2013 Vol. 31, No. 5
Display Method:
2013, 31(5): 321-325,379.
doi: 10.3969/j.issn.1006-0111.2013.05.001
Abstract:
Objective To review recent progress of antifungal drug targets and their inhibitors. Methods Literatures in recent five years were analyzed in combination of the authors'own research work and recent developments of antifungal targets and inhibitors were summarized. Results Current research focused on lanosterol 14-demethylase, β-1,3-glucan synthase, N-myristoyltransferase and secreted aspartic protease. The inhibitors of these targets showed promising future for the development of new antifungal drugs. Conclusion Optimizing the chemical structures of current antifungal agents and discover lead compounds with novel mode of action are of great importance to develop new generation of antifungal agents.
Objective To review recent progress of antifungal drug targets and their inhibitors. Methods Literatures in recent five years were analyzed in combination of the authors'own research work and recent developments of antifungal targets and inhibitors were summarized. Results Current research focused on lanosterol 14-demethylase, β-1,3-glucan synthase, N-myristoyltransferase and secreted aspartic protease. The inhibitors of these targets showed promising future for the development of new antifungal drugs. Conclusion Optimizing the chemical structures of current antifungal agents and discover lead compounds with novel mode of action are of great importance to develop new generation of antifungal agents.
2013, 31(5): 326-329.
doi: 10.3969/j.issn.1006-0111.2013.05.002
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In recent years, the increasing incidence of ischemic disease, especially for myocardial ischemia and other vascular diseases had become one of the most important causes of human death. Therapeutic angiogenesis attracted many scientists' attention, a large amount of studies showed that more and more traditional Chinese medicine extracts and natural products with bioactivities and prescriptions were effective in angiogenesis. the literatures at home and abroad of researching on angiogenesis were summarize and analyzed for further more studies.
In recent years, the increasing incidence of ischemic disease, especially for myocardial ischemia and other vascular diseases had become one of the most important causes of human death. Therapeutic angiogenesis attracted many scientists' attention, a large amount of studies showed that more and more traditional Chinese medicine extracts and natural products with bioactivities and prescriptions were effective in angiogenesis. the literatures at home and abroad of researching on angiogenesis were summarize and analyzed for further more studies.
2013, 31(5): 330-333,350.
doi: 10.3969/j.issn.1006-0111.2013.05.003
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The lack of folic acid which could cause hyperhomocysteine had revealed an obviously relationship with cardiovascular and cerebrovascular diseases. Plenty of studies had shown that hyperhomocysteine was an independent risk factor of cardiovascular and cerebrovascular diseases. Folic acid supplementation might be an effective method to decrease homocysteine and prevent cardiovascular and cerebrovascular diseases,while some studies question about it. So there was a new challenge of folic acid on prevention of cardiovascular and cerebrovascular diseases.
The lack of folic acid which could cause hyperhomocysteine had revealed an obviously relationship with cardiovascular and cerebrovascular diseases. Plenty of studies had shown that hyperhomocysteine was an independent risk factor of cardiovascular and cerebrovascular diseases. Folic acid supplementation might be an effective method to decrease homocysteine and prevent cardiovascular and cerebrovascular diseases,while some studies question about it. So there was a new challenge of folic acid on prevention of cardiovascular and cerebrovascular diseases.
2013, 31(5): 334-337.
doi: 10.3969/j.issn.1006-0111.2013.05.004
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Objective To evaluate the differential proteomics of human keratinocytes with transient receptor potential vanilloid-1(TRPV1) activated by capsaicin. Methods Human keratinocytes were cultured and treated by capsaicin. Two-dimensional polyacrylamide gel electrophoresis(2D-PAGE) combined with MALDI-TOF/TOF identification were used to investigate the effect of TRPV1 activation on the proteome of keratinocytes. Results Compared with blank control, triosephosphate isomerase(TPI), enolase 1,6-phosphogluconolactonase, cathepsin D had higher expression in peritoneal macrophages of experimental endometriosis, while keratin 14 and 60 S acidic ribosomal protein P2 expressed lower. Conclusion It was revealed that there was a potential mechanism of TRPV1 activation in keratinocytes, which gave a new sight to find targets and screen drugs in skin disorders.
Objective To evaluate the differential proteomics of human keratinocytes with transient receptor potential vanilloid-1(TRPV1) activated by capsaicin. Methods Human keratinocytes were cultured and treated by capsaicin. Two-dimensional polyacrylamide gel electrophoresis(2D-PAGE) combined with MALDI-TOF/TOF identification were used to investigate the effect of TRPV1 activation on the proteome of keratinocytes. Results Compared with blank control, triosephosphate isomerase(TPI), enolase 1,6-phosphogluconolactonase, cathepsin D had higher expression in peritoneal macrophages of experimental endometriosis, while keratin 14 and 60 S acidic ribosomal protein P2 expressed lower. Conclusion It was revealed that there was a potential mechanism of TRPV1 activation in keratinocytes, which gave a new sight to find targets and screen drugs in skin disorders.
