OBJECTIVE:To study the contents of the medicinal components in Artemisia annua from different habitats.METHODS:A total of 22 batches of Artemisia annua samples from different habitats throughout China were collected with artemisinic acid,arteannuin B,artemisinin and scopoletin determined by HPLC.The contents of the constituents were taken as indexes to conduct correlation analysis and cluster analysis.RESULTS:The results of correlation analysis and cluster analysis showed that there were marked differences in the contents of the above-mentioned 4 constituents in Artemisia annua from various habitats.CONCLUSION:Accumulation of active ingredients of Artemisia annua is correlated to the habitats to some degree.

AIM: To establish a standard for quality control of Xinfang Biyan Capsule(Radix Saponikovae, Radix Angelicae Dahuricae, Radix Scutellariae, etc.). METHODS: TLC and HPLC were used. RESULTS: Flos Magnoliae, Radix Saponikovae, Flos Chrysanthemi, Radix Bupleuri in the capsule could be identified by TLC, and baicalin content in the capsule could be measured by RP-HPLC with a linear relatioship at a range of 0.243 ?g- 2.43 ?g(r= 0.999 8 ). The average recovery was 98.15% and RSD was 0.15% . CONCLUSION: The methods are accurate and can be used for the quality control of Xinfang Biyan Capsules.

Objective To optimize and establish the extractive technology of taxol from Taxus baccatal L.. Methods HPLC was applied to determine the content of taxol. The orthogonal test was adopted to examine the effects of the 4 factors consisting of ethanol concentration,ethanol volume,extractive times and extractive time. Results Ethanol concentration and ethanol volume were essential factors influencing the extraction of taxol. High concentration and amount of ethanol facilitated the extraction. Extractive times and extractive time were also important. By single-factorial effect,2 h and 2 times in each extraction of taxol were the best. Conclusion The optimum extractive condition is T9 (A3B3C2D1) and T8 (A3B2C1D3).

Objective To examine the effects and mechanisms of simvastatin and fenofibrate, and combination of the two drugs on the expression of apolipoprotein M (apoM). Methods The male C57BL/6N mice ( n =32) were random divided into four groups, including control group (with no special treatment), statin group (with simvastatin [10mg/( kg · d) for 4 weeks], fibrate group (with fenofibrate [100mg/( kg · d) for 4 weeks] and combination group ( with simvastatin [10mg/( kg· d)] and fenofibrate [100mg/( kg · d) for 4 weeks]. The levels of apoMmRNA and protein, hepatic nuclear factor (HNF-1α)mRNA, liver X receptor-α (LXRα) mRNA in mouse liver were measured. Results Both of simvastatin and fenofibrate can increase the expression of apolipoprotein M ( 1.97 ± 0. 04,2. 02 ± 0. 02 ) and HNF-1αmRNA ( 1.74 ± 0. 05,1.71 ± 0. 04). Combination group obtained more effects than either single agent ( P ＜ 0. 05 ). Simvastatin could decrease the expression of LXRα mRNA ( 1.00 ± 0. 02 ) ( P ＜ 0. 05 ). Fenofibrate could increase the expression of LXRα mRNA(2. 80 ±0. 04) ( P ＜0. 05). No significant difference in LXRα expression was seen between combination( 1.56 ±0. 03 ) and control group( 1.53 ±0. 03 )( P ＞0. 05). Conclusions Simvastatin and fenofibrate can increase apoM expression. Treatment with combination of the two drugs is more effective, and the mechanism might be related to the regulation of HNF-1α and LXRα.

