Umejima H, Kim N S, Ito T, Uchida T, Goto S
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
J Pharm Sci. 1993 Feb;82(2):195-9. doi: 10.1002/jps.2600820216.
Eudispert hv hydrogel and xerogel preparations containing salicylamide displayed sustained-release plasma profiles when compared with other conventional rectal preparations. The absolute bioavailability of salicylamide was 97.3% for the hydrogel preparation and 98.4% for the xerogel preparation. These results may arise because the gel preparation stays at the application site, the lower part of the rectum, over a fairly long period because of its bioadhesive force. Furthermore, the gastrointestinal and hepatic first-pass elimination of salicylamide can be avoided completely by rectal administration of these preparations. Visual and optical microscopic observation of rectal membranes indicated no irritation or abnormality after administration of Eudispert hv hydrogel and xerogel.
与其他传统直肠制剂相比，含有水杨酰胺的Eudispert hv水凝胶和干凝胶制剂呈现出缓释的血浆特征。水杨酰胺水凝胶制剂的绝对生物利用度为97.3%，干凝胶制剂为98.4%。这些结果可能是因为凝胶制剂凭借其生物粘附力在相当长的一段时间内停留在应用部位，即直肠下部。此外，通过直肠给药这些制剂可完全避免水杨酰胺在胃肠道和肝脏的首过消除。对直肠膜的视觉和光学显微镜观察表明，给予Eudispert hv水凝胶和干凝胶后未出现刺激或异常。
