2017 Vol. 35, No. 1
Display Method:
2017, 35(1): 1-5,16.
doi: 10.3969/j.issn.1006-0111.2017.01.001
Abstract:
Baphicacanthus cusia, widely distributed in the Southwest, Southern and Eastern regions of China, is an important medicinal plant of Acanthaceae family. Indigo made from stem and leaf of Baphicacanthus cusia in Fujian has the best quality in China, and is known as "Jian Indigo naturalis", which is the genuine medicinal of Fujian Province. The rhizoma of Baphicacanthus cusia could be used as medicine, called "Nanbanlangen", which together with indigo were included in the "Chinese Pharmacopoeia". Indigo and its original plant both contain indirubin, which has anti-cancer activity. Indirubin is an active ingredient of Huangdai Pian and Danggui Longhui Wan, two kinds of traditional Chinese medicine, which have been successfully used in the treatment of malignancies such as chronic myelogenous leukemia. The international advances in the biological characteristics, genetic diversity, cultivation technology and molecular biology of Baphicacanthus cusia germplasm resources were summarized. The main problems in Baphicacanthus cusia germplasm resources research are indicated, which could provide references for the further study and application of Baphicacanthus cusia germplasm resources.
Baphicacanthus cusia, widely distributed in the Southwest, Southern and Eastern regions of China, is an important medicinal plant of Acanthaceae family. Indigo made from stem and leaf of Baphicacanthus cusia in Fujian has the best quality in China, and is known as "Jian Indigo naturalis", which is the genuine medicinal of Fujian Province. The rhizoma of Baphicacanthus cusia could be used as medicine, called "Nanbanlangen", which together with indigo were included in the "Chinese Pharmacopoeia". Indigo and its original plant both contain indirubin, which has anti-cancer activity. Indirubin is an active ingredient of Huangdai Pian and Danggui Longhui Wan, two kinds of traditional Chinese medicine, which have been successfully used in the treatment of malignancies such as chronic myelogenous leukemia. The international advances in the biological characteristics, genetic diversity, cultivation technology and molecular biology of Baphicacanthus cusia germplasm resources were summarized. The main problems in Baphicacanthus cusia germplasm resources research are indicated, which could provide references for the further study and application of Baphicacanthus cusia germplasm resources.
2017, 35(1)
doi: 10.3969/j.issn.1006-0111.2017.01.002
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Organoselenium compounds are bioactive substances with extensive physiological activities. As a representative compound, ebselen could be used as mimics of glutathione peroxidase, and in the treatment of many diseases, such as cardiovascular and cerebrovascular diseases, inflammation and noise-induced hearing loss. the research progress in physiological activities and synthetic methods of ebselen were reviewed in this paper.
Organoselenium compounds are bioactive substances with extensive physiological activities. As a representative compound, ebselen could be used as mimics of glutathione peroxidase, and in the treatment of many diseases, such as cardiovascular and cerebrovascular diseases, inflammation and noise-induced hearing loss. the research progress in physiological activities and synthetic methods of ebselen were reviewed in this paper.
2017, 35(1): 8-11.
doi: 10.3969/j.issn.1006-0111.2017.01.003
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People do have some risks of exposing to the radiation during their daily life.Longtime or megadose ionizing radiation can induce tissue damage, which is related to cell apoptosis, necrosis and inflammation, etc..Currently, more and more radio protective agents were developed and several signaling pathways were involved. NFκB, MAPK, PI3k/Akt, p53 and STAT3 signaling pathways were reviewed in this article.
People do have some risks of exposing to the radiation during their daily life.Longtime or megadose ionizing radiation can induce tissue damage, which is related to cell apoptosis, necrosis and inflammation, etc..Currently, more and more radio protective agents were developed and several signaling pathways were involved. NFκB, MAPK, PI3k/Akt, p53 and STAT3 signaling pathways were reviewed in this article.
2017, 35(1): 12-16.
doi: 10.3969/j.issn.1006-0111.2017.01.004
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Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity. Methods Using sophocarpine as the starting material,a series of new compounds were synthesized through Michael addition,Staudinger reduction and acylation.The structure of target compounds were confirmed by 1H NMR and MS techniques. Their antitumor activity against human hepatoma cells(BEL-7404) and mice melanoma cells (K111) were evaluated in vitro by MTT assay. Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111. Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404).
Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity. Methods Using sophocarpine as the starting material,a series of new compounds were synthesized through Michael addition,Staudinger reduction and acylation.The structure of target compounds were confirmed by 1H NMR and MS techniques. Their antitumor activity against human hepatoma cells(BEL-7404) and mice melanoma cells (K111) were evaluated in vitro by MTT assay. Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111. Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404).
2017, 35(1): 17-21,86.
doi: 10.3969/j.issn.1006-0111.2017.01.005
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Objective Based on the structure-activity relationships on the reported antifungal agents bearing quinoline or thiophene moieties, novel compounds bearing both quinoline and thiophene were designed, synthesized, and evaluated for in vitro antifungal activity against Candida albicans. Methods With 5-cyanothiophene-2-carbaldehyde or 5-cyanothiophene-3-carbaldehyde as starting materials, 13 compounds were synthesized via reductive amination, reduction of cyano group and amidation of quinoline-or isoquinoline-carboxylic acid. Their chemical structures were characterized by 1H NMR and MS. In vitro antifungal screening against Candida albicans SC5314 was performed with the microbroth dilution method. Results All the compounds exhibited potent antifungal activities against Candida albicans. Among them, compound 6k showed the highest antifungal activity with MIC80 value of 0.5 μg/ml, which is same potent as fluconazole. Conclusion The designed compounds bearing both quinoline and thiophene exhibited potent antifungal activities, and deserve further research.
