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三种口服400毫克布洛芬剂型在健康志愿者体内的相对药代动力学。

Relative pharmacokinetics of three oral 400 mg ibuprofen dosage forms in healthy volunteers.

作者信息

Saano V, Paronen P, Peura P, Vidgren M

机构信息

Department of Pharmacology, University of Kuopio, Finland.

出版信息

Int J Clin Pharmacol Ther Toxicol. 1991 Oct;29(10):381-5.

PMID:1748537
Abstract

The pharmacokinetic properties of two solid form, 400 mg ibuprofen (IP) preparations, a soft gelatin capsule and a film-coated tablet, were compared to those obtained after the administration of liquid prepared from effervescent IP tablets. IP was absorbed rapidly (tmax 0.6-1.9 h). The fastest absorption was observed after the ingestion of the soft gelatin capsule; liquid and film-coated tablet produced 12.2-7.8 times longer absorption half-lives, 50-39% lower peak concentrations of IP in serum and 3.5-3.2 times higher tmax values. Bioavailabilities were close to similar after all products. All products were tolerated without side effects in this single-dose, crossover study on 14 healthy volunteers. The results of this study support the earlier findings that after oral administration, IP is absorbed equally well from solid formulations as from liquid form. Liquid formulations of IP often deliver slower absorption than expected probably due to incomplete dissolution of the active principle. This may have therapeutic significance, and it should be taken into account when studies on the relative bioavailability of IP from pharmaceutical drug products are planned.

摘要

比较了两种固体剂型的400毫克布洛芬(IP)制剂(软胶囊和薄膜包衣片)与泡腾IP片制成的液体制剂给药后的药代动力学特性。IP吸收迅速(达峰时间0.6 - 1.9小时)。摄入软胶囊后观察到吸收最快;液体和薄膜包衣片的吸收半衰期延长了12.2 - 7.8倍,血清中IP的峰值浓度降低了50 - 39%,达峰时间值高3.5 - 3.2倍。所有产品的生物利用度相近。在这项针对14名健康志愿者的单剂量交叉研究中,所有产品耐受性良好,无副作用。本研究结果支持了早期的发现,即口服给药后,IP从固体剂型和液体制剂中的吸收情况相同。IP的液体制剂通常吸收比预期慢,可能是由于活性成分溶解不完全。这可能具有治疗意义,在计划对药品中IP的相对生物利用度进行研究时应予以考虑。

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