2013, 31(5): 338-343,346.
doi: 10.3969/j.issn.1006-0111.2013.05.005
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Objective To establish a population pharmacokinetic (PPK) model of metformin in healthy Chinese subjects, and evaluate the effect of different physiological factors on pharmacokinetic parameters of metformin. Methods A single dose, open label PK study was designed to assess the pharmacokinetics of metformin in healthy Chinese subjects (11 male and 9 female subjects). After 1 000 mg single dose of metformin sustained release tablets being taken, 0~24 h blood samples of each subject were collected. Concentration of plasma metformin was measured by the LC-MS/MS method. Non-compartment analysis was carried out through Winonlin 5.01 software. A PPK model in healthy Chinese subjects was established by using NONMEM. The effects of body weight and other physiological factors on metformin pharmacokinetics were assessed. Results One-compartment model with first-order absorption was the best for the PPK of metformin and the CL/F, Vd/F and Ka were (95.8±7.46) L/h, (553±45.9) L, and (0.596±0.070)/h, respectively. It was proved that, the simulation of model improved significantly (P<0.05) when body weight was used as the covariate of CL/F and Vd/F. Conclusion The PPK method could be used in the metformin pharmacokinetic study and body weight had statistically significant effect on the clearance of metformin.
Objective To establish a population pharmacokinetic (PPK) model of metformin in healthy Chinese subjects, and evaluate the effect of different physiological factors on pharmacokinetic parameters of metformin. Methods A single dose, open label PK study was designed to assess the pharmacokinetics of metformin in healthy Chinese subjects (11 male and 9 female subjects). After 1 000 mg single dose of metformin sustained release tablets being taken, 0~24 h blood samples of each subject were collected. Concentration of plasma metformin was measured by the LC-MS/MS method. Non-compartment analysis was carried out through Winonlin 5.01 software. A PPK model in healthy Chinese subjects was established by using NONMEM. The effects of body weight and other physiological factors on metformin pharmacokinetics were assessed. Results One-compartment model with first-order absorption was the best for the PPK of metformin and the CL/F, Vd/F and Ka were (95.8±7.46) L/h, (553±45.9) L, and (0.596±0.070)/h, respectively. It was proved that, the simulation of model improved significantly (P<0.05) when body weight was used as the covariate of CL/F and Vd/F. Conclusion The PPK method could be used in the metformin pharmacokinetic study and body weight had statistically significant effect on the clearance of metformin.
2013, 31(5): 344-346.
doi: 10.3969/j.issn.1006-0111.2013.05.006
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Objective To develop and evaluate the stable method for the determination of impurity D (kanamycin) in amikacin sulfate injection with pre-column derivatization HPLC. Methods The lower concentration of sample was used. An Agilent ZORBAX SB-C18 column(4.6 mmá150 mm, 5 μm) was used for the chromatographic separations. The mobile phase consisted of mixture of a 2.7% solution of potassium dihydrogen phosphate adjusted to pH 6.5 (using 22 g/L solution of potassium hydroxide) and methanol (30:70, v/v). The flow rate was 1 ml/min. A 50μl volume of each sample was injected. The column temperature was maintained at 30℃. Results The linear range of kanamycin was 2~80 μg/ml (r=0.999 8), accuracy was (93.08±9.65)%. Conclusions The development method was successfully applied to the quantitative determination of kanamycin in amikacin sulfate injection and also offered a new perspective for safety evaluation of amikacin sulfate injection.
Objective To develop and evaluate the stable method for the determination of impurity D (kanamycin) in amikacin sulfate injection with pre-column derivatization HPLC. Methods The lower concentration of sample was used. An Agilent ZORBAX SB-C18 column(4.6 mmá150 mm, 5 μm) was used for the chromatographic separations. The mobile phase consisted of mixture of a 2.7% solution of potassium dihydrogen phosphate adjusted to pH 6.5 (using 22 g/L solution of potassium hydroxide) and methanol (30:70, v/v). The flow rate was 1 ml/min. A 50μl volume of each sample was injected. The column temperature was maintained at 30℃. Results The linear range of kanamycin was 2~80 μg/ml (r=0.999 8), accuracy was (93.08±9.65)%. Conclusions The development method was successfully applied to the quantitative determination of kanamycin in amikacin sulfate injection and also offered a new perspective for safety evaluation of amikacin sulfate injection.
2013, 31(5): 347-350.
doi: 10.3969/j.issn.1006-0111.2013.05.007
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Objective To construct the recombinant adenovirus expression vector containing ribosomal protein RPS3a and detect its expression in NIH3T3 cells. Method The RPS3a gene was obtained by RT-PCR.,total RNA was extracted from human HEK293 cell as the template. The cDNA fragments were cloned into the shuttle vector pAdTrack-CMV. After identified by enzyme digested and DNA sequence analysis,the product pAdTrack-RPS3a was lineared by PmeI and transformed into competent E.Coli BJ5183 carrying backbone plasmid pAdeasy-1 for homologous recombination. The identified positive recombinant adenoviral plasmid was then lineared by PacI and transfected into 293 cells for packaging and amplifying. Western blotting was used to detect the expression of RPS3a protein in the NIH3T3 cells infected with adenovirus. Results The pAdTrack-RPS3a and pAd-RPS3a plasmids had been successfully constructed. Protein expression was markedly increased in the NIH3T3 cells infected with Ad-RPS3a compared to that with control Ad-GFP. Conclusion The recombinant adenovirus harboring the RPS3a gene was successfully constructed, which could provide a useful tool for further investigating its biological function.
