OBJECTIVE: To examine the acute toxicity of an aqueous extract of Aspidopterys obcordata(A. obcordata) in Sprague Dawley rats.METHODS: The rats were orally administered a dose of 5000 mg/kg body weight and observed co...OBJECTIVE: To examine the acute toxicity of an aqueous extract of Aspidopterys obcordata(A. obcordata) in Sprague Dawley rats.METHODS: The rats were orally administered a dose of 5000 mg/kg body weight and observed continuously for 6 h and then daily for 14 days. Control rats were administered distilled water. The effect of the extract on general behavior, body weight, and food and water intake were measured.After 14 days, the rats were sacrificed and their organs(liver, heart, spleen, lungs, kidney, adrenal glands, ovaries, and testes) were removed for macroscopic examination. The body and organ weights in addition to hematology(e.g., hemoglobin and white blood cell counts) and clinical blood biochemistry(e.g., albumin and bilirubin) were also examined.RESULTS: There were no deaths recorded, and the rats treated with A. obcordata showed no signs of toxicity. All measured parameters in rats treated with A. obcordata were unaffected when compared with those in control rats. The acute toxicity(LD_(50))was estimated to be > 5000 mg/kg body weight.CONCLUSION: Our results demonstrate the safety of an acute oral administration of an aqueous extract of A. obcordata in rats and indicate that future subacute and long-term toxicity testing of A. obcordata is warranted.展开更多
OBJECTIVE: To assess the safety and effectiveness of Dengzhanxixin injection(DZI) extracted from Dengzhanxixin(Herba Erigerontis Breviscapi) and identify its potential risks.METHODS: A series of studies were conducted...OBJECTIVE: To assess the safety and effectiveness of Dengzhanxixin injection(DZI) extracted from Dengzhanxixin(Herba Erigerontis Breviscapi) and identify its potential risks.METHODS: A series of studies were conducted on the production process, quality standards, and pharmacology. Postmarketing clinical studies and literature reviews including adverse reactions(ADR),adverse events(ADE), case analysis and systematic reviews were also conducted. Data from the hospital information system and spontaneous reporting system were analyzed.RESULTS: The acute toxicity test indicated that the Lethal Dose 50 test( LD 50) dosage was 250 times more than the clinical maximum daily dosage(6mg/kg). In long-term toxicity tests, rats experi-enced renal tubular damage at 480 mg/kg. However, the dose of 120 mg/kg is safe and non-toxic,which is 40 times above the clinical daily maximum. Beagles had increased serum creatinine at160 mg/kg. In a prospective study, 15 962 cases experienced 16 ADR/ADE. The rate of ADR/ADE was0.1002%. ADR symptoms included rash(16.00%),chills(16.00%), and fever(16.00%).CONCLUSION: There is significant evidence that DZI is safe and effective in a clinical setting.展开更多
This study aimed to investigate the effects of different process parameters on the physical properties, in vitro dissolution rate, and short and long-term stability of diclofenac potassium（DFP） granules and capsules...This study aimed to investigate the effects of different process parameters on the physical properties, in vitro dissolution rate, and short and long-term stability of diclofenac potassium（DFP） granules and capsules. DFP granules exhibited low total amounts of impurities when prepared through the wet granulation method using a granulating solvent with a low water/ethanol ratio. The impurities of the wet DFP mass dried at 70 ℃ were higher than those dried at 50 ℃ or 60 ℃. DFP granules were stable under strong light exposure during preparation. DFP granules prepared using a granulating solvent with a 1：4 water/ethanol ratio had a relatively smaller particle size and higher angle of repose than those prepared using granulating solvents with other water/ethanol ratios. The dissolution rate of DFP capsules prepared using four different water/ethanol ratios was less than 2% after 10 min of dissolution and increased to 95% within 30 min of dissolution. The total amount of drug impurities of DFP capsules prepared using a granulating solvent with 1：4 water/ethanol ratio was considerably lower than those of DFP capsules prepared using a granulating solvent with a 1：0 water/ethanol solvent ratio. Regardless of the water/ethanol ratio, the capsules showed poor stability when exposed to high temperature（60 ℃） and strong light（4500±500 Lux） for 10 days, but were relatively stable at high humidity（92.5% RH）. The results of the long-term stability（25±2 ℃ and 60%±10% relative humidity） study showed that DFP granules were more stable than DFP capsules, and were stable for 12 months. The type of encapsulating material did not affect the 2-month stability of DFP. DFP granules are sensitive to granulating solvent and drying temperature and DFP capsules should be stored away from high temperature and strong light.展开更多
