2013 Vol. 31, No. 6
Display Method:
2013, 31(6): 401-404,423.
doi: 10.3969/j.issn.1006-0111.2013.06.001
Abstract:
Vascular disrupting agents (VDAs) are a novel class of the antitumor agents that selectively damage the established tumor vessel. This kind of agents can selectively damage the tumor vascular, which apply adequate oxygen and nutrient for tumor growth and metabolism, and result in the tumor cell necrosis. In recent years, a number of VDAs that interact with microtubule had been involved in clinical trials, and showed good prospects for development and application, which were summarized in this paper.
Vascular disrupting agents (VDAs) are a novel class of the antitumor agents that selectively damage the established tumor vessel. This kind of agents can selectively damage the tumor vascular, which apply adequate oxygen and nutrient for tumor growth and metabolism, and result in the tumor cell necrosis. In recent years, a number of VDAs that interact with microtubule had been involved in clinical trials, and showed good prospects for development and application, which were summarized in this paper.
2013, 31(6): 405-408,480.
doi: 10.3969/j.issn.1006-0111.2013.06.002
Abstract:
Chinese medicinal formula was the main form of Chinese clinical medicine. The compatibility mechanism was an important part of the modernization of Traditional Chinese Medicine. The study of Chinese medicine compound compatibility mechanism explored the relationship between the formula compatibility, the changes of material basis and pharmacological effects and pharmacokinetics from pharmacology and chemistry aspects. The basic characteristics of compatibility mechanism of Chinese medicinal formula, modern research ideas and methods were reviewed in this paper.
Chinese medicinal formula was the main form of Chinese clinical medicine. The compatibility mechanism was an important part of the modernization of Traditional Chinese Medicine. The study of Chinese medicine compound compatibility mechanism explored the relationship between the formula compatibility, the changes of material basis and pharmacological effects and pharmacokinetics from pharmacology and chemistry aspects. The basic characteristics of compatibility mechanism of Chinese medicinal formula, modern research ideas and methods were reviewed in this paper.
2013, 31(6): 409-411,435.
doi: 10.3969/j.issn.1006-0111.2013.06.003
Abstract:
Objective To optimize matrix formula and process conditions and control the quality of propranolol hydrochloride cream. Methods Emulsifying temperature, dosages of the stearic acid, glyceryl monostearate and Tween-80 were taken as variable factors and the orthogonal experiment was adopted to optimize matrix formula and process conditions. HPLC was chosen to determine the content of propranolol hydrochloride and control its quality. Results The optimized matrix formula of propranolol hydrochloride cream was composed of 10%of stearic acid, 7.5%of glyceryl monostearate, 3% of Tween-80 and emulsifying temperature was 70℃. The appearance and stability were good and the quality was good. The average recovery rate was 98.65%, RSD was 0.52% (n=9). Conclusion The preparation process of propranolol hydrochloride cream was rational and stable in quality. The quality control method was simple and fast.
Objective To optimize matrix formula and process conditions and control the quality of propranolol hydrochloride cream. Methods Emulsifying temperature, dosages of the stearic acid, glyceryl monostearate and Tween-80 were taken as variable factors and the orthogonal experiment was adopted to optimize matrix formula and process conditions. HPLC was chosen to determine the content of propranolol hydrochloride and control its quality. Results The optimized matrix formula of propranolol hydrochloride cream was composed of 10%of stearic acid, 7.5%of glyceryl monostearate, 3% of Tween-80 and emulsifying temperature was 70℃. The appearance and stability were good and the quality was good. The average recovery rate was 98.65%, RSD was 0.52% (n=9). Conclusion The preparation process of propranolol hydrochloride cream was rational and stable in quality. The quality control method was simple and fast.
2013, 31(6): 412-414,453.
doi: 10.3969/j.issn.1006-0111.2013.06.04
Abstract:
Objective To develop a HPLC method for simultaneous determination of four polyamines (putrescine, cadaverine, spermidine, spermine) in Candida albicans. Methods HPLC analysis was performed on a Shiseido C18 column(100 mm×3.0 mm, 3.0 μm) after benzoyl chloride derivatization.The mobile phase consist of methanol (A) and water containing 0.1%methane acid (B). The gradient elution program was as follow:0~5 min, 30%~48% B; 5~12 min, 48% B;12~15 min, 48%~70% B;15~25 min, 70% B, the flow rate was 0.6 ml/min, the detection wavelength was 254 nm. Results The linearity was obtained over 0.775~77.50 μg/ml (r=0.999 9) for putrescine, 1.160~116.0 μg/ml (r=0.999 9) for cadaverine, 5.800~580.0 μg/ml (r=0.999 8) for spermidine and 2.533~192.7 μg/ml (r=0.999 9) for spermine. The average recoveries were between 94.27%~109.3%.The RSDs of precision were less than 4%. Conclusion The present study provided a sensitive and reproducible method for the simultaneously determination of four polyamines levels in Candida albicans.
