Improvement of Intestinal Absorption of Poorly Absorbable Drugs by Chemical Modification and Pharmaceutical Excipients.

Yamamoto Akira

doi:10.5360/membrane.28.248

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ＤＤＳと膜輸送ＡＴＰａｓｅ研究の最前線　　化学修飾ならびに製剤添加物を用いた難吸収性薬物の消化管吸収改善
カガクシュウショクナラビニセイザイテンカブツオモチイタナンキュウシュウセイヤクブツノショウカカンキュウシュウカイゼン

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Abstract

The oral bioavailability of hydrophilic drugs and macromolecular drugs is generally poor because they are impermeable through the intestinal mucosa. For systemic delivery of these drugs, parenteral administration is currently required to achieve their therapeutic activities. However, this administration is poorly accepted by patients and may cause allergic reactions and serious side effects. Therefore, various approaches have been examined to overcome the delivery problems of these drugs when they administered to the gastrointestinal tract and other mucosal sites. These approaches include (1) to use additives such as absorption enhancers, (2) to develop an administration method for drugs that can serve as an alternative to oral and injection administration, (3) to modify the molecular structure of drugs to produce prodrugs and analogues, and (4) to use the dosage forms to these drugs. In this study, we demonstrated that intestinal absorption of poorly absorbable drugs including peptide drugs could be improved by using these approaches. Therefore, these approaches may give us basic information to improve the intestinal absorption of poorly absorbable drugs.

Journal

MEMBRANE

MEMBRANE 28 (6), 248-254, 2003

THE MEMBRANE SOCIETY OF JAPAN

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