2005 Vol. 23, No. 5
Display Method:
2005, (5): 266-269.
Abstract:
Objective To study the effects of KNT009 on nervous, cardiovascular and respiratory system in animals. Methods Mice were randomly divided to receive single 160, 80, 40, and 0 mg/kg dose of KNT009 and 80 mg/kg dose of gatigloxacin respectively and the spontaneous activities and pull-down ability of animals were observed. Dogs were randomly divided to receive single 40, 20, 10 and 0 mg/kg dose of KNT009 and 20 mg/kg dose of gatigloxacin respectively and the blood pressure, ECG, respiratory rate and width of dogs were measured. Results No effects on spontaneous activities and pull-down ability in mice were observed. The systolic blood pressure, diastolic blood pressure, mean arterial pressure, heart rate and respiratory rate of dogs were decreased, the QT interval was prolonged and the respiratory width was increased in dogs, and there were dose effective relationship, however, these parameters return to normal within 3h. Conclusion KNT009 has some effects on cardiovascular system in dogs such as the blood pressure and heart rate may be decreased and the QT interval may be prolonged, KNT009 also has some effects on respiratory system in dogs such as the respiratory rate may be decreased and the respiratory width may be increased.
Objective To study the effects of KNT009 on nervous, cardiovascular and respiratory system in animals. Methods Mice were randomly divided to receive single 160, 80, 40, and 0 mg/kg dose of KNT009 and 80 mg/kg dose of gatigloxacin respectively and the spontaneous activities and pull-down ability of animals were observed. Dogs were randomly divided to receive single 40, 20, 10 and 0 mg/kg dose of KNT009 and 20 mg/kg dose of gatigloxacin respectively and the blood pressure, ECG, respiratory rate and width of dogs were measured. Results No effects on spontaneous activities and pull-down ability in mice were observed. The systolic blood pressure, diastolic blood pressure, mean arterial pressure, heart rate and respiratory rate of dogs were decreased, the QT interval was prolonged and the respiratory width was increased in dogs, and there were dose effective relationship, however, these parameters return to normal within 3h. Conclusion KNT009 has some effects on cardiovascular system in dogs such as the blood pressure and heart rate may be decreased and the QT interval may be prolonged, KNT009 also has some effects on respiratory system in dogs such as the respiratory rate may be decreased and the respiratory width may be increased.
2005, (5): 269-270.
Abstract:
Objective To optimize the preparation procedure of aripiprazole. Methods 7-hydroxy-3,4-dihydro-2(1H)-quinolin-one was used as starting material and etherified with 1,4-dibromobutane, then alkylated with 1-(2,3-dichlorophenyl) piperazine to yield the target compound aripiprazole. Results The DMF was replaced by acetone as solvent when etherification. The extraction purification method in the last step was replaced by washing precipitates with water. Aripiprazole was prepared in overall yield of 71. 3%. Conclusion The optimal preparation procedure is stable and available for industrial production.
Objective To optimize the preparation procedure of aripiprazole. Methods 7-hydroxy-3,4-dihydro-2(1H)-quinolin-one was used as starting material and etherified with 1,4-dibromobutane, then alkylated with 1-(2,3-dichlorophenyl) piperazine to yield the target compound aripiprazole. Results The DMF was replaced by acetone as solvent when etherification. The extraction purification method in the last step was replaced by washing precipitates with water. Aripiprazole was prepared in overall yield of 71. 3%. Conclusion The optimal preparation procedure is stable and available for industrial production.
2005, (5): 271-272,281.
Abstract:
Objective To establish a practical and effective animal model in order to study gastric mucosal precancerous lesion (GPL) in rat. Methods Three group were classified in the experimental. Normal group:not to establish the model; Model group Ⅰ established the model only use N-methyl-N'-nitro-N'-nitrosoguanididne (MNNG). Model group Ⅱ:established the model by com-plexed method such as the diet, N-methyl-N'-nirtro-N-nitrosoguanidine(MNNG), alcohol, ranitidine and so on. The change of GPL in pathohistologic were observed. Results Experimental GPL of rats were induced successfully. Conclusion It was found that the rate of GPL in model group Ⅱ is higher than that in model group Ⅰ. And the established time was only 20 weeks which was less than 35 weeks that have ever reproted. The model is a practical and effective animal model in studying on GPL in rat.