Objective Based on the structure-activity relationships on the reported antifungal agents bearing quinoline or thiophene moieties, novel compounds bearing both quinoline and thiophene were designed, synthesized, and evaluated for in vitro antifungal activity against Candida albicans. Methods With 5-cyanothiophene-2-carbaldehyde or 5-cyanothiophene-3-carbaldehyde as starting materials, 13 compounds were synthesized via reductive amination, reduction of cyano group and amidation of quinoline-or isoquinoline-carboxylic acid. Their chemical structures were characterized by 1H NMR and MS. In vitro antifungal screening against Candida albicans SC5314 was performed with the microbroth dilution method. Results All the compounds exhibited potent antifungal activities against Candida albicans. Among them, compound 6k showed the highest antifungal activity with MIC80 value of 0.5 μg/ml, which is same potent as fluconazole. Conclusion The designed compounds bearing both quinoline and thiophene exhibited potent antifungal activities, and deserve further research.
2017, 35(1): 22-25,59.
doi: 10.3969/j.issn.1006-0111.2017.01.006
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Objective To design and synthesize novel triazole antifungal derivatives with 1,3,4-oxadiazole side chain for the study of antifungal activities. Methods Fourteen title compounds were synthesized via acylation, aminolysis reaction, cyclization, nucleophilic substitution, etc. All the compounds were characterized by 1H NMR, MS spectra. The in vitro antifungal activities were evaluated against six human pathogenic fungi through the micro-broth dilution method. Results The title compounds exhibited strong antifungal activities against all the tested fungi, especially against Candida albicans. Compounds 10d , 10i , 10l , and 10n were found to be the most effective, with a minimum inhibitory concentration(MIC80) of 0.003 9 μg/ml.They are 16-fold more potent than ICZ (MIC80 0.062 5 μg/ml) and 64-fold more potent than FCZ (MIC80 0.25 μg/ml). Conclusion The 1,3,4-oxadiazole side chain could affect the antifungal activities. That could be due to the proper incorporation between the 1,3,4-oxadiazole substituted phenyl ring with the target enzyme.
Objective To design and synthesize novel triazole antifungal derivatives with 1,3,4-oxadiazole side chain for the study of antifungal activities. Methods Fourteen title compounds were synthesized via acylation, aminolysis reaction, cyclization, nucleophilic substitution, etc. All the compounds were characterized by 1H NMR, MS spectra. The in vitro antifungal activities were evaluated against six human pathogenic fungi through the micro-broth dilution method. Results The title compounds exhibited strong antifungal activities against all the tested fungi, especially against Candida albicans. Compounds 10d , 10i , 10l , and 10n were found to be the most effective, with a minimum inhibitory concentration(MIC80) of 0.003 9 μg/ml.They are 16-fold more potent than ICZ (MIC80 0.062 5 μg/ml) and 64-fold more potent than FCZ (MIC80 0.25 μg/ml). Conclusion The 1,3,4-oxadiazole side chain could affect the antifungal activities. That could be due to the proper incorporation between the 1,3,4-oxadiazole substituted phenyl ring with the target enzyme.
2017, 35(1): 26-30,35.
doi: 10.3969/j.issn.1006-0111.2017.01.007
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Objective To design and prepare 13,15-cycloimides chlorin p6 ( 1 ),a class of chlorin related antitumor photosensitizers,which contain a more stable six-membered cyclic imide comparing to the exocyclic anhydride ring of purpurin-18 ( 2 ). Compounds ( 1 ) exhibit strong absorption at long wavelengths near λmax 700 nm to take full advantage of greater tissue penetration. Methods Pheophorbide a ( 3 ) was obtained by acid hydrolysis of chlorophylla,which was from crude chlorophyll extracts of Chinese traditional herb named Silkworm excrement. Purpurin-18 ( 2 ) was prepared by air oxidation and alkali open loop simultaneously on five-membered beta-keto carboxylic ester ring of pheophorbide a ( 3 ). Finally,the target compounds 1a ~ 1j were synthesized via condensation of its anhydride ring with various amines including carboxyl-protected amino acids. Results Target compounds 1a ~ 1j were successfully synthesized in yields ranged from 32.6% to 65.2%. Their structures were confirmed by elemental analysis,ESI-MS and 1H NMR spectra. Conclusion Treatment of purpurin-18 ( 2 ) with amines can produce target compounds 1a ~ 1j . The starting raw material was inexpensive and readily available. The reaction conditions were mild and workup was convinient.
Objective To design and prepare 13,15-cycloimides chlorin p6 ( 1 ),a class of chlorin related antitumor photosensitizers,which contain a more stable six-membered cyclic imide comparing to the exocyclic anhydride ring of purpurin-18 ( 2 ). Compounds ( 1 ) exhibit strong absorption at long wavelengths near λmax 700 nm to take full advantage of greater tissue penetration. Methods Pheophorbide a ( 3 ) was obtained by acid hydrolysis of chlorophylla,which was from crude chlorophyll extracts of Chinese traditional herb named Silkworm excrement. Purpurin-18 ( 2 ) was prepared by air oxidation and alkali open loop simultaneously on five-membered beta-keto carboxylic ester ring of pheophorbide a ( 3 ). Finally,the target compounds 1a ~ 1j were synthesized via condensation of its anhydride ring with various amines including carboxyl-protected amino acids. Results Target compounds 1a ~ 1j were successfully synthesized in yields ranged from 32.6% to 65.2%. Their structures were confirmed by elemental analysis,ESI-MS and 1H NMR spectra. Conclusion Treatment of purpurin-18 ( 2 ) with amines can produce target compounds 1a ~ 1j . The starting raw material was inexpensive and readily available. The reaction conditions were mild and workup was convinient.
