6): 536-538.
doi: 10.3969/j.issn.1006-0111.2015.06.015
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Objective To investigate the application of microemulsion thin layer chromatography (TLC) for separation and identification of various active components in Xinnaomaitong capsule. Methods The all-grass of Bluecalyx japanese rabodosia, root of Pueraria lobata, root and rhizome of Salvia miltiorrhiza, rhizome of Ligusticum chuanxiong in Xinnaomaitong capsule were separated and identified simultaneously with the polyamide film as stationary phase and the microemulsion as mobile phases. Different factors, such as the sodium dodecyl sulfate (SDS), oil phase and water phase which effect on the separation of the components were evaluated. Results The all-grass of Bluecalyx japanese rabodosia, root of Pueraria lobata, root and rhizome of Salvia miltiorrhiza, rhizome of Ligusticum chuanxiong in Xinnaomaitong capsule were separated and identified simultaneously with mobile phase of microemulsion:formic acid:acetone (5:1:1). The constituent of microemulsion was SDS:butyl alcohol:n-Heptane:water = 6.7:15.8:2.5:75.0 (g/g). The spots were clear, the negative control was no interference, and it showed an ideal separation. Conclusion Microemulsion TLC is simple, accurate, and reproducible. It can identify a variety of active components in traditional Chinese medicine simultaneously.
Objective To investigate the application of microemulsion thin layer chromatography (TLC) for separation and identification of various active components in Xinnaomaitong capsule. Methods The all-grass of Bluecalyx japanese rabodosia, root of Pueraria lobata, root and rhizome of Salvia miltiorrhiza, rhizome of Ligusticum chuanxiong in Xinnaomaitong capsule were separated and identified simultaneously with the polyamide film as stationary phase and the microemulsion as mobile phases. Different factors, such as the sodium dodecyl sulfate (SDS), oil phase and water phase which effect on the separation of the components were evaluated. Results The all-grass of Bluecalyx japanese rabodosia, root of Pueraria lobata, root and rhizome of Salvia miltiorrhiza, rhizome of Ligusticum chuanxiong in Xinnaomaitong capsule were separated and identified simultaneously with mobile phase of microemulsion:formic acid:acetone (5:1:1). The constituent of microemulsion was SDS:butyl alcohol:n-Heptane:water = 6.7:15.8:2.5:75.0 (g/g). The spots were clear, the negative control was no interference, and it showed an ideal separation. Conclusion Microemulsion TLC is simple, accurate, and reproducible. It can identify a variety of active components in traditional Chinese medicine simultaneously.
2015, 33(6): 539-543.
doi: 10.3969/j.issn.1006-0111.2015.06.016
Abstract:
Objective To construct a gene delivery carrier with aptamer-polyethylene glycol-dendrimer-polyamidoamine (APT-PEG-PAMAM), forming nanoparticles to specifically target prostate cancer cell lines, carrying prostate cancer cell proliferative suppressor microRNA: miRNA-34a. We investigated the transfection efficiency of this gene delivery system as well as functionally studied its inhibitory effect on prostate cancer (PCa) cell proliferation. Methods The construction of APT-PEG-PAMAM gene carrier was identified and confirmed by nuclear magnetic resonance (NMR). The nano-complex sizes and zeta potential of APT-PEG-PAMAM gene carrier complexes were measured by zeta sizer. The efficiency of gene transfection of APT-PEG-PAMAM / miRNA nano-complexes were investigated by measuring the expression miRNA-34a in prostate cancer cells (PC3 and LNCaP);the PCa specific cell proliferation inhibition of APT-PEG-PAMAM / miRNA-34a nano-complexes were investigated by measuring CCK-8 cell proliferation inhibition experiments by comparing with APT-PEG-PAMAM and APT-PEG-PAMAM / miRNA-34a nano-complexes. Results NMR Results demonstrated that APT-PEG-PAMAM / miRNA-34a nano-complexes were successfully synthesized by structural identification. Qualitative and quantitative transfection efficiency experiments data show that the cellular uptake of vectors were concentration-dependent, after the APT further modified it significantly and increased the LNCaP cell transfection efficiency and specificity of PCa cells targeting ability. CCK8 cell proliferation assay data indicated that APT-PEG-PAMAM/miRNA-34a has the anti-PCa cells effect. Conclusion APT-PEG-PAMAM/miRNA-34a may prove to see its efficacy for near future in pre-clinical and clinical study on the treatment of PCa.