Objective To develop a HPLC method for simultaneous determination of four polyamines (putrescine, cadaverine, spermidine, spermine) in Candida albicans. Methods HPLC analysis was performed on a Shiseido C18 column(100 mm×3.0 mm, 3.0 μm) after benzoyl chloride derivatization.The mobile phase consist of methanol (A) and water containing 0.1%methane acid (B). The gradient elution program was as follow:0~5 min, 30%~48% B; 5~12 min, 48% B;12~15 min, 48%~70% B;15~25 min, 70% B, the flow rate was 0.6 ml/min, the detection wavelength was 254 nm. Results The linearity was obtained over 0.775~77.50 μg/ml (r=0.999 9) for putrescine, 1.160~116.0 μg/ml (r=0.999 9) for cadaverine, 5.800~580.0 μg/ml (r=0.999 8) for spermidine and 2.533~192.7 μg/ml (r=0.999 9) for spermine. The average recoveries were between 94.27%~109.3%.The RSDs of precision were less than 4%. Conclusion The present study provided a sensitive and reproducible method for the simultaneously determination of four polyamines levels in Candida albicans.
2013, 31(6): 415-417,461.
doi: 10.3969/j.issn.1006-0111.2013.06.005
Abstract:
Objective To study the effects of different density microneedle-roller arrays on transdermal delivery of triamcinolone acetonide. Methods The in vitro permeation characteristics through isolated nude mouse skin were studied by modified Franz diffusion cells. Levels in the receptor solution of the control group, the 192 needles microneedle rooler group and the 540 needles microneedle rooler group were measured by HPLC at 2、4、6、8、10 and 12 h, and sampling volume was 0.2 ml. The accumulative penetration amount were counted and the level of triamcinolone acetonide in skin were determined. Plasma concentrations of triamcinolone acetonide and skin volume were measured 2 hours later after administration by HPLC to observe the penetration of triamcinolone acetonide in vivo. Results Different density microneedle-roller could promote the transdermal delivery of triamcinolone acetonide respectively. Transdermal experiment results showed that the cumulative infiltration volume of 192 needles group was about 1.3 times of the control samples, and 540 needles was 2.2 times. Accordingly, skin retention volume were1.9times and 2.8 times of the control group respectively. In vivo results showed that skin retention volume were 2.1 times and 2.3 times of control group, while triamcinolone acetonide in plasma were 1.3 times and 1.4 times of control group. Conclusion Microneedles could effectively promote the skin permeability and deposition of triamcinolone acetonide, and triamcinolone acetonide in plasma was increased at the same time. The promoting of different density was diverse.
Objective To study the effects of different density microneedle-roller arrays on transdermal delivery of triamcinolone acetonide. Methods The in vitro permeation characteristics through isolated nude mouse skin were studied by modified Franz diffusion cells. Levels in the receptor solution of the control group, the 192 needles microneedle rooler group and the 540 needles microneedle rooler group were measured by HPLC at 2、4、6、8、10 and 12 h, and sampling volume was 0.2 ml. The accumulative penetration amount were counted and the level of triamcinolone acetonide in skin were determined. Plasma concentrations of triamcinolone acetonide and skin volume were measured 2 hours later after administration by HPLC to observe the penetration of triamcinolone acetonide in vivo. Results Different density microneedle-roller could promote the transdermal delivery of triamcinolone acetonide respectively. Transdermal experiment results showed that the cumulative infiltration volume of 192 needles group was about 1.3 times of the control samples, and 540 needles was 2.2 times. Accordingly, skin retention volume were1.9times and 2.8 times of the control group respectively. In vivo results showed that skin retention volume were 2.1 times and 2.3 times of control group, while triamcinolone acetonide in plasma were 1.3 times and 1.4 times of control group. Conclusion Microneedles could effectively promote the skin permeability and deposition of triamcinolone acetonide, and triamcinolone acetonide in plasma was increased at the same time. The promoting of different density was diverse.
2013, 31(6): 418-423.
doi: 10.3969/j.issn.1006-0111.2013.06.06
Abstract:
Objective To optimize the extraction technology of aloe. Methods The samples were scanned from 200 to 400 nm by ultraviolet spectrophotometry, then the average ultraviolet absorption was calculated in UVC, UVB and UVA. The quantity of aloin was determined by HPLC. With ultraviolet absorption, aloin content and extraction rate as indexes, the single factor tests and orthogonal experimental design tests L9(34)were applied to investigate the influence of each factor during ultrasonic extraction. Results The extraction of aloe had strong UV absorption effect in the whole UV range. The optimal conditions for extracting were as follows:50% ethanol concentration, 1:30 solid-liquid ration, 30 min and 30℃ ultrasound extraction. Conclusion The extraction of aloe had good ability of ultraviolet absorption and broad-spectrum sun protection. Ultrasonic wave extraction had high extraction yield and required short time which could be used to extract sunscreen formulation from aloe.
Objective To optimize the extraction technology of aloe. Methods The samples were scanned from 200 to 400 nm by ultraviolet spectrophotometry, then the average ultraviolet absorption was calculated in UVC, UVB and UVA. The quantity of aloin was determined by HPLC. With ultraviolet absorption, aloin content and extraction rate as indexes, the single factor tests and orthogonal experimental design tests L9(34)were applied to investigate the influence of each factor during ultrasonic extraction. Results The extraction of aloe had strong UV absorption effect in the whole UV range. The optimal conditions for extracting were as follows:50% ethanol concentration, 1:30 solid-liquid ration, 30 min and 30℃ ultrasound extraction. Conclusion The extraction of aloe had good ability of ultraviolet absorption and broad-spectrum sun protection. Ultrasonic wave extraction had high extraction yield and required short time which could be used to extract sunscreen formulation from aloe.