Objective To construct the recombinant adenovirus expression vector containing ribosomal protein RPS3a and detect its expression in NIH3T3 cells. Method The RPS3a gene was obtained by RT-PCR.,total RNA was extracted from human HEK293 cell as the template. The cDNA fragments were cloned into the shuttle vector pAdTrack-CMV. After identified by enzyme digested and DNA sequence analysis,the product pAdTrack-RPS3a was lineared by PmeI and transformed into competent E.Coli BJ5183 carrying backbone plasmid pAdeasy-1 for homologous recombination. The identified positive recombinant adenoviral plasmid was then lineared by PacI and transfected into 293 cells for packaging and amplifying. Western blotting was used to detect the expression of RPS3a protein in the NIH3T3 cells infected with adenovirus. Results The pAdTrack-RPS3a and pAd-RPS3a plasmids had been successfully constructed. Protein expression was markedly increased in the NIH3T3 cells infected with Ad-RPS3a compared to that with control Ad-GFP. Conclusion The recombinant adenovirus harboring the RPS3a gene was successfully constructed, which could provide a useful tool for further investigating its biological function.
2013, 31(5): 351-354.
doi: 10.3969/j.issn.1006-0111.2013.05.008
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Objective To study the chemical constituents and antioxidant activityof the root tubers of Cynanchum auriculatum Royle ex Wight (asclepiadaceae). Methods The root tubers were extracted with 95% EtOH, and the ethanol extract was further separated and purified by repeated column chromatography of silica gel and Sephadex LH-20. Structures of the compounds were identified on the basis of spectral analysis (including NMR and MS) and chemical evidences. Results Five acetophenones were isolated from Cynanchum auriculatum Royle ex Wight. Their structures were characterized as cynandione A (I), cynandione B (II), cynandione C (III), cynanchone A (IV), cynantetrone (V). H2O2 decreases SOD, CAT and GSH-Px activities, while the acetophenones could inhibit H2O2-induced oxidative damage. Conclusion The acetophenones isolated from the root tubers of Cynanchum auriculatum Royle ex Wight possessed potent antioxidant activities.
Objective To study the chemical constituents and antioxidant activityof the root tubers of Cynanchum auriculatum Royle ex Wight (asclepiadaceae). Methods The root tubers were extracted with 95% EtOH, and the ethanol extract was further separated and purified by repeated column chromatography of silica gel and Sephadex LH-20. Structures of the compounds were identified on the basis of spectral analysis (including NMR and MS) and chemical evidences. Results Five acetophenones were isolated from Cynanchum auriculatum Royle ex Wight. Their structures were characterized as cynandione A (I), cynandione B (II), cynandione C (III), cynanchone A (IV), cynantetrone (V). H2O2 decreases SOD, CAT and GSH-Px activities, while the acetophenones could inhibit H2O2-induced oxidative damage. Conclusion The acetophenones isolated from the root tubers of Cynanchum auriculatum Royle ex Wight possessed potent antioxidant activities.
2013, 31(5): 355-356.
doi: 10.3969/j.issn.1006-0111.2013.05.009
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Objective To observe clinical efficacy of budesonide suspension for inhalation (pulmicort respules) for treatment of upper airway cough syndrome. Methods The treatment group(31 patients) used 1mg budesonide suspension for inhalation partly by atomization inhalation via mask nose and mouth, which were used 2 times a day and course of two weeks. The control group (30 patients) were not used budesonide aerosol at all. At the same time, the two groups were added in oral loratadine 1 time a day and gino capsule 3 times a day and course of two weeks. Symptoms changes of twogroups used medication for 2 courses were observed before and after treatment. Results The overall effect of the patients treated with an effective rate of 96.8%, significantly better than the control group, which had a effective rate of 53.3%. (P<0.05). Conclusions Treatment of upper airway cough syndrome by aerosol inhalation budesonide suspension was effective, and the onset time and efficacy were higher than that in the control group.
Objective To observe clinical efficacy of budesonide suspension for inhalation (pulmicort respules) for treatment of upper airway cough syndrome. Methods The treatment group(31 patients) used 1mg budesonide suspension for inhalation partly by atomization inhalation via mask nose and mouth, which were used 2 times a day and course of two weeks. The control group (30 patients) were not used budesonide aerosol at all. At the same time, the two groups were added in oral loratadine 1 time a day and gino capsule 3 times a day and course of two weeks. Symptoms changes of twogroups used medication for 2 courses were observed before and after treatment. Results The overall effect of the patients treated with an effective rate of 96.8%, significantly better than the control group, which had a effective rate of 53.3%. (P<0.05). Conclusions Treatment of upper airway cough syndrome by aerosol inhalation budesonide suspension was effective, and the onset time and efficacy were higher than that in the control group.
