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非洛地平缓释片的吸收、胃肠道转运及片剂溶蚀

Absorption, gastrointestinal transit, and tablet erosion of felodipine extended-release (ER) tablets.

作者信息

Abrahamsson B, Alpsten M, Hugosson M, Jonsson U E, Sundgren M, Svenheden A, Tölli J

机构信息

Pharmaceutical R&D, Astra Hässle AB, Mölndal, Sweden.

出版信息

Pharm Res. 1993 May;10(5):709-14. doi: 10.1023/a:1018959732744.

Abstract

The gastrointestinal transit and tablet erosion of felodipine extended release (ER) tablets 10 mg were studied by gamma scintigraphy in eight healthy young males after administration under fasting and nonfasting conditions. Plasma concentrations of felodipine were also measured. Gastric emptying after administration together with food (mean, 3.2 hr) was slower in all subjects compared to emptying under fasting conditions (mean, 0.6 hr). The mean small intestinal transit times for the two study conditions did not differ significantly (5.1 and 4.7 hr, respectively). Tablets did not leave the colon in any subject within 14 hr after administration. Felodipine was shown to be absorbed in the colon, although the major part of the dose was absorbed in the small intestine. The absorption rate of felodipine was related to erosion of the hydrophilic matrix tablet. Tablet erosion and hence drug absorption were slower in the more distal parts of the gastrointestinal tract. Administration together with food did not significantly affect tablet erosion.

摘要

在8名健康年轻男性中,通过γ闪烁扫描技术研究了10毫克非洛地平缓释片在禁食和非禁食条件下给药后的胃肠道转运和片剂侵蚀情况。同时也测量了非洛地平的血浆浓度。与禁食条件下的排空情况(平均0.6小时)相比,所有受试者在与食物一起给药后的胃排空(平均3.2小时)较慢。两种研究条件下的平均小肠转运时间无显著差异(分别为5.1小时和4.7小时)。给药后14小时内,所有受试者的片剂均未离开结肠。尽管大部分剂量的非洛地平在小肠吸收,但仍显示其在结肠被吸收。非洛地平的吸收速率与亲水性骨架片的侵蚀有关。胃肠道越远端,片剂侵蚀及药物吸收越慢。与食物一起给药对片剂侵蚀无显著影响。

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