Objective To establish a practical and effective animal model in order to study gastric mucosal precancerous lesion (GPL) in rat. Methods Three group were classified in the experimental. Normal group:not to establish the model; Model group Ⅰ established the model only use N-methyl-N'-nitro-N'-nitrosoguanididne (MNNG). Model group Ⅱ:established the model by com-plexed method such as the diet, N-methyl-N'-nirtro-N-nitrosoguanidine(MNNG), alcohol, ranitidine and so on. The change of GPL in pathohistologic were observed. Results Experimental GPL of rats were induced successfully. Conclusion It was found that the rate of GPL in model group Ⅱ is higher than that in model group Ⅰ. And the established time was only 20 weeks which was less than 35 weeks that have ever reproted. The model is a practical and effective animal model in studying on GPL in rat.
2005, (5): 282-284.
Abstract:
Objective To investigate the status and tendency of β-receptor antagonists usage, and offer scientific basis for reasonable usage of the drugs in clinic treatment. Methods The data of β-receptor antagonists usage in Wuhan Asia Heart Hospital during 2003 to 2004 were collected and analyzed. Results The expense and frequency of β-receptor antagonists usage increase year by year. Conclusion The usage of p-receptor antagonists is reasonable in our hospital. The second generation of β-receptor antagonists, such as metoprolol and atenolol, are dominant in clinic use.
Objective To investigate the status and tendency of β-receptor antagonists usage, and offer scientific basis for reasonable usage of the drugs in clinic treatment. Methods The data of β-receptor antagonists usage in Wuhan Asia Heart Hospital during 2003 to 2004 were collected and analyzed. Results The expense and frequency of β-receptor antagonists usage increase year by year. Conclusion The usage of p-receptor antagonists is reasonable in our hospital. The second generation of β-receptor antagonists, such as metoprolol and atenolol, are dominant in clinic use.
2005, (5): 288-291.
Abstract:
Objective To predict the developing trend of non-steroidal anti-inflammatory drugs and offer the base for drug development and clinical application by analyzing the current use situation of these drugs. Methods The use amount of non-steroidal anti-inflammatory drugs and sell sum were analysed according to the DDDs order and the sum order in Second Affiliated Hospital of Jiaxing College during 2002～2004. Results Aspirin enteric coated tablets were used most frequently. There are many varieties and dosage forms of single and compound preparation contained paracetamol, which have been widely applied in the treatment of cold and all kinds of chronic pain. The clinical application of selective cyclooxygenase (COX)-2 inhibitor, such as meloxicam, is increasing according to the DDDs order. With marketing of new products, the competition between different non-steroidal anti-inflammatory drugs will be more complicated. Conclusion The more efficient and less toxic non-steroidal anti-inflammatory drugs are being developed.
Objective To predict the developing trend of non-steroidal anti-inflammatory drugs and offer the base for drug development and clinical application by analyzing the current use situation of these drugs. Methods The use amount of non-steroidal anti-inflammatory drugs and sell sum were analysed according to the DDDs order and the sum order in Second Affiliated Hospital of Jiaxing College during 2002～2004. Results Aspirin enteric coated tablets were used most frequently. There are many varieties and dosage forms of single and compound preparation contained paracetamol, which have been widely applied in the treatment of cold and all kinds of chronic pain. The clinical application of selective cyclooxygenase (COX)-2 inhibitor, such as meloxicam, is increasing according to the DDDs order. With marketing of new products, the competition between different non-steroidal anti-inflammatory drugs will be more complicated. Conclusion The more efficient and less toxic non-steroidal anti-inflammatory drugs are being developed.
2005, (5): 291-294.
Abstract:
Objective To investigate the application and trend of antimierobial drugs in our hospital in order to provide some references for medical staffs and related unites. Methods Taking DDD, DDDs, total expenditure(yuan) and daily cost as statistic index, the condition of antimicrobial drugs used in our hospital during 2003～2004 was counted and analyzed. Results Of the variety which DDDs stood at the top 20 ranks in 2003, 14drugs entered top 20 ranks of the vear 2004. Of the variety which sales sum stood at the top 20 ranks in 2003, 16 drugs entered top 20 ranks of the year 2004. Compared with 2003, the variety of antimicrobial drugs in 2004 increased by 14, total expenditure increased by 311% and daily used drug cost increased by 16.93%. The ratio of DDDs and expenditure of oral preparation decreased, whereas those of mjective preparation increased. Conclusion Antimicrobial drugs have been widely used in our hospital. The condition of application is basically rational.
