Ritschel W A, Menon A, Sakr A
University of Cincinnati Medical Center, Division of Pharmaceutics and Drug Delivery Systems, OH.
Methods Find Exp Clin Pharmacol. 1991 Nov;13(9):629-36.
An attempt was made to evaluate some of the criteria for developing a modified release peroral dosage form for furosemide which has a poor bioavailability when given in the conventional peroral dosage forms. The pathway of absorption for furosemide was studied ex vivo employing the Wilson-Wiseman test. Passive absorption was found to be the predominant mechanism of transport across the ileum of the guinea pig followed by active transport to the extent of about 17%. The in situ procedure to study the extent of absorption of furosemide from the various sites in the lumen of the gastrointestinal tract of the rat indicated the stomach to be the major site of absorption followed by the duodenum. It is hence postulated that due to the site-specificity and mechanism of absorption a peroral modified release dosage form having a longer gastric residence time could possibly increase the bioavailability of furosemide.
呋塞米以传统口服剂型给药时生物利用度较差，因此尝试评估开发其口服缓控释剂型的一些标准。采用Wilson-Wiseman试验体外研究了呋塞米的吸收途径。发现被动吸收是呋塞米跨豚鼠回肠转运的主要机制，其次是约17%的主动转运。研究大鼠胃肠道管腔内不同部位呋塞米吸收程度的原位试验表明，胃是主要吸收部位，其次是十二指肠。因此推测，由于吸收的部位特异性和机制，具有较长胃滞留时间的口服缓控释剂型可能会提高呋塞米的生物利用度。
