Kimura S, Imai T, Ueno M, Otagiri M
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
J Pharm Sci. 1992 Feb;81(2):141-4. doi: 10.1002/jps.2600810208.
Two kinds of ibuprofen syrups were prepared and evaluated. One was a suspending syrup, prepared by using hydroxypropyl methylcellulose (HPMC) as a dispersing agent, and the other was a dry syrup containing low-molecular-weight gelatin (LM gelatin). The dissolution behaviors of ibuprofen from syrups were studied, and both syrups showed size-dependent dissolution; the smaller particles exhibited faster dissolution. The in vivo absorption behaviors of the syrups were compared with that of commercial tablets of ibuprofen in beagle dogs and human volunteers. The absorption rates following oral administrations of syrups were much greater than those following administration of commercial tablets. Moreover, both syrups reduced the bitter taste and irritation of the oral mucosa caused by ibuprofen; the dry syrup markedly masked these side effects. These results suggest that the dry syrup containing LM gelatin improves some of the pharmaceutical properties of ibuprofen, and that the LM gelatin may be used in a variety of oral dosage forms.
制备并评估了两种布洛芬糖浆。一种是混悬糖浆,使用羟丙基甲基纤维素(HPMC)作为分散剂制备;另一种是含有低分子量明胶(LM明胶)的干糖浆。研究了布洛芬在糖浆中的溶出行为,两种糖浆均表现出粒径依赖性溶出;较小的颗粒溶出更快。在比格犬和人类志愿者中,将这些糖浆的体内吸收行为与市售布洛芬片剂进行了比较。口服糖浆后的吸收速率远高于口服市售片剂后的吸收速率。此外,两种糖浆均减轻了布洛芬引起的苦味和口腔黏膜刺激;干糖浆显著掩盖了这些副作用。这些结果表明,含有LM明胶的干糖浆改善了布洛芬的一些药学性质,并且LM明胶可用于多种口服剂型。