2014 Vol. 32, No. 1
Display Method:
2014, 32(1): 1-4,8.
doi: 10.3969/j.issn.1006-0111.2014.01.001
Abstract:
Objective Amphotericin B (AmB) was a polyene antifungal agent. Because of its lowest resistance rate and broad antibiotic spectrum, AmB was considered as a "gold standard" for the treatment of deep fungal infections. However, the occurrence of toxicity and serious side effects, especially renal toxicity, greatly limited the application of AmB in clinical antifungal therapy. Due to the lack of antifungal with high efficiency and low toxicity, the combination of antifungal agents with different mechanisms of action was a promising research direction. The advantage of the combinations was the course of treatment shortened, drug side effects reduced, the antibacterial spectrum expanded, and drug resistance avoided. The research progress in the combined use of AmB with different types of antifungal compounds were introduced in this article.
Objective Amphotericin B (AmB) was a polyene antifungal agent. Because of its lowest resistance rate and broad antibiotic spectrum, AmB was considered as a "gold standard" for the treatment of deep fungal infections. However, the occurrence of toxicity and serious side effects, especially renal toxicity, greatly limited the application of AmB in clinical antifungal therapy. Due to the lack of antifungal with high efficiency and low toxicity, the combination of antifungal agents with different mechanisms of action was a promising research direction. The advantage of the combinations was the course of treatment shortened, drug side effects reduced, the antibacterial spectrum expanded, and drug resistance avoided. The research progress in the combined use of AmB with different types of antifungal compounds were introduced in this article.
2014, 32(1): 5-8.
doi: 10.3969/j.issn.1006-0111.2014.01.002
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Objective To update the application of Caenorhabditis elegans as a model host of infection in anti-infection research field, and provide references for the further application of C. elegans in the research field. Methods The related literatures at home and abroad in recent years were analyzed, integrated and concluded. Results C. elegans had been widely used to study pathogenesis of microorganisms and to screen anti-infective agents, since the nemades had short life cycle and cost low. Conclusion C. elegans would be promising to be further more widely used to study pathogenesis and anti-infective agents.
Objective To update the application of Caenorhabditis elegans as a model host of infection in anti-infection research field, and provide references for the further application of C. elegans in the research field. Methods The related literatures at home and abroad in recent years were analyzed, integrated and concluded. Results C. elegans had been widely used to study pathogenesis of microorganisms and to screen anti-infective agents, since the nemades had short life cycle and cost low. Conclusion C. elegans would be promising to be further more widely used to study pathogenesis and anti-infective agents.
2014, 32(1): 9-15,34.
doi: 10.3969/j.issn.1006-0111.2014.01.003
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Computer aided drug design had become part of the drug discovery process, greatly improved the speed of drug development compared with traditional drug finding methods. In particular, the de novo drug design method could be used to identify ligands with novel structure for a special target. Through computer simulation, researchers could find new ideas about how to change a compound to improve the drug properties or how to assemble some fragments to generate candidates which be drug-like, synthetically accessible and high affinity for a target. The common software of de novo design included LUDI, MCSS, LigBuilder, SPROUT, SYNOPSIS, BREED, LeapFrog and RACHEL, etc. The methods were fragments link and grow, side chain replacement, parent molecule evolve, template, scaffold hopping and so on. Discovery and development of cancer drugs had been revolutionized over the last decade. De novo drug design methods had already played a significant role in the discovery of some anticancer compounds such as kinesin spindle protein inhibitors, vascular endothelial growth factor inhibitors, cyclophilin A inhibitors, cell division cycle protein CDC25 inhibitors and BRAF inhibitors. The common software and methods of de novo drug design were summarized in this review and their applications in antitumor drug design were discussed.
Computer aided drug design had become part of the drug discovery process, greatly improved the speed of drug development compared with traditional drug finding methods. In particular, the de novo drug design method could be used to identify ligands with novel structure for a special target. Through computer simulation, researchers could find new ideas about how to change a compound to improve the drug properties or how to assemble some fragments to generate candidates which be drug-like, synthetically accessible and high affinity for a target. The common software of de novo design included LUDI, MCSS, LigBuilder, SPROUT, SYNOPSIS, BREED, LeapFrog and RACHEL, etc. The methods were fragments link and grow, side chain replacement, parent molecule evolve, template, scaffold hopping and so on. Discovery and development of cancer drugs had been revolutionized over the last decade. De novo drug design methods had already played a significant role in the discovery of some anticancer compounds such as kinesin spindle protein inhibitors, vascular endothelial growth factor inhibitors, cyclophilin A inhibitors, cell division cycle protein CDC25 inhibitors and BRAF inhibitors. The common software and methods of de novo drug design were summarized in this review and their applications in antitumor drug design were discussed.
2014, 32(1): 16-18,22.
doi: 10.3969/j.issn.1006-0111.2014.01.004
Abstract:
Objective To summarize the new dosage forms and new ways to the quality research of Rupixiao in the modern dosage forms. Methods The literatures were reviewed, sorted, and summarized. Results Mostly modern dosage forms of Rupixiao were tablets, capsules, and ointment paste. The quality was studied by high performance liquid chromatography, thin layer scanning method, and gas chromatography. Conclusion The study on modern dosage forms of Rupixiao should be according to the principle of stable quality, safe and effective, by using new analytical methods and improving the quality of research related to new dosage forms.
