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关于用水溶性膳食纤维、黄原胶和刺槐豆胶制备的吲哚美辛缓释水凝胶栓剂直肠吸收的研究。

Investigation on rectal absorption of indomethacin from sustained-release hydrogel suppositories prepared with water-soluble dietary fibers, xanthan gum and locust bean gum.

作者信息

Watanabe K, Yakou S, Takayama K, Machida Y, Isowa K, Nagai T

机构信息

Hospital Pharmacy, Tokyo Women's Medical College Daini Hospital, Japan.

出版信息

Biol Pharm Bull. 1993 Apr;16(4):391-4. doi: 10.1248/bpb.16.391.

Abstract

Sustained-release hydrogel suppositories prepared with water-soluble dietary fibers, xanthan gum and locust bean gum, were evaluated as a vehicle for rectal administration of indomethacin (IMC) in rabbits. The drug plasma levels were compared with those after rectal administration of commercial suppositories. When the commercial suppositories were given to rabbits, the plasma concentration reached the maximum level at 30 min after administration followed by a quick reduction, while no sharp peak of plasma levels was seen with the hydrogel suppositories. In particular, the plasma levels observed with the hydrogel suppositories of 1% (w/v) gum concentration were sustained much longer than those after dosing with the commercial suppositories; the mean residence times had higher values without a decrease in the area under the plasma concentration vs. time curves. Histopathological study showed good biological safety of the hydrogel suppositories to the rectal mucosa. These results suggested that the IMC hydrogel suppositories prepared with xanthan gum and locust bean gum were a practical rectal preparation with prolonged action and reduced side effects.

摘要

用水溶性膳食纤维、黄原胶和刺槐豆胶制备的缓释水凝胶栓剂,被评估为家兔直肠给药吲哚美辛(IMC)的一种载体。将药物血浆水平与直肠给予市售栓剂后的水平进行了比较。当给家兔使用市售栓剂时,血浆浓度在给药后30分钟达到最高水平,随后迅速下降,而水凝胶栓剂未见血浆水平的 sharp peak 。特别是,1%(w/v)胶浓度的水凝胶栓剂观察到的血浆水平比给予市售栓剂后的血浆水平持续时间长得多;平均驻留时间值更高,血浆浓度与时间曲线下面积没有减少。组织病理学研究表明水凝胶栓剂对直肠黏膜具有良好的生物安全性。这些结果表明,用黄原胶和刺槐豆胶制备的IMC水凝胶栓剂是一种具有延长作用和减少副作用的实用直肠制剂。

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