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育亨宾水基提取物对普萘洛尔生物利用度的修饰。

Modification of propranolol's bioavailability by Eurycoma longifolia water-based extract.

机构信息

Department of Pharmacology, School of Medical Sciences, Universiti Sains Malaysia, Kubang Kerian, Kelantan, Penang, Malaysia.

出版信息

J Clin Pharm Ther. 2010 Dec;35(6):691-6. doi: 10.1111/j.1365-2710.2009.01147.x.

Abstract

WHAT IS KNOWN AND BACKGROUND

Eurycoma longifolia (E. longifolia), a herb commonly consumed for its aphrodisiac properties, is widely used by Asian males. This may include hypertensive patients receiving propranolol which may cause sexual dysfunction as one of its side-effects. There is no published study of the potential pharmacokinetic interaction between propranolol and the herb.

OBJECTIVE

To study propranolol's pharmacokinetics when E. longifolia is consumed, comparing volunteers given either propranolol or a placebo.

METHODS

This is a placebo-controlled randomized single-blinded crossover study of the effect of a water-based extract of E. longifolia on the pharmacokinetics of a single dose of proporanolol (Inderal(®)) in 14 healthy non-smoker young males. Eighty milligram of propranonol was orally administered with (i) placebo (Lactose) or (ii) 200 mg of water-based extract of E. longifolia (0·0272 ± 0·0026%eurycomanone) following an overnight fasting. Blood samples were collected at 0, 0·5, 1, 1·5, 2, 3, 4, 6, 8 and 10 h for propranolol's plasma concentration determinations using a validated high-performance liquid chromatography (HPLC) method.

RESULTS AND DISCUSSION

When propranolol was administered with E. longifolia, its bioavailability (AUC0-∞) decreased by 29% while C(max) was reduced by 42% and T(max) was significantly prolonged by almost 86%. The terminal elimination half-life, however, was not significantly affected.

CONCLUSION

The bioavailability of propranolol is significantly decreased when consumed together with E. longifolia. The interaction is due to a reduction in absorption, rather than an increase in propranolol's metabolism. Although the pharmacodynamics of propranolol was not affected in healthy volunteers, caution is still advisable with co-administration of the drug and the herb.

摘要

已知和背景

育亨宾(E. longifolia)是一种常用于壮阳的草药,被亚洲男性广泛食用。这可能包括正在服用普萘洛尔的高血压患者,因为它的一种副作用可能会导致性功能障碍。目前还没有关于普萘洛尔和这种草药之间潜在药代动力学相互作用的发表研究。

目的

研究育亨宾对健康非吸烟年轻男性单次服用普萘洛尔(心得安(®))药代动力学的影响,比较给予普萘洛尔或安慰剂的志愿者。

方法

这是一项安慰剂对照随机单盲交叉研究,研究了育亨宾水提取物对 14 名健康非吸烟年轻男性单次口服 80 毫克普萘洛尔(心得安(®))的药代动力学的影响。志愿者在禁食过夜后,口服给予 80 毫克普萘洛尔(心得安(®))(i)安慰剂(乳糖)或(ii)200 毫克育亨宾水提取物(0·0272 ± 0·0026%eurycomanone)。采用经验证的高效液相色谱(HPLC)法测定血浆中普萘洛尔的浓度,于 0、0·5、1、1·5、2、3、4、6、8 和 10 h 采集血样。

结果与讨论

当普萘洛尔与育亨宾一起服用时,其生物利用度(AUC0-∞)降低了 29%,而 C(max)降低了 42%,T(max)显著延长了近 86%。然而,终末消除半衰期没有显著影响。

结论

当与育亨宾一起服用时,普萘洛尔的生物利用度显著降低。这种相互作用是由于吸收减少,而不是普萘洛尔代谢增加所致。虽然在健康志愿者中,普萘洛尔的药效学没有受到影响,但在药物和草药同时使用时仍需谨慎。

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