Objective To assess the efficacy and safety of fluvastatin sodium extended-release tablets (fluvastatin XL) 80 mg once daily compared to fluvastatin sodium immediate-release capsules (fluvastatin IR) 40 mg twice daily in Chinese hyperlipidemic patients with moderate or high cardiovascular risk.Methods In this multi-center,randomized,double-blind,double-dummy,active-controlled,parallel-group study,after 6-week open-label treatment with fluvastatin IR 40 mg once daily,patients who did not reach their lipid goals were randomized to 12-week double-blind treatment with fluvastatin XL 80 mg once daily or fluvastatin IR 40 mg twice daily.Results (1) There were 218 patients enrolled in each group.At the study endpoint,no statistical difference was found in the mean percent change from baseline for LDL-C with-8.69％ [from (3.504 ±0.060) mmol/L to (3.153 ±0.065) mmol/L] in the fluvastatin XL group and-7.89％ [from (3.491 ±0.050) mmol/L to (3.181 ±0.060) mmol/L] in the fluvastatin IR group (P ＞ 0.05).The 95％ CI for difference between the two groups in adjusted mean percent change from baseline was (-4.70％-3.09％),which was within the pre-specified non-inferiority margin.In the fluvastatin XL group,the proportion of patients with moderate cardiovascular(CV) risk and high CV risk achieving their LDL-C treatment goals at endpoint was 50.0％ and 31.5％ respectively,while the proportion was 42.5％ and 24.5％ respectively in the fluvastatin IR group.No significant difference was found between the two groups in the proportion of patients who reached their lipid goals and the changes from baseline with other lipid parameters.(2)Similar safety profiles were observed in the two treatment groups,with 21.1％ adverse event (AE) (8.3％ study-drug related AE) in the fluvastatin XL group and 17.0％ AE (6.3％ study-drug related AE) in the fluvastatin IR group.Conclusion The efficacy of fluvastatin XL 80 mg once daily is comparable to fluvastatin IR 40 mg twice daily in Chinese hyperlipidemic patients with moderate or high cardiovascular risk and both treatments are safe and well-tolerated.

OBJECTIVETo develop an HPLC-UV-ELSD method for the determination of aucubi, harpagide, harpagoside, angoroside C and cinnamic acid in Scrophularia ningpoensis.

METHODThe analytical column was SHIMADZU C18 (4.6 mm x 250 mm, 5 microm). The mobile phase was acetonirile-0.4% acetic acid in a gradient elution. Initial conditions was 5% A; 0-20 min, changed to 10% A; 20-50 min, to 55% A. The flow rate was 0.8 mL x min(-1) and the column temperature was 30 degrees C. The UV detector wavelength was set at 280 nm for harpagoside, angoroside C and cinnamic acid, and the evaporative light-scattering detector (ELSD) drift tube temperature was 105 degrees C, the flow rate of nebulizer gas was 1.2 L x min(-1) for aucubi and harpagide.

RESULTAucubi, harpagide, harpagoside, angoroside C and cinnamic acid was separated well. The linear calibration curves were obtained over of 0.752-13.536 microg for aucubi (r=0.9993, n=6), 0.8280-14.90 microg for harpagide (r=0.9994, n=6), 0.6360-11.45 microg for harpagoside (r=0.9997, n=6), 0.5440- 9.792 microg for angoroside C, (r=0.9997, n=6) and 0.0108-0.1939 microg for cinnamic acid (r=0.9999, n=6). The mean recovers of five compounds were 98.12%, 99.14%, 100.21%, 98.17% and 100.35% with RSD of 2.3%, 1.5%, 1.9%, 1.7% and 0.5%.

CONCLUSIONThis method could simultaneously determinate the content of the five compounds in the S. ningpoensis.

Objective To investigate the bioavailability and pharmacokinetics of silybin A and silybin B in rats,respectively.Methods Following iv and ig administration of silybin to 20 Wistar rats,the plasma samples were collected at different time points up to 12 h.Sample pretreatment was involved in one-step protein precipitation with acetonitrile.Silybin A and silybin B were simultaneously determined by LC-MS/MS.Results After ig dosing silybin 28,56,and 112 mg/kg to rats,the t1/2β values were 5.48,5.08,and 5.73 h for silybin A,and 4.56,4.12,and 5.53 h for silybin B; The Cmax were 674.3,1349.4,and 2042.5 ng/mL for silybin A,and 671.0,1365.4,and 2066.2 ng/mL for silybin B; The Tmax were 0.20,0.23,and 0.20 h for silybin A,and 0.20,0.23,and 0.20 h for silybin B; The AUC were 454.4,845.9,and 1219.5 h·ng/mL for silybin A,and 432.0,817.1,and 1153.6 h·ng/mL for silybin B.The absolute bioavailabilities of silybin A and silybin B were 2.86％ and 1.93％,respectively.Conclusion Silybin A and silybin B have very low bioavailability after ig administration,and there is no significant difference in the pharmacokinetic parameters between silybin A and silybin B,which indicates that the two diastereoisomers have similar pharmacokinetic behavior in rats.