2013, 31(5): 357-358,395.
doi: 10.3969/j.issn.1006-0111.2013.05.010
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Objective To evaluate the value and safety of combined therapy of growth hormone and gonadotropin on male delayed puberty caused by hypogonadotropic hypogonadism. Methods A retrospective analysis was undergoing in Shanghai First Maternity and Infant Hospital from 2010 Jun to 2012 May. 28 cases with male delayed puberty caused by hypogonadotropic hypogonadism were enrolled. The average age was (15.25±1.11) years. All the cases were given a combined therapy of human chorionic gonadotrophin, follicle stimulating hormone and growth hormone. After 3 months therapy, the growth condition such as sexual hormone levels, height, and volume of testis were recorded to inspect the treatment effect. Results All 28 cases had a follow-up visit. No short term complications occurred. The height and testosterone level was higher than which before therapy (P<0.05). And the volume of testis, follicle stimulating hormone and luteinizing hormone level were significantly higher than before the therapy. Conclusion Combined therapy of human chorionic gonadotrophin, follicle stimulating hormone and growth hormone could be a safe and effective method to treat male delayed puberty caused by hypogonadotropic hypogonadism.
Objective To evaluate the value and safety of combined therapy of growth hormone and gonadotropin on male delayed puberty caused by hypogonadotropic hypogonadism. Methods A retrospective analysis was undergoing in Shanghai First Maternity and Infant Hospital from 2010 Jun to 2012 May. 28 cases with male delayed puberty caused by hypogonadotropic hypogonadism were enrolled. The average age was (15.25±1.11) years. All the cases were given a combined therapy of human chorionic gonadotrophin, follicle stimulating hormone and growth hormone. After 3 months therapy, the growth condition such as sexual hormone levels, height, and volume of testis were recorded to inspect the treatment effect. Results All 28 cases had a follow-up visit. No short term complications occurred. The height and testosterone level was higher than which before therapy (P<0.05). And the volume of testis, follicle stimulating hormone and luteinizing hormone level were significantly higher than before the therapy. Conclusion Combined therapy of human chorionic gonadotrophin, follicle stimulating hormone and growth hormone could be a safe and effective method to treat male delayed puberty caused by hypogonadotropic hypogonadism.
2013, 31(5): 359-361,365.
doi: 10.3969/j.issn.1006-0111.2013.05.011
Abstract:
Objective To study the effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide. Methods The inhibitory effect of butenafine on ergosterol biosynthesis in whole-cell fungi was studied by measuring the incorporation of [1-14C] acetate into nonsaponifiable lipids( NSLs), while the effect in cell-free extracts was studied by measuring the incorporation of [2-14C] mevalonate into NSLs. Results The synthesis of ergosterol in fungi was significantly decreased after butenafine treatment, whereas the level of squalene was increased. The IC50 value of butenafine on ergosterol biosynthesis was 136.19 nmol/L in whole-cell study and 203.15 nmol/L in cell-free study. Conclusion The method to measure the incorporation of [1-14C]acetate and [2-14C] mevalonate into NSLs of fungi, which could indicate the level of squalene, might be widely used to study the mechanism of inhibitor of squalene epoxidase.
Objective To study the effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide. Methods The inhibitory effect of butenafine on ergosterol biosynthesis in whole-cell fungi was studied by measuring the incorporation of [1-14C] acetate into nonsaponifiable lipids( NSLs), while the effect in cell-free extracts was studied by measuring the incorporation of [2-14C] mevalonate into NSLs. Results The synthesis of ergosterol in fungi was significantly decreased after butenafine treatment, whereas the level of squalene was increased. The IC50 value of butenafine on ergosterol biosynthesis was 136.19 nmol/L in whole-cell study and 203.15 nmol/L in cell-free study. Conclusion The method to measure the incorporation of [1-14C]acetate and [2-14C] mevalonate into NSLs of fungi, which could indicate the level of squalene, might be widely used to study the mechanism of inhibitor of squalene epoxidase.
2013, 31(5): 362-365.
doi: 10.3969/j.issn.1006-0111.2013.05.012
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Objective To study the antioxidant effects of grape seed proanthocyanidins phospholipid complex(GSPPC). Methods Eighty rats were randomly divided into eight groups: normal control, model control, Proanthocyanidins, Soybean phospholipids, Vitamin C and low dose of GSPPC, moderate dose of GSPPC, and high dose of GSPPC. Drugs were given orally to rats once a day for 30 days. And then, 50% ethanol was given to rats once by oral gavages to make the ethanol oxidative damage model at the end of experiment. The body weight of rats was measured. The contents of MDA, Protein carbonyl (PC), SOD, GSH and GSH-PX in hepatic tissue and blood serum were detected. Results The results showed there were no significant differences in the body weight among the three GSPPC groups, normal control and model control(P>0.05). Compared with the model control group, the content of MDA in low dosage of the GSPPC group was decreased in blood serum and hepatic tissue(P<0.05), and the content of GSH-PX was increased in blood serum and hepatic tissue (P<0.05).Compared with the model control group, the contents of GSH, SOD and GSH-PX were increased in blood serum and hepatic tissue(P<0.05, P<0.01), the contents of MDA and PC in middle and high dosage of the GSPPC group were decreased in hepatic tissue and blood serum(P<0.05, P<0.01). Conclusion The GSPPC showed significantly antioxidant effect.