2017, 35(1): 31-35.
doi: 10.3969/j.issn.1006-0111.2017.01.008
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Objective To prepare micronized nimodipine push-pull osmotic pump (PPOP) controlled release tablets. Methods The nimodipine as a model drug, micronization technique was applied to the PPOP method. Designed and prepared the controlled release of the nimodipine tablet for 12 hours in vitro. The factor f2 was used to evaluate the similarities of different dissolution profiles, and the optimal formulation was performed. Results The micronized nimodipine PPOP controlled release tablets were successfully prepared with excellent zero-order release characteristics. The PPOP tablet's release behavior was close to the zero-order release equation (r=0.998 4). Conclusions The controlled-release formulation was prepared successfully. Micronized technique combined with the PPOP method significantly increased the release of the nimodipine tablet, the poorly soluble drug, in vitro.
Objective To prepare micronized nimodipine push-pull osmotic pump (PPOP) controlled release tablets. Methods The nimodipine as a model drug, micronization technique was applied to the PPOP method. Designed and prepared the controlled release of the nimodipine tablet for 12 hours in vitro. The factor f2 was used to evaluate the similarities of different dissolution profiles, and the optimal formulation was performed. Results The micronized nimodipine PPOP controlled release tablets were successfully prepared with excellent zero-order release characteristics. The PPOP tablet's release behavior was close to the zero-order release equation (r=0.998 4). Conclusions The controlled-release formulation was prepared successfully. Micronized technique combined with the PPOP method significantly increased the release of the nimodipine tablet, the poorly soluble drug, in vitro.
2017, 35(1): 36-38,66.
doi: 10.3969/j.issn.1006-0111.2017.01.009
Abstract:
Objective To study the physicochemical properties of aqueous solution of surface active drug montelukast sodium (MS), which could provide experimental basis for further development of micelle or mixed micelle preparations. Methods Critical micelle concentration (CMC) of MS at different temperatures were determined by conductivity measurements. The absorbance and transmittance of MS aqueous solution were measured by UV at different sodium chloride concentration levels. The micelle stability was evaluated via high speed centrifugal. Results The CMC of MS aqueous solution at 25℃, 30℃, 35℃ were 0.75, 0.82, 0.90 mmol/L. The absorbance and transmittance of MS aqueous solution were affected by the sodium chloride concentration and the concentration of MS itself. It was observed that a clear solution was obtained when MS concentration >7.5 mmol/L and no precipitation was noticed even after high speed centrifugal. Conclusion Montelukast sodium is a surface active drug. Its solubility is related to MS concentration. The solubility is also sensitive to the temperature and the electrolyte concentration. These unique physicochemical properties could be used to develop micelle or mixed micelle pharmaceutical preparations.
Objective To study the physicochemical properties of aqueous solution of surface active drug montelukast sodium (MS), which could provide experimental basis for further development of micelle or mixed micelle preparations. Methods Critical micelle concentration (CMC) of MS at different temperatures were determined by conductivity measurements. The absorbance and transmittance of MS aqueous solution were measured by UV at different sodium chloride concentration levels. The micelle stability was evaluated via high speed centrifugal. Results The CMC of MS aqueous solution at 25℃, 30℃, 35℃ were 0.75, 0.82, 0.90 mmol/L. The absorbance and transmittance of MS aqueous solution were affected by the sodium chloride concentration and the concentration of MS itself. It was observed that a clear solution was obtained when MS concentration >7.5 mmol/L and no precipitation was noticed even after high speed centrifugal. Conclusion Montelukast sodium is a surface active drug. Its solubility is related to MS concentration. The solubility is also sensitive to the temperature and the electrolyte concentration. These unique physicochemical properties could be used to develop micelle or mixed micelle pharmaceutical preparations.
2017, 35(1): 39-42.
doi: 10.3969/j.issn.1006-0111.2017.01.010
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Objective To utilize and evaluate the resources of Abrus cantoniensis Hance (AC) and Abrus mollis Hance (AM) by analyzing and comparing their essential oils and fatty acids. Method The essential oils of AC and AM were extracted with the hydro distillation method. Fatty acids were obtained by petroleum ether extraction of the 95% ethanol concentrate.Fatty acid extract was further reacted with BSTFA for GC-MS analysis. Components were identified by searching NIST MS library. Result Forty-two and thirty-three chemical constituents were identified from the essential oil of AC and AM respectively, which accounted for 56.76% and 63.45% of their volatile components. (±)-α-terpinyl acetate are the common essential oils found in both AC and AM. Thirteen and fourteen chemical constituents were identified from the fatty acid extract of AC and AM respectively.AC and AM have different chemical components and compositions. Conclusion Our results provide a scientific basis for the bioactivities, quality control and resource utilization of AC and AM.