Objective To construct a gene delivery carrier with aptamer-polyethylene glycol-dendrimer-polyamidoamine (APT-PEG-PAMAM), forming nanoparticles to specifically target prostate cancer cell lines, carrying prostate cancer cell proliferative suppressor microRNA: miRNA-34a. We investigated the transfection efficiency of this gene delivery system as well as functionally studied its inhibitory effect on prostate cancer (PCa) cell proliferation. Methods The construction of APT-PEG-PAMAM gene carrier was identified and confirmed by nuclear magnetic resonance (NMR). The nano-complex sizes and zeta potential of APT-PEG-PAMAM gene carrier complexes were measured by zeta sizer. The efficiency of gene transfection of APT-PEG-PAMAM / miRNA nano-complexes were investigated by measuring the expression miRNA-34a in prostate cancer cells (PC3 and LNCaP);the PCa specific cell proliferation inhibition of APT-PEG-PAMAM / miRNA-34a nano-complexes were investigated by measuring CCK-8 cell proliferation inhibition experiments by comparing with APT-PEG-PAMAM and APT-PEG-PAMAM / miRNA-34a nano-complexes. Results NMR Results demonstrated that APT-PEG-PAMAM / miRNA-34a nano-complexes were successfully synthesized by structural identification. Qualitative and quantitative transfection efficiency experiments data show that the cellular uptake of vectors were concentration-dependent, after the APT further modified it significantly and increased the LNCaP cell transfection efficiency and specificity of PCa cells targeting ability. CCK8 cell proliferation assay data indicated that APT-PEG-PAMAM/miRNA-34a has the anti-PCa cells effect. Conclusion APT-PEG-PAMAM/miRNA-34a may prove to see its efficacy for near future in pre-clinical and clinical study on the treatment of PCa.
2015, 33(6): 544-546,565.
doi: 10.3969/j.issn.1006-0111.2015.06.017
Abstract:
Objective To explore and analyze the current status of the postgraduate education of clinical pharmacy in China for improving its level and quality. Methods Comprehensive analysis and evaluation were applied for the education models and trends of clinical pharmacy in China through the internet and related databases. Results 136 articles were analyzed, of which 70 articles (51.47%) involved status analysis, education pattern discussion, in China and international comparison and curriculum optimization. The analysis result indicates that there are two main cultivation models for postgraduate education of clinical pharmacy: professional degree and scientific degree. The educational model is still immature in curriculum and teaching methods. The main problems are: curriculum unreasonable, lack of clinical practice hours, and disconnection of teaching contents and clinical needs. Conclusion The current postgraduate education of clinical pharmacy in China cannot achieve the goal of postgraduate education, it is hard to meet the needs of clinical pharmacy postgraduate talents. We recommended that clinical pharmacy postgraduate training process should focus on linking theory with practice, outstanding mastery medicine as well as clinical pharmacy, optimizing teaching content and methods, and regulating the quality of teaching standards.