Objective To study the antioxidant effects of grape seed proanthocyanidins phospholipid complex(GSPPC). Methods Eighty rats were randomly divided into eight groups: normal control, model control, Proanthocyanidins, Soybean phospholipids, Vitamin C and low dose of GSPPC, moderate dose of GSPPC, and high dose of GSPPC. Drugs were given orally to rats once a day for 30 days. And then, 50% ethanol was given to rats once by oral gavages to make the ethanol oxidative damage model at the end of experiment. The body weight of rats was measured. The contents of MDA, Protein carbonyl (PC), SOD, GSH and GSH-PX in hepatic tissue and blood serum were detected. Results The results showed there were no significant differences in the body weight among the three GSPPC groups, normal control and model control(P>0.05). Compared with the model control group, the content of MDA in low dosage of the GSPPC group was decreased in blood serum and hepatic tissue(P<0.05), and the content of GSH-PX was increased in blood serum and hepatic tissue (P<0.05).Compared with the model control group, the contents of GSH, SOD and GSH-PX were increased in blood serum and hepatic tissue(P<0.05, P<0.01), the contents of MDA and PC in middle and high dosage of the GSPPC group were decreased in hepatic tissue and blood serum(P<0.05, P<0.01). Conclusion The GSPPC showed significantly antioxidant effect.
2013, 31(5): 366-367,383.
doi: 10.3969/j.issn.1006-0111.2013.05.013
Abstract:
Objective To prepare ropivacaine hydrochloride thermosensitive gel injection and establish the determination methods of contents. Methods Ropivacaine hydrochloride thermosensitive gel injection was prepared by cold methods with poloxamer as thermosensitive materials. The contents of ropivacaine hydrochloride were determined by RP-HPLC. Result The formulation contained 2% ropivacaine hydrochloride, poloxamer P407 and P188 (28:1) with phase-transition temperature of 37℃. Ropivacaine hydrochloride presented a good linearity in the range of 2.03~48.72 μg/ml (r=0.999 8), which had good precision, and reproducibility. The recovery rate of low, middle and high concentrations of ropivacaine hydrochloride were (99.58±0.20)%, (97.80±0.35)% and (103.60±0.63)%,n=3,respectively. The average contents of ropivacaine hydrochloride in three batches of sample were (98.92±0.35)%, (99.18±0.38)% and (98.72±0.62)%,n=3. Conclusion The quality of Ropivacaine hydrochloride thermosensitive gel injection with poloxamer as matrix could be controlled. It had a new development prospects for relieving pain.
Objective To prepare ropivacaine hydrochloride thermosensitive gel injection and establish the determination methods of contents. Methods Ropivacaine hydrochloride thermosensitive gel injection was prepared by cold methods with poloxamer as thermosensitive materials. The contents of ropivacaine hydrochloride were determined by RP-HPLC. Result The formulation contained 2% ropivacaine hydrochloride, poloxamer P407 and P188 (28:1) with phase-transition temperature of 37℃. Ropivacaine hydrochloride presented a good linearity in the range of 2.03~48.72 μg/ml (r=0.999 8), which had good precision, and reproducibility. The recovery rate of low, middle and high concentrations of ropivacaine hydrochloride were (99.58±0.20)%, (97.80±0.35)% and (103.60±0.63)%,n=3,respectively. The average contents of ropivacaine hydrochloride in three batches of sample were (98.92±0.35)%, (99.18±0.38)% and (98.72±0.62)%,n=3. Conclusion The quality of Ropivacaine hydrochloride thermosensitive gel injection with poloxamer as matrix could be controlled. It had a new development prospects for relieving pain.
2013, 31(5): 368-370.
doi: 10.3969/j.issn.1006-0111.2013.03.014
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Objective To establish a method for determining the microbial assays of doxycycline by turbidimetric method in order to provide a basis for further development. Methods Staphylococcus aureus was chosen as the test organism that the microbiological assay of doxycycline was determined by turbidimetric method while a comparision of turbidimetric method and cyclinder-plate was carried out. Results The linearity range of doxycycline was 1.0~3.3 u/ml( r=0.997 9).The average recoveries of doxycycline was 99.84%.The method had a good reproducible( RSD:0.42%).The microbiological assay of doxycycline pharmaceutical preparations were united which determined by turbidimetric method and cylinder-plate method. The confidence rates were also less than 5%. Conclusion The results indicated that the turbidimetric method could be used as quality control because of its convenience,accuracy and quickness.
Objective To establish a method for determining the microbial assays of doxycycline by turbidimetric method in order to provide a basis for further development. Methods Staphylococcus aureus was chosen as the test organism that the microbiological assay of doxycycline was determined by turbidimetric method while a comparision of turbidimetric method and cyclinder-plate was carried out. Results The linearity range of doxycycline was 1.0~3.3 u/ml( r=0.997 9).The average recoveries of doxycycline was 99.84%.The method had a good reproducible( RSD:0.42%).The microbiological assay of doxycycline pharmaceutical preparations were united which determined by turbidimetric method and cylinder-plate method. The confidence rates were also less than 5%. Conclusion The results indicated that the turbidimetric method could be used as quality control because of its convenience,accuracy and quickness.