Objective To utilize and evaluate the resources of Abrus cantoniensis Hance (AC) and Abrus mollis Hance (AM) by analyzing and comparing their essential oils and fatty acids. Method The essential oils of AC and AM were extracted with the hydro distillation method. Fatty acids were obtained by petroleum ether extraction of the 95% ethanol concentrate.Fatty acid extract was further reacted with BSTFA for GC-MS analysis. Components were identified by searching NIST MS library. Result Forty-two and thirty-three chemical constituents were identified from the essential oil of AC and AM respectively, which accounted for 56.76% and 63.45% of their volatile components. (±)-α-terpinyl acetate are the common essential oils found in both AC and AM. Thirteen and fourteen chemical constituents were identified from the fatty acid extract of AC and AM respectively.AC and AM have different chemical components and compositions. Conclusion Our results provide a scientific basis for the bioactivities, quality control and resource utilization of AC and AM.
2017, 35(1): 43-47,53.
doi: 10.3969/j.issn.1006-0111.2017.01.011
Abstract:
Objective To confirm the hepatotoxicity of valproic acid (VPA) and its metabolites(2-propyl-4-pentenoic acid, 3-hydroxy valproic acid, 5-hydroxy valproic acid) on human liver cells. Methods Cells were divided into control group and VPA-treated group. The control group was conventionally cultured while the VPA-treated group was treated with valproic acid and its metabolites. The rate of cell proliferation was assayed by CCK 8 protocol. The mRNA levels of CYP1A1, CYP1A2, PCNA, Bax and Bcl-2 were measured by real time PCR. The correlated protein levels were measured by Western Blotting. The activity of LDH, AST and ALT were also detected. Results Compared to the control group, with the increases of concentrations and reaction time of VPA and its metabolites, the proliferation rate of L02-cell was reduced, the mRNA and protein levels of CYP1A1, CYP1A2, and Bax was increased, the mRNA and protein level of PCNA and Bcl-2 was decreased, AST, ALT, and LDH were also elevated in the treated group. Conclusion Valproic acid and its metabolites were positively related to hepatotoxicity.
Objective To confirm the hepatotoxicity of valproic acid (VPA) and its metabolites(2-propyl-4-pentenoic acid, 3-hydroxy valproic acid, 5-hydroxy valproic acid) on human liver cells. Methods Cells were divided into control group and VPA-treated group. The control group was conventionally cultured while the VPA-treated group was treated with valproic acid and its metabolites. The rate of cell proliferation was assayed by CCK 8 protocol. The mRNA levels of CYP1A1, CYP1A2, PCNA, Bax and Bcl-2 were measured by real time PCR. The correlated protein levels were measured by Western Blotting. The activity of LDH, AST and ALT were also detected. Results Compared to the control group, with the increases of concentrations and reaction time of VPA and its metabolites, the proliferation rate of L02-cell was reduced, the mRNA and protein levels of CYP1A1, CYP1A2, and Bax was increased, the mRNA and protein level of PCNA and Bcl-2 was decreased, AST, ALT, and LDH were also elevated in the treated group. Conclusion Valproic acid and its metabolites were positively related to hepatotoxicity.
2017, 35(1): 48-53.
doi: 10.3969/j.issn.1006-0111.2017.01.012
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Objective To explore the feasibility of bletilla striata polysaccharide as a drug delivery material. Method With hydrophobic cholesterol succinyl bletilla striata polysaccharide (CHSB) as the carrier, the model drug paclitaxel (PTX) loaded nanoparticles were prepared via dialysis method. The morphology of nanoparticles was observed by Transmission Electron Microscope (TEM). The particle size, distribution and zeta potential were characterized by Dynamic Light Scattering instrument (DLS). The entrapment efficiency, drug loading and in vitro release were determined by high performance liquid chromatography (HPLC). Differential Scanning Calorimetry (DSC) was used to confirm the drug form in the drug loaded nanoparticles. The in vitro antitumor activity of nanoparticles was assayed by MTT. The uptake of nanoparticles by QGY-7703 liver cancer cells was observed by fluorescence labeling method. Results The prepared nanoparticles had spherical shape with uniform particle size distribution. The drug was loaded in the interior of the nanoparticles. Drug loading and encapsulation efficiency were affected by the CHSB in certain range. The cytotoxicity of drug loaded nanoparticles on liver cancer cells was stronger than the free drug. The fluorescence of Rhodamine B labeled drug nanoparticles were observed in the cells. Conclusion Cholesterol succinyl bletilla striata polysaccharide (CHSB) is highly feasible as an insoluble drug carrier. It can be used as a potential Nano carrier material.
Objective To explore the feasibility of bletilla striata polysaccharide as a drug delivery material. Method With hydrophobic cholesterol succinyl bletilla striata polysaccharide (CHSB) as the carrier, the model drug paclitaxel (PTX) loaded nanoparticles were prepared via dialysis method. The morphology of nanoparticles was observed by Transmission Electron Microscope (TEM). The particle size, distribution and zeta potential were characterized by Dynamic Light Scattering instrument (DLS). The entrapment efficiency, drug loading and in vitro release were determined by high performance liquid chromatography (HPLC). Differential Scanning Calorimetry (DSC) was used to confirm the drug form in the drug loaded nanoparticles. The in vitro antitumor activity of nanoparticles was assayed by MTT. The uptake of nanoparticles by QGY-7703 liver cancer cells was observed by fluorescence labeling method. Results The prepared nanoparticles had spherical shape with uniform particle size distribution. The drug was loaded in the interior of the nanoparticles. Drug loading and encapsulation efficiency were affected by the CHSB in certain range. The cytotoxicity of drug loaded nanoparticles on liver cancer cells was stronger than the free drug. The fluorescence of Rhodamine B labeled drug nanoparticles were observed in the cells. Conclusion Cholesterol succinyl bletilla striata polysaccharide (CHSB) is highly feasible as an insoluble drug carrier. It can be used as a potential Nano carrier material.