Objective To explore and analyze the current status of the postgraduate education of clinical pharmacy in China for improving its level and quality. Methods Comprehensive analysis and evaluation were applied for the education models and trends of clinical pharmacy in China through the internet and related databases. Results 136 articles were analyzed, of which 70 articles (51.47%) involved status analysis, education pattern discussion, in China and international comparison and curriculum optimization. The analysis result indicates that there are two main cultivation models for postgraduate education of clinical pharmacy: professional degree and scientific degree. The educational model is still immature in curriculum and teaching methods. The main problems are: curriculum unreasonable, lack of clinical practice hours, and disconnection of teaching contents and clinical needs. Conclusion The current postgraduate education of clinical pharmacy in China cannot achieve the goal of postgraduate education, it is hard to meet the needs of clinical pharmacy postgraduate talents. We recommended that clinical pharmacy postgraduate training process should focus on linking theory with practice, outstanding mastery medicine as well as clinical pharmacy, optimizing teaching content and methods, and regulating the quality of teaching standards.
2015, 33(6): 547-551.
doi: 10.3969/j.issn.1006-0111.2015.06.018
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Objective To evaluate the implementation of hospital pharmacy distribution for inpatient pharmacy services, with impact on understanding investigation for ward nurse awareness of the drug storage management, and to optimize ward base drug administration. Methods By improving the drug delivery service process in a hospital ward, the statistical base variety and number of the base drugs were counted two years in 2012 and in 2014 respectively;with a questionnaire analysis in ward nurses on base drug awareness and drug management situation. Results After the drug distribution process optimization, time that nurses receive medicines from pharmacies decreased from 90 min to 20 min;base ward drugs from 2012 of 16 categories, 237 varieties, down to 2014 of 13 categories, 209 species. Questionnaire survey Results showed that the ward nurse awareness of drug administration should be improved further. Conclusion By optimizing the drug distribution process, reduced storage ward medicines can increase the time nurses for patients and services as well as reduce the risk faced by the ward base drug administration.
Objective To evaluate the implementation of hospital pharmacy distribution for inpatient pharmacy services, with impact on understanding investigation for ward nurse awareness of the drug storage management, and to optimize ward base drug administration. Methods By improving the drug delivery service process in a hospital ward, the statistical base variety and number of the base drugs were counted two years in 2012 and in 2014 respectively;with a questionnaire analysis in ward nurses on base drug awareness and drug management situation. Results After the drug distribution process optimization, time that nurses receive medicines from pharmacies decreased from 90 min to 20 min;base ward drugs from 2012 of 16 categories, 237 varieties, down to 2014 of 13 categories, 209 species. Questionnaire survey Results showed that the ward nurse awareness of drug administration should be improved further. Conclusion By optimizing the drug distribution process, reduced storage ward medicines can increase the time nurses for patients and services as well as reduce the risk faced by the ward base drug administration.
Establishment and validation of sterility test of levofloxacin lactate and sodium chloride injection
2015, 33(6): 552-554.
doi: 10.3969/j.issn.1006-0111.2015.06.019
Abstract:
Objective To establish a sterility test of levofloxacin lactate and sodium chloride injection. Methods The test was carried out by thin-membrane filtration method with different volume of flushing liquid or adding neutralization into culture medium according to the Appendix of Chinese Pharmacopoeia (2010 edition). Results When 0.1% peptone water was used as flushing liquid, Staphylococcus aureus gave no evidence of growth until the amount of flushing liquid reached 700 ml per tube (100 ml each time). At the same time, all of the six positive control bacteria grew normally when there was 300 ml flushing liquid in each tube with neutralization as culture medium. Conclusion This method was simple and convenient, suggesting that it was suitable for the sterility test of levofloxacin lactate and sodium chloride injection.
Objective To establish a sterility test of levofloxacin lactate and sodium chloride injection. Methods The test was carried out by thin-membrane filtration method with different volume of flushing liquid or adding neutralization into culture medium according to the Appendix of Chinese Pharmacopoeia (2010 edition). Results When 0.1% peptone water was used as flushing liquid, Staphylococcus aureus gave no evidence of growth until the amount of flushing liquid reached 700 ml per tube (100 ml each time). At the same time, all of the six positive control bacteria grew normally when there was 300 ml flushing liquid in each tube with neutralization as culture medium. Conclusion This method was simple and convenient, suggesting that it was suitable for the sterility test of levofloxacin lactate and sodium chloride injection.
