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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Strolin Benedetti M, Efthymiopoulos C, Sassella D, Moro E, Repetto M

Department of Pharmacokinetics and Metabolism, Farmitalia Carlo Erba Research and Development, Erbamont Group, Milan, Italy.

Xenobiotica. 1990 Nov;20(11):1113-9. doi: 10.3109/00498259009046832.

The pharmacokinetics of the antimycobacterial agent rifabutin were studied in healthy volunteers, following single (450 mg) and repeated (450 mg once daily for 10 days) oral administration. 2. After repeated administration, induction of metabolism was indicated by lower AUC and Cmin values, compared to the corresponding theoretical values. The elimination half-life was unchanged after repeated administration. 3. Induction of presystemic extrahepatic metabolism, which seems to be important in the availability of rifabutin, should be mainly responsible for the decrease in the AUC observed, while induced systemic clearance (if any) should be of minor importance. 4. Induction of presystemic extrahepatic metabolism after repeated administration has also been reported for rifampicin, an antibiotic agent with hepatic enzyme-inducing properties, which has a structure similar to rifabutin but a different pharmacokinetic profile.

在健康志愿者中研究了抗分枝杆菌药物利福布汀单次（450毫克）和重复（每日450毫克，共10天）口服给药后的药代动力学。2. 重复给药后，与相应的理论值相比，AUC和Cmin值降低表明代谢被诱导。重复给药后消除半衰期不变。3. 肝外首过代谢的诱导似乎在利福布汀的可利用性中起重要作用，这应该是观察到的AUC降低的主要原因，而诱导的全身清除率（如果有的话）应该不太重要。4. 利福平是一种具有肝酶诱导特性的抗生素，其结构与利福布汀相似但药代动力学特征不同，重复给药后也有肝外首过代谢诱导的报道。

Strolin Benedetti M, Efthymiopoulos C, Sassella D, Moro E, Repetto M

Department of Pharmacokinetics and Metabolism, Farmitalia Carlo Erba Research and Development, Erbamont Group, Milan, Italy.

Xenobiotica. 1990 Nov;20(11):1113-9. doi: 10.3109/00498259009046832.

The pharmacokinetics of the antimycobacterial agent rifabutin were studied in healthy volunteers, following single (450 mg) and repeated (450 mg once daily for 10 days) oral administration. 2. After repeated administration, induction of metabolism was indicated by lower AUC and Cmin values, compared to the corresponding theoretical values. The elimination half-life was unchanged after repeated administration. 3. Induction of presystemic extrahepatic metabolism, which seems to be important in the availability of rifabutin, should be mainly responsible for the decrease in the AUC observed, while induced systemic clearance (if any) should be of minor importance. 4. Induction of presystemic extrahepatic metabolism after repeated administration has also been reported for rifampicin, an antibiotic agent with hepatic enzyme-inducing properties, which has a structure similar to rifabutin but a different pharmacokinetic profile.

在健康志愿者中研究了抗分枝杆菌药物利福布汀单次（450毫克）和重复（每日450毫克，共10天）口服给药后的药代动力学。2. 重复给药后，与相应的理论值相比，AUC和Cmin值降低表明代谢被诱导。重复给药后消除半衰期不变。3. 肝外首过代谢的诱导似乎在利福布汀的可利用性中起重要作用，这应该是观察到的AUC降低的主要原因，而诱导的全身清除率（如果有的话）应该不太重要。4. 利福平是一种具有肝酶诱导特性的抗生素，其结构与利福布汀相似但药代动力学特征不同，重复给药后也有肝外首过代谢诱导的报道。