2017, 35(1): 54-59.
doi: 10.3969/j.issn.1006-0111.2017.01.013
Abstract:
Objective Risk management is one of the strong measurements to ensure the conduction of new drug research and development (R&D) projects. Therefore, establishing a set of evaluation index system in the new drug R&D projects is of great significance to increase the project success rate. Methods By analyzing more than 20 new drug R&D projects of "the military science and technology major projects" in five years, the risk factors were induced, sorted and summed up, and a set of evaluation indicator was built up through Delphi method and experts interview. The quantitative study was completed through fuzzy comprehensive evaluation method. Results According to the different stages of new drug R&D projects, the risk assessment indictors and their weight were established. Conclusion These indicators are more objective and accurate which contribute to the risk control in the process of new drug R&D projects.
Objective Risk management is one of the strong measurements to ensure the conduction of new drug research and development (R&D) projects. Therefore, establishing a set of evaluation index system in the new drug R&D projects is of great significance to increase the project success rate. Methods By analyzing more than 20 new drug R&D projects of "the military science and technology major projects" in five years, the risk factors were induced, sorted and summed up, and a set of evaluation indicator was built up through Delphi method and experts interview. The quantitative study was completed through fuzzy comprehensive evaluation method. Results According to the different stages of new drug R&D projects, the risk assessment indictors and their weight were established. Conclusion These indicators are more objective and accurate which contribute to the risk control in the process of new drug R&D projects.
2017, 35(1): 60-63,69.
doi: 10.3969/j.issn.1006-0111.2017.01.014
Abstract:
Objective To establish a HPLC method for the assay of cyproheptadine hydrochloride and the related substances. Methods The HPLC was performed on an Agilent Eclipse XDB-C18 column (4.6 mm×250 mm, 5 μm) at the temperature of 25℃ with the mobile phase of acetonitrile-buffer Solution (Dissolve 2.16 g of sodium octane-1-sulfonate with about 500 ml of water and mix well. Add 10.0 ml of glacial acetic acid and 5.0 ml of triethylamine, and dilute with water to 1 000 ml, mix well and adjust to pH 7.0 with triethylamine) (85:15,V/V). The flow rate was 1.0 ml/min and detection wavelength was 286 nm. The injection volume was 10 μl. Results The calibration curves of cyproheptadine hydrochloride, impurity A, B and C showed good linear response in the range from 0.056 2 to 5.620 μg/ml (r=0.999 8), 0.052 4 to 5.240 μg/ml(r=1.000 0),0.050 3 to 5.032 μg/ml (r=0.999 9) and 0.053 2 to 5.316 μg/ml(r=0.999 8) respectively. The LOQs for cyproheptadine hydrochloride, impurity A, B and C were within 0.049-0.054 μg/ml, LODs were within 0.019-0.022 μg/ml with recovery between 98%-100%. RSD of repeatability was 5.5% (n=6). Conclusion This method gave an accurate and reliable results. It can be used for quality control of cyproheptadine hydrochloride.
Objective To establish a HPLC method for the assay of cyproheptadine hydrochloride and the related substances. Methods The HPLC was performed on an Agilent Eclipse XDB-C18 column (4.6 mm×250 mm, 5 μm) at the temperature of 25℃ with the mobile phase of acetonitrile-buffer Solution (Dissolve 2.16 g of sodium octane-1-sulfonate with about 500 ml of water and mix well. Add 10.0 ml of glacial acetic acid and 5.0 ml of triethylamine, and dilute with water to 1 000 ml, mix well and adjust to pH 7.0 with triethylamine) (85:15,V/V). The flow rate was 1.0 ml/min and detection wavelength was 286 nm. The injection volume was 10 μl. Results The calibration curves of cyproheptadine hydrochloride, impurity A, B and C showed good linear response in the range from 0.056 2 to 5.620 μg/ml (r=0.999 8), 0.052 4 to 5.240 μg/ml(r=1.000 0),0.050 3 to 5.032 μg/ml (r=0.999 9) and 0.053 2 to 5.316 μg/ml(r=0.999 8) respectively. The LOQs for cyproheptadine hydrochloride, impurity A, B and C were within 0.049-0.054 μg/ml, LODs were within 0.019-0.022 μg/ml with recovery between 98%-100%. RSD of repeatability was 5.5% (n=6). Conclusion This method gave an accurate and reliable results. It can be used for quality control of cyproheptadine hydrochloride.
2017, 35(1): 64-66.
doi: 10.3969/j.issn.1006-0111.2017.01.015
Abstract:
Objective To develop a HPLC method for determination of baicalin. Methods The separation was carried out on a Waters XBridge C18 column(4.6 mm×250 mm, 5 μm), the mobile phase was composed of acetonitrile and 0.8% formic acid (25:75), the detection wavelength was set at 276 nm, the flow rate was 1.0 ml/min, the column temperature was 30℃ and the injection volume was 10 μl. Results The linearity was obtained over 1.25-40 μg/ml(r=0.999 9) for baicalin. The RSD of precision were less than 2%. The average recovery was between 95% and 100%. Conclusion This HPLC method was simple, accuracy and suitable for the quality control of Biyanling capsule.
