哈尔滨商业大学学报(自然科学版)
哈爾濱商業大學學報(自然科學版)
합이빈상업대학학보(자연과학판)
JOURNAL OF HARBIN UNIVERSITY OF COMMERCE(NATURAL SCIENCES EDITION)
2015年
2期
146-148,165
,共4页
郭玉岩%孟令超%吕邵娃%王锐%李永吉
郭玉巖%孟令超%呂邵娃%王銳%李永吉
곽옥암%맹령초%려소왜%왕예%리영길
盐酸青藤碱%局部给药%药代动力学
鹽痠青籐堿%跼部給藥%藥代動力學
염산청등감%국부급약%약대동역학
sinomenine hydrochloride%topical drug delivery system%topical pharmacokinet-ics
研究外用给药制剂盐酸青藤外敷散多次给药后有效成分盐酸青藤碱在实验大鼠局部组织的药代动力学,探索其在局部给药系统中的药动学行为.对实验大鼠后足造模并贴敷给药后,测定大鼠给药足组织内盐酸青藤碱的吸收量,并用PKSolver药动学软件进行药动学参数的计算与曲线的拟合.药动学参数Lambda_z、Vz/F_obs、Tmax、Css、DF%值分别为0.14 d-1、5.64 mL/mg、2 d、0.24 mg/mL、75%.从药动学数据可知药物在局部组织中含量较高,局部患处在高质量浓度的药物作用下,可达到较好的治疗效果,且外用局部给药可减少全身用药的不良反应,耐受性良好.
研究外用給藥製劑鹽痠青籐外敷散多次給藥後有效成分鹽痠青籐堿在實驗大鼠跼部組織的藥代動力學,探索其在跼部給藥繫統中的藥動學行為.對實驗大鼠後足造模併貼敷給藥後,測定大鼠給藥足組織內鹽痠青籐堿的吸收量,併用PKSolver藥動學軟件進行藥動學參數的計算與麯線的擬閤.藥動學參數Lambda_z、Vz/F_obs、Tmax、Css、DF%值分彆為0.14 d-1、5.64 mL/mg、2 d、0.24 mg/mL、75%.從藥動學數據可知藥物在跼部組織中含量較高,跼部患處在高質量濃度的藥物作用下,可達到較好的治療效果,且外用跼部給藥可減少全身用藥的不良反應,耐受性良好.
연구외용급약제제염산청등외부산다차급약후유효성분염산청등감재실험대서국부조직적약대동역학,탐색기재국부급약계통중적약동학행위.대실험대서후족조모병첩부급약후,측정대서급약족조직내염산청등감적흡수량,병용PKSolver약동학연건진행약동학삼수적계산여곡선적의합.약동학삼수Lambda_z、Vz/F_obs、Tmax、Css、DF%치분별위0.14 d-1、5.64 mL/mg、2 d、0.24 mg/mL、75%.종약동학수거가지약물재국부조직중함량교고,국부환처재고질량농도적약물작용하,가체도교호적치료효과,차외용국부급약가감소전신용약적불량반응,내수성량호.
To study pharmacokinetics of sinomenine hydrochloride which is the active ingredi-ent of Qingfangzhongtongwaifusan in local tissue of rats, and to explore the behavior of the topical drug delivery system through the experiment.After inducing animal model of human arthritis, the rats were applied to SHPEA in the form of transdermal administration.Subse-quently, the absorption of sinomenine hydrochloride was examined in dosed pedis of rats. The pharmacokinetics parameters were calculated and the curve was fitted by the PKS phar-macokinetic software automatically.The pharmacokinetic parameters were as follows Lambda_z(0.14)d-1, Vz/F_obs(5.64) mL/mg, Tmax(2)d, Css(0.24) mg/mL, DF%(75)%, respectively.The pharmacokinetic data showed that drug concentration was higher in local tissue of rats and the topical efficacy was powerful.With the effect of higher concentration of drug in topical lesions, it not only achieved a good treatment results but also reduced system adverse reactions.Topical delivery system also produced well toleration.