2013, 31(6): 424-427,466.
doi: 10.3969/j.issn.1006-0111.2013.06.007
Abstract:
Objective To evaluate the pharmacokinetics and relative bioavailability of sulfasalazine enteric-coated tablets from two different factories in healthy volunteers. Methods 24 healthy male volunteers were enrolled in the study.A single oral dose(500 mg) of test and reference Sulfasalazine Enteric-coated tablet preparations were given respectively to the volunteers according to randomized two way cross over study design.The washout period was l week.The plasma concentrations of Sulfasalazine(SASP)and sulfapyridine(SP)were determined by HPLC-UV method, the plasma concentrations of 5-aminosalicylic acid(5-ASA) were determined by HPLC-FLU method. Results The pharmacokinetic parameters of SASP, SP and 5-ASA in plasma were as follows:according to AUC0→t, the relative bioavailability of SASP、SP and 5-ASA was (108.8±24.1)%, (105.0±25.0)% and (94.1±22.0)% in the test preparations; while according to AUC0→∞, the relative bioavailability of SASP、SP and 5-ASA was (106.9±23.4)%, (104.1±25.0)% and (93.6±22.2)% in the test preparations. Mean plasma concentration-time curve of the test product was highly close to that of the reference product.There was no significant difference in pharmacokinetic parameters between the test and reference preparations of sulfasalazine enteric-coated tablets (P>0.05). Conclusion The results of statistical analysis showed that the two sulfasalazine enteric-coated tablets from different factories in healthy volunteers were bioequivalent.
Objective To evaluate the pharmacokinetics and relative bioavailability of sulfasalazine enteric-coated tablets from two different factories in healthy volunteers. Methods 24 healthy male volunteers were enrolled in the study.A single oral dose(500 mg) of test and reference Sulfasalazine Enteric-coated tablet preparations were given respectively to the volunteers according to randomized two way cross over study design.The washout period was l week.The plasma concentrations of Sulfasalazine(SASP)and sulfapyridine(SP)were determined by HPLC-UV method, the plasma concentrations of 5-aminosalicylic acid(5-ASA) were determined by HPLC-FLU method. Results The pharmacokinetic parameters of SASP, SP and 5-ASA in plasma were as follows:according to AUC0→t, the relative bioavailability of SASP、SP and 5-ASA was (108.8±24.1)%, (105.0±25.0)% and (94.1±22.0)% in the test preparations; while according to AUC0→∞, the relative bioavailability of SASP、SP and 5-ASA was (106.9±23.4)%, (104.1±25.0)% and (93.6±22.2)% in the test preparations. Mean plasma concentration-time curve of the test product was highly close to that of the reference product.There was no significant difference in pharmacokinetic parameters between the test and reference preparations of sulfasalazine enteric-coated tablets (P>0.05). Conclusion The results of statistical analysis showed that the two sulfasalazine enteric-coated tablets from different factories in healthy volunteers were bioequivalent.
2013, 31(6): 428-431,475.
doi: 10.3969/j.issn.1006-0111.2013.06.008
Abstract:
Objective To determine the acute toxicity of imperatorin on rats and mice, and the influence of imperatorin on the nervous system of mice and the cardiovascular and respiratory systems of beagle dogs. Methods intraperitoneal injection (ip) and intragastric administration (ig) were performed to mice and ig to rats to determine the acute toxicity of imperatorin. In safety pharmacology experiments, ip of imperatorin was performed to mice in single doses of 50, 100, and 200 mg/kg to observe its influence on the nervous system of mice (including locomotor activity, pole climbing ability, and collaborative hyposis experiment of threshold dose of sodium pentobarbital, etc.). Oral administration (po) of imperatorin was also performed in single doses of 25, 50, 100 mg/kg to beagle dogs to observe its influence on the cardiovascular and respiratory systems of dogs (including ECG, blood pressure, heart rate, and breathing indexes, etc.). Results The LD50 of imperatorin to mice is 988.5 mg/kg by ig and 603.3 mg/kg by ip, and to rats is 3188.7 mg/kg by ig. No significant effects on the nervous system of mice were observed by single ip of imperatorin. And no significant effects on the cardiovascular and respiratory systems of beagle dogs were observed by single po of imperatorin. Conclusion Imperatorin had a wide range of safety application, and its toxicity was relatively easy to control. The antihypertensive effects of imperatorin on normal animals (including mice, rats and dogs) were not significant, therefore it had a great possibility in clinical application.
