摘要
目的在消化性溃疡病人中观察兰索拉唑的药代动力学的变化，进一步了解该药的代谢规律。方法选取经胃镜检查确诊为消化性溃疡的患者为试验组（Ｇ组，ｎ＝６）及健康志愿者为对照组（Ｃ组，ｎ＝６），口服兰索拉唑胶囊３０ｍｇ，定时取血通过高压液相方法测定血药浓度。利用３Ｐ８７药代动力学程序模拟药时曲线，计算药代动力学参数。结果兰索拉唑符合一房室模型。试验组中，５位患者的吸收速率常数Ｋα较对照组的Ｋα明显增加，吸收半衰期Ｔ１２α及达峰时间Ｔｍａｘ明显减少。血药浓度高峰Ｃｍａｘ有明显提高。而清除速率常数Ｋβ、清除半衰期Ｔ１２β也有较明显的差别，其表观分布容积Ｖ／Ｆ、清除率ＣＬ／Ｆ及血药浓度曲线下面积ＡＵＣ差别均不显著。１位幽门不全梗阻患者的药代动力学曲线表明吸收明显延迟。结论兰索拉唑口服后，分布广泛，代谢迅速。消化性溃疡患者应用时，其吸收速率和其排泄明显加快。血药浓度高峰明显增加，对于治疗该病可能具有重要的意义。
AIM The pharmacokinetics study on Lansoprazole were carried out in peptic ulcers. METHODS The plasma concentrations of lansoprazole were determined by HPLC in healthy volunteers (C group n=6) and peptic ulcer patients (G group n=6) after oral administration of lansoprazole 30 mg. RESULTS Large inter individual variations in blood concentrations have been observed. The semi logarithmic plots of the plasma concentration time conformed to a one compartment model, and the parameters T max and T 1〖〗2〖SX)〗α in G group were faster than in C group; C max in G group 1 30±0 35 mg·L -1 was heigher than in C group 0 52±0 22 mg·L -1 , AUC、 Volume of distribution ( V/F ) and clearance ( CL ) in G group were similar to those in C group. CONCLUSIONS Lansoprazole is a drug which distributes extensively, metabolizes rapidly following oral administration. The peptic ulcer patient may absorb promptly and eliminate Lansoprazole through the gastrointestinal tract with abnormal function. The increase of C max indicates that the patient has higher drug concentration and the drug may have importent therapeutic efficacy.
出处
《中国药理学通报》
CAS
CSCD
北大核心
1998年第6期555-558,共4页
Chinese Pharmacological Bulletin
