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感染性鼻炎患者及使用局部减充血剂后尼古丁鼻喷雾剂中尼古丁的相对生物利用度。

Relative bioavailability of nicotine from a nasal spray in infectious rhinitis and after use of a topical decongestant.

作者信息

Lunell E, Molander L, Andersson M

机构信息

Pharmacia Research Laboratories, Lund, Sweden.

出版信息

Eur J Clin Pharmacol. 1995;48(1):71-5. doi: 10.1007/BF00202176.

Abstract

The relative bioavailability of nicotine from a nasal spray was assessed in 15 smokers suffering a common cold and rhinitis according to generally accepted criteria. The patients were given a single dose of 2 mg nicotine from the nasal spray with and without concurrent administration of a nasal vasoconstrictor decongestant, xylometazoline, in randomised order. Control session measurements were made in the disease-free state. Applying strict bioequivalence criteria, we found that common cold/rhinitis slightly reduced the bioavailability of nicotine, both in its rate and extent; the geometric mean of the ratio of Cmax, AUC and tmax were 0.81, 0.93 and 1.36, respectively. The nasal vasoconstrictor, xylometazoline, normalised the extent of the bioavailability of nicotine, but further prolonged the time for absorption to almost twice that measured in the disease-free state, increasing the tmax ratio to 1.72. The results suggest that a minor proportion of people stopping smoking with the help of a nicotine nasal spray may experience a minor reduction in the effect of the spray during common cold/rhinitis. However, the nicotine self-titration behaviour found with most smoking cessation products (except the nicotine patch) will automatically lead to an adjustment of the dosage to achieve the desired effect.

摘要

根据普遍认可的标准,对15名患有普通感冒和鼻炎的吸烟者使用鼻腔喷雾剂后尼古丁的相对生物利用度进行了评估。患者随机接受单剂量2毫克来自鼻腔喷雾剂的尼古丁,同时或不同时给予鼻腔血管收缩剂减充血剂赛洛唑啉。在无疾病状态下进行对照测量。应用严格的生物等效性标准,我们发现普通感冒/鼻炎会略微降低尼古丁的生物利用度,包括其速率和程度;Cmax、AUC和tmax比值的几何平均值分别为0.81、0.93和1.36。鼻腔血管收缩剂赛洛唑啉使尼古丁生物利用度的程度恢复正常,但进一步延长了吸收时间,几乎是无疾病状态下测量值的两倍,使tmax比值增加到1.72。结果表明,少数借助尼古丁鼻腔喷雾剂戒烟的人在患普通感冒/鼻炎期间,喷雾剂的效果可能会略有降低。然而,大多数戒烟产品(除尼古丁贴片外)所具有的尼古丁自我滴定行为会自动导致剂量调整以达到预期效果。

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