2013, 31(5): 371-372,400.
doi: 10.3969/j.issn.1006-0111.2013.05.015
Abstract:
Objective To study the alcohol-soluble component abstraction procedure of Xinshu Granula. Methods The optional extraction process was selected for the yields of extracts & Tanshinone ⅡA by using L9(34) orthogonal design.The effects of alcohol concentration,alcohol amount,reflux time and times of reflux were observed. Results The optimal extraction process was determined by adding 90% alcohol,10 times the amount of Chinese medicinal materials,reflux extracting 2 times,1.5 hours per time. Conclusions The selected processing method was stable and feasible.
Objective To study the alcohol-soluble component abstraction procedure of Xinshu Granula. Methods The optional extraction process was selected for the yields of extracts & Tanshinone ⅡA by using L9(34) orthogonal design.The effects of alcohol concentration,alcohol amount,reflux time and times of reflux were observed. Results The optimal extraction process was determined by adding 90% alcohol,10 times the amount of Chinese medicinal materials,reflux extracting 2 times,1.5 hours per time. Conclusions The selected processing method was stable and feasible.
2013, 31(5): 373-376.
doi: 10.3969/j.issn.1006-0111.2013.05.016
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Objective To design and synthesis novel triazole antifungal derivatives and study the antifungal activity. Methods All the target compounds were prepared from 1,3-difluorobenzene via click reaction;The antibacterial activities of the title compounds were determined with broth dilution method. Results Twelve compounds were synthesized and characterized by 1H NMR and MS. All the title compounds exhibited potent antifungal activities against nearly all fungi tested. Conclusion The electronic effects of the substituents affected the activity of compounds, specifically the electron-donating groups.
Objective To design and synthesis novel triazole antifungal derivatives and study the antifungal activity. Methods All the target compounds were prepared from 1,3-difluorobenzene via click reaction;The antibacterial activities of the title compounds were determined with broth dilution method. Results Twelve compounds were synthesized and characterized by 1H NMR and MS. All the title compounds exhibited potent antifungal activities against nearly all fungi tested. Conclusion The electronic effects of the substituents affected the activity of compounds, specifically the electron-donating groups.
2013, 31(5): 377-379.
doi: 10.3969/j.issn.1006-0111.2013.05.017
Abstract:
Objective To improve the synthetic process of 2-methyl-5-methoxy benzoic acid ethyl ester. Methods The target compounds were prepared from 2-methyl-5-nitro-benzoic acid through esterification, reduction, diazotization hydrolysis and methylation. Results In the procedure of reduction, Pd/H2 system was replaced by Fe/AcOH with a yield of 92.7%. In the produce of methylation, potassium carbonate were used to take place of the NaH as deacid reagent with a yield of 89.1%. The yield of the new synthesis process was promoted from 75% to 89.1%. Conclusions This study provided a synthesis process route of 2-methyl-5-methoxy benzoic acid ethyl ester with simple operation, mild reaction condition, low price, which was suitable for the amplification of the preparation.
Objective To improve the synthetic process of 2-methyl-5-methoxy benzoic acid ethyl ester. Methods The target compounds were prepared from 2-methyl-5-nitro-benzoic acid through esterification, reduction, diazotization hydrolysis and methylation. Results In the procedure of reduction, Pd/H2 system was replaced by Fe/AcOH with a yield of 92.7%. In the produce of methylation, potassium carbonate were used to take place of the NaH as deacid reagent with a yield of 89.1%. The yield of the new synthesis process was promoted from 75% to 89.1%. Conclusions This study provided a synthesis process route of 2-methyl-5-methoxy benzoic acid ethyl ester with simple operation, mild reaction condition, low price, which was suitable for the amplification of the preparation.
2013, 31(5): 380-383.
doi: 10.3969/j.issn.1006-0111.2013.05.018
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Objective To establish a method for the simultaneous determination of vitamin C and vitamin B1 in ferrous fumarate granules. Methods The procedure was performed on the Insteril ODS-3 C18 column at 30℃, detected at 244 nm. The mobile phase was composed by a gradient of 0.03 mol/L of ammonium phosphate solution (in which 0.01% of sodium heptanesulfonate was added and the pH was adjusted to 3.0 by phosphoric acid) and methanol, with the flux at 0.6~1.0 ml/min. Results Either vitamin C or vitamin B1 was in good linear at 0.501~6.011 μg, r=1.0000 and 0.038~0.456 μg, r=0.999 9, respectively. The mean recoveries were 99.51% and 99.20%, with the RSD 0.55% and 0.49%, n=9. Conclusion The method was proved to be simple, accurate and reliable, appropriate for the quality control for vitamin C and vitamin B1 in ferrous fumarate granules.
Objective To establish a method for the simultaneous determination of vitamin C and vitamin B1 in ferrous fumarate granules. Methods The procedure was performed on the Insteril ODS-3 C18 column at 30℃, detected at 244 nm. The mobile phase was composed by a gradient of 0.03 mol/L of ammonium phosphate solution (in which 0.01% of sodium heptanesulfonate was added and the pH was adjusted to 3.0 by phosphoric acid) and methanol, with the flux at 0.6~1.0 ml/min. Results Either vitamin C or vitamin B1 was in good linear at 0.501~6.011 μg, r=1.0000 and 0.038~0.456 μg, r=0.999 9, respectively. The mean recoveries were 99.51% and 99.20%, with the RSD 0.55% and 0.49%, n=9. Conclusion The method was proved to be simple, accurate and reliable, appropriate for the quality control for vitamin C and vitamin B1 in ferrous fumarate granules.