Objective To investigate the application and trend of antimierobial drugs in our hospital in order to provide some references for medical staffs and related unites. Methods Taking DDD, DDDs, total expenditure(yuan) and daily cost as statistic index, the condition of antimicrobial drugs used in our hospital during 2003～2004 was counted and analyzed. Results Of the variety which DDDs stood at the top 20 ranks in 2003, 14drugs entered top 20 ranks of the vear 2004. Of the variety which sales sum stood at the top 20 ranks in 2003, 16 drugs entered top 20 ranks of the year 2004. Compared with 2003, the variety of antimicrobial drugs in 2004 increased by 14, total expenditure increased by 311% and daily used drug cost increased by 16.93%. The ratio of DDDs and expenditure of oral preparation decreased, whereas those of mjective preparation increased. Conclusion Antimicrobial drugs have been widely used in our hospital. The condition of application is basically rational.
2005, (5): 295-297.
Abstract:
Objective To determine astragaloside Ⅳ in Radix Astragali by HPLC-KLSD. Methods Radix Astragali was extracted with MeOH-NH3·H2O(v/v 9:1),the condition was confirmed and the validation of the method was also tested. The chromatogra phy condition was with Hypersil ODS 2 column (4.6mm×250mm,5μm); mobile phase was A; ACN,B:H2O, gradient elutron,flow speed was 1.0 ml/min, temperature of column was room temperature, inject volume:20μL. The KLSD conditions were as follows:the temperature of drift tube was 40℃, the gas pressure was 3.5Bar, the value of gain was 7. Results The intra-day and mter-day precision (RSD)at low, middle and high injection amount were all less than 2.0%. The stability (RSD) was 1.24% in 48h. The recuerence (RSD, n=5) was 1.26%. The limit of detection was 0.6930mg/mL The recoveries were 97.05% (KSD=0.17%, n=3) for astragaloside Ⅳ. The contents of astragaloside Ⅳ in (en different batch of Astragalus membranaceus (Fisch.) Bge. were accord to the standard of Chinese Pharmacopoeia. Conclusion The method covild shorten the process and time of Radix Astragali pretreatment with character of simple, suitable and reliable. The studies could apply to determine the content of astragaloside Ⅳ in Radix Astragalt.
Objective To determine astragaloside Ⅳ in Radix Astragali by HPLC-KLSD. Methods Radix Astragali was extracted with MeOH-NH3·H2O(v/v 9:1),the condition was confirmed and the validation of the method was also tested. The chromatogra phy condition was with Hypersil ODS 2 column (4.6mm×250mm,5μm); mobile phase was A; ACN,B:H2O, gradient elutron,flow speed was 1.0 ml/min, temperature of column was room temperature, inject volume:20μL. The KLSD conditions were as follows:the temperature of drift tube was 40℃, the gas pressure was 3.5Bar, the value of gain was 7. Results The intra-day and mter-day precision (RSD)at low, middle and high injection amount were all less than 2.0%. The stability (RSD) was 1.24% in 48h. The recuerence (RSD, n=5) was 1.26%. The limit of detection was 0.6930mg/mL The recoveries were 97.05% (KSD=0.17%, n=3) for astragaloside Ⅳ. The contents of astragaloside Ⅳ in (en different batch of Astragalus membranaceus (Fisch.) Bge. were accord to the standard of Chinese Pharmacopoeia. Conclusion The method covild shorten the process and time of Radix Astragali pretreatment with character of simple, suitable and reliable. The studies could apply to determine the content of astragaloside Ⅳ in Radix Astragalt.
2005, (5): 297-299.
Abstract:
Objective To established a HPLC method for the determination of alipaizuo in its tablets. Method Alipaizuo can be separated on column with a mixture of 0.02% phosphoric acid(pH=3.0, adjusted with triethylamine) and acetonitrile (46:54) as mobile phase and detected at 254 nm. Result The linear range was from 2.088μg/mL to 66. 816μg/mL (r=0.99999) for alipaizuo. The average recovery was 99.39%. Conclusion The method is simple, rapid, accurate and reliable.
Objective To established a HPLC method for the determination of alipaizuo in its tablets. Method Alipaizuo can be separated on column with a mixture of 0.02% phosphoric acid(pH=3.0, adjusted with triethylamine) and acetonitrile (46:54) as mobile phase and detected at 254 nm. Result The linear range was from 2.088μg/mL to 66. 816μg/mL (r=0.99999) for alipaizuo. The average recovery was 99.39%. Conclusion The method is simple, rapid, accurate and reliable.
2005, (5): 300-301.
