速释和缓释氧烯洛尔的吸收与排泄及其对运动时心率和血压的影响。
Absorption and excretion of rapid and slow release oxprenolol and their effects on heart rate and blood pressure during exercise.
作者信息
Bobik A, Jennings G L, Korner P I, Ashley P, Jackman G
出版信息
Br J Clin Pharmacol. 1979 Jun;7(6):545-9. doi: 10.1111/j.1365-2125.1979.tb04640.x.
Abstract
- Plasma concentrations and heart rate and blood pressure effects of 160 mg oxprenolol as standard rapid release (RR) and slow release (SR) tablets were compared in healthy volunteers. Peak plasma concentrations were lower with SR tablets than with RR tablets and the peak was delayed. 2. Absorption of oxprenolol was described adequately by first order kinetics with both preparations. The apparent half-life of absorption was 0.40 h with RR and 2.4 h for the SR formulation. The apparent elimination half-life of oxprenolol was about 2 h. Relative bioavailabilities of the two formulations were similar. 3. The effectiveness of oxprenolol RR and SR were assessed by their effects on heart rate in severe exercise (EHR) and also by their effects on blood pressure at rest and during exercise. 4. Maximum reductions in these variables coincided with peak oxprenolol concentrations. The effects on EHR and blood pressure parameters had a distinct time course but there was no difference between the time course of inhibition of each variable for the two formulations over 24 h.
摘要
- 在健康志愿者中比较了160毫克氧烯洛尔标准速释（RR）片和缓释（SR）片的血浆浓度、心率及血压效应。SR片的血浆峰浓度低于RR片，且峰浓度出现延迟。2. 两种制剂的氧烯洛尔吸收均可用一级动力学充分描述。RR制剂的表观吸收半衰期为0.40小时，SR制剂为2.4小时。氧烯洛尔的表观消除半衰期约为2小时。两种制剂的相对生物利用度相似。3. 通过观察氧烯洛尔RR和SR对剧烈运动时心率（EHR）的影响以及对静息和运动时血压的影响来评估其有效性。4. 这些变量的最大降幅与氧烯洛尔峰浓度一致。对EHR和血压参数的影响有明显的时间过程，但两种制剂在24小时内对各变量的抑制时间过程无差异。
相似文献
1
Absorption and excretion of rapid and slow release oxprenolol and their effects on heart rate and blood pressure during exercise.速释和缓释氧烯洛尔的吸收与排泄及其对运动时心率和血压的影响。
Br J Clin Pharmacol. 1979 Jun;7(6):545-9. doi: 10.1111/j.1365-2125.1979.tb04640.x.
2
A multiple dose comparative study of the pharmacodynamic and pharmacokinetic behaviour of polymer-matrix and Oros dosage forms of oxprenolol in healthy volunteers.在健康志愿者中进行的氧烯洛尔聚合物基质剂型和渗透泵控释剂型的药效学及药代动力学行为的多剂量对比研究。
Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):177S-184S. doi: 10.1111/j.1365-2125.1985.tb02759.x.
3
Single-dose pharmacokinetic and pharmacodynamic comparison of polymer-matrix (Slow Trasicor) and Oros dosage forms of oxprenolol in healthy volunteers.健康志愿者中氧烯洛尔聚合物基质剂型（Slow Trasicor）和渗透泵控释剂型的单剂量药代动力学和药效学比较。
Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):171S-175S. doi: 10.1111/j.1365-2125.1985.tb02758.x.
4
A comparison of slow release with conventional oxprenolol: plasma concentrations and clinical effects.缓释氧烯洛尔与传统氧烯洛尔的比较：血浆浓度及临床效果
Br J Clin Pharmacol. 1976 Jun;3(3):439-43. doi: 10.1111/j.1365-2125.1976.tb00619.x.
5
Exercise and resting blood pressure and heart rate changes 24 h after dosing in patients with essential hypertension receiving 16/260 oxprenolol Oros once daily.原发性高血压患者每日一次服用16/260氧烯洛尔渗透泵片后24小时的运动及静息血压和心率变化
Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):207S-212S. doi: 10.1111/j.1365-2125.1985.tb02764.x.
6
Comparison of the beta-adrenoceptor blocking activity of oxprenolol, slow release oxprenolol and a combined oxprenolol diuretic preparation.氧烯洛尔、缓释氧烯洛尔及氧烯洛尔利尿剂复方制剂的β-肾上腺素受体阻断活性比较
Br J Clin Pharmacol. 1981 Dec;12(6):869-71. doi: 10.1111/j.1365-2125.1981.tb01323.x.
7
Comparison of the activity and plasma levels of oxprenolol, slow release oxprenolol, long acting propranolol and sotalol.氧烯洛尔、缓释氧烯洛尔、长效普萘洛尔和索他洛尔的活性及血药浓度比较。
Eur J Clin Pharmacol. 1980 Jun;17(6):419-24. doi: 10.1007/BF00570158.
8
Bioavailability of conventional and slow-release oxprenolol in fasted and nonfasted individuals.传统型和缓释型氧烯洛尔在空腹和非空腹个体中的生物利用度。
Br J Clin Pharmacol. 1979 Mar;7(3):299-302. doi: 10.1111/j.1365-2125.1979.tb00936.x.
9
Concentration-effect relationship of oxprenolol in healthy volunteers: a retrospective analysis.心得安在健康志愿者中的浓度-效应关系：一项回顾性分析。
Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):143S-149S. doi: 10.1111/j.1365-2125.1985.tb02755.x.
10
Pharmacokinetics of oxprenolol in normal subjects.氧烯洛尔在正常受试者体内的药代动力学。
Clin Pharmacol Ther. 1976 Oct;20(4):401-12. doi: 10.1002/cpt1976204401.