Objective To determine the acute toxicity of imperatorin on rats and mice, and the influence of imperatorin on the nervous system of mice and the cardiovascular and respiratory systems of beagle dogs. Methods intraperitoneal injection (ip) and intragastric administration (ig) were performed to mice and ig to rats to determine the acute toxicity of imperatorin. In safety pharmacology experiments, ip of imperatorin was performed to mice in single doses of 50, 100, and 200 mg/kg to observe its influence on the nervous system of mice (including locomotor activity, pole climbing ability, and collaborative hyposis experiment of threshold dose of sodium pentobarbital, etc.). Oral administration (po) of imperatorin was also performed in single doses of 25, 50, 100 mg/kg to beagle dogs to observe its influence on the cardiovascular and respiratory systems of dogs (including ECG, blood pressure, heart rate, and breathing indexes, etc.). Results The LD50 of imperatorin to mice is 988.5 mg/kg by ig and 603.3 mg/kg by ip, and to rats is 3188.7 mg/kg by ig. No significant effects on the nervous system of mice were observed by single ip of imperatorin. And no significant effects on the cardiovascular and respiratory systems of beagle dogs were observed by single po of imperatorin. Conclusion Imperatorin had a wide range of safety application, and its toxicity was relatively easy to control. The antihypertensive effects of imperatorin on normal animals (including mice, rats and dogs) were not significant, therefore it had a great possibility in clinical application.
2013, 31(6): 432-435.
doi: 10.3969/j.issn.1006-0111.2013.06.009
Abstract:
Objective To optimize the extraction methods and develop a HPLC-DAD assay for the determination of three effective ingredients in Moutan Coretex. Methods The analysis was performed on an Agilent ZORBAX Eclipse Plus (4.6 mm×150 mm, 5 μm) column with acetonitrile and water (0.6% formic acid) as mobile phase at a rate of 1.0 ml/min, the detection wavelength was 254 nm, the injection volume was 10 μl. Results The regress equation of gallic acid, paeoniflorin and paeonol were Y=16.598 0X+4.950 2, r=0.999 9; Y=1.613 1X+0.995 1, r=0.999 9; Y=5.981 7X+54.103 0, r=0.999 7, respectively. The average recoveries were 100.7%, 99.2%, 97.8% and RSD(n=9) were 1.6%, 3.0%, 1.1%. Conclusion The extraction effect was good and the determination assay was reliable and accurate.
Objective To optimize the extraction methods and develop a HPLC-DAD assay for the determination of three effective ingredients in Moutan Coretex. Methods The analysis was performed on an Agilent ZORBAX Eclipse Plus (4.6 mm×150 mm, 5 μm) column with acetonitrile and water (0.6% formic acid) as mobile phase at a rate of 1.0 ml/min, the detection wavelength was 254 nm, the injection volume was 10 μl. Results The regress equation of gallic acid, paeoniflorin and paeonol were Y=16.598 0X+4.950 2, r=0.999 9; Y=1.613 1X+0.995 1, r=0.999 9; Y=5.981 7X+54.103 0, r=0.999 7, respectively. The average recoveries were 100.7%, 99.2%, 97.8% and RSD(n=9) were 1.6%, 3.0%, 1.1%. Conclusion The extraction effect was good and the determination assay was reliable and accurate.
2013, 31(6): 436-437,472.
doi: 10.3969/j.issn.1006-0111.2013.06.010
Abstract:
Objective To introduce the Origin software to enhance the pharmaceutical R & D personnel's level of the experimental data processing. Methods The application of Origin software in the data processing of several classic pharmaceutical experiments was demonstrated. Results The capabilities of the data analysis and graphics processing with Origin software were very powerful, convenient and accurate. The graphs drawn according to the data were intuitive and rich information. Conclusion The software had significant value in data processing of pharmaceutical experiment.
Objective To introduce the Origin software to enhance the pharmaceutical R & D personnel's level of the experimental data processing. Methods The application of Origin software in the data processing of several classic pharmaceutical experiments was demonstrated. Results The capabilities of the data analysis and graphics processing with Origin software were very powerful, convenient and accurate. The graphs drawn according to the data were intuitive and rich information. Conclusion The software had significant value in data processing of pharmaceutical experiment.
2013, 31(6): 438-441,158.
doi: 10.3969/j.issn.1006-0111.2013.06.011
Abstract:
Objective To study the effect of the new type of hemostat for nano-fibers tunic carbonized hair loaded drug (NTCH) on skin wound healing in rabbits. Methods Bilateral round wounds were made on the backs of rabbits.There were six wounds in each rabbit, treated with medical gauze, absorbable gelatin sponge and NCTH. The effect of NCTH on the skin wound was evaluated by the index of closure time and healing rate. The variation of histopathological characteristics and the content of hydroxyproline in the wound tissue were observed. Results Animal experimental results showed that the NCTH hemostasis performance was better, also significantly reduced closure time, and improve healing rate. The hydroxyproline content in the wound tissue in the NCTH group on days 3, 7, 14 post-treatment was higher than that in medical gauze group (P<0.01).7 days post-treatment, the hydroxyproline content in the wound tissue in the NCTH group was higher than that in gelatin sponge group (P<0.05).On histology observation, 3 days and 7 days post-treatment, the numbers of collagenoblast was contrasted, there was statistical difference among the NCTH group, gelatin sponge group and medical gauze group(P<0.05, P<0.01). 3 days and 7 days post-treatment, the numbers of newly-born blood capillary was contrasted, there was statistical significance difference among the NCTH group, gelatin sponge group and medical gauze group(P<0.05, P<0.01). Conclusion The NCTH had significantly acceleration effect on the skin wound healing.
