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- 저자 : Dongxun Li (검색결과 4 건)
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Lihua Chen,Dongxun Li,Guosong Zhang,Wei Zhang,Lihua Zhang,Yongmei Guan,Weifeng Zhu,Hongning Liu 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.6
Peimisine, the common ingredient of ‘‘zhebeimu’’groups and ‘‘chuanbeimu’’ groups, is responsiblefor the expectorant and cough relieving effects. The aim ofthis study was to investigate the pharmacokinetics, tissuedistribution and excretion of peimisine in male and femaleSD (Sprague-Dawley) rats by a rapid and sensitive LC-MS/MS (liquid chromatography-tandem mass spectrometry)method used carbamazepine as the internal standard afteroral administration, carbamazepine was stated as an IS. The results showed that peimisine was slowly distributed,and eliminated from rat plasma and manifested lineardynamics in a dose range of 0.26–6.5 mg/kg. Tested byANOVA, there were gender differences in the pharmacokineticparameters of AUC0-t, AUC0-? among a singledose of 0.26, 1.3, 6.5 mg/kg (P\0.05). Drug blood andtissue levels in male rats were significantly higher than thefemale counterparts after oral administration, while boththe males and the females showed high drug levels inspleen, kidney, lung, liver and heart. On the other hand, thepeimisine levels that can be reached in uterus, ovary, testisand brain is low. The excretion study showed that littleadministered peimisine (\0.7 %) was recovered in themale and female bile. Approximately 13.46 and 15.05 %were recovered in female urine and feces, while 43.07 and7.49 % were recovered in male urine and feces, respectively,which indicated that the major elimination route ofmale rats was urine excretion. In addition, there was significantdifferences in total cumulative excretive ratio ofpeimisine in feces (P\0.05) and no significant differencesin the urine (P[0.05) at a dose of 1.3 mg/kg.
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김경수,김정현,진성규,김동욱,김동식,김종오,용철순,조관형,Dongxun Li,우종수,최한곤 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.4
To investigate the possibility of developing anovel oral pharmaceutical product using fenofibric acidinstead of choline fenofibrate, the powder properties, solubility,dissolution and pharmacokinetics in rats offenofibrate, choline fenofibrate and fenofibric acid werecompared. Furthermore, the effect of magnesium carbonate,an alkalising agent on the solubility, dissolution andoral bioavailability of fenofibric acid was assessed, amixture of fenofibric acid and magnesium carbonate beingprepared by simple blending at a weight ratio of 2/1. Thethree fenofibrate derivatives showed different particle sizesand melting points with similar crystalline shape. Fenofibric acid had a significantly higher aqueous solubilityand dissolution than fenofibrate, but significantlylower solubility and dissolution than choline fenofibrate. However, the fenofibric acid/magnesium carbonate mixturegreatly improved the solubility and dissolution of fenofibricacid with an enhancement to levels similar with thosefor choline fenofibrate. Fenofibric acid gave lower plasmaconcentrations, AUC and Cmax values compared to cholinefenofibrate in rats. However, the mixture resulted in plasmaconcentrations, AUC and Cmax values levels not significantlydifferent from those for choline fenofibrate. Specifically, magnesium carbonate increased the aqueoussolubility, dissolution and bioavailability of fenofibric acidby about 7.5-, 4- and 1.6-fold, respectively. Thus, themixture of fenofibric acid and magnesium carbonate at theweight ratio of 2/1 might be a candidate for an oral pharmaceuticalproduct with improved oral bioavailability.
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김동욱,김영훈,Abid Mehmood Yousaf,김동식,권택관,박정희,김영일,박재현,진성규,김경수,조관형,Dongxun Li,김종오,용철순,우종수,최한곤 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.4
To develop a montelukast sodium–loadedstable oral suspension bioequivalent to the commercialgranules in rats, several montelukast sodium-loaded suspensionswere prepared with a suspending agent, stabilizersand anti-aggregation agents, and their stabilities wereinvestigated by visually observing the sedimentation phenomenonand determining the concentration of the degradationproduct. Moreover, dissolution and pharmacokineticstudies of the optimized formulation were examined in ratscompared to commercial montelukast sodium-loadedgranules. Avicel RC-591 (Avicel), a suspending agent,prevented the sedimentation of these suspensions at[2.496(w/v) per cent composition. Amongst the stabilizers tested,fumaric acid provided the lowest concentration of montelukastsulphoxide (a degradation product) in these suspensionsat 40 C, demonstrating its excellent stabilizingactivity. Furthermore, as an anti-aggregation agent, glyceringave lower amounts of degradation product than thosewith poloxamer 407 and Tween 80. In particular, montelukast-loaded oral suspension, an aqueous suspensioncontaining montelukast sodium/Avicel/fumaric acid/glycerinat a concentration of 312/2496/15.6/62.4 (mg/100 ml),and the commercial granules exhibited similar dissolutionprofiles in 0.5 % (w/v) aqueous solution of sodium laurylsulphate. Moreover, the pharmacokinetics in rats providedby this suspension was comparable to that of the commercialgranules, suggesting that they were bioequivalent. In addition, it was physically and chemically stable at40 C for at least 6 months. Thus, this montelukastsodium-loaded oral suspension, with bioequivalence to thecommercial granules and excellent stability, could be aprospective dosage form for the treatment of asthma.
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