Objective To summarize the new dosage forms and new ways to the quality research of Rupixiao in the modern dosage forms. Methods The literatures were reviewed, sorted, and summarized. Results Mostly modern dosage forms of Rupixiao were tablets, capsules, and ointment paste. The quality was studied by high performance liquid chromatography, thin layer scanning method, and gas chromatography. Conclusion The study on modern dosage forms of Rupixiao should be according to the principle of stable quality, safe and effective, by using new analytical methods and improving the quality of research related to new dosage forms.
2014, 32(1): 19-22.
doi: 10.3969/j.issn.1006-0111.2014.01.005
Abstract:
Magnesium stearate as a lubricant plays an important role in the direct compression of tablet technology, but the use of magnesium stearate often causes negative effect on tablet strength. The reasons of decreasing tablet strength from the aspects of excipients classification, particle size, blending time and lubricant concentration were briefly analyzed, which was helpful for the promotion and improvement of the tablet manufacturing level.
Magnesium stearate as a lubricant plays an important role in the direct compression of tablet technology, but the use of magnesium stearate often causes negative effect on tablet strength. The reasons of decreasing tablet strength from the aspects of excipients classification, particle size, blending time and lubricant concentration were briefly analyzed, which was helpful for the promotion and improvement of the tablet manufacturing level.
2014, 32(1): 23-26,30.
doi: 10.3969/j.issn.1006-0111.2014.01.006
Abstract:
Objective To compare the effect and safety of the two regimens of topotecan by means of Meta-analysis, in order to give evidences for doctors when selecting regimens. Methods All the studies that have been searched in Pub Med from setup data base to 2013-07-10 were evaluated strictly and meta-analysis was used to study the effect and safety of two regimens contain standard regimens and weekly regimens. The odds radio(OR) was calculate for incidence of efficiency and safety of two regimens. Results Totally 3 studies including 288 cases were analyzed in efficiency. 17 cases were effective in 165 cases of weekly regimens; 21 cases were effective in 123 cases of standard regimens. Totally 2 studies including 132 cases were analyzed in safety. 89 cases were in weekly regimens. Of which 26 cases of Ⅲ/Ⅳ neutropenia and 17cases of Ⅲ/Ⅳ low-hemoglobin and 32 cases of Ⅲ/Ⅳ thrombopenia. 43 cases were in standard regimens. Of which 39 cases of Ⅲ/Ⅳ neutropenia and 24 cases of Ⅲ/Ⅳ low-hemoglobin and 32 cases of Ⅲ/Ⅳ thrombopenia. The pooled OR of efficiency was 0.49 with a 95% confidence interval(0.23-1.01);the pooled OR of Ⅲ/Ⅳ neutropenia was 0.04 with a 95% confidence interval(0.01-0.14); the pooled OR of Ⅲ/Ⅳ low-hemoglobin was 0.27 with a 95% confidence interval(0.11-0.63); the pooled OR of Ⅲ/Ⅳ thrombopenia was 0.12 with a 95% confidence interval(0.04-0.32). Conclusion Weekly regimens group compared to standard regimens group in efficiency had no statistical significance; Weekly regimens group compared to standard regimens group for preventing Ⅲ/Ⅳ neutropenia, Ⅲ/Ⅳ low-hemoglobin and Ⅲ/Ⅳ thrombopenia had statistical significance. Weekly regimens group was better to standard regimens group for preventing Ⅲ/Ⅳ neutropenia, Ⅲ/Ⅳ low-hemoglobin and Ⅲ/Ⅳ thrombopenia.
Objective To compare the effect and safety of the two regimens of topotecan by means of Meta-analysis, in order to give evidences for doctors when selecting regimens. Methods All the studies that have been searched in Pub Med from setup data base to 2013-07-10 were evaluated strictly and meta-analysis was used to study the effect and safety of two regimens contain standard regimens and weekly regimens. The odds radio(OR) was calculate for incidence of efficiency and safety of two regimens. Results Totally 3 studies including 288 cases were analyzed in efficiency. 17 cases were effective in 165 cases of weekly regimens; 21 cases were effective in 123 cases of standard regimens. Totally 2 studies including 132 cases were analyzed in safety. 89 cases were in weekly regimens. Of which 26 cases of Ⅲ/Ⅳ neutropenia and 17cases of Ⅲ/Ⅳ low-hemoglobin and 32 cases of Ⅲ/Ⅳ thrombopenia. 43 cases were in standard regimens. Of which 39 cases of Ⅲ/Ⅳ neutropenia and 24 cases of Ⅲ/Ⅳ low-hemoglobin and 32 cases of Ⅲ/Ⅳ thrombopenia. The pooled OR of efficiency was 0.49 with a 95% confidence interval(0.23-1.01);the pooled OR of Ⅲ/Ⅳ neutropenia was 0.04 with a 95% confidence interval(0.01-0.14); the pooled OR of Ⅲ/Ⅳ low-hemoglobin was 0.27 with a 95% confidence interval(0.11-0.63); the pooled OR of Ⅲ/Ⅳ thrombopenia was 0.12 with a 95% confidence interval(0.04-0.32). Conclusion Weekly regimens group compared to standard regimens group in efficiency had no statistical significance; Weekly regimens group compared to standard regimens group for preventing Ⅲ/Ⅳ neutropenia, Ⅲ/Ⅳ low-hemoglobin and Ⅲ/Ⅳ thrombopenia had statistical significance. Weekly regimens group was better to standard regimens group for preventing Ⅲ/Ⅳ neutropenia, Ⅲ/Ⅳ low-hemoglobin and Ⅲ/Ⅳ thrombopenia.