基金National Natural Science Foundation of China(Transport Characters and Mechanism Research of Multiplicity Ingredient TCM Utilizing Sensitive Bioactivity in Caco-2 Cell Model,No.81173645)Program for Innovative Research Team in IMPLAD(Discovery and foundation of new drug of TCM)+2 种基金a grant from the Basic Scientific Research Special of the Central Public Welfare Research Institutes of IMPLAD(Research on the Kidney Stone Activities and Preliminary Mechanisms of Aspidopterys Obcordata,No.YZYN-15-06)PUMC Youth Fund(Study of Anti-Tumor Activities of Pegylation Artemisinin Prodrugs Based on PK-PD Binding Model,No.33320140076)Beijing Municipal Natural Science Foundation(Preparation of Silica-Based Nanoparticles/PDMS Hybrid Membranes for Pervaporation of Ethanol/Water Mixtures,No.2132010)
文摘OBJECTIVE: To examine the acute toxicity of an aqueous extract of Aspidopterys obcordata(A. obcordata) in Sprague Dawley rats.METHODS: The rats were orally administered a dose of 5000 mg/kg body weight and observed continuously for 6 h and then daily for 14 days. Control rats were administered distilled water. The effect of the extract on general behavior, body weight, and food and water intake were measured.After 14 days, the rats were sacrificed and their organs(liver, heart, spleen, lungs, kidney, adrenal glands, ovaries, and testes) were removed for macroscopic examination. The body and organ weights in addition to hematology(e.g., hemoglobin and white blood cell counts) and clinical blood biochemistry(e.g., albumin and bilirubin) were also examined.RESULTS: There were no deaths recorded, and the rats treated with A. obcordata showed no signs of toxicity. All measured parameters in rats treated with A. obcordata were unaffected when compared with those in control rats. The acute toxicity(LD_(50))was estimated to be > 5000 mg/kg body weight.CONCLUSION: Our results demonstrate the safety of an acute oral administration of an aqueous extract of A. obcordata in rats and indicate that future subacute and long-term toxicity testing of A. obcordata is warranted.
基金Supported by National Science and Technology Major Projects for"Major New Drugs Innovation and Development":Study on Key Technologies of Postmarketing Evaluation for Chinese Medicine(No.2009ZX09502-030)
文摘OBJECTIVE: To assess the safety and effectiveness of Dengzhanxixin injection(DZI) extracted from Dengzhanxixin(Herba Erigerontis Breviscapi) and identify its potential risks.METHODS: A series of studies were conducted on the production process, quality standards, and pharmacology. Postmarketing clinical studies and literature reviews including adverse reactions(ADR),adverse events(ADE), case analysis and systematic reviews were also conducted. Data from the hospital information system and spontaneous reporting system were analyzed.RESULTS: The acute toxicity test indicated that the Lethal Dose 50 test( LD 50) dosage was 250 times more than the clinical maximum daily dosage(6mg/kg). In long-term toxicity tests, rats experi-enced renal tubular damage at 480 mg/kg. However, the dose of 120 mg/kg is safe and non-toxic,which is 40 times above the clinical daily maximum. Beagles had increased serum creatinine at160 mg/kg. In a prospective study, 15 962 cases experienced 16 ADR/ADE. The rate of ADR/ADE was0.1002%. ADR symptoms included rash(16.00%),chills(16.00%), and fever(16.00%).CONCLUSION: There is significant evidence that DZI is safe and effective in a clinical setting.
基金National Natural Science Foundation of China(Grant No.81373333,81311140267)
文摘This study aimed to investigate the effects of different process parameters on the physical properties, in vitro dissolution rate, and short and long-term stability of diclofenac potassium（DFP） granules and capsules. DFP granules exhibited low total amounts of impurities when prepared through the wet granulation method using a granulating solvent with a low water/ethanol ratio. The impurities of the wet DFP mass dried at 70 ℃ were higher than those dried at 50 ℃ or 60 ℃. DFP granules were stable under strong light exposure during preparation. DFP granules prepared using a granulating solvent with a 1：4 water/ethanol ratio had a relatively smaller particle size and higher angle of repose than those prepared using granulating solvents with other water/ethanol ratios. The dissolution rate of DFP capsules prepared using four different water/ethanol ratios was less than 2% after 10 min of dissolution and increased to 95% within 30 min of dissolution. The total amount of drug impurities of DFP capsules prepared using a granulating solvent with 1：4 water/ethanol ratio was considerably lower than those of DFP capsules prepared using a granulating solvent with a 1：0 water/ethanol solvent ratio. Regardless of the water/ethanol ratio, the capsules showed poor stability when exposed to high temperature（60 ℃） and strong light（4500±500 Lux） for 10 days, but were relatively stable at high humidity（92.5% RH）. The results of the long-term stability（25±2 ℃ and 60%±10% relative humidity） study showed that DFP granules were more stable than DFP capsules, and were stable for 12 months. The type of encapsulating material did not affect the 2-month stability of DFP. DFP granules are sensitive to granulating solvent and drying temperature and DFP capsules should be stored away from high temperature and strong light.
