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氟比洛芬酯乳剂因游离丙泊酚浓度降低而减轻丙泊酚注射痛。

Emulsion of flurbiprofen axetil reduces propofol injection pain due to a decrease in free propofol concentration.

作者信息

Ueki Ryusuke, Tanimoto Masaaki, Tatara Tsuneo, Tsujimoto Saburo, Kaminoh Yoshiroh, Tashiro Chikara

机构信息

Department of Anesthesiology, Hyogo College of Medicine, Nishinomiya, Hyogo 663-8501, Japan.

出版信息

J Anesth. 2007;21(3):325-9. doi: 10.1007/s00540-007-0530-1. Epub 2007 Aug 1.

DOI:10.1007/s00540-007-0530-1
PMID:17680183
Abstract

PURPOSE

Flurbiprofen axetil emulsion (FA), a prodrug of nonsteroidal anti-inflammatory drugs (NSAIDs) that is widely used for perioperative pain relief in Japan, has been effective for reducing propofol injection pain, but the mechanism is unclear. The purpose of this study was to test the hypothesis that the reduction of propofol injection pain by FA may be attributed to a decrease in free propofol concentration.

METHODS

Diprivan (propofol emulsion; Dipri; AstraZeneca, Cheshire, UK) and Propofol-Lipuro (Lipuro; B. Braun, Melsungen, Germany) were used. A randomized double-blind study was performed to compare pain on injection with six kinds of propofol solution: plain Dipri, a 3 : 1 (v/v) mixture of Dipri and saline (Dipri-S), a 3 : 1 mixture of Dipri and FA (Dipri-FA), plain Lipuro, a 3 : 1 mixture of Lipuro and saline (Lipuro-S), and a 3 : 1 mixture of Lipuro and FA (Lipuro-FA). Three hundred patients (American Society of Anesthesiologists [ASA] physical status [PS] I-II) scheduled for elective surgery received one of these six propofol emulsions (n = 50, each group). Injection pain was evaluated every 10 s after the start of a 1-min infusion of up to 2 mg x kg(-1) propofol. We also measured the in vitro free propofol concentrations of the propofol preparations that we tested (n = 5, each).

RESULTS

The mixture of FA with propofol decreased the incidence of injection pain, compared with plain propofol, for Lipuro (P < 0.01) but not for Dipri. The free propofol concentration in each emulsion in vitro was also decreased by mixing the propofol with saline or FA. The incidence of pain was reduced in a free-propofol concentration-dependent manner (R(2) = 0.926).

CONCLUSION

The findings suggest that the reduction of propofol injection pain by FA may be explained, at least in part, by a reduction in the free propofol concentration.

摘要

目的

氟比洛芬酯乳剂(FA)是一种非甾体抗炎药的前体药物,在日本被广泛用于围手术期疼痛缓解,已证实其对减轻丙泊酚注射痛有效,但作用机制尚不清楚。本研究旨在验证FA减轻丙泊酚注射痛可能归因于游离丙泊酚浓度降低这一假说。

方法

使用得普利麻(丙泊酚乳剂;Dipri;阿斯利康,英国柴郡)和丙泊酚中/长链脂肪乳(Lipuro;贝朗医疗,德国梅尔松根)。进行一项随机双盲研究,比较六种丙泊酚溶液注射时的疼痛情况:单纯Dipri、Dipri与生理盐水按3:1(v/v)混合而成的溶液(Dipri-S)、Dipri与FA按3:1混合而成的溶液(Dipri-FA)、单纯Lipuro、Lipuro与生理盐水按3:1混合而成的溶液(Lipuro-S)以及Lipuro与FA按3:1混合而成的溶液(Lipuro-FA)。300例计划接受择期手术的患者(美国麻醉医师协会[ASA]身体状况[PS] I-II级)接受上述六种丙泊酚乳剂中的一种(每组n = 50)。在以高达2 mg·kg⁻¹的丙泊酚进行1分钟输注开始后,每隔10秒评估一次注射痛。我们还测定了所测试的丙泊酚制剂的体外游离丙泊酚浓度(每种n = 5)。

结果

与单纯丙泊酚相比,FA与丙泊酚的混合物可降低Lipuro注射痛的发生率(P < 0.01),但对Dipri无效。将丙泊酚与生理盐水或FA混合也可降低各乳剂中的游离丙泊酚浓度。疼痛发生率以游离丙泊酚浓度依赖的方式降低(R² = 0.926)。

结论

研究结果表明,FA减轻丙泊酚注射痛至少部分可归因于游离丙泊酚浓度的降低。

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Clin Ther. 2005 May;27(5):588-93. doi: 10.1016/j.clinthera.2005.05.003.
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Acta Anaesthesiol Scand. 2005 Feb;49(2):248-51. doi: 10.1111/j.1399-6576.2004.00573.x.
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Simple high-performance liquid chromatographic assay of propofol in human and rat plasma and various rat tissues.人及大鼠血浆和大鼠各种组织中丙泊酚的简易高效液相色谱测定法。
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