2014, 32(1): 27-30.
doi: 10.3969/j.issn.1006-0111.2014.01.007
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Objective To explore the anti-hyperlipidemic effects and mechanism of polysaccharide MA from Mytilus coruscus in the experimental atherosclerosis rabbits and to observe the effects of MA on liver and aorta. Methods The atherosclerosis rabbit model was established by high-fat diet. The blood lipid such as triglyceride (TG), total cholesterol (TC), low-density lipoprotein (LDL), high-density lipoprotein (HDL) in serum and enzymes metabolizing blood lipid such as lipoprteinlipase (LPL), hepaticlipase (HL) and hydroxymethylglutaryl CoA reductase (HMG-CoAR) were measured after atherosclerosis rabbits fed MA for 4 weeks. Histopathology and ultramicroscopic structure of hepatic tissue was observed. Lipid storage in aortic atherosclerotic plaque was observed by the oil red staining method. Results MA significantly reduced the level of TG, TC, LDL in serum and increased HL, LPL (P<0.05). MA reduced lipid storage in liver and aortic atherosclerotic plaque. Conclusion MA might play regulating effects in serum lipid by enhancing the activities of LPL and HL, and inhibit formation of atherosclerosis and fatty liver.
Objective To explore the anti-hyperlipidemic effects and mechanism of polysaccharide MA from Mytilus coruscus in the experimental atherosclerosis rabbits and to observe the effects of MA on liver and aorta. Methods The atherosclerosis rabbit model was established by high-fat diet. The blood lipid such as triglyceride (TG), total cholesterol (TC), low-density lipoprotein (LDL), high-density lipoprotein (HDL) in serum and enzymes metabolizing blood lipid such as lipoprteinlipase (LPL), hepaticlipase (HL) and hydroxymethylglutaryl CoA reductase (HMG-CoAR) were measured after atherosclerosis rabbits fed MA for 4 weeks. Histopathology and ultramicroscopic structure of hepatic tissue was observed. Lipid storage in aortic atherosclerotic plaque was observed by the oil red staining method. Results MA significantly reduced the level of TG, TC, LDL in serum and increased HL, LPL (P<0.05). MA reduced lipid storage in liver and aortic atherosclerotic plaque. Conclusion MA might play regulating effects in serum lipid by enhancing the activities of LPL and HL, and inhibit formation of atherosclerosis and fatty liver.
2014, 32(1): 31-34.
doi: 10.3969/j.issn.1006-0111.2014.01.008
Abstract:
Objective To prepare proanthocyanidins phospholipids complex, investigate the physicochemical properties and study the formulation. Methods Proanthocyanidins phospholipids complex was prepared and optimized by solvent evaporation method and physicochemical characteristics of the complex were investigated by means of apparent solubility studies. Results The average entrapment efficiencies of phospholipid complex for proanthocyanidins of grasp seed was 97%. Moreover, there was a great improvement of the solubility of proanthocyanidins phospholipid complex both in water and n-octanol. Conclusion The best method to proanthocyanidins phospholipid complex was achieved, and the physicochemical properties were significantly better from those of proanthocyanidins.
Objective To prepare proanthocyanidins phospholipids complex, investigate the physicochemical properties and study the formulation. Methods Proanthocyanidins phospholipids complex was prepared and optimized by solvent evaporation method and physicochemical characteristics of the complex were investigated by means of apparent solubility studies. Results The average entrapment efficiencies of phospholipid complex for proanthocyanidins of grasp seed was 97%. Moreover, there was a great improvement of the solubility of proanthocyanidins phospholipid complex both in water and n-octanol. Conclusion The best method to proanthocyanidins phospholipid complex was achieved, and the physicochemical properties were significantly better from those of proanthocyanidins.