AIM: To optimize the preparation of cholic acid-hydroxypropy-?-cyclodextrin inclusion complex,and its phase solubility analysis. METHODS: Orthogonal test,including molar ratio,inclusion temperature,mixing time and liquid dropping rate of cholic acid-HP-?-CD,was adopted to screen the optimal preparation,based on the inclusion efficiency by HPLC method.The solubilization effect was evaluated by using phase solubility.(RESULTS): The optimal preparation consisted of the molar ratio of cholic acid-HP-?-CD was 1∶3,60 ℃ inclusion temperature,60 min mixing time,1.6 mL/min liquid dropping rate;A_L type of phase solubility curve,K=564.30 L/mol,and 11.81 times solubilization. CONCLUSION: The optimal preparation is stable,reasonable and practicable with the encapsulation efficiency of 97.1%.Inclusing cholic acid with HP-?-CD is feasible,and the solubilization effect is significant.

Objective To investigate effects of hyperbaric oxygen (HBO) therapy on C-reactive protein (CRP) and tumor necrosis factor-α (TNF-α) levels in patients with moderate or severe traumatic brain injury (TBI)and to analyze its therapeutic efficacy. Methods One hundred and eight patients with moderate or severe TBI were randomly divided into a control group (54 cases) and an HBO adjunctive therapy group (HBO group, 54 cases).Both groups received essential neurosurgical treatment and conventional drug treatment, and the HBO group was given one session of HBO therapy in addition. Serum CRP and TNF-α were detected, and the scores on the Glasgow coma scale (GCS) were measured before and after treatment. CRP was detected by turbidimetric immunoassay and TNF-α using ELISA. Glasgow outcome scale (GOS) scores were evaluated in a follow-up 6 months after injury. Results Average CRP, TNF-α and GCS measurements showed no statistically significant difference between the groups before treatment. After treatment, CRP and TNF-α were significantly lower and GCS scores significantly better in both groups, but patients in the HBO group were, on average, significantly better than the controls on all three measures.Six months later, GOS evaluation gave a significantly larger number of patients with a better prognosis in the HBO group compared with the controls. Conclusion HBO therapy can significantly decrease serum CRP and TNF-α after severe TBI, thus enhancing therapeutic efficacy.

Aim To investigate the pharmacokinetic characteristics of silibinin in Chinese healthy volunteers.Methods Nine Chinese male healthy volunteers were divided into receiving orally a single dose of silibinin capsule corresponded 70,140 and 280 mg of silibinin,respectively,in Latin square design study.After administration of silibinin capsule,the plasma concentrations were determined by HPLC with UV detection.The pharmacokinetic parameters were analyzed by Topfit 2.0 program.Results The linearity of this method was found to be from 3.125 to 10 000 μg·L~(-1) with a lower limit of quantitation(LLOQ) of 3.125 μg·L~(-1) for silibinin.The pharmacokinetic parameters were calculated as the follows:at the three different dosages(70,140 and 280 mg),T_(1/2) was 2.44,2.38 and 2.47 h;C_(max) was 1135.6,2841.1 and 3946.9 μg·L~(-1);T_(max) was 1.35,1.26 and 1.39 h;AUC_(0-11 h) was 1287.2,3337.8 and 5398.5 μg·h·L~(-1);AUC_(0-∞)was 1300.7,3377.1 and 5453.9 μg·h·L~(-1);CL/F was 1062.1,824.7 and 943.2 ml·min~(-1);And V_d was 219.9,167.1 and 212.0 L,respectively.Conclusions The developed method is shown to be sensitive,accurate and simple,and can satisfy the requirement of pharmacokinetic study of silibinin in human.The C_(max),AUC_(0-11 h) and AUC_(0-∞) of silibinin in Chinese healthy volunteers(in ranges of 40～120 mg)are fitted with non-linear kinetic model,while there are no significant differences in T_(1/2) at the three different dosages.