ABSTRACT
A total of twenty-two compounds were isolated from the 95% EtOH extract of Eclipta prostrata by various purification steps, and their structures were established as ecliptalignin A (1)，ecliptasaponin Ⅰ (2), ecliptasaponin Ⅱ (3), echinocystic acid (4), 3-oxo-16α-hydroxy-olean-12-en-28-oic acid (5), acacetin-7--rutinoside (6), luteoloside (7), apigenin (8), luteolin (9), acacetin (10), skullcapflavone Ⅱ (11), kaempferol (12), kaempferide (13), quercetin (14), 4',7-dihydroxyl-3',6'-dimethoxylisoflavone-7--glucoside (15), ecliptal (16), 5-hydroxymethyl-(2,2',5',2″)-terthienyl tiglate (17), psoralen (18), isopsoralen (19), wedelolactone (20), crinumaquine (21), and 2,3,9,12-tetramethoxyprotoberberine (22) mainly based on the spectroscopic techniques, of which 1 was a new lignin analogue, and 5, 6, 10-13, 15, 18, 19, 21 and 22 were isolated form this plant for the first time.
ABSTRACT
OBJECTIVE The purpose of the present study was to investigate the impact of fluvas-tatin formulation on the pharmacokinetics-genetic polymorphis relationship. METHODS We compared the difference between the pharmacokinetics of fluvastatin as an extended-release (ER) 80 mg tablet and an immediate-release(IR)40 mg capsule in terms of drug metabolism enzyme and transporter ge-netic polymorphisms. In this open-label, randomized, two-period, two-treatment, crossover study, ef-fects of BCRP, SLCO1B1, MDR1, CYP2C9, and CYP3A5 polymorphisms on the pharmacokinetics of fluvastatin were analyzed in 24 healthy individuals.Each treatment duration was 7 days with a washout period of 7 days between the crossover.Serum concentration of fluvastatin was evaluated using high-performance liquid chromatography-tandem mass spectrometry. RESULTS The SLCO1B1 T521C genotype had no statistically significant effect on IR 40 mg capsule of fluvastatinafter single or repeated doses.However,for the ER 80 mg tablet,the SLCO1B1 T521C genotype correlated with the AUC0-24of repeat doses (P=0.01). The CYP2C9*3 genotype correlated with the AUC0- 24after the first dose IR 40 mg capsule (P<0.05); however, the difference between CYP2C9*1/*1 and CYP2C9*1/*3 was not statistically significant after repeated doses. CONCLUSION The effect of SLCO1B1 T521C on fluvas-tatin exposure was observed and was more profound in ER and repeated dose administration than in IR and single dose administration.We recommend that formulation should be incorporated into future pharmacogenomics studies and clinical implication guidelines.
ABSTRACT
<p><b>OBJECTIVE</b>Development and use of better medicine for children is a worldwide problem recently, especially in China. The current situation of drugs for children's renal diseases is far from well-understood now. This survey focused on drugs for pediatric renal diseases including immunosuppressants, corticosteroids, diuretics, anticoagulants, hypotensives and antilipemic agents.Information regarding the dosage, form, precaution, usage and administration in inserts was collected in this study.</p><p><b>METHOD</b>Drugs for pediatric renal diseases were selected according to the guidelines established by the Chinese Society of Pediatric Nephrology. The detailed information about the dosage, form of drugs was searched on the website of China-State Food and Drug (SFDA). The information of the precaution, usage and administration was obtained from the China Pharmaceutical Reference, the first edition.</p><p><b>RESULT</b>In this study, there were 5 categories of medicine including immunosuppressants, corticosteroids, diuretics, anticoagulants, hypotensives and antilipemic agents, and 89 kinds of medicine for renal diseases. Among these medicines, 65.2% were found not suitable for children in terms of drug dosage and form, 19.1% did not indicate the precaution, 51.7% did not indicate clearly the safety and effectiveness for children, and 56.2% lacked the detailed information about the usage and administration for children. There were only 4 kinds of these medicines which were studied via clinical trials in children population.</p><p><b>CONCLUSION</b>There is a lack of drugs for children with renal diseases. Most of the time, the medicines used by doctors are not specially manufactured for children. The safety and efficacy of drugs that are currently used to treat pediatric renal diseases are not clear and definite.In addition, few clinical trials have been conducted for evaluation of drugs for pediatric renal diseases.In clinic, the situation of off-label drug treatment is very serious.</p>