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以胶囊和控释片形式给药的丙吡胺的血浆浓度。

Plasma concentration of disopyramide given as capsules and controlled release tablets.

作者信息

Arnman K, Graffner C, Rikner L, Ryden L, Voog L

出版信息

Eur J Clin Pharmacol. 1983;24(2):199-203. doi: 10.1007/BF00613817.

Abstract

Steady state plasma levels and clinical effects of disopyramide have been compared following administration of standard capsules and controlled release (CR) tablets. Nineteen patients (29-70 years) with atrial or ventricular arrhythmias were treated for two weeks with disopyramide capsules 200 mg t.i.d. and then with CR tablets 300 mg b.i.d. for 14 weeks. After treatment either with capsules or CR tablets, plasma concentrations of disopyramide and its metabolite N-deisopropyldisopyramide were similar within 1 dosage interval. Maximum and minimum concentrations of the parent drug were 10.1 +/- 0.9 mumol/l (mean +/- SEM) and 5.7 +/- 0.5 mumol/l with CR tablets, and 10.2 +/- 0.5 mumol/l and 5.6 +/- 0.5 mumol/l with standard capsules. The bioavailability of disopyramide was the same after capsules and CR tablets. Disopyramide, independent of the formulation, produced good antiarrhythmic effects. The side-effects reported on questioning were mainly of the anti-cholinergic type and there was no significant difference between the formulations with respect to their incidence, type or severity. Of 16 patients who stated a preference for one of the dosage forms, 11 prefered the CR tablets. The study confirms the good antiarrhythmic effect of disopyramide and shows that the CR preparation permits twice daily administration of disopyramide.

摘要

已对服用标准胶囊和控释(CR)片后丙吡胺的稳态血浆水平及临床效果进行了比较。19例年龄在29至70岁之间的房性或室性心律失常患者先接受丙吡胺胶囊200mg每日3次治疗两周,然后接受CR片300mg每日2次治疗14周。在用胶囊或CR片治疗后,丙吡胺及其代谢产物N-去异丙基丙吡胺的血浆浓度在1个给药间隔内相似。母体药物的最大和最小浓度,CR片分别为10.1±0.9μmol/L(均值±标准误)和5.7±0.5μmol/L,标准胶囊分别为10.2±0.5μmol/L和5.6±0.5μmol/L。丙吡胺在胶囊和CR片后的生物利用度相同。无论制剂如何,丙吡胺均产生良好的抗心律失常效果。询问时报告的副作用主要为抗胆碱能类型,两种制剂在发生率、类型或严重程度方面无显著差异。在16例表示对其中一种剂型有偏好的患者中,11例更喜欢CR片。该研究证实了丙吡胺良好的抗心律失常效果,并表明CR制剂允许丙吡胺每日给药两次。

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