2014, 32(1): 35-41,48.
doi: 10.3969/j.issn.1006-0111.2014.01.009
Abstract:
Salvia miltiorrhiza (Bung), a famous medicinal plant, is widely used in China, Japan, America and European countries to treat various conditions, such as cardiovascular and cerebrovascular disease, due to their excellent medicinal values. A novel fructose-bisphosphate aldolase gene (designated as SmFBA, GenBank accession no. FJ540907) was cloned from S. miltiorrhiza for the first time. The full-length cDNA of SmFBA was 1 390 bp with an open reading frame (ORF) of 1 065 bp which encoding a protein of 355 amino acid residues. The deduced protein had isoelectric point (pI) of 5.60 and a calculated molecular weight of about 37.78 ku. The deduced amino acid sequence of SmFBA gene shared high homology and identity with other plant FBAs. The SmFBA genomic DNA sequence was also obtained, revealing SmFBA had three exons and two introns. Southern-blot analysis indicated that SmFBA was a low-copy gene in S. miltiorrhiza genomic. Real-time quantitative PCR analysis showed that SmFBA expressed constitutively in all tested organs, with the highest expression level in roots. In addition, the recombinant SmFBA protein has enzyme activity in E. coli and could improve the high-salinity stress tolerance of E. coli. The successful isolation of the SmFBA gene will be helpful for studying EMP pathway in the near future.
Salvia miltiorrhiza (Bung), a famous medicinal plant, is widely used in China, Japan, America and European countries to treat various conditions, such as cardiovascular and cerebrovascular disease, due to their excellent medicinal values. A novel fructose-bisphosphate aldolase gene (designated as SmFBA, GenBank accession no. FJ540907) was cloned from S. miltiorrhiza for the first time. The full-length cDNA of SmFBA was 1 390 bp with an open reading frame (ORF) of 1 065 bp which encoding a protein of 355 amino acid residues. The deduced protein had isoelectric point (pI) of 5.60 and a calculated molecular weight of about 37.78 ku. The deduced amino acid sequence of SmFBA gene shared high homology and identity with other plant FBAs. The SmFBA genomic DNA sequence was also obtained, revealing SmFBA had three exons and two introns. Southern-blot analysis indicated that SmFBA was a low-copy gene in S. miltiorrhiza genomic. Real-time quantitative PCR analysis showed that SmFBA expressed constitutively in all tested organs, with the highest expression level in roots. In addition, the recombinant SmFBA protein has enzyme activity in E. coli and could improve the high-salinity stress tolerance of E. coli. The successful isolation of the SmFBA gene will be helpful for studying EMP pathway in the near future.
2014, 32(1): 42-44.
doi: 10.3969/j.issn.1006-0111.2014.01.010
Abstract:
Objective To purify the total flavones from Resina Draconis using D101 resin, and set up a method of simultaneously determining the contents of loureirin A and B in the extract. Methods Fractions in 70% and 95% ethanol were collected. Mixture of acetonitrile and l% acetic acid (34.5:65.5) was used as the mobile phase and ODS column was used as stationary phase to determine loureirin A and B. The detecting wave length was 280 nm. Results In the established HPLC method, the linear range of loureirin A was 11.00-275.00 g/ml, and that of loureirin B was 20.00-500.00 g/ml. Linear equation of loureirin A was Y=35 844C+44 725(r=0.999 9) and that of loureirin B was Y=28 533C-41 085, r=0.999 9.The accuracy, precision and stability of this method were satisfactory. Conclusion The proposed method was suitable for preparation of total flavones and determination of its active components from Resina Draconis.
Objective To purify the total flavones from Resina Draconis using D101 resin, and set up a method of simultaneously determining the contents of loureirin A and B in the extract. Methods Fractions in 70% and 95% ethanol were collected. Mixture of acetonitrile and l% acetic acid (34.5:65.5) was used as the mobile phase and ODS column was used as stationary phase to determine loureirin A and B. The detecting wave length was 280 nm. Results In the established HPLC method, the linear range of loureirin A was 11.00-275.00 g/ml, and that of loureirin B was 20.00-500.00 g/ml. Linear equation of loureirin A was Y=35 844C+44 725(r=0.999 9) and that of loureirin B was Y=28 533C-41 085, r=0.999 9.The accuracy, precision and stability of this method were satisfactory. Conclusion The proposed method was suitable for preparation of total flavones and determination of its active components from Resina Draconis.
2014, 32(1): 45-48.
doi: 10.3969/j.issn.1006-0111.2014.01.011
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Objective To establish a sensitive and specific LC-MS/MS method for the determination of mitiglinide calcium in human plasma, and investigate the pharmacokinetics of mitiglinide calcium tablets in healthy volunteers. Methods 30 healthy volunteers were randomly divided into three groups with 5 men and 5 women in each group. The volunteers in three groups were administrated with single dose of mitiglinide calcium tablets 5, 10, 20 mg, respectively. The pharmacokinetic parameters were calculated by non-compartment model. Results The main pharmacokinetics parameters of mitiglinide in volunteers who were administrated with a single dose of 5, 10, 20 mg were as follows:Cmax(799.5±189.8), (1 689.8±348.4)and(3 032.9±755.6)ng/ml; tmax(0.38±0.16), (0.43±0.16)and(0.54±0.26)h; AUC0-10(1 051.3±276.4), (2 324.5±481.8)and(5 028.8±1 283.6)ng·h/ml; AUC0-∞(1 059.4±278.2), (2 342.8±488.6)and(5 073.9±1 315.9)ng·h/ml; t1/2(1.80±0.42), (1.68±0.37)and(1.56±0.19)h, respectively. Conclusion The present method was accurate, sensitive and reproducible for the determination of mitiglinide levels in human plasma, which was suitable for pharmacokinetic study on mitiglinide tables in human.
