以甘氨脱氧胆酸盐作为吸收促进剂，在猪体内经颊部给药荧光素异硫氰酸酯 - 葡聚糖4400 。

In-vivo buccal delivery of fluorescein isothiocyanate-dextran 4400 with glycodeoxycholate as an absorption enhancer in pigs.

作者信息

Hoogstraate A J, Verhoef J C, Tuk B, Pijpers A, van Leengoed L A, Verheijden J H, Junginger H E, Boddé H E

机构信息

Division of Pharmaceutical Technology, Leiden/Amsterdam Center for Drug Research, Leiden University, The Netherlands.

出版信息

J Pharm Sci. 1996 May;85(5):457-60. doi: 10.1021/js950129k.

DOI:10.1021/js950129k

PMID:8742934

Abstract

Buccal delivery of fluorescein isothiocyanate labeled dextran 4400 (FD4) was investigated in-vivo in pigs. The delivery device consisted of an application chamber with a solution of FD4 and was adhered to the buccal mucosa for 4 h using an adhesive patch. A randomized crossover study including intravenous administration and buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer was performed in five pigs. After buccal administration, steady state plasma levels were rapidly reached. Coadministration of 10 mM GDC increased the absolute bioavailability of FD4 from 1.8 +/- 0.5% to 12.7 +/- 2.0%. Since FD4 is a macromolecular and hydrophilic compound such as peptide and protein drugs, buccal delivery would provide an adequate alternative to the parenteral administration of these drugs.

摘要

在猪体内对异硫氰酸荧光素标记的葡聚糖4400（FD4）的颊部给药进行了研究。给药装置由一个装有FD4溶液的给药腔室组成，并使用粘性贴片将其贴附在颊粘膜上4小时。在五头猪身上进行了一项随机交叉研究，包括静脉给药以及在有和没有10 mM甘氨脱氧胆酸钠（GDC）作为吸收促进剂的情况下进行颊部给药。颊部给药后，迅速达到稳态血浆水平。共同给予10 mM GDC可使FD4的绝对生物利用度从1.8±0.5%提高到12.7±2.0%。由于FD4是一种大分子亲水性化合物，如肽和蛋白质药物，颊部给药将为这些药物的肠胃外给药提供一种合适的替代方法。