Abstract:
Objective To establish a method of bacterial endotoxin test for fluconazole and glucose injection using limulus lysate a-gent. Methods The experiment was made according to bacterial endotoxin test in China Pharmacopeia 2000 (vol. Ⅱ). Results Fluconazole and glucose injection has not interference on bacterial endotoxin inspection. Conclusion Bacterial endotoxin test can be used for fluconazole and glucose injection.
Objective To establish a method of bacterial endotoxin test for fluconazole and glucose injection using limulus lysate a-gent. Methods The experiment was made according to bacterial endotoxin test in China Pharmacopeia 2000 (vol. Ⅱ). Results Fluconazole and glucose injection has not interference on bacterial endotoxin inspection. Conclusion Bacterial endotoxin test can be used for fluconazole and glucose injection.
2005, (5): 302-304.
Abstract:
Objective To observe the chemical stabihty of seven common injections (5% glucose injection, 10% glucose injection, 5% glucose and sodium chloride injection, 10% glucose and sodium chloride injection, compound sodium chloride injection, 0.9% sodium chloride injection, sodium lactate injection) mixed with norfloxacin at room temperature for 8 hours. Methods A convolution spectrometry was used, the appearance was observed and pH value was tested. The results were described quantitatively by subtract spectrometry value. Results There were no obvious changes in the appearances and pH in 8 hours. Except that the subtract spectrometry values of norfloxacin with sodium lactate injection in 4, 6, 8h were 11.51%,19.73%,24.81%, the others were less than 10%. Conclusion Norfloxacin can be mixed with other common injections except sodium lactate injection at room temperature for 8 hours. The convolution spectrometry provides a new method for the research of the stability of drugs.
Objective To observe the chemical stabihty of seven common injections (5% glucose injection, 10% glucose injection, 5% glucose and sodium chloride injection, 10% glucose and sodium chloride injection, compound sodium chloride injection, 0.9% sodium chloride injection, sodium lactate injection) mixed with norfloxacin at room temperature for 8 hours. Methods A convolution spectrometry was used, the appearance was observed and pH value was tested. The results were described quantitatively by subtract spectrometry value. Results There were no obvious changes in the appearances and pH in 8 hours. Except that the subtract spectrometry values of norfloxacin with sodium lactate injection in 4, 6, 8h were 11.51%,19.73%,24.81%, the others were less than 10%. Conclusion Norfloxacin can be mixed with other common injections except sodium lactate injection at room temperature for 8 hours. The convolution spectrometry provides a new method for the research of the stability of drugs.
2005, (5): 306-308.
Abstract:
Objective To Establish the kinetre-turbidimetrie techmque for practical quahly control on endotoxin content in elmda invcin hydrochloride mjection Methods The kmetie-turbidimetrie techmque and ehminated interfere factors approved by Chinese pharmacopoeia 2000 edition were used. Results Endotoxin added to clindamyem hydrochloride mjection was recovered in a quantitative manner showing neither inhibition nor enhancement in diluted solution concentration 0.075 mg/mL, the endotoxin recovery was more than 50 percent and less than 200 percent. Conclusion These results suggested that the kinetre-turbidimetrie technique of LAL-test was suitable for the detection of eudoloxin in elindamycin hydrochloride mjection.
Objective To Establish the kinetre-turbidimetrie techmque for practical quahly control on endotoxin content in elmda invcin hydrochloride mjection Methods The kmetie-turbidimetrie techmque and ehminated interfere factors approved by Chinese pharmacopoeia 2000 edition were used. Results Endotoxin added to clindamyem hydrochloride mjection was recovered in a quantitative manner showing neither inhibition nor enhancement in diluted solution concentration 0.075 mg/mL, the endotoxin recovery was more than 50 percent and less than 200 percent. Conclusion These results suggested that the kinetre-turbidimetrie technique of LAL-test was suitable for the detection of eudoloxin in elindamycin hydrochloride mjection.
2005, (5): 309-312.
Abstract:
Objective Pharmaceutical care is a brand-new model that rises rapidly in the 1990s. It's in the stage of spreading and popularizing in our country. However, pharmaceutical information work is the center and foundation of all the pharmaceutical care work, therefore, expanding pharmaceutical information work is very importance in developing pharmaceutical care practice.
Objective Pharmaceutical care is a brand-new model that rises rapidly in the 1990s. It's in the stage of spreading and popularizing in our country. However, pharmaceutical information work is the center and foundation of all the pharmaceutical care work, therefore, expanding pharmaceutical information work is very importance in developing pharmaceutical care practice.
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