Objective To establish a sensitive and specific LC-MS/MS method for the determination of mitiglinide calcium in human plasma, and investigate the pharmacokinetics of mitiglinide calcium tablets in healthy volunteers. Methods 30 healthy volunteers were randomly divided into three groups with 5 men and 5 women in each group. The volunteers in three groups were administrated with single dose of mitiglinide calcium tablets 5, 10, 20 mg, respectively. The pharmacokinetic parameters were calculated by non-compartment model. Results The main pharmacokinetics parameters of mitiglinide in volunteers who were administrated with a single dose of 5, 10, 20 mg were as follows:Cmax(799.5±189.8), (1 689.8±348.4)and(3 032.9±755.6)ng/ml; tmax(0.38±0.16), (0.43±0.16)and(0.54±0.26)h; AUC0-10(1 051.3±276.4), (2 324.5±481.8)and(5 028.8±1 283.6)ng·h/ml; AUC0-∞(1 059.4±278.2), (2 342.8±488.6)and(5 073.9±1 315.9)ng·h/ml; t1/2(1.80±0.42), (1.68±0.37)and(1.56±0.19)h, respectively. Conclusion The present method was accurate, sensitive and reproducible for the determination of mitiglinide levels in human plasma, which was suitable for pharmacokinetic study on mitiglinide tables in human.
2014, 32(1): 49-50,64.
doi: 10.3969/j.issn.1006-0111.2014.01.012
Abstract:
Objective To compare the stability of ethacridine solution influenced by three factors:pH value, antioxidants and inert gas, to find out the most economical and effective production of ethacridine solution for the hospital with the consideration of economic benefits. Methods The content of ethacridine solution was determined by UV spectrophotometry, and the room-temperature storage period was predicted with the initial uniform rate method. Finally, the optimal conditions for producing the ethacridine solution was selected by orthogonal design. Results Ethacridine solution was the most stable under the condition of pH4.0, 0.10% p-phenetidine and nitrogen of 2 minutes. Ethacridine solution was the second most stable under the condition of pH4.5, 0.00% p-phenetidine and nitrogen of 2 minutes. Conclusion The condition of pH4.5 and nitrogen of 2 minutes was the optimal choice by considering the irritation of ethacridine solution, the cost of production and operation difficulty. However, more tests should be done to find out the optimal plan of production.
Objective To compare the stability of ethacridine solution influenced by three factors:pH value, antioxidants and inert gas, to find out the most economical and effective production of ethacridine solution for the hospital with the consideration of economic benefits. Methods The content of ethacridine solution was determined by UV spectrophotometry, and the room-temperature storage period was predicted with the initial uniform rate method. Finally, the optimal conditions for producing the ethacridine solution was selected by orthogonal design. Results Ethacridine solution was the most stable under the condition of pH4.0, 0.10% p-phenetidine and nitrogen of 2 minutes. Ethacridine solution was the second most stable under the condition of pH4.5, 0.00% p-phenetidine and nitrogen of 2 minutes. Conclusion The condition of pH4.5 and nitrogen of 2 minutes was the optimal choice by considering the irritation of ethacridine solution, the cost of production and operation difficulty. However, more tests should be done to find out the optimal plan of production.
2014, 32(1): 51-52.
doi: 10.3969/j.issn.1006-0111.2014.01.013
Abstract:
Objective To synthesize the antitumor activity of twenty-six peptide melittin. Methods The melittin was synthesized by stepwise solid-phase peptide synthesis (SPPS). During the synthesis of melittin, wang-resin was chosen as solid supporter and HOBt/DCC were used as the coupling reagent. Results The melittin was synthesized with yield of 32%. Conclusion The synthetic method was feasible, simple and with high yield for long chain polypeptide synthesis.
Objective To synthesize the antitumor activity of twenty-six peptide melittin. Methods The melittin was synthesized by stepwise solid-phase peptide synthesis (SPPS). During the synthesis of melittin, wang-resin was chosen as solid supporter and HOBt/DCC were used as the coupling reagent. Results The melittin was synthesized with yield of 32%. Conclusion The synthetic method was feasible, simple and with high yield for long chain polypeptide synthesis.
2014, 32(1): 53-55.
doi: 10.3969/j.issn.1006-0111.2014.01.014
Abstract:
Objective To investigate the chemical constituents of Phyllanthus urinaria. Methods Multi-chromatographic methods were employed for the isolation and purification of chemical constituents of Phyllanthus urinaria. The structures were identified on the basis of physical and spectral data. Results Nine compounds were isolated and identified as gallic acid (1), ethyl gallate(2), guercetin (3), rutin (4), stigmasterol (5), kaempferol (6), chlorogenic acid (7), 4-ethoxy-gallic acid (8), eupatilin (9). Conclusion Compounds 7-9 were all isolated form Phyllanthus urinaria for the first time.