2013, 31(5): 384-385,392.
doi: 10.3969/j.issn.1006-0111.2013.05.019
Abstract:
Objective To develop a method for determination of assiticoside in Centella asiatica and its formula particles. Methods Hypersil ODS C18 column was used(4.6 mmá250 mm,5 μm),withacetonitrile-water(v/v=3:8) as mobile phase, and a flow rate of 0.6 ml/min. Results The result showed that the calibration curve was linear in the range of 23.2~580.0 μg/ml for asiaticoside, intra-day and inter-day precision results were 2.1% and 3.6%, the average recovery of asiaticoside were 95.2%(RSD=3.2%, n=6) in centella asiatica and 104.6%(RSD=1.0%,n=6) in its formula particles. The contents of asiaticoside in 5 medicinal materials were 0.33%,0.52%,0.22%,0.28% and 0.39%;while in 5 formula particles were 0.40%,0.44%,0.39%,0.44% and 0.42%. Conclusions The method was simple and accurate for quality control of Centella asiatica and its formula particles.
Objective To develop a method for determination of assiticoside in Centella asiatica and its formula particles. Methods Hypersil ODS C18 column was used(4.6 mmá250 mm,5 μm),withacetonitrile-water(v/v=3:8) as mobile phase, and a flow rate of 0.6 ml/min. Results The result showed that the calibration curve was linear in the range of 23.2~580.0 μg/ml for asiaticoside, intra-day and inter-day precision results were 2.1% and 3.6%, the average recovery of asiaticoside were 95.2%(RSD=3.2%, n=6) in centella asiatica and 104.6%(RSD=1.0%,n=6) in its formula particles. The contents of asiaticoside in 5 medicinal materials were 0.33%,0.52%,0.22%,0.28% and 0.39%;while in 5 formula particles were 0.40%,0.44%,0.39%,0.44% and 0.42%. Conclusions The method was simple and accurate for quality control of Centella asiatica and its formula particles.
2013, 31(5): 386-387.
doi: 10.3969/j.issn.1006-0111.2013.05.020
Abstract:
Objective To establish a HPLC method for determination of stilbene glucoside in Yangxueanshen Pills. Methods The Waters C18 column (4.6 mm×250 mm, 5 μm) was used. The mobile phase was acetonitrile-water (20:80).The flow rate was 1.0 ml/min.The detection wavelength was 320 nm. Results The linear range was 0.086 7 μg~1.083 5 μg(r=0.999 8). The average recovery was 99.2% with RSD=1.1% (n=9). Conclusion The determination method was simple, accurate, sensitive and reproducible which could be used for quality control of Yangxueanshen Pills.
Objective To establish a HPLC method for determination of stilbene glucoside in Yangxueanshen Pills. Methods The Waters C18 column (4.6 mm×250 mm, 5 μm) was used. The mobile phase was acetonitrile-water (20:80).The flow rate was 1.0 ml/min.The detection wavelength was 320 nm. Results The linear range was 0.086 7 μg~1.083 5 μg(r=0.999 8). The average recovery was 99.2% with RSD=1.1% (n=9). Conclusion The determination method was simple, accurate, sensitive and reproducible which could be used for quality control of Yangxueanshen Pills.
2013, 31(5): 388-389.
doi: 10.3969/j.issn.1006-0111.2013.05.021
Abstract:
Objective To study the validity and affordability between joint venture entercavier and domestic entercavier in treating patients with chronic hepatitis B. Methods 65 patients with chronic hepatitis B were select who were treated with entercavier between Oct. 2009 to Oct.2010 in Ningbo No. 2 Hospital expert outpatient service. These patients were divide into group A (33 cases) and B(32 cases). Group A was treated with joint venture entecavier and group B was treated with domestic ones. all patients were given 0.5 mg daily and treated for 48 weeks. The cost-minimization analysis was made between two groups. Results ALT recovery rate, HBV-DNA negative conversion rate and HBeAg serum conversion rate had no statistically significant between two groups (P>0.05), but the cost of group A was 12 028.8, and the cost of group B was 7 996.8. Conclusions The domestic entecavier was better than the joint venture entecavier in treating the patients with chronic hepatitis B by cost-minimization analysis.
Objective To study the validity and affordability between joint venture entercavier and domestic entercavier in treating patients with chronic hepatitis B. Methods 65 patients with chronic hepatitis B were select who were treated with entercavier between Oct. 2009 to Oct.2010 in Ningbo No. 2 Hospital expert outpatient service. These patients were divide into group A (33 cases) and B(32 cases). Group A was treated with joint venture entecavier and group B was treated with domestic ones. all patients were given 0.5 mg daily and treated for 48 weeks. The cost-minimization analysis was made between two groups. Results ALT recovery rate, HBV-DNA negative conversion rate and HBeAg serum conversion rate had no statistically significant between two groups (P>0.05), but the cost of group A was 12 028.8, and the cost of group B was 7 996.8. Conclusions The domestic entecavier was better than the joint venture entecavier in treating the patients with chronic hepatitis B by cost-minimization analysis.
