实用药物与临床
實用藥物與臨床
실용약물여림상
Practical Pharmacy and Clinical Remedies
2015年
11期
1280-1283
,共4页
李婷婷%刘艳%冯立影%梁晓玲%赵海峰%刘高峰
李婷婷%劉豔%馮立影%樑曉玲%趙海峰%劉高峰
리정정%류염%풍립영%량효령%조해봉%류고봉
华法林%刺五加注射液%抗凝作用%药物相互作用
華法林%刺五加註射液%抗凝作用%藥物相互作用
화법림%자오가주사액%항응작용%약물상호작용
Warfarin%Ciwujia injection%Anticoagulant effect%Drug interactions
目的 研究刺五加注射液对大鼠华法林抗凝作用的药效学和药动学影响,为临床合理用药提供参考. 方法 将Wistar雄性大鼠随机分成空白对照组( A组)、刺五加注射液给药组( B组)、华法林对照组( C组)、华法林-刺五加注射液联合给药组(D组),4 组大鼠连续腹腔注射生理盐水或刺五加注射液(15 mL/kg) 14 d. 第8天,A、B两组灌胃给予相同剂量的生理盐水,C、D两组灌胃给予华法林溶液(0.2 mg/kg),并于设定的一系列时间点取血. 用血凝分析仪测定凝血酶原时间( PT)、活化部分凝血活酶时间( APTT) ,并计算国际标准化比值( INR). 用UPLC-MS/MS法联合手性色谱柱技术测定血浆中华法林(包括S-型和R-型)浓度,用 DAS 2. 0软件计算药代动力学参数. 结果 刺五加注射液对PT、APTT及INR无明显影响;与华法林对照组比较,合用刺五加注射液后,华法林(包括S-型和R-型)的药动学参数Cmax、AUC0-t和AUC0-∞等显著升高( P<0. 05或P<0. 01),药效学参数PT及INR显著增加(P<0. 05或P<0. 01). 结论 刺五加注射液可减慢华法林(包括S-型和R-型)的代谢,使华法林抗凝作用增强. 提示临床用药时应尽量避免两药联合应用,以避免出血风险,如必须联用,应密切监测.
目的 研究刺五加註射液對大鼠華法林抗凝作用的藥效學和藥動學影響,為臨床閤理用藥提供參攷. 方法 將Wistar雄性大鼠隨機分成空白對照組( A組)、刺五加註射液給藥組( B組)、華法林對照組( C組)、華法林-刺五加註射液聯閤給藥組(D組),4 組大鼠連續腹腔註射生理鹽水或刺五加註射液(15 mL/kg) 14 d. 第8天,A、B兩組灌胃給予相同劑量的生理鹽水,C、D兩組灌胃給予華法林溶液(0.2 mg/kg),併于設定的一繫列時間點取血. 用血凝分析儀測定凝血酶原時間( PT)、活化部分凝血活酶時間( APTT) ,併計算國際標準化比值( INR). 用UPLC-MS/MS法聯閤手性色譜柱技術測定血漿中華法林(包括S-型和R-型)濃度,用 DAS 2. 0軟件計算藥代動力學參數. 結果 刺五加註射液對PT、APTT及INR無明顯影響;與華法林對照組比較,閤用刺五加註射液後,華法林(包括S-型和R-型)的藥動學參數Cmax、AUC0-t和AUC0-∞等顯著升高( P<0. 05或P<0. 01),藥效學參數PT及INR顯著增加(P<0. 05或P<0. 01). 結論 刺五加註射液可減慢華法林(包括S-型和R-型)的代謝,使華法林抗凝作用增彊. 提示臨床用藥時應儘量避免兩藥聯閤應用,以避免齣血風險,如必鬚聯用,應密切鑑測.
목적 연구자오가주사액대대서화법림항응작용적약효학화약동학영향,위림상합리용약제공삼고. 방법 장Wistar웅성대서수궤분성공백대조조( A조)、자오가주사액급약조( B조)、화법림대조조( C조)、화법림-자오가주사액연합급약조(D조),4 조대서련속복강주사생리염수혹자오가주사액(15 mL/kg) 14 d. 제8천,A、B량조관위급여상동제량적생리염수,C、D량조관위급여화법림용액(0.2 mg/kg),병우설정적일계렬시간점취혈. 용혈응분석의측정응혈매원시간( PT)、활화부분응혈활매시간( APTT) ,병계산국제표준화비치( INR). 용UPLC-MS/MS법연합수성색보주기술측정혈장중화법림(포괄S-형화R-형)농도,용 DAS 2. 0연건계산약대동역학삼수. 결과 자오가주사액대PT、APTT급INR무명현영향;여화법림대조조비교,합용자오가주사액후,화법림(포괄S-형화R-형)적약동학삼수Cmax、AUC0-t화AUC0-∞등현저승고( P<0. 05혹P<0. 01),약효학삼수PT급INR현저증가(P<0. 05혹P<0. 01). 결론 자오가주사액가감만화법림(포괄S-형화R-형)적대사,사화법림항응작용증강. 제시림상용약시응진량피면량약연합응용,이피면출혈풍험,여필수련용,응밀절감측.
Objective To study the effects of ciwujia injection on the pharmacodynamics and pharmacokinet-ics of warfarin in rats, and to provide reference for rational drug use of combination therapy. Methods Wistar rats were randomly divided into four groups,blank control group (group A),ciwujia injection group (group B),warfarin control group ( group C) ,warfarin combined ciwujia injection group ( group D) ,eight rats in each group. The rats of four group swere administered physiological saline or ciwujia injection (15 mL/kg) by caudal vein for 14 consecutive days. On the 8th day,rats in group A and group B were orally administered with the same dose of physiological saline, and rats in group C and group D were orally administered with warfarin solution ( 0. 2 mg/kg ) . The blood samples were collected from the caudal veins at different time points. The prothrombintime ( PT) and activated partial thrombo-plastin time ( APTT) of the blood samples were determined by coagulation analyzer,and the blood concentrations of S-warfarin and R-warfarin were determined by UPLC-MS/MS. Pharmacokinetic parameters were calculated by DAS 2. 0 software. Results Ciwujia injection had no effect on PT,APTT and INR,but ciwujia injecion combined with warfarin could increase the blood concentrations of warfarin (including S-type and R-type,P<0. 05 or P<0. 01)and the valne of PT and INR significantly (P<0. 05 or P<0. 01). Conclusion Ciwujia injection could decrease the metabolism of warfarin ( including S-type and R-type) ,and increase the anticoagulant effect. Therefore,the combination use of the two drugs should be refrained,in order to avoid the risk of bleeding. Special monitoring should be carried out if the combi-nation therapy is used.