2015, 33(6): 555-556,560.
doi: 10.3969/j.issn.1006-0111.2015.06.020
Abstract:
Objective To develop a method for determination of the rosmarinic acid in Xiaokang capsules. Methods An HPLC method was developed. The determination was performed on Agilent C18 column at 30℃ with a mobile phase composed of methanol: 0.5% formic acid (50:50) run at a flow rate of 1.0 ml/min. The detection wavelength was set at 330 nm and the injection volume was 10 μl. Results The linear range of rosmarinic acid concentrations was 2.88 to 20.1 μg/ml (r=0.999 8). The average recovery was 99.5% (RSD=0.40%,r=9). Conclusion An assay for the determination of the rosmarinic acid in Xiaokang capsule that is simple, rapid, accurate and reliable has been developed.
Objective To develop a method for determination of the rosmarinic acid in Xiaokang capsules. Methods An HPLC method was developed. The determination was performed on Agilent C18 column at 30℃ with a mobile phase composed of methanol: 0.5% formic acid (50:50) run at a flow rate of 1.0 ml/min. The detection wavelength was set at 330 nm and the injection volume was 10 μl. Results The linear range of rosmarinic acid concentrations was 2.88 to 20.1 μg/ml (r=0.999 8). The average recovery was 99.5% (RSD=0.40%,r=9). Conclusion An assay for the determination of the rosmarinic acid in Xiaokang capsule that is simple, rapid, accurate and reliable has been developed.
2015, 33(6): 557-560.
doi: 10.3969/j.issn.1006-0111.2015.06.021
Abstract:
S-1 is the third generation of fluorouracil derivative anti-cancer agent with small side effects, efficacy, and drug delivery is convenient.In a large number of clinical trials and continuous clinical application, it showed the good effect for the treatment of advanced breast cancer, which was expected to become the first-line chemotherapy drug for breast cancer treatment in the future.
S-1 is the third generation of fluorouracil derivative anti-cancer agent with small side effects, efficacy, and drug delivery is convenient.In a large number of clinical trials and continuous clinical application, it showed the good effect for the treatment of advanced breast cancer, which was expected to become the first-line chemotherapy drug for breast cancer treatment in the future.
2015, 33(6): 561-565.
doi: 10.3969/j.issn.1006-0111.2015.06.022
Abstract:
Chronic hepatitis B is a worldwide infectious diseases caused by hepatitis B virus (HBV). HBV infection is an important reason for liver cirrhosis and liver cancer in our country. Currently, the interferon and nucleoside analogs antiviral drugs (nucleotides) is widely used in clinical practice. These drugs inhibit the replication of the virus and disease development to a certain extent, but not fundamentally eliminate the virus. Various therapeutic vaccines have also made certain curative effect in anti HBV, but the effect is not perfect clinically. At present, many research Results demonstrate that biological immunotherapy can successfully eliminate HBV virus in the body, therefore it has brought a new hope for the treatment of hepatitis B.
Chronic hepatitis B is a worldwide infectious diseases caused by hepatitis B virus (HBV). HBV infection is an important reason for liver cirrhosis and liver cancer in our country. Currently, the interferon and nucleoside analogs antiviral drugs (nucleotides) is widely used in clinical practice. These drugs inhibit the replication of the virus and disease development to a certain extent, but not fundamentally eliminate the virus. Various therapeutic vaccines have also made certain curative effect in anti HBV, but the effect is not perfect clinically. At present, many research Results demonstrate that biological immunotherapy can successfully eliminate HBV virus in the body, therefore it has brought a new hope for the treatment of hepatitis B.
