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三种硝酸甘油贴剂制剂(Nitradisc、Transiderm-Nitro和Nitro-Dur)以及一种软膏制剂(Nitrobid)产生的血浆硝酸甘油水平。

Plasma levels of nitroglycerin generated by three nitroglycerin patch preparations, Nitradisc, Transiderm-Nitro and Nitro-Dur and one ointment formulation, Nitrobid.

作者信息

McAllister A, Mosberg H, Settlage J A, Steiner J A

出版信息

Br J Clin Pharmacol. 1986 Apr;21(4):365-9. doi: 10.1111/j.1365-2125.1986.tb05208.x.

Abstract

Twenty-four healthy male subjects participated in a study comparing plasma concentrations of nitroglycerin generated by single applications of Nitradisc 32 mg, Transiderm-Nitro 50 mg and Nitro-Dur 104 mg patches and from one inch of Nitrobid 2% ointment. The three patch preparations are designed to release 10 mg nitroglycerin systemically over a 24 h period. Nitrobid ointment is intended to deliver 15 mg nitroglycerin per inch of ointment, and to be reapplied at least every 8 h. Blood was taken for nitroglycerin assay up to and including 24 h after each application. Assay for nitroglycerin was performed using a gas chromatography-mass spectrometry technique. Plasma concentrations of nitroglycerin were sustained up to the 24 h mark with all three patch preparations, but not with application of Nitrobid ointment. Nitrobid was associated with a rapid rise in nitroglycerin plasma concentrations maximal 1 h after application. Plasma concentrations of nitroglycerin absorbed from Nitrobid ointment fell below those absorbed from all three patch preparations after 8 h. Clinically, all four formulations were similar with respect to side effects, with headache and dizziness being the most common.

摘要

24名健康男性受试者参与了一项研究,该研究比较了单次使用32毫克硝酸甘油贴膜、50毫克硝酸甘油透皮贴剂和104毫克硝酸甘油控释贴剂以及一英寸2%硝酸甘油软膏所产生的血浆硝酸甘油浓度。这三种贴剂制剂设计为在24小时内全身释放10毫克硝酸甘油。硝酸甘油软膏每英寸旨在递送15毫克硝酸甘油,并且至少每8小时重新涂抹一次。在每次用药后直至包括24小时内采集血液进行硝酸甘油测定。使用气相色谱-质谱技术进行硝酸甘油测定。所有三种贴剂制剂的血浆硝酸甘油浓度在24小时标记时均保持稳定,但硝酸甘油软膏用药时则不然。硝酸甘油软膏与用药后1小时血浆硝酸甘油浓度迅速升高至最大值相关。8小时后,从硝酸甘油软膏吸收的血浆硝酸甘油浓度低于从所有三种贴剂制剂吸收的浓度。临床上,所有四种制剂在副作用方面相似,头痛和头晕最为常见。

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