Objective To investigate the chemical constituents of Phyllanthus urinaria. Methods Multi-chromatographic methods were employed for the isolation and purification of chemical constituents of Phyllanthus urinaria. The structures were identified on the basis of physical and spectral data. Results Nine compounds were isolated and identified as gallic acid (1), ethyl gallate(2), guercetin (3), rutin (4), stigmasterol (5), kaempferol (6), chlorogenic acid (7), 4-ethoxy-gallic acid (8), eupatilin (9). Conclusion Compounds 7-9 were all isolated form Phyllanthus urinaria for the first time.
2014, 32(1): 56-58,67.
doi: 10.3969/j.issn.1006-0111.2014.01.016
Abstract:
Objective To establish HPLC method for the content determination of insulin in thermosensitive slow-release rectal liquid suppository, evaluate release characteristics in vitro. Methods The separation was performed on a Welch ultimate column(4.6 mm×250 mm, 5 μm).The mobile phase was composed of 0.2 mol/L sodium sulfate buffer (pH was adjusted to 2.3 with ethanolamine)-acetonitrile (74:26) with flow rate 1ml/min, detected at 214 nm, the insulin levels were determined. Adopting membrane less release model, bovine intestinal mucosa release model, the gut mucosa release model, insulin was used as model drug, drug release mechanism of thermosensitive slow-release rectal liquid suppository of insulin in vitro was evaluate. Results The insulin in situ gel was linear in the range of 1.0-40.0 U/ml(r=0.999 1).The average recovery was 99.35%, RSD was 0.79;membrane-less release:Q=0.495 4t-2.611 8(r=0.997 7);bovine intestinal mucosa release:(1-Q)1/3=0.001 6t+2.927 4(r=0.975 5);gut-mucosa release:lnQ=0.878 3lnt-4.931 1(r=0.970 5). Conclusion The method was simple, fine repeatability, sensitive, accurate and reliable. The method could be applicable to the preparation of the content determination of insulin and evaluate release mechanism thermosensitive slow-release rectal liquid suppository of insulin.
Objective To establish HPLC method for the content determination of insulin in thermosensitive slow-release rectal liquid suppository, evaluate release characteristics in vitro. Methods The separation was performed on a Welch ultimate column(4.6 mm×250 mm, 5 μm).The mobile phase was composed of 0.2 mol/L sodium sulfate buffer (pH was adjusted to 2.3 with ethanolamine)-acetonitrile (74:26) with flow rate 1ml/min, detected at 214 nm, the insulin levels were determined. Adopting membrane less release model, bovine intestinal mucosa release model, the gut mucosa release model, insulin was used as model drug, drug release mechanism of thermosensitive slow-release rectal liquid suppository of insulin in vitro was evaluate. Results The insulin in situ gel was linear in the range of 1.0-40.0 U/ml(r=0.999 1).The average recovery was 99.35%, RSD was 0.79;membrane-less release:Q=0.495 4t-2.611 8(r=0.997 7);bovine intestinal mucosa release:(1-Q)1/3=0.001 6t+2.927 4(r=0.975 5);gut-mucosa release:lnQ=0.878 3lnt-4.931 1(r=0.970 5). Conclusion The method was simple, fine repeatability, sensitive, accurate and reliable. The method could be applicable to the preparation of the content determination of insulin and evaluate release mechanism thermosensitive slow-release rectal liquid suppository of insulin.
2014, 32(1): 59-60,77.
doi: 10.3969/j.issn.1006-0111.2014.01.016
Abstract:
Objective To explore the clinical effect and identify the optimal concentration of different concentration of ropivacaine in ropivacaine combined with butorphanol in epidural anesthesia for cesarean section. Methods 1 038 patients for cesarean section were randomly divided into three groups including group A(n=341), group B (n=353) and group C (n=344). All the patients were performed by epidural anesthesia, and given 3 mg butorphanol combined with 0.125%, 0.15%, 0.20% ropivacaine separately. Results The onset time of sense block, disappeared time of pain in group B and group C were significantly shorter than those in group A (P<0.05), while there was not significantly different between group B and group C (P>0.05). Compared with group A and group B, the onset time, duration and degree of motor block in group C was much longer, while there was no significantly different between group A and group B (P>0.05). The VAS scores after cesarean section for 2 h, 12 h in group B and group C were significantly lower than that in group A(P<0.05), while there was no significantly difference between Group B and Group C (P>0.05). The VAS scores after cesarean section for 24 h among the three groups were not statistically different (P<0.05). The rate of side effects including nausea and vomiting, sleepiness and itchy skin in group A and group B were lower than that in group C(P<0.05). Conclusion The concentration of 0.15% ropivacaine combined with 3 mg butorphanol in epidural anesthesia for cesarean section could contribute to provide good effect of anesthesia and analgesia, and reduce the side effect.