2015, 33(6): 566-569.
doi: 10.3969/j.issn.1006-0111.2015.06.023
Abstract:
Objective To explore the role of clinical pharmacists in analyzing and dealing with abnormal INR value fluctuations caused by the drug interaction of warfarin and amiodarone in a post heart valve replacement patient. Methods By comparing interactions between warfarin and other drugs, we investigated the drugs the patient was using, found the cause of unusual INR value fluctuations, and regulated warfarin dosage in time. After that, we intensified the monitoring of coagulation function and offered detailed pharmaceutical care to the patient. In addition, we studied the possible reasons for the phenomenon from the following aspects such as the drug action mechanisms of warfarin and amiodarone;the interaction mechanisms of the two drugs;the correlation of anticoagulation effects of warfarin, the dosage and concentration of combined use of these two drugs. Results The reason for unusal INR value fluctuations was identified as the drug interaction between warfarin and amiodarone. Amiodarone can enhance the anticoagulant effects of warfarin, increase the risk of bleeding. By stoping warfarin for 3 days, INR value was restored to the target range. Then we continued the anticoagulant therapy, and the condition of the patient was controlled steadily, and he was discharged smoothly. Conclusion Clinical pharmacists can help doctors find out problems related to drug therapy in time by providing effective pharmaceutical care to patients, so doctors may adjust the treatment in time. When using the drugs interacted with warfarin, we have to consider the those drug effects on anticoagulant therapy. In order to adjust regimens in time, we must understand the pharmacology and pharmacokinetics of the drugs we used at the same time;as well, we must intensify monitoring. Therefore, we can improve the safety and rationality of clinical medication, and also can provide better pharmaceutical care for patients.
Objective To explore the role of clinical pharmacists in analyzing and dealing with abnormal INR value fluctuations caused by the drug interaction of warfarin and amiodarone in a post heart valve replacement patient. Methods By comparing interactions between warfarin and other drugs, we investigated the drugs the patient was using, found the cause of unusual INR value fluctuations, and regulated warfarin dosage in time. After that, we intensified the monitoring of coagulation function and offered detailed pharmaceutical care to the patient. In addition, we studied the possible reasons for the phenomenon from the following aspects such as the drug action mechanisms of warfarin and amiodarone;the interaction mechanisms of the two drugs;the correlation of anticoagulation effects of warfarin, the dosage and concentration of combined use of these two drugs. Results The reason for unusal INR value fluctuations was identified as the drug interaction between warfarin and amiodarone. Amiodarone can enhance the anticoagulant effects of warfarin, increase the risk of bleeding. By stoping warfarin for 3 days, INR value was restored to the target range. Then we continued the anticoagulant therapy, and the condition of the patient was controlled steadily, and he was discharged smoothly. Conclusion Clinical pharmacists can help doctors find out problems related to drug therapy in time by providing effective pharmaceutical care to patients, so doctors may adjust the treatment in time. When using the drugs interacted with warfarin, we have to consider the those drug effects on anticoagulant therapy. In order to adjust regimens in time, we must understand the pharmacology and pharmacokinetics of the drugs we used at the same time;as well, we must intensify monitoring. Therefore, we can improve the safety and rationality of clinical medication, and also can provide better pharmaceutical care for patients.
2015, 33(6): 570-572.
doi: 10.3969/j.issn.1006-0111.2015.06.024
Abstract:
Objective To investigate the practices and experience in the organization and implementation process of practical training drill for medical supply support. Methods To review and comment on the overall design ideas, specific steps, practical effect and experience of medical supply support in practical training drill. Results Through six years of exploration and practice, we established a training method of implementation of practical training drill for medical supply support. Conclusion It is right and effective in the organization and implementation of practical training drill for medical supply support. It is necessary to continue improving the mode of organization and implementation with combination of practical teaching and research.
Objective To investigate the practices and experience in the organization and implementation process of practical training drill for medical supply support. Methods To review and comment on the overall design ideas, specific steps, practical effect and experience of medical supply support in practical training drill. Results Through six years of exploration and practice, we established a training method of implementation of practical training drill for medical supply support. Conclusion It is right and effective in the organization and implementation of practical training drill for medical supply support. It is necessary to continue improving the mode of organization and implementation with combination of practical teaching and research.
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