中华胃肠外科杂志
中華胃腸外科雜誌
중화위장외과잡지
CHINESE JOURNAL OF GASTROINTESTINAL SURGERY
2011年
12期
973-976
,共4页
卡纳琳%卡纳琳-紫杉醇混悬剂%腹腔化疗%淋巴靶向化疗%药代动力学
卡納琳%卡納琳-紫杉醇混懸劑%腹腔化療%淋巴靶嚮化療%藥代動力學
잡납림%잡납림-자삼순혼현제%복강화료%림파파향화료%약대동역학
Carbon nanoparticle suspension%Carbon nanoparticle-paclitaxel suspension%Intraperitoneal chemotherapy%Lymph-targeted chemotherapy
目的 制备卡纳琳-紫杉醇混悬剂并研究其腹腔化疗的药代动力学.方法 高效液相色谱法测定卡纳琳-紫杉醇的饱和吸附率,制备混悬剂.将34只Wistar大鼠随机分为实验组与对照组,分别腹腔注射卡纳琳-紫杉醇混悬液及单纯紫杉醇溶液,给药后7d内的不同时间点取各组大鼠血液、肠系膜淋巴结及腹腔洗液样本,采用高效液相-二级质谱联用法对紫杉醇浓度进行分析.结果 每1ml卡纳琳可饱和吸附7 mg紫杉醇.实验组血浆药物曲线下面积(AUC)为对照组的0.63倍；淋巴结药物AUC为对照组的0.73倍；腹水药物AUC为对照组的1.25倍.实验组血浆药物代谢半衰期(t1/2)为对照组的1.61倍；腹水药物t1/2为对照组的0.88倍；淋巴结药物t1/2为对照组的1.10倍.结论 卡纳琳对紫杉醇吸附作用良好.以卡纳琳-紫杉醇混悬剂行腹腔化疗具有血药浓度低、腹腔药物浓度高、安全性高的特点,但淋巴靶向性及淋巴组织滞留作用不明显,其机制有待进一步研究.
目的 製備卡納琳-紫杉醇混懸劑併研究其腹腔化療的藥代動力學.方法 高效液相色譜法測定卡納琳-紫杉醇的飽和吸附率,製備混懸劑.將34隻Wistar大鼠隨機分為實驗組與對照組,分彆腹腔註射卡納琳-紫杉醇混懸液及單純紫杉醇溶液,給藥後7d內的不同時間點取各組大鼠血液、腸繫膜淋巴結及腹腔洗液樣本,採用高效液相-二級質譜聯用法對紫杉醇濃度進行分析.結果 每1ml卡納琳可飽和吸附7 mg紫杉醇.實驗組血漿藥物麯線下麵積(AUC)為對照組的0.63倍；淋巴結藥物AUC為對照組的0.73倍；腹水藥物AUC為對照組的1.25倍.實驗組血漿藥物代謝半衰期(t1/2)為對照組的1.61倍；腹水藥物t1/2為對照組的0.88倍；淋巴結藥物t1/2為對照組的1.10倍.結論 卡納琳對紫杉醇吸附作用良好.以卡納琳-紫杉醇混懸劑行腹腔化療具有血藥濃度低、腹腔藥物濃度高、安全性高的特點,但淋巴靶嚮性及淋巴組織滯留作用不明顯,其機製有待進一步研究.
목적 제비잡납림-자삼순혼현제병연구기복강화료적약대동역학.방법 고효액상색보법측정잡납림-자삼순적포화흡부솔,제비혼현제.장34지Wistar대서수궤분위실험조여대조조,분별복강주사잡납림-자삼순혼현액급단순자삼순용액,급약후7d내적불동시간점취각조대서혈액、장계막림파결급복강세액양본,채용고효액상-이급질보련용법대자삼순농도진행분석.결과 매1ml잡납림가포화흡부7 mg자삼순.실험조혈장약물곡선하면적(AUC)위대조조적0.63배；림파결약물AUC위대조조적0.73배；복수약물AUC위대조조적1.25배.실험조혈장약물대사반쇠기(t1/2)위대조조적1.61배；복수약물t1/2위대조조적0.88배；림파결약물t1/2위대조조적1.10배.결론 잡납림대자삼순흡부작용량호.이잡납림-자삼순혼현제행복강화료구유혈약농도저、복강약물농도고、안전성고적특점,단림파파향성급림파조직체류작용불명현,기궤제유대진일보연구.
Objective To prepare carbon nanoparticle-paclitaxel suspension (CNPS) and to study the pharmacokinetics of intraperitoneal chemotherapy with CNPS.Methods Saturated absorption capacity of carbon nanoparticle suspension (CNS) and paclitaxel were detected by high performance liquid chromatography in order to prepare the above suspension.Wistar rats were randomly divided into the experimental group (A) and the control group (B),to which intraperitoneal injections of CNPS and paclitaxel were given respectively.At different time points,measure the blood samples,mesenteric lymph nodes,and intraperitoneal lavage fluid were collected to measure the concentration of paclitaxel.Results One ml CNS could absorb 7 mg paclitaxel by maximum.The ratio of area under the curve (AUC) in the plasma of group A to group B was 0.63.The ratio of AUC in lymph nodes of group A to group B was 0.75 and that in intraperitoneal lavage fluid was 1.25.The metabolic half-life (t1/2) of paclitaxel in the plasma of group A was 1.61 times as long as that of group B.The t1/2 of paclitaxel in intraperitoneal lavage fluid of group A was 0.88 as long as that of Group B.The t1/2 of paclitaxel in lymph nodes of group A was 1.10 as long as that of Group B.Conclusions CNS has a high absorption capacity with paclitaxel.Intraperitoneal chemotherapy by CNPS is characterized by low drug concentration in the blood,high drug concentration in the peritoneal cavity and high safety.However,the targeting and lymphatic retention effect are not significant.The mechanism warrants further investigation.