Objective To study the effect of the new type of hemostat for nano-fibers tunic carbonized hair loaded drug (NTCH) on skin wound healing in rabbits. Methods Bilateral round wounds were made on the backs of rabbits.There were six wounds in each rabbit, treated with medical gauze, absorbable gelatin sponge and NCTH. The effect of NCTH on the skin wound was evaluated by the index of closure time and healing rate. The variation of histopathological characteristics and the content of hydroxyproline in the wound tissue were observed. Results Animal experimental results showed that the NCTH hemostasis performance was better, also significantly reduced closure time, and improve healing rate. The hydroxyproline content in the wound tissue in the NCTH group on days 3, 7, 14 post-treatment was higher than that in medical gauze group (P<0.01).7 days post-treatment, the hydroxyproline content in the wound tissue in the NCTH group was higher than that in gelatin sponge group (P<0.05).On histology observation, 3 days and 7 days post-treatment, the numbers of collagenoblast was contrasted, there was statistical difference among the NCTH group, gelatin sponge group and medical gauze group(P<0.05, P<0.01). 3 days and 7 days post-treatment, the numbers of newly-born blood capillary was contrasted, there was statistical significance difference among the NCTH group, gelatin sponge group and medical gauze group(P<0.05, P<0.01). Conclusion The NCTH had significantly acceleration effect on the skin wound healing.
2013, 31(6): 442-445.
doi: 10.3969/j.issn.1006-0111.2013.06.012
Abstract:
Objective To prepare 4-[1-alkyl-5-oxo-1H-1,2,4-triazol-4 (5H)-yl] benzoic acids (5), which was the key fatty acid chain pharmaceutical intermediates for the total synthesis of novel caspofungin-like cyclohexa lipopeptide antifungal agents. Methods Starting from 4-aminobenzoic acid (1), the target compounds 5a~5n were prepared via amino phenoxy-carbonyl acylation, hydrazinolysis, formamidine cyclization, and the N-alkylation reaction, respectively. Results Target compounds 5a~5n had been successfully synthesized with the overall yield ranged from 42.9% to 46.2%. Their structures were confirmed by ESI-MS and 1H-NMR spectra. All target compounds were reported for the first time. Conclusion The process developed had several advantages such as convenient workup and high yield, which was suitable to industrial production.
Objective To prepare 4-[1-alkyl-5-oxo-1H-1,2,4-triazol-4 (5H)-yl] benzoic acids (5), which was the key fatty acid chain pharmaceutical intermediates for the total synthesis of novel caspofungin-like cyclohexa lipopeptide antifungal agents. Methods Starting from 4-aminobenzoic acid (1), the target compounds 5a~5n were prepared via amino phenoxy-carbonyl acylation, hydrazinolysis, formamidine cyclization, and the N-alkylation reaction, respectively. Results Target compounds 5a~5n had been successfully synthesized with the overall yield ranged from 42.9% to 46.2%. Their structures were confirmed by ESI-MS and 1H-NMR spectra. All target compounds were reported for the first time. Conclusion The process developed had several advantages such as convenient workup and high yield, which was suitable to industrial production.
2013, 31(6): 446-447,469.
doi: 10.3969/j.issn.1006-0111.2013.06.013
Abstract:
Objective To prepare 2-substitudephenoxy-5-benzyloxypyrimidines and 2-substitudephenoxy-5-hydroxypyrimidines which had not been reported. Methods The target compounds were prepared from 2-chlorine-5-hydroxypyrimidine through hydroxy protection, Williamsom reaction and reduction of benzyl group. Results The synthetic process provided a simple, easy diposal procedure and high overall yield. Fourteen new phenoxy pyrimidines compounds were prepared. Conclusions It was a new synthetic method which was easy to operate with moderate reaction conditions.
Objective To prepare 2-substitudephenoxy-5-benzyloxypyrimidines and 2-substitudephenoxy-5-hydroxypyrimidines which had not been reported. Methods The target compounds were prepared from 2-chlorine-5-hydroxypyrimidine through hydroxy protection, Williamsom reaction and reduction of benzyl group. Results The synthetic process provided a simple, easy diposal procedure and high overall yield. Fourteen new phenoxy pyrimidines compounds were prepared. Conclusions It was a new synthetic method which was easy to operate with moderate reaction conditions.
2013, 31(6): 448-450.
doi: 10.3969/j.issn.1006-0111.2013.06.014
Abstract:
Objective To synthesis the new anti-osteoporotic risedronate sodium. Methods Nicotinic acid was used as raw material, by esterification, condensation, Willgerodt reaction and hydrolysis steps to get the key intermediate 3-pyridine acetic acid hydrochloride.Then 3-pyridine acetic acid hydrochloride and phosphorous acid reacted to obtain the risedronate sodium. Results The reaction time, reaction conditions and the yield of Willgerodt reaction were explored. The synthetic route was optimized and the total yield of the reactions was increased. Conclusion This synthetic route of risedronate sodium could be applied to industrial production.
Objective To synthesis the new anti-osteoporotic risedronate sodium. Methods Nicotinic acid was used as raw material, by esterification, condensation, Willgerodt reaction and hydrolysis steps to get the key intermediate 3-pyridine acetic acid hydrochloride.Then 3-pyridine acetic acid hydrochloride and phosphorous acid reacted to obtain the risedronate sodium. Results The reaction time, reaction conditions and the yield of Willgerodt reaction were explored. The synthetic route was optimized and the total yield of the reactions was increased. Conclusion This synthetic route of risedronate sodium could be applied to industrial production.