Objective To explore the clinical effect and identify the optimal concentration of different concentration of ropivacaine in ropivacaine combined with butorphanol in epidural anesthesia for cesarean section. Methods 1 038 patients for cesarean section were randomly divided into three groups including group A(n=341), group B (n=353) and group C (n=344). All the patients were performed by epidural anesthesia, and given 3 mg butorphanol combined with 0.125%, 0.15%, 0.20% ropivacaine separately. Results The onset time of sense block, disappeared time of pain in group B and group C were significantly shorter than those in group A (P<0.05), while there was not significantly different between group B and group C (P>0.05). Compared with group A and group B, the onset time, duration and degree of motor block in group C was much longer, while there was no significantly different between group A and group B (P>0.05). The VAS scores after cesarean section for 2 h, 12 h in group B and group C were significantly lower than that in group A(P<0.05), while there was no significantly difference between Group B and Group C (P>0.05). The VAS scores after cesarean section for 24 h among the three groups were not statistically different (P<0.05). The rate of side effects including nausea and vomiting, sleepiness and itchy skin in group A and group B were lower than that in group C(P<0.05). Conclusion The concentration of 0.15% ropivacaine combined with 3 mg butorphanol in epidural anesthesia for cesarean section could contribute to provide good effect of anesthesia and analgesia, and reduce the side effect.
2014, 32(1): 61-64.
doi: 10.3969/j.issn.1006-0111.2014.01.017
Abstract:
Objective To compare the clinical effect of moxifloxacin and levofloxacin on treatment of multi-drug resistant pulmonary tuberculosis(TB). Methods From Jan 2011 to Dec 2012, 108 patients who were proved to be multi-drug resistant to tuberculosis in Yuhuan County People's Hospital of Zhejiang Province were included in the study. The patients were divided into moxifloxacin treatment group or levofloxacin treatment group by computer-generated random number and randomly allocated method. The treatment regimens were as follows:in moxifloxacin treatment group, the patients were given moxifloxacin, pasiniazid, pyrazinamide, protionamide, rifapentine, sodium aminosalicylate, and amikacin for 3 months, followed by 6 months treatment of moxifloxacin, pyrazinamide, protionamide, pasiniazid and rifapentine, then moxifloxacin, rifapentine, pyrazinamide, andpasiniazid for 9 months. In levofloxacin treatment group, moxifloxacin was replaced by levofloxacin, and other combinations were same as moxifloxacin group. The treatment time was 18 months in 2 groups. Results At the end of the study, 41 of 53 patients finished the treatment in moxifloxacin-group and 44 of 55 patients finished the treatment in levofloxacin-group. Mortalities were 9.4%(5/53)in moxifloxacin-group and 9.1%(5/55) in levofloxacin-group, respectively. The sputum negative rate was 87.8%(36/41) and 84.1%(37/44) in each group, respectively. The effective rate of chest X ray was 92.7%(38/41) in moxifloxacin group and 93.2%(41/44) in levofloxacin group, and the cavity closure rate were 39%(16/41)and 43.2%(19/44). The rate of serious adverse drug reactions was 13.2%(7/53) and 10.9%(6/55), respectively. There was no significant difference between 2 groups. Conclusion Moxifloxacin combined with other drugs to treat multi-drug-resistant TB had no significant advantages compared to levofloxacin combined with the same drugs.
Objective To compare the clinical effect of moxifloxacin and levofloxacin on treatment of multi-drug resistant pulmonary tuberculosis(TB). Methods From Jan 2011 to Dec 2012, 108 patients who were proved to be multi-drug resistant to tuberculosis in Yuhuan County People's Hospital of Zhejiang Province were included in the study. The patients were divided into moxifloxacin treatment group or levofloxacin treatment group by computer-generated random number and randomly allocated method. The treatment regimens were as follows:in moxifloxacin treatment group, the patients were given moxifloxacin, pasiniazid, pyrazinamide, protionamide, rifapentine, sodium aminosalicylate, and amikacin for 3 months, followed by 6 months treatment of moxifloxacin, pyrazinamide, protionamide, pasiniazid and rifapentine, then moxifloxacin, rifapentine, pyrazinamide, andpasiniazid for 9 months. In levofloxacin treatment group, moxifloxacin was replaced by levofloxacin, and other combinations were same as moxifloxacin group. The treatment time was 18 months in 2 groups. Results At the end of the study, 41 of 53 patients finished the treatment in moxifloxacin-group and 44 of 55 patients finished the treatment in levofloxacin-group. Mortalities were 9.4%(5/53)in moxifloxacin-group and 9.1%(5/55) in levofloxacin-group, respectively. The sputum negative rate was 87.8%(36/41) and 84.1%(37/44) in each group, respectively. The effective rate of chest X ray was 92.7%(38/41) in moxifloxacin group and 93.2%(41/44) in levofloxacin group, and the cavity closure rate were 39%(16/41)and 43.2%(19/44). The rate of serious adverse drug reactions was 13.2%(7/53) and 10.9%(6/55), respectively. There was no significant difference between 2 groups. Conclusion Moxifloxacin combined with other drugs to treat multi-drug-resistant TB had no significant advantages compared to levofloxacin combined with the same drugs.
