波吲洛尔新型透皮给药系统的药代动力学与药效学
Pharmacokinetics and pharmacodynamics of a new transdermal delivery system for bopindolol.
作者信息
Drewe J, Meier R, Timonen U, Thumshirn M, Munzer J, Kissel T, Gyr K
机构信息
Department of Anaesthesia, University of Basel/Kantonsspital, Switzerland.
出版信息
Br J Clin Pharmacol. 1991 Jun;31(6):671-6. doi: 10.1111/j.1365-2125.1991.tb05591.x.
Abstract
- In two separate studies, each with 12 healthy male volunteers, the pharmacokinetic and dynamic properties of a transdermal delivery system for bopindolol were evaluated. 2. In study I it was shown that bopindolol absorption from a 14 mg patch occurred over the whole 7-day application period. No signs of a significant skin depot were found. 3. In study II, a linear pharmacokinetic behaviour but a non-linear kinetic/dynamic relationship was established for the patches over a dose range from 7 to 21 mg. Comparable peak effects of reduction in exercise-induced tachycardia were observed after different patch doses and an i.v. injection. However, the effect was significantly prolonged with the patches compared with the injection and was maintained over 7 days. 4. The patches showed a good local and systemic tolerability in both studies over a dosing interval of up to 7 days.
摘要
- 在两项独立研究中，每项研究有12名健康男性志愿者，对波吲洛尔透皮给药系统的药代动力学和动力学特性进行了评估。2. 在研究I中表明，从14毫克贴片吸收的波吲洛尔在整个7天的应用期内都有发生。未发现明显皮肤贮库的迹象。3. 在研究II中，在7至21毫克的剂量范围内，贴片建立了线性药代动力学行为，但动力学/动力学关系是非线性的。不同贴片剂量和静脉注射后，观察到运动诱发心动过速降低的可比峰值效应。然而，与注射相比，贴片的效应显著延长，并维持7天以上。4. 在两项研究中，贴片在长达7天的给药间隔内均显示出良好的局部和全身耐受性。
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本文引用的文献
1
Simultaneous modeling of bopindolol kinetics and dynamics.
Clin Pharmacol Ther. 1984 Jul;36(1):5-13. doi: 10.1038/clpt.1984.130.
2
Duration of action and plasma levels of beta-adrenoceptor blocking drugs.
Arch Int Pharmacodyn Ther. 1980;Suppl:32-7.
3
Pharmacokinetic criteria for the evaluation of retard formulations.
Eur J Clin Pharmacol. 1974 Oct 4;7(6):429-32. doi: 10.1007/BF00560355.
4
Pharmacokinetics of transdermally delivered clonidine.经皮给药可乐定的药代动力学
Clin Pharmacol Ther. 1985 Sep;38(3):278-84. doi: 10.1038/clpt.1985.171.
5
Transdermal bioavailability and first-pass skin metabolism: a preliminary evaluation with nitroglycerin.经皮生物利用度与首过皮肤代谢：硝酸甘油的初步评估
J Pharmacokinet Biopharm. 1987 Aug;15(4):423-37. doi: 10.1007/BF01066522.
6
Transdermal delivery of bupranolol: pharmacodynamics and beta-adrenoceptor occupancy.布普萘洛尔的经皮给药：药效学和β-肾上腺素能受体占有率。
Eur J Clin Pharmacol. 1986;31(4):419-22. doi: 10.1007/BF00613517.
7
The clinical pharmacology of bopindolol, a new long-acting beta-adrenoceptor antagonist, in hypertension.
Clin Pharmacol Ther. 1987 Oct;42(4):411-9. doi: 10.1038/clpt.1987.171.
8
Initial evaluation of transdermal timolol: serum concentrations and beta-blockade.
J Cardiovasc Pharmacol. 1985 Mar-Apr;7(2):245-50. doi: 10.1097/00005344-198503000-00006.
9
Rate and extent of absorption of clonidine from a transdermal therapeutic system.
J Pharm Pharmacol. 1989 Jan;41(1):17-21. doi: 10.1111/j.2042-7158.1989.tb06321.x.
10
Determination of mepindolol in plasma after transdermal drug delivery by high-performance liquid chromatography with electrochemical detection.采用高效液相色谱-电化学检测法测定透皮给药后血浆中甲吲哚心安的含量。
J Chromatogr. 1990 Mar 16;526(1):240-5. doi: 10.1016/s0378-4347(00)82505-0.
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