OBJECTIVE: To study the pharmacokinetics and bioavailability of Ibuprofen Sustained Release Tablets in healthy volunteers.METHODS: A total of 18 male healthy volunteers were randomly divided into two groups.They were assigned to receive Ibuprofen Sustained Release Tablets(trial preparation) and Ibuprofen Sustained Release Capsules(reference preparation) respectively.The concentrations of ibuprofen in plasma were determined by RP-HPLC.The main pharmacokinetic parameters were obtained using 3p97 program.RESULTS: The Cmax of the two preparations were(25.43?0.78) ?g?mL-1 and(26.87?0.66)?g?mL-1 respectively;tmax were(3.67?0.52) h and(3.83?0.75) h;AUC0～24 were(181.20?5.12)?g?h?mL-1 and(187.58?5.29)?g?h?mL-1;AUC0～∞ were(184.34?5.35)、(191.19?4.87)?g?h?mL-1;MRT were(6.51?0.73)h and(6.80?0.48) h,respectively.The relative bioavailability of the sustained-release tablets was 103.7%.CONCLUSION: The ibuprofen sustained release tablets have remarkable sustained release efficacy.

Objective To study the determination of chromium in human hair by spectrophotometry using starch as color agent. Methods The total chromium(Cr)in human hair was oxidized by (NH4?雪2S2O3 into Cr6+,which could oxidize KI to form I-3 in acid medium. I-3 reacted with starch to form a blue colored complex,which revealed the maximum absorption peak at 590 nm. Results The contents of Cr in human hair were 8.46-29.56 ?g/g.The lowest detection limit and linear range were 0.02 and 0.02-1.0 ?g/ml respectively.The coefficient of variation and standard material-added recovery rates were 3.3% and 94.8%-104.5% respectively. Conclusion This methods was rapid,accurate and convenient for the determination of chromium in human hair.

OBJECTIVE: To prepare and evaluate the quality of clarithromycin microcapsules.METHODS: Clarithromycin microcapsules were prepared by emulsion-solvent volatilixation method using ethylcellulose as capsule wall material.The particle size,entrapment efficiency,the loading amount and the drug release property in vitro were investigated.RESULTS: The prepared microcapsules were well-distributed in particle size with average particle size at 33.0～38.0 ?m,encapsulation efficiency at above 87%,loading amount above 45%,and accumulative drug release rate of 75% at 6 h.CONCLUSION: The method is simple and feasible and the quality of prepared microcapsules is up to the standard.

OBJECTIVE:To observe the anti-inflammatory,diuretic,and antipyretic action of Miniaoning granules after improvement of its preparation technology.METHODS:The rats' feet swelling degree and the mice's ear swelling degree,the urine volume,and the body temperature action of Miniaoning granules in vitro were observed through rats' feet swelling method,dimethyl benzene-induced mice ear swelling method,diuretic experiment,yeast-induced rats' febrile,respectively.RESULTS:After medication,the degree of rats' feet swelling and mice's ear swelling were significantly attenuated,and the urine volume increased markedly and body temperature lowered.CONCLUSION:As compared with the original formulations,Miniaoning granules prepared in improved technology have similar antipyretic effect but more potent anti-inflammatory and.diuretic action.

To develop a method for the distinction of genuine Gastrodia elata B1. from its four falsified plants of common occurrence and determination of its active principle, gastrodin by capillary electrophoresis. Methods　The electrophoretic conditions were a buffer solution containing 24 mmol/L borate (pH=9.4), at a voltage of 16 kV. Results　The electrophorograms obtained under the above conditions showed easily distinguishable differences. Baseline separation of gastrodin was achieved and its quantitative analysis can be accomplished within 15 min. The linear correlation equation was Y=-0.048+7.79X (r=0.999). Conclusion　This method could serve as an easy and precise method for the quality control of G. elata.

A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2-amines were prepared from thiophenol by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol x L(-1), and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.

N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.

A series of novel 2-amino-4-phenylthiazole derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase were investigated. 2-Amino-4-phenylthiazoles were prepared from alpha-bromoacetophenones by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 8a was the best of them. The IC50 of 8a to AChE is 3.54 micromol x L(-1), and the value was better than that of rivastigmine. 2-Amino-4-phenylthiazole derivatives showed a certain bioactivity in vitro, which were worth further investigation.

