期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 92, 期 -, 页码 49-55出版社
ELSEVIER
DOI: 10.1016/j.ejpb.2015.02.021
关键词
Tranilast; alpha-Glucosyl rutin; Nanostructure; Spray-drying; Oral bioavailability; Composite
资金
- JSPS KAKENHI (Tokyo, Japan) [25504018]
- Grants-in-Aid for Scientific Research [25504018] Funding Source: KAKEN
Tranilast (TL) composite particles with ct-glucosyl rutin (Rutin-G) were developed to improve the solubility and oral bioavailability of TL Composite formulation of TL/Rutin-G was prepared using the spray-drying method, and their physicochemical properties were evaluated with respect to the morphology, particle size distribution, solubility and crystallinity. The nanostructure formation of Rutin-G was characterized by dynamic light scattering and transmission electron microscopy when Rutin-G or TL/Rutin-G spray-dried particles (SDPs) were introduced into water. A pharmacokinetic study was also performed to assess the improvement of oral absorption in rats. TL/Rutin-G SDPs were spherical particles with a diameter of 5.5 mu m. Even in the acidic condition, the remarkable improvement in solubility of TL was achieved, as evidenced by a 32.2-fold increase in solubility compared with untreated TL. The median size of Rutin-G nanostructures in water was 2 nm, The formation of Rutin-G nanostructures and their drug inclusion properties may enhance the solubility and dissolution behavior of TL. A drastic increase was found in the exposure of TL in rats, with an increase in C-max and AUC values of 114- and 36.4-fold, respectively, compared with those of untreated TL These findings indicated that a TL formulation spraydried with Rutin-G could enhance its solubility and absorption and thus its therapeutic properties. (C) 2015 Elsevier B.V. All rights reserved.
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