title: Low hygroscopic spray-dried powders with trans-glycosylated food additives enhance the solubility and oral bioavailability of ipriflavone.
abstract: The improvement in the solubility and dissolution rate may promote a superior absorption property towards the human body. The spray-dried powders (SDPs) of ipriflavone, which was used as a model hydrophobic flavone, with trans-glycosylated rutin (Rutin-G) showed the highest solubilizing effect of ipriflavone among three types of trans-glycosylated food additives. The SDPs of ipriflavone with Rutin-G have both a significant higher dissolution rate and solubility enhancement of ipriflavone. This spray-dried formulation of ipriflavone with Rutin-G exhibited a low hygroscopicity as a critical factor in product preservation. In addition, an improvement in the oral absorption of ipriflavone was achieved by means of preparing composite particles of ipriflavone/Rutin-G via spray drying, indicating a 4.3-fold increase in the area under the plasma concentration-time curve compared with that of untreated ipriflavone. These phenomena could be applicable to food ingredients involving hydrophobic flavones for producing healthy food with a high quality.
authors.affiliation: Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Miki
authors.initials: M
authors.lastname: Fujimori
authors.affiliation: Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Kazunori
authors.initials: K
authors.lastname: Kadota
authors.affiliation: Department of Pharmacokinetics & Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga, Shizuoka 422-8526, Japan.
authors.forename: Kouki
authors.initials: K
authors.lastname: Kato
authors.affiliation: Department of Pharmacokinetics & Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga, Shizuoka 422-8526, Japan.
authors.forename: Yoshiki
authors.initials: Y
authors.lastname: Seto
authors.affiliation: Department of Pharmacokinetics & Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga, Shizuoka 422-8526, Japan.
authors.forename: Satomi
authors.initials: S
authors.lastname: Onoue
authors.affiliation: Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Hideyuki
authors.initials: H
authors.lastname: Sato
authors.affiliation: Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan; Physicochemical and Preformulation, Applied Chemistry for Drug Discovery, Innovative Drug Discovery Research Laboratories, Shionogi & Co., Ltd., 3-1-1, Futaba, Toyonaka, Osaka 561-0825, Japan.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Ueda
authors.affiliation: Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan. Electronic address: ytozuka@gly.oups.ac.jp.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Tozuka
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D005503:Food Additives / Q000032:analysis / Q000737:chemistry*; D006031:Glycosylation; D007529:Isoflavones / Q000737:chemistry*; D011208:Powders / Q000737:chemistry*; D017155:Wettability
chemical_list: D005503:Food Additives; D007529:Isoflavones; D011208:Powders; C018986:ipriflavone
keywords: Dissolution rate; Ipriflavone; Surface tension; Trans-glycosylated rutin; Water sorption