中国药业2017，Vol.26Issue(10)：21-26,6.DOI:10.3969/j.issn.1006-4931.2017.10.006
伊潘立酮-羟丙基-β-环糊精包合物的制备及表征、肌肉刺激和药代动力学研究
Preparation,Characterization,Muscular Stimulation and Pharmacokinetics of the Inclusion Complex of Iloperidone-Hydroxypropyl-β-Cyclodextrin
欧云国 1何海云 2单雪峰 2黄华2
作者信息
- 1. 重庆医药工业研究院有限责任公司,重庆 400061
- 2. 重庆医科大学,重庆 400016
- 折叠
摘要
Abstract
Objective To study the inclusion complex of Iloperdone-Hydroxypropyl-β-Cyclodextrin(HP-β-CD),in order to prepare a stable and effective parenteral formulation. Methods Phase solubility study was carried out using distilled water and 0. 2% phospho-ric acid solution as dissolution medium,respecticely;the solution method and lyophilization techniques were used for inclusion complex preparation. The complexes were characterized by fourier transform infrared spectroscopy and differential scanning calorimetry studies and the solubility was determined by UV spectroscopy. The muscular stimulation test of Iloperdone-HP-β-CD inclusion complex solution was perform in rabbits,the pharmacokinetic of Iloperdone tablet and Iloperdone inclusion complex were evaluated after oral administration and muscular injection in dogs. Results The phase-solubility profiles were classified as Ap type,indicating the formation of 1: n(n≥2) stoichiometric inclusion complexes. The complexes were characterized by fourier transform infrared spectroscopy(IR)and differential scan-ning calorimetry(DSC)indicated that Iloperdone was able to form an inclusion complex with HP-β-CD. Iloperdone- HP-β-CD inclusion complex solution had no significant stimulation on muscles. In vivo pharmacokinetic study showed that the absorption rates of Iloperdone across muscles tissues were enhanced compared with oral administra tion . The relative bioavailabity was 143%. Conclusion The Iloperdone-HP-β-CD complex can significantly improve the sotubility,it is an attractive formulation for use in the parenteral.关键词
羟丙基-β-环糊精/伊潘立酮/包合物/注射剂Key words
HP-β-CD/Iloperdone/inclusion complex/injection分类
医药卫生引用本文复制引用
欧云国,何海云,单雪峰,黄华..伊潘立酮-羟丙基-β-环糊精包合物的制备及表征、肌肉刺激和药代动力学研究[J].中国药业,2017,26(10):21-26,6.