Object To develop a method for the distinction of genuine Gastrodia elata B1 from its four falsified plants of common occurrence and determination of its active principle, gastrodin by capillary electrophoresis Methods The electrophoretic conditions were a buffer solution containing 24 mmol/L borate (pH=9 4), at a voltage of 16 kV Results The electrophorograms obtained under the above conditions showed easily distinguishable differences Baseline separation of gastrodin was achieved and its quantitative analysis can be accomplished within 15 min The linear correlation equation was Y=-0 048+7 79X (r=0 999) Conclusion This method could serve as an easy and precise method for the quality control of G elata

BACKGROUND: Recently, it is investigated that shell of plantain seed is a soluble dietary fiber which can be added into foods to regulate content of cholesterol.OBJECTIVE: To investigate the interventional effect of plantain seed on lipid and its lipid peroxidation in rats with hyperlipidemia.DESIGN: Completely randomized grouping design and controlled animal study.SETTING: Laboratory of Pharmacology and Toxicology for New Drug in Hebei Province.MATERIALS: ① A total of 24 healthy SD rats, of grade I, aged 60-70 days, weighting (210±22) g, of either gender, were selected in this study. ② Basic feed was provided by Experimental Animal Center in Hebei Province,and the fractional mass of each component was mentioned as following:flour 0.25, bran 0.1, corn dust 0.22, bean cake 0.22, fish dust 0.02, bone dust 0.02, grass dust 0.05, salt 0.01, yeast dust 0.02, and sunflower seed 0.03. High fat feed was provided by Experimental Animal Center in Hebei Province, and the fractional mass of each component was mentioned as following: basic 0.9, cholesterol 0.015, lard 0.08, and hyocholic salt 0.003.③ Lipid kit was provided by Baoding Changcheng Clinical Reagent Company, and kits of superoxide dismutase (SOD), catalase (CAT),glutathione peroxidase (GSH-Px) and malondialdehyde (MDA) were provided by Nanjing Jiancheng Bioengineering Institute.METHODS: The experiment was completed at the Laboratory of Pharmacology and Toxicology for New Drug in Hebei Province from June to December 2004. ① All 24 rats were randomly divided into 3 groups:normal control group, model group and plantain seed group with 8 in each group. Rats in the normal control group were fed with basic feed. Rats in plantain seed group were fed with high fat feed + 15 g/kg plantain seed and drank routinely. Experimental rats were fed in cages, respectively.Each one was fed with 25 g/d food and drunk freely. The experimental cycle was 12 weeks. ② At the end of experiment, rats were anesthetized to assayed levels of serum triacylglycerol (TG), total cholesterol (TC), high density lipoprotein cholesterol (HDL-C), serum SOD and MDA, activities of CAT and SOD in myocardial tissue, content of MDA, and activities of CAT and GSH-Px in hepatic tissue with related kits. ③ Measurement data were compared between each two group with t test.MAIN OUTCOME MEASURES:Comparison of serum lipid level and anti-oxidation among groups at 12 weeks after modeling.RESULTS: All 24 rats were involved in the final analysis. ① At 12 weeks after modeling, activities of SOD in serum and myocardial tissue were lower in model group than those in normal control group and plantain seed group (P ＜ 0.05), but levels of MDA in serum and myocardial tissue were higher in model group than those in normal control group and plantain seed group (P ＜ 0.05). ② At 12weeks after modeling, activities of CAT and GSH-Px in serum and myocardial tissue were lower in model group than those in normal control group and plantain seed group (P ＜ 0.05). ③ At 12 weeks after modeling, levels of TC and TG in serum were higher in model group than those in normal control group and plantain seed group (P ＜ 0.05), but level of HDL-C and ratio between HDL-C and TC in serum were lower in model group than those in normal control group and plantain seed group (P ＜ 0.05).CONCLUSION: Plantain seed at dosage of 15 g/kg can decrease content of lipid and strengthen anti-oxidation of economy in rats with hyperlipidemia.