2013, 31(6): 451-453.
doi: 10.3969/j.issn.1006-0111.2013.06.015
Abstract:
Objective To establish an HPLC method for determination of baicalin and cinnamic acid in Bianyan oral solution simultaneously. Methods The Agilent Eclipse XDB-C18(4.6 mm×150 mm, 5 μm)was used, the mobile phase consisted of ACN-2% acetic acid (23:77), the flow rate was 1.0 ml/min, the detection wavelength was at 280 nm, the column temperature was at room temperature, and the inject volume was 10 μl. Results A good linear correlation was observed within the range of 0.085 1~3.404 8 g for baicalin (r=0.999 9) and 0.020 3~0.811 2 g for cinnamic acid(r=0.999 9). The average recovery (n=6) was 101.68% with RSD 2.85% for baicalin and 101.46% with RSD 2.07% for cinnamic acid. Conclusion The method was rapid, simple and accurate, which could be used for the overall quality control of Bianyan oral solution.
Objective To establish an HPLC method for determination of baicalin and cinnamic acid in Bianyan oral solution simultaneously. Methods The Agilent Eclipse XDB-C18(4.6 mm×150 mm, 5 μm)was used, the mobile phase consisted of ACN-2% acetic acid (23:77), the flow rate was 1.0 ml/min, the detection wavelength was at 280 nm, the column temperature was at room temperature, and the inject volume was 10 μl. Results A good linear correlation was observed within the range of 0.085 1~3.404 8 g for baicalin (r=0.999 9) and 0.020 3~0.811 2 g for cinnamic acid(r=0.999 9). The average recovery (n=6) was 101.68% with RSD 2.85% for baicalin and 101.46% with RSD 2.07% for cinnamic acid. Conclusion The method was rapid, simple and accurate, which could be used for the overall quality control of Bianyan oral solution.
2013, 31(6): 454-458.
doi: 10.3969/j.issn.1006-0111.2013.06.016
Abstract:
Objective To determine whether Xiao Chai Hu Tang have liver toxicity and the sources of toxicity. Methods HPLC-TOF/MS method and the MTT were used to assay the Xiao Chai Hu Tang chemical composition and the survival of SMMC-7721 cells, respectively. Then the stepwise multiple linear regression was used to analysis the chemical composition of Xiao Chai Hu Tang which affected SMMC-7721 cells survival. Results The possible toxic component were found from Scutellaria:X3, chrysin-8-C-β-D-glucose the pyrano base-6-C-α in-L-Arab pyran-glucosidase or its isomers. Conclusion The method initially found potentially toxic constituents of Xiao Chai Hu Tang, which provided a research base for Attenuated compatibility, in order to optimize the prescription, develop the preparation process of science, and improve the quality of the preparations.
Objective To determine whether Xiao Chai Hu Tang have liver toxicity and the sources of toxicity. Methods HPLC-TOF/MS method and the MTT were used to assay the Xiao Chai Hu Tang chemical composition and the survival of SMMC-7721 cells, respectively. Then the stepwise multiple linear regression was used to analysis the chemical composition of Xiao Chai Hu Tang which affected SMMC-7721 cells survival. Results The possible toxic component were found from Scutellaria:X3, chrysin-8-C-β-D-glucose the pyrano base-6-C-α in-L-Arab pyran-glucosidase or its isomers. Conclusion The method initially found potentially toxic constituents of Xiao Chai Hu Tang, which provided a research base for Attenuated compatibility, in order to optimize the prescription, develop the preparation process of science, and improve the quality of the preparations.
2013, 31(6): 459-461.
doi: 10.3969/j.issn.1006-0111.2013.06.017
Abstract:
Objective To establish a HPLC method for determination of silybin contents in Gan'an capsule. Methods Angilent Zorbax SB C18(4.6 mm×250 mm, 5 μm) column was used with 1% acetic acid:methanol=50:50 as the mobile phase. The flow rate was 1.0 ml/min, and the temperature was at 30℃.The detection wavelength was 287 nm.Determination of silybin contents in Gan'an capsule of 10 batches of preparations. Results The silybin calibration curve was at the range of 10.28~123.36 μg/ml(r=1)with average recovery of 97.00%(RSD=0.68%).10 batches of preparations silybin contents in Gan'an capsule was 11.11~16.65 mg/granule. Conclusion The method was simple accurate and reproducible which could be used for the quality control of Gan'an capsule.
Objective To establish a HPLC method for determination of silybin contents in Gan'an capsule. Methods Angilent Zorbax SB C18(4.6 mm×250 mm, 5 μm) column was used with 1% acetic acid:methanol=50:50 as the mobile phase. The flow rate was 1.0 ml/min, and the temperature was at 30℃.The detection wavelength was 287 nm.Determination of silybin contents in Gan'an capsule of 10 batches of preparations. Results The silybin calibration curve was at the range of 10.28~123.36 μg/ml(r=1)with average recovery of 97.00%(RSD=0.68%).10 batches of preparations silybin contents in Gan'an capsule was 11.11~16.65 mg/granule. Conclusion The method was simple accurate and reproducible which could be used for the quality control of Gan'an capsule.
