title: Study on absorption of indomethacin from sustained-release suppositories containing hydrogenated soybean lecithin in rabbits.
abstract: The absorption of indomethacin (IM) from suppositories containing hydrogenated soybean lecithin (HL) after rectal administration in rabbits was investigated with the aim of producing sustained-release suppositories. The suppositories were prepared by the fusion method with IM, HL and Witepsol H-15 (H-15). The IM release rate from the suppositories (IM 10 mg, HL 200 mg, total weight 1 g) was faster than that of the control suppositories without HL. The release of IM from the suppositories (IM 10 mg, HL 300 mg or 350 mg) showed slow-release profiles. In absorption studies in rabbits, sustained-plasma levels of IM were obtained when suppositories having an HL content of more than 300 mg were administered. The suppositories composed of Witepsol E-85 (melting point approximately 43 degrees C), 10 mg of IM, and 200 mg of HL, showed slow-release profiles in the release test, but did not show sustained plasma levels of IM in the absorption test. These results indicate that sustained-release suppositories able to release IM gradually from the surface of the suppositories can be obtained when HL, IM and H-15, whose melting point is lower than body temperature, are used in the preparation of the suppositories, provided that the HL content is high enough in relation to IM.
authors.forename: T
authors.initials: T
authors.lastname: Nakajima
authors.forename: Y
authors.initials: Y
authors.lastname: Takashima
authors.forename: A
authors.initials: A
authors.lastname: Furuya
authors.forename: Y
authors.initials: Y
authors.lastname: Ozawa
authors.forename: Y
authors.initials: Y
authors.lastname: Kawashima
mesh_terms: D000818:Animals; D003692:Delayed-Action Preparations; D005079:Excipients; D007213:Indomethacin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D008297:Male; D010713:Phosphatidylcholines; D011817:Rabbits; D013025:Glycine max / Q000032:analysis; D013488:Suppositories
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D010713:Phosphatidylcholines; D013488:Suppositories; D007213:Indomethacin