2014, 32(1): 65-67.
doi: 10.3969/j.issn.1006-0111.2014.01.018
Abstract:
Objective To study the clinical effect of mifepristone combined with misoprostol and misoprostol in missed abortion curettage. Methods Seventy cases from April 2010 to August 2011 of medical termination of pregnancy in Huzhou family planning service station of Zhejiang Province were collected. All cases were divided randomly into research group (38 cases) and the control group (32 cases). The patients in research group were treated with mifepristone 50 mg once per 12 h, 3 times, on 3rd day, 600 μg misoprostol 2 h before abortion curettage; the patients in control group were treated with 600 μg misoprostol 2 h before abortion curettage. Results There was no significant difference between the 2 groups in complete abortion rate (P>0.05). Vaginal bleeding time in research group was significantly less than that in control group, there was significant difference between 2 groups, with χ2=4.12 and P<0.05. Blood volume in research group was significantly less than in control group, there was significant difference between the 2 groups, with χ2=5.30, and P<0.05.The incidence of side effects of research group was significantly less than that of control group, there was significant difference between 2 groups, with χ2=5.61 and P<0.05. Conclusion Mifepristone combined with misoprostol and misoprostol only for pregnancy termination had the same clinical effect. But mifepristone combined with misoprostol could effectively reduce the vaginal bleeding time and blood loss, and have fewer side effects.
Objective To study the clinical effect of mifepristone combined with misoprostol and misoprostol in missed abortion curettage. Methods Seventy cases from April 2010 to August 2011 of medical termination of pregnancy in Huzhou family planning service station of Zhejiang Province were collected. All cases were divided randomly into research group (38 cases) and the control group (32 cases). The patients in research group were treated with mifepristone 50 mg once per 12 h, 3 times, on 3rd day, 600 μg misoprostol 2 h before abortion curettage; the patients in control group were treated with 600 μg misoprostol 2 h before abortion curettage. Results There was no significant difference between the 2 groups in complete abortion rate (P>0.05). Vaginal bleeding time in research group was significantly less than that in control group, there was significant difference between 2 groups, with χ2=4.12 and P<0.05. Blood volume in research group was significantly less than in control group, there was significant difference between the 2 groups, with χ2=5.30, and P<0.05.The incidence of side effects of research group was significantly less than that of control group, there was significant difference between 2 groups, with χ2=5.61 and P<0.05. Conclusion Mifepristone combined with misoprostol and misoprostol only for pregnancy termination had the same clinical effect. But mifepristone combined with misoprostol could effectively reduce the vaginal bleeding time and blood loss, and have fewer side effects.
2014, 32(1): 68-70,73.
doi: 10.3969/j.issn.1006-0111.2014.01.019
Abstract:
Objective To investigate the utilization of clinical nutrition drugs in Hospital. Methods The utilization of EN and PN in Beijing Anzhen Union Hospital during 2009-2012 was analyzed statistically through hospital information system in respects of variety, consumption sum amount, DDDs and DDC by the defined daily dose method. Results From 2009 to 2012, the total consumption of clinical nutrition drugs increased year on year with increase range of 25.88%;the utilization ratio of enteral nutrition drugs to the whole nutrition drugs increased continuously from 16.05% to 24.24% during 2009 to 2012. Conclusion The based clinical nutrition therapy in our hospital was still the parenteral nutrition drugs; but with the rising trend of using the enteral nutrition drugs. The hospital would become more and more rational in utilizing nutritional medicine.
Objective To investigate the utilization of clinical nutrition drugs in Hospital. Methods The utilization of EN and PN in Beijing Anzhen Union Hospital during 2009-2012 was analyzed statistically through hospital information system in respects of variety, consumption sum amount, DDDs and DDC by the defined daily dose method. Results From 2009 to 2012, the total consumption of clinical nutrition drugs increased year on year with increase range of 25.88%;the utilization ratio of enteral nutrition drugs to the whole nutrition drugs increased continuously from 16.05% to 24.24% during 2009 to 2012. Conclusion The based clinical nutrition therapy in our hospital was still the parenteral nutrition drugs; but with the rising trend of using the enteral nutrition drugs. The hospital would become more and more rational in utilizing nutritional medicine.
2014, 32(1): 71-73.
doi: 10.3969/j.issn.1006-0111.2014.01.020
Abstract:
Objective To compare the differences in the drug utilization for infection prevention in combat injuries between the PLA and USA armed force. Methods The guidelines for the prevention of infections associated with combat-related injuries and tactical medical emergency protocols of USA armed force were compared with the combat injury treatment regulation of PLA. Results There are some differences between the prevention and medicine use of war injure infection of Chinese and American Armed Force, especially in variety selection and principle of drug selection in different echelon. Conclusion The references could be taken from the principle of drug utilization of prevention and treatment in combat injuries from USA Armed Force.
Objective To compare the differences in the drug utilization for infection prevention in combat injuries between the PLA and USA armed force. Methods The guidelines for the prevention of infections associated with combat-related injuries and tactical medical emergency protocols of USA armed force were compared with the combat injury treatment regulation of PLA. Results There are some differences between the prevention and medicine use of war injure infection of Chinese and American Armed Force, especially in variety selection and principle of drug selection in different echelon. Conclusion The references could be taken from the principle of drug utilization of prevention and treatment in combat injuries from USA Armed Force.
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