Objective To develop a HPLC method for determination of baicalin. Methods The separation was carried out on a Waters XBridge C18 column(4.6 mm×250 mm, 5 μm), the mobile phase was composed of acetonitrile and 0.8% formic acid (25:75), the detection wavelength was set at 276 nm, the flow rate was 1.0 ml/min, the column temperature was 30℃ and the injection volume was 10 μl. Results The linearity was obtained over 1.25-40 μg/ml(r=0.999 9) for baicalin. The RSD of precision were less than 2%. The average recovery was between 95% and 100%. Conclusion This HPLC method was simple, accuracy and suitable for the quality control of Biyanling capsule.
2017, 35(1): 67-69.
doi: 10.3969/j.issn.1006-0111.2017.01.016
Abstract:
Objective To determine the quercetin content in Folium Apocyni Veneti from different commercial markets and harvest time by HPLC. Methods The determination was performed on an Aglient Eclipse XDB-C18 column (250 mm×4.6 mm,5 μm)at 30℃ with a mobile phase composed of Methanol:0.1% phosphoric acid run at gradient elution; the detection wavelength was 360 nm. Results It is a better timing to harvest when the flower is turning fruit and the leaf color is turning from green to yellow. Our results have demonstrated that at that time, the content of quercetin in Folium Apocyni Veneti was relatively higher. In addition, this report also shows that the concentration of quercetin in most medicinal materials from domestic market complies with the requirement of the Pharmacopoeia, but there were still a small percent of samples that didn't meet the Pharmacopoeia standards. Conclusion We suggested that the quality supervision and inspection on Folium Apocyni Veneti needs to be strengthened.
Objective To determine the quercetin content in Folium Apocyni Veneti from different commercial markets and harvest time by HPLC. Methods The determination was performed on an Aglient Eclipse XDB-C18 column (250 mm×4.6 mm,5 μm)at 30℃ with a mobile phase composed of Methanol:0.1% phosphoric acid run at gradient elution; the detection wavelength was 360 nm. Results It is a better timing to harvest when the flower is turning fruit and the leaf color is turning from green to yellow. Our results have demonstrated that at that time, the content of quercetin in Folium Apocyni Veneti was relatively higher. In addition, this report also shows that the concentration of quercetin in most medicinal materials from domestic market complies with the requirement of the Pharmacopoeia, but there were still a small percent of samples that didn't meet the Pharmacopoeia standards. Conclusion We suggested that the quality supervision and inspection on Folium Apocyni Veneti needs to be strengthened.
2017, 35(1): 70-72.
doi: 10.3969/j.issn.1006-0111.2017.01.017
Abstract:
Objective To discuss the evaluation method of anti-infective therapy by clinical pharmacist. Methods Anti-infection therapy for an AECOPD patient in department of respiration in our hospital was analyzed to discuss the evaluation method of anti- infective therapy. Results The patient had indication to use antibacterial, and combination of Amikacin and Piperacillin-sulbactam were selected as initial empirical treatment for common respiratory G--bacilli including drug resistant of Pseudomonas aeruginosa, which was rationality. But the whole process of using the initial combination linked to the hospital was unreasonable. Conclusion To evaluate the rationality of anti-infection treatment, the indication to use antibacterial need to be determined firstly, and combined with the severity of the patient, prior treatment, etiology of the site of infection, and choice of antibiotics to evaluate the rationality of initial empiric regimen secondly. For etiology positive results, the efficacy of initial empiric therapy, interpretation of etiology results and the clinical significance, guidelines recommend should be combined, following-up selection of drug to evaluate the rationality of follow-up treatment.
Objective To discuss the evaluation method of anti-infective therapy by clinical pharmacist. Methods Anti-infection therapy for an AECOPD patient in department of respiration in our hospital was analyzed to discuss the evaluation method of anti- infective therapy. Results The patient had indication to use antibacterial, and combination of Amikacin and Piperacillin-sulbactam were selected as initial empirical treatment for common respiratory G--bacilli including drug resistant of Pseudomonas aeruginosa, which was rationality. But the whole process of using the initial combination linked to the hospital was unreasonable. Conclusion To evaluate the rationality of anti-infection treatment, the indication to use antibacterial need to be determined firstly, and combined with the severity of the patient, prior treatment, etiology of the site of infection, and choice of antibiotics to evaluate the rationality of initial empiric regimen secondly. For etiology positive results, the efficacy of initial empiric therapy, interpretation of etiology results and the clinical significance, guidelines recommend should be combined, following-up selection of drug to evaluate the rationality of follow-up treatment.
2017, 35(1): 73-74,81.
doi: 10.3969/j.issn.1006-0111.2017.01.018
Abstract:
Objective To investigate the analgesia effects of dynastat in hepatic cancer patients after liver resection. Methods From June to December of year 2015, we collected 200 cases of hepatic cancer operation in the Eastern Hepatobiliary Surgery Hospital retrospectively. Those patients were divided into 2 groups (the dynastat treated group, n=100; the untreated group, n=100).The patients in treated group were given dynastat 3 times (40 mg/5 ml,iv, 6 hours,18 hours and 30 hours after operation respectively), while the control group did not received any dynastat. The sufentanil analgesia pumps were used in both groups. The treated group received a lower sufentanil dose. The pain severity (VAS score) of patients and the postoperative untoward effects were compared between these two groups. The results were analyzed statistically. Results The VAS score and the postoperative untoward effects of the treated group were clearly lower than the control group. All differences have statistical significance(P<0.05) Conclusions As a new-type selective COX-2 inhibitor for injection, dynastat can reduce the dosage and side effects of opioid medicine. It deserves to be popularized in post operation analgesia.