2013, 31(6): 462-463.
doi: 10.3969/j.issn.1006-0111.2013.06.018
Abstract:
Objective To explore the effect of combined therapy with alprostadil and mecobalamin injection on diabetic foot. Methods By simple randomization, the patients were divided into the observe group (accepted treatment of alprostadil and mecobalamin injection) and the control group(accepted treatment of salvia miltiorrhiza injection and mecobalamin tablets). The difference of effective rate, superficial peroneal sensory nerve conduction velocity and dorsalis pedis artery flow velocity were compared. Results ①The effective rate in the observed group was significantly higher than that in the control group(P<0.05); ② The superficial peroneal sensory nerve conduction velocity and dorsalis pedis artery flow velocity were significantly higher in the observed group than that of the control group after treatment(P<0.05). Conclusion Combined use of alprostadil and mecobalamin injection had a good effect in treatment of diabetic foot.
Objective To explore the effect of combined therapy with alprostadil and mecobalamin injection on diabetic foot. Methods By simple randomization, the patients were divided into the observe group (accepted treatment of alprostadil and mecobalamin injection) and the control group(accepted treatment of salvia miltiorrhiza injection and mecobalamin tablets). The difference of effective rate, superficial peroneal sensory nerve conduction velocity and dorsalis pedis artery flow velocity were compared. Results ①The effective rate in the observed group was significantly higher than that in the control group(P<0.05); ② The superficial peroneal sensory nerve conduction velocity and dorsalis pedis artery flow velocity were significantly higher in the observed group than that of the control group after treatment(P<0.05). Conclusion Combined use of alprostadil and mecobalamin injection had a good effect in treatment of diabetic foot.
2013, 31(6): 464-466.
doi: 10.3969/j.issn.1006-0111.2013.06.019
Abstract:
Objective To study the anti-inflammatory and analgesic effects of Tuishao granule, and provide the basis for clinical studies of the drug. Methods The analgesic effects of Tuishao granule were evaluated by the writhing reaction of mice induced by glacial acetic acid and hot plate, while the anti-inflammatory effects were analyzed by using the mouse's ear swelling with xylene and the rats paw swelling with egg white.Result Compared with the model group and the control group, latent time was lengthened significantly and the pain threshold was increased, the frequency of writhing was reduced in mice by Tuishao granule, which showed that the paw swelling percentage of rats and ear swelling of mice were inhibited by Tuishao granule. Conclusion Tuishao granule had significant effects on anti-inflammatory and analgesic, which indicatedthat it had favorable effect on the treatment of inflammation and analgesic by anemopyretic cold.
Objective To study the anti-inflammatory and analgesic effects of Tuishao granule, and provide the basis for clinical studies of the drug. Methods The analgesic effects of Tuishao granule were evaluated by the writhing reaction of mice induced by glacial acetic acid and hot plate, while the anti-inflammatory effects were analyzed by using the mouse's ear swelling with xylene and the rats paw swelling with egg white.Result Compared with the model group and the control group, latent time was lengthened significantly and the pain threshold was increased, the frequency of writhing was reduced in mice by Tuishao granule, which showed that the paw swelling percentage of rats and ear swelling of mice were inhibited by Tuishao granule. Conclusion Tuishao granule had significant effects on anti-inflammatory and analgesic, which indicatedthat it had favorable effect on the treatment of inflammation and analgesic by anemopyretic cold.
2013, 31(6): 467-469.
doi: 10.3969/j.issn.1006-0111.2013.06.020
Abstract:
Objective To explore the efficacy of WuzhiPian in the treatment of alcoholic Hepatitis. Methods 110 patients with alcoholic hepatitis were randomly divided into the observed group(accepted treatment of WuzhiPian) and the control group(accepted treatment of Diammonium glycyrrhizinate enteric-coated capsules). The difference of clinical efficacy and alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TBIL), gamma glutamyl transpeptidase (γ-GT) were compared between the two groups. Results The effective rate in the observed group(92.86%) was significantly higher than that in the control group(77.78%)(P<0.05); ② The concentration of ALT, AST, TBIL andγ-GT after treatment were significantly lower than that before the treatment(P<0.01); ③After treatment, the concentration of ALT, AST, TBIL andγ-GT in the observed group were significantly lower than that in the control group(P<0.01). Conclusion WuzhiPian could increase therapeutic effect and improve liver function in alcoholic hepatitis patients.
Objective To explore the efficacy of WuzhiPian in the treatment of alcoholic Hepatitis. Methods 110 patients with alcoholic hepatitis were randomly divided into the observed group(accepted treatment of WuzhiPian) and the control group(accepted treatment of Diammonium glycyrrhizinate enteric-coated capsules). The difference of clinical efficacy and alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin (TBIL), gamma glutamyl transpeptidase (γ-GT) were compared between the two groups. Results The effective rate in the observed group(92.86%) was significantly higher than that in the control group(77.78%)(P<0.05); ② The concentration of ALT, AST, TBIL andγ-GT after treatment were significantly lower than that before the treatment(P<0.01); ③After treatment, the concentration of ALT, AST, TBIL andγ-GT in the observed group were significantly lower than that in the control group(P<0.01). Conclusion WuzhiPian could increase therapeutic effect and improve liver function in alcoholic hepatitis patients.