2013, 31(5): 390-392.
doi: 10.3969/j.issn.1006-0111.2013.05.022
Abstract:
Objective To summarize the experience and lessens after intervention in outpatient return drugs process. Methods Return-drugs prescriptions in 2011 and 2012 in our hospital were retrospectively analyzed, focusing on reasons of return drugs events and effects after intervention in return drugs process. Results After intervention in return drugs process since 2012, the outpatient return-drugs rate got down from1.86‰to 0.7‰. Conclusions The interventions such as strict return drugs program, feedback between pharmacists and prescribers in return drugs process, enhancing communication with patients and pharmacists to return drugs, were the effective measures in reducing the outpatient return drugs rate in our hospital.
Objective To summarize the experience and lessens after intervention in outpatient return drugs process. Methods Return-drugs prescriptions in 2011 and 2012 in our hospital were retrospectively analyzed, focusing on reasons of return drugs events and effects after intervention in return drugs process. Results After intervention in return drugs process since 2012, the outpatient return-drugs rate got down from1.86‰to 0.7‰. Conclusions The interventions such as strict return drugs program, feedback between pharmacists and prescribers in return drugs process, enhancing communication with patients and pharmacists to return drugs, were the effective measures in reducing the outpatient return drugs rate in our hospital.
2013, 31(5): 393-395.
doi: 10.3969/j.issn.1006-0111.2015.03.023
Abstract:
Objective To evaluate and analyze the prescription writing and irrational drug uses in order to improve the quality of prescription and promote rational drug use in clinic. Methods 14 872 pieces of prescriptions were randomly selected one day per month randomly in the outpatient and emergency department of our hospital from July of 2011 to June of 2012. According to the Hospital Management of Prescription, the prescriptions were reviewed and analyzed. Results 3.7%(545/14 872) prescriptions were found to be irrational. The main problems were incidences of irregularly writing and inappropriate use, which accounted for irrational prescription of 60.2% and 39.8%,respectively. Conclusion Prescriptions in outpatient and emergency department were basically rational in our hospital except some cases of misuses and the management of prescription should be implemented conscientiously to improve the quality of prescription and promote rational drug use in clinical.
Objective To evaluate and analyze the prescription writing and irrational drug uses in order to improve the quality of prescription and promote rational drug use in clinic. Methods 14 872 pieces of prescriptions were randomly selected one day per month randomly in the outpatient and emergency department of our hospital from July of 2011 to June of 2012. According to the Hospital Management of Prescription, the prescriptions were reviewed and analyzed. Results 3.7%(545/14 872) prescriptions were found to be irrational. The main problems were incidences of irregularly writing and inappropriate use, which accounted for irrational prescription of 60.2% and 39.8%,respectively. Conclusion Prescriptions in outpatient and emergency department were basically rational in our hospital except some cases of misuses and the management of prescription should be implemented conscientiously to improve the quality of prescription and promote rational drug use in clinical.
2013, 31(5): 396-397.
doi: 10.3969/j.issn.1006-0111.2013.05.024
Abstract:
Objective To improve the ability of medical material service in contract tactical maneuver in order to prevent the drug backlog and out-dated. Method The medical material services in contract tactical maneuver in recent years were analyzed. The plans of medical material service were made according to the relevant information from annual task scales. Result and conclusion In making plan for medical service, according to types completes, fine species, the right amount, oral primarily, the range of first aid medicine were the most comprehensive principles to finish the medical service in high quality.
Objective To improve the ability of medical material service in contract tactical maneuver in order to prevent the drug backlog and out-dated. Method The medical material services in contract tactical maneuver in recent years were analyzed. The plans of medical material service were made according to the relevant information from annual task scales. Result and conclusion In making plan for medical service, according to types completes, fine species, the right amount, oral primarily, the range of first aid medicine were the most comprehensive principles to finish the medical service in high quality.
2013, 31(5): 398-400.
doi: 10.3969/j.issn.1006-0111.2013.05.025
Abstract:
Objective To build up the teaching tactics of research in the current organic chemistry course teaching for pharmic students,promote the ability of practicing and innovation,discuss how to accommodate the development of modern pharmacy education. Method Methods of experimentation,investigation,operation and literature research were used. Result The corresponding teaching content and teaching platform in experiment course for pharmaceutical specialties were built up. Conclusion It was necessary to ① adjust teaching methods based on the characteristics of pharmaceutical major;②select appropriate content of lectures with variety of teaching methods, in order to stimulate students' interesting;③ design organic chemistry experiments with clinical drugs;④encourage students to expand their knowledge to inspire students' interests.
Objective To build up the teaching tactics of research in the current organic chemistry course teaching for pharmic students,promote the ability of practicing and innovation,discuss how to accommodate the development of modern pharmacy education. Method Methods of experimentation,investigation,operation and literature research were used. Result The corresponding teaching content and teaching platform in experiment course for pharmaceutical specialties were built up. Conclusion It was necessary to ① adjust teaching methods based on the characteristics of pharmaceutical major;②select appropriate content of lectures with variety of teaching methods, in order to stimulate students' interesting;③ design organic chemistry experiments with clinical drugs;④encourage students to expand their knowledge to inspire students' interests.
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