Objective To investigate the analgesia effects of dynastat in hepatic cancer patients after liver resection. Methods From June to December of year 2015, we collected 200 cases of hepatic cancer operation in the Eastern Hepatobiliary Surgery Hospital retrospectively. Those patients were divided into 2 groups (the dynastat treated group, n=100; the untreated group, n=100).The patients in treated group were given dynastat 3 times (40 mg/5 ml,iv, 6 hours,18 hours and 30 hours after operation respectively), while the control group did not received any dynastat. The sufentanil analgesia pumps were used in both groups. The treated group received a lower sufentanil dose. The pain severity (VAS score) of patients and the postoperative untoward effects were compared between these two groups. The results were analyzed statistically. Results The VAS score and the postoperative untoward effects of the treated group were clearly lower than the control group. All differences have statistical significance(P<0.05) Conclusions As a new-type selective COX-2 inhibitor for injection, dynastat can reduce the dosage and side effects of opioid medicine. It deserves to be popularized in post operation analgesia.
2017, 35(1): 75-77.
doi: 10.3969/j.issn.1006-0111.2017.01.019
Abstract:
Objective To evaluate the effects of fentanyl transdermal combined with morphine subcutaneous injection in the management of advanced liver cancer pain after intervention. Methods 166 patients who suffered from advanced liver cancer and received intervention therapy in our hospital were divided into two groups. 89 patients belong to the fentanyl transdermal combined with morphine subcutaneous injection treatment group. 77 patients belong to the morphine subcutaneous injection treatment group. The pain score and the remission rate of the two groups were compared and analyzed statistically. Meanwhile, the side effects of each group were recorded. Results Pain score in the group with fentanyl transdermal and morphine treatment was significantly lower than morphine mono therapy. 12 hours after intervention therapy, (1.97±0.56 for combination treatment vs 3.23±1.49 for morphine only group, P<0.05). 24 hours after intervention therapy, (1.63±0.44 for combination vs 4.19±1.68 for morphine only group, P<0.01). Similarly, the remission rate of the fentanyl transdermal combined with morphine subcutaneous injection group improved significantly, (92.1% vs 76.6% P<0.05) 12 hours after intervention therapy, and(97.8% vs 70.1%, P<0.05) 24 hours after intervention therapy. Conclusions The addition of fentanyl transdermal to morphine subcutaneous injection treatment significantly improve the pain remission rate for the patients with advanced liver cancer pain 72 hours after intervention therapy.
Objective To evaluate the effects of fentanyl transdermal combined with morphine subcutaneous injection in the management of advanced liver cancer pain after intervention. Methods 166 patients who suffered from advanced liver cancer and received intervention therapy in our hospital were divided into two groups. 89 patients belong to the fentanyl transdermal combined with morphine subcutaneous injection treatment group. 77 patients belong to the morphine subcutaneous injection treatment group. The pain score and the remission rate of the two groups were compared and analyzed statistically. Meanwhile, the side effects of each group were recorded. Results Pain score in the group with fentanyl transdermal and morphine treatment was significantly lower than morphine mono therapy. 12 hours after intervention therapy, (1.97±0.56 for combination treatment vs 3.23±1.49 for morphine only group, P<0.05). 24 hours after intervention therapy, (1.63±0.44 for combination vs 4.19±1.68 for morphine only group, P<0.01). Similarly, the remission rate of the fentanyl transdermal combined with morphine subcutaneous injection group improved significantly, (92.1% vs 76.6% P<0.05) 12 hours after intervention therapy, and(97.8% vs 70.1%, P<0.05) 24 hours after intervention therapy. Conclusions The addition of fentanyl transdermal to morphine subcutaneous injection treatment significantly improve the pain remission rate for the patients with advanced liver cancer pain 72 hours after intervention therapy.
2017, 35(1): 78-81.
doi: 10.3969/j.issn.1006-0111.2017.01.020
Abstract:
Objective To review the package inserts of children's common antineoplastic agents in Shanghai, identify problems, and seek countermeasures. Methods Reference summarizing and data analysis were used. Results The labeling rate of dosage for children in package inserts was only 38.2%. There were no uniform standards for dosage modification. 70.6% of package inserts used the following ambiguous words to describe children dosage, such as "no reliable reference" or "activity and safety are uncertain". Only a few package inserts used words like "use with caution" or "not recommend" or "contraindicated". Conclusion The off-label use of children's anti-tumor medications is unavoidable due to the limited children dosage information in the package inserts. We recommend that hospital should have a protocol for off-label use which should be examined by the ethics committee. The off-label uses and package insert standardization should be regulated by the related departments in the government. Pharmaceutical manufacturers are encouraged to carry out post market research on children's drug.
Objective To review the package inserts of children's common antineoplastic agents in Shanghai, identify problems, and seek countermeasures. Methods Reference summarizing and data analysis were used. Results The labeling rate of dosage for children in package inserts was only 38.2%. There were no uniform standards for dosage modification. 70.6% of package inserts used the following ambiguous words to describe children dosage, such as "no reliable reference" or "activity and safety are uncertain". Only a few package inserts used words like "use with caution" or "not recommend" or "contraindicated". Conclusion The off-label use of children's anti-tumor medications is unavoidable due to the limited children dosage information in the package inserts. We recommend that hospital should have a protocol for off-label use which should be examined by the ethics committee. The off-label uses and package insert standardization should be regulated by the related departments in the government. Pharmaceutical manufacturers are encouraged to carry out post market research on children's drug.