2013, 31(6): 470-472.
doi: 10.3969/j.issn.1006-0111.2013.06.021
Abstract:
To explore the pharmaceutical department how to combine own characteristics and updating ideas in highly modern of pharmaceutical companies based on construction process and the current situation of Pharmaceutical Department of Changzheng Hospital affiliated to Second Military Medical University. The service range should be expanded and the service ability should be promoted in order to complete transformation from supply style to technological development style, passive service to active service, and simple service to integrated service and be suitable to strategic development of hospital pharmaceutics in new period.
To explore the pharmaceutical department how to combine own characteristics and updating ideas in highly modern of pharmaceutical companies based on construction process and the current situation of Pharmaceutical Department of Changzheng Hospital affiliated to Second Military Medical University. The service range should be expanded and the service ability should be promoted in order to complete transformation from supply style to technological development style, passive service to active service, and simple service to integrated service and be suitable to strategic development of hospital pharmaceutics in new period.
2013, 31(6): 473-475.
doi: 10.3969/j.issn.1006-0111.2013.06.022
Abstract:
Logistics visualization is a developing trend of military logistics informatization. A solution was proposed in this paper which the information management in the whole process of military medical supply would be achieved based-on logistics visualization technology. The constructed system included three subsystems, medicinal packaging and code-printing systems, in-storage military medical management system, and in-transit military medicinal tracking system. The system could provide new decision support functions for headquarters in strategic decisions and primary business units in managements.
Logistics visualization is a developing trend of military logistics informatization. A solution was proposed in this paper which the information management in the whole process of military medical supply would be achieved based-on logistics visualization technology. The constructed system included three subsystems, medicinal packaging and code-printing systems, in-storage military medical management system, and in-transit military medicinal tracking system. The system could provide new decision support functions for headquarters in strategic decisions and primary business units in managements.
2013, 31(6): 476-477.
doi: 10.3969/j.issn.1006-0111.2013.06.023
Abstract:
Objective To explore the characteristics of medical materials support in earthquake relief mission in subtropical forest areas and put forward some suggestions and countermeasures of medical materials support. Methods Experiences and practices of medical materials support in earthquake relief were summarized, which focused on the subtropical jungle geographical climate, the characteristics of casualties and diseases in the earthquake, as well as the difficulties of medical materials support. Results and Conclusion To ensure the medical materials support in earthquake relief accomplish successfully, scientific practical scheme should be work out, medical materials reserve standard should be improved, supply channels should be explored to ensure supply in time, medical materials manage should be strengthened to ensure supply quality, and investigation of epidemic situation should be carried out to ensure the epidemic prevention drugs.
Objective To explore the characteristics of medical materials support in earthquake relief mission in subtropical forest areas and put forward some suggestions and countermeasures of medical materials support. Methods Experiences and practices of medical materials support in earthquake relief were summarized, which focused on the subtropical jungle geographical climate, the characteristics of casualties and diseases in the earthquake, as well as the difficulties of medical materials support. Results and Conclusion To ensure the medical materials support in earthquake relief accomplish successfully, scientific practical scheme should be work out, medical materials reserve standard should be improved, supply channels should be explored to ensure supply in time, medical materials manage should be strengthened to ensure supply quality, and investigation of epidemic situation should be carried out to ensure the epidemic prevention drugs.
2013, 31(6): 478-480.
doi: 10.3969/j.issn.1006-0111.2013.06.024
Abstract:
Objective To examine the dose measurement methods of popular oral liquid OTC TCM, and to evaluate the recognition accuracy of patient. Methods The types and features of oral liquid measurement methods provided with packages obtained from hospital pharmacies were recorded and outpatients were selected randomly to assess the accuracy rate of dose measuring. Results Of the 45 oral liquid OTC TCM multiple-dosage package products, only 11(24%) provided a dosing cup with package, 31(69%) provided mark on bottles, 3(6.7%) provided none of them. 49(94%) outpatients could measure accurately using dosing cup while resulted in wrong dosage by the mark on bottles because of variable marked volume. Conclusion Results suggest that dosing measurement variability presented a challenge to patient operation, which might result in a medication dosing error, whereas pharmacists should strive to provide understandable care information to promote proper medication use.
Objective To examine the dose measurement methods of popular oral liquid OTC TCM, and to evaluate the recognition accuracy of patient. Methods The types and features of oral liquid measurement methods provided with packages obtained from hospital pharmacies were recorded and outpatients were selected randomly to assess the accuracy rate of dose measuring. Results Of the 45 oral liquid OTC TCM multiple-dosage package products, only 11(24%) provided a dosing cup with package, 31(69%) provided mark on bottles, 3(6.7%) provided none of them. 49(94%) outpatients could measure accurately using dosing cup while resulted in wrong dosage by the mark on bottles because of variable marked volume. Conclusion Results suggest that dosing measurement variability presented a challenge to patient operation, which might result in a medication dosing error, whereas pharmacists should strive to provide understandable care information to promote proper medication use.
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