引用本文的文献
1
Multi-functional scaling methodology for translational pharmacokinetic and pharmacodynamic applications using integrated microphysiological systems (MPS).使用集成微生理系统（MPS）进行转化药代动力学和药效学应用的多功能缩放方法。
Integr Biol (Camb). 2017 Apr 18;9(4):290-302. doi: 10.1039/c6ib00243a.
2
Novel oral drug formulations. Their potential in modulating adverse effects.新型口服药物制剂。它们在调节不良反应方面的潜力。
Drug Saf. 1994 Mar;10(3):233-66. doi: 10.2165/00002018-199410030-00005.
3
Comparison of two long-acting preparations of metoprolol with conventional metoprolol and atenolol in healthy men during chronic dosing.慢性给药期间，健康男性中两种长效美托洛尔制剂与常规美托洛尔及阿替洛尔的比较。
Br J Clin Pharmacol. 1982 Nov;14(5):713-8. doi: 10.1111/j.1365-2125.1982.tb04962.x.
4
Atenolol, sustained-release oxprenolol, and long-acting propranolol in hypertension.阿替洛尔、缓释氧烯洛尔及长效普萘洛尔治疗高血压
Br Med J. 1980 Jun 28;280(6231):1573-4. doi: 10.1136/bmj.280.6231.1573.
5
Comparison of the beta-adrenoceptor blocking activity of oxprenolol, slow release oxprenolol and a combined oxprenolol diuretic preparation.氧烯洛尔、缓释氧烯洛尔及氧烯洛尔利尿剂复方制剂的β-肾上腺素受体阻断活性比较
Br J Clin Pharmacol. 1981 Dec;12(6):869-71. doi: 10.1111/j.1365-2125.1981.tb01323.x.
6
Influence of intrinsic sympathomimetic activity of beta-adrenoceptor blockers on the heart rate and blood pressure responses to graded exercise.β-肾上腺素能受体阻滞剂的内在拟交感活性对心率及血压对分级运动反应的影响。
Br J Clin Pharmacol. 1981 Sep;12(3):355-62. doi: 10.1111/j.1365-2125.1981.tb01226.x.
7
Observation on the efficacy and pharmacokinetics of betaxolol (SL 75212), a cardioselective beta-adrenoceptor blocking drug.心脏选择性β-肾上腺素能受体阻断药倍他洛尔（SL 75212）的疗效及药代动力学观察
Br J Clin Pharmacol. 1981 Feb;11(2):171-80. doi: 10.1111/j.1365-2125.1981.tb01121.x.
8
Comparison of two slow-release formulations of metoprolol with conventional metoprolol and atenolol in hypertensive patients.美托洛尔两种缓释制剂与传统美托洛尔及阿替洛尔在高血压患者中的比较。
Br J Clin Pharmacol. 1985 Oct;20(4):387-91. doi: 10.1111/j.1365-2125.1985.tb05082.x.
9
Osmotic delivery systems for the beta-adrenoceptor antagonists metoprolol and oxprenolol: design and evaluation of systems for once-daily administration.β-肾上腺素受体拮抗剂美托洛尔和氧烯洛尔的渗透给药系统：每日一次给药系统的设计与评价
Br J Clin Pharmacol. 1985;19 Suppl 2(Suppl 2):69S-76S. doi: 10.1111/j.1365-2125.1985.tb02745.x.
10
Evaluation of oxprenolol slow release and osmotic release by exercise testing and ambulatory electrocardiographic monitoring in patients with chronic stable angina pectoris.
Eur J Clin Pharmacol. 1987;32(2):127-33. doi: 10.1007/BF00542184.
本文引用的文献
1
Per cent absorbed time plots derived from blood level and/or urinary excretion data.根据血药浓度和/或尿排泄数据得出的吸收百分比-时间曲线图。
J Pharm Sci. 1963 Jun;52:610-1. doi: 10.1002/jps.2600520629.
2
Absorption of alprenolol in man from tablets with different rates of release.不同释放速率的阿普洛尔片剂在人体中的吸收情况。
Acta Pharm Suec. 1971 Mar;8(1):59-70.
3
Comparative bioavailability and effect studies on metoprolol administered as ordinary and slow-release tablets in single and multiple doses.美托洛尔普通片与缓释片单剂量及多剂量给药的比较生物利用度和效应研究。
Acta Pharmacol Toxicol (Copenh). 1975;36(Suppl 5):45-58. doi: 10.1111/j.1600-0773.1975.tb03321.x.
4
A comparison of slow release with conventional oxprenolol: plasma concentrations and clinical effects.缓释氧烯洛尔与传统氧烯洛尔的比较：血浆浓度及临床效果
Br J Clin Pharmacol. 1976 Jun;3(3):439-43. doi: 10.1111/j.1365-2125.1976.tb00619.x.
5
Pharmacokinetic and pharmacodynamic studies with long-acting propranolol.长效普萘洛尔的药代动力学和药效学研究。
Br J Clin Pharmacol. 1978 Aug;6(2):115-21. doi: 10.1111/j.1365-2125.1978.tb00835.x.
6
Pharmacokinetics of oxprenolol in normal subjects.氧烯洛尔在正常受试者体内的药代动力学。
Clin Pharmacol Ther. 1976 Oct;20(4):401-12. doi: 10.1002/cpt1976204401.
7
Simplified method for the determination of oxprenolol and other beta-receptor-blocking agents in biological fluids by gas-liquid chromatography.
J Chromatogr. 1976 Jun 9;121(1):72-5. doi: 10.1016/s0021-9673(00)82299-2.
Zotero 插件