2017, 35(1): 82-86.
doi: 10.3969/j.issn.1006-0111.2017.01.021
Abstract:
Objective To evaluate the efficacy and safety of amrubicin for small-cell lung cancer(SCLC). Methods PubMed, Embase, the Cochrane Library and CNKI were searched to collect amrubicin data in the treatment of SCLC. A Meta-analysis was performed over the published clinical trials. The efficacy and safety of amrubicin were evaluated based on overall survival (OS), progression-free survival (PFS), overall response rate (ORR) and toxicity. Results Our analysis for 6 clinical trials indicated that amrubicin had significantly higher ORR than control group[RR 1.72,95% CI (1.39, 2.14),P=0.000], the OS, PFS and toxicity were no-inferior to the control group(P=0.405,P=0.456). Conclusion Amrubicin can be considered as a good second-line treatment for relapsed SCLC.
Objective To evaluate the efficacy and safety of amrubicin for small-cell lung cancer(SCLC). Methods PubMed, Embase, the Cochrane Library and CNKI were searched to collect amrubicin data in the treatment of SCLC. A Meta-analysis was performed over the published clinical trials. The efficacy and safety of amrubicin were evaluated based on overall survival (OS), progression-free survival (PFS), overall response rate (ORR) and toxicity. Results Our analysis for 6 clinical trials indicated that amrubicin had significantly higher ORR than control group[RR 1.72,95% CI (1.39, 2.14),P=0.000], the OS, PFS and toxicity were no-inferior to the control group(P=0.405,P=0.456). Conclusion Amrubicin can be considered as a good second-line treatment for relapsed SCLC.
2017, 35(1): 87-88,93.
doi: 10.3969/j.issn.1006-0111.2017.01.022
Abstract:
Objective To understand outpatient's attention and comprehension to package insert in the grassroots hospital. Methods 608 outpatients were randomly selected to answer the questionnaires designed with relevant data. Results Patients paid the highest attention to effective period, indication, adverse reactions and dosage in package insert with rate above 80%. The comprehension rate was low. Only three items (indication, dosage and expiration date) were above 30%. Patient's capability to understand package insert is related to their educational level and the area they live (urban area verse rural area). Conclusion Patient's attention to package insert is high, but comprehension level is low. We recommend that package insert should be written in the way of easy to understand for patients. Pharmacists should play an importent role in teaching patients rational drug use to ensure medication safety.
Objective To understand outpatient's attention and comprehension to package insert in the grassroots hospital. Methods 608 outpatients were randomly selected to answer the questionnaires designed with relevant data. Results Patients paid the highest attention to effective period, indication, adverse reactions and dosage in package insert with rate above 80%. The comprehension rate was low. Only three items (indication, dosage and expiration date) were above 30%. Patient's capability to understand package insert is related to their educational level and the area they live (urban area verse rural area). Conclusion Patient's attention to package insert is high, but comprehension level is low. We recommend that package insert should be written in the way of easy to understand for patients. Pharmacists should play an importent role in teaching patients rational drug use to ensure medication safety.
2017, 35(1): 89-93.
doi: 10.3969/j.issn.1006-0111.2017.01.023
Abstract:
Objective To investigate how the clinical pharmacists participate in the regime design and adjustment in the treatment of infectious disease and to show how clinical pharmacists to team with physicians for patient's infection control by contributing their special knowledge. Method From August 2012 to April 2014, 141 patients were consulted by the clinical pharmacists for the infectious diseases. The patient's basic information, ward distribution, consultation purpose, etiology of infections and adoption of the suggestions were analyzed. Results Among 141 consulted cases, most patients belonged to the urology, hepatobiliary surgery and neurosurgery department (accounted for 26.95%, 21.99% and 17.73% respectively). The top three consultation subjects are the use of ‘special use class’ antimicrobials, regime adjustment and medication choice (accounted for 85.82%, 74.62% and 59.57%). 133 suggestions from clinical pharmacists were accepted, 1 was partially adopted and 7 were rejected (accounted for 94.33%, 0.71% and 4.96%). Conclusion The clinical pharmacists play important roles in the treatment of infectious disease by providing the consultations to clinicians. With their special knowledge, clinical pharmacists can make a good contribution to ensure the safe and effective drug therapies.
Objective To investigate how the clinical pharmacists participate in the regime design and adjustment in the treatment of infectious disease and to show how clinical pharmacists to team with physicians for patient's infection control by contributing their special knowledge. Method From August 2012 to April 2014, 141 patients were consulted by the clinical pharmacists for the infectious diseases. The patient's basic information, ward distribution, consultation purpose, etiology of infections and adoption of the suggestions were analyzed. Results Among 141 consulted cases, most patients belonged to the urology, hepatobiliary surgery and neurosurgery department (accounted for 26.95%, 21.99% and 17.73% respectively). The top three consultation subjects are the use of ‘special use class’ antimicrobials, regime adjustment and medication choice (accounted for 85.82%, 74.62% and 59.57%). 133 suggestions from clinical pharmacists were accepted, 1 was partially adopted and 7 were rejected (accounted for 94.33%, 0.71% and 4.96%). Conclusion The clinical pharmacists play important roles in the treatment of infectious disease by providing the consultations to clinicians. With their special knowledge, clinical pharmacists can make a good contribution to ensure the safe and effective drug therapies.
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