title: A solid self-nanoemulsifying system of the BCS class IIb drug dabigatran etexilate to improve oral bioavailability.
abstract: To develop dabigatran etexilate (DE)-loaded self-nanoemulsifying drug delivery systems (SNEDDS) for the prevention of stroke and thromboembolism.
  
  
  
  SNEDDS were optimized by ternary phase diagrams and then further solidified into dispersible tablets. In vitro dissolution was analyzed by a phase distribution study. In situ absorption and in vivo pharmacokinetic studies were tested in male Sprague-Dawley rats.
  
  
  
  The phase distribution study showed that more than 60% of DE was retained in the oil phase. Dissolution rate was dramatically enhanced without significant precipitation (<30%) in simulated intestinal fluid. Optimized SNEDDS had 531.80% relative bioavailability compared with Pradaxa(®) capsules (a commercial DE product).
  
  
  
  The developed SNEDDS are promising materials for improving the dissolution and oral bioavailability of BCS class IIb drugs.
authors.affiliation: Pharmaceutical Research Institute, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Fujuan
authors.initials: F
authors.lastname: Chai
authors.affiliation: Wenzhou Institute of Biomaterials & Engineering, Wenzhou Medical University, Wenzhou, Zhejiang, 325001, China.|Department of Chemical Engineering, Northeastern University, Boston, MA 02115, USA.
authors.forename: Linlin
authors.initials: L
authors.lastname: Sun
authors.affiliation: Jiangsu Hengrui Medicine Co., Ltd., 7 Kunshan Road, Lianyungang 222047, China.
authors.forename: Yafei
authors.initials: Y
authors.lastname: Ding
authors.affiliation: Pharmacy Department, Shanghai Pudong New District Zhoupu Hospital, 1500 Zhouyuan Road, Pudong New District, Shanghai, China.
authors.forename: Xiaoqing
authors.initials: X
authors.lastname: Liu
authors.affiliation: Pharmaceutical Research Institute, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Yajie
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Wenzhou Institute of Biomaterials & Engineering, Wenzhou Medical University, Wenzhou, Zhejiang, 325001, China.|Department of Chemical Engineering, Northeastern University, Boston, MA 02115, USA.|Center of Excellence for Advanced Materials Research, King Abdulaziz University, Jeddah, Saudi Arabia.
authors.forename: Thomas J
authors.initials: TJ
authors.lastname: Webster
authors.affiliation: Pharmaceutical Research Institute, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Chunli
authors.initials: C
authors.lastname: Zheng
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000991:Antithrombins / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001682:Biological Availability; D000069604:Dabigatran / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D004655:Emulsions / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry; D008297:Male; D010316:Particle Size; D014677:Pharmaceutical Vehicles / Q000737:chemistry*; D044367:Phase Transition; D017207:Rats, Sprague-Dawley; D012995:Solubility; D020521:Stroke / Q000517:prevention & control; D013501:Surface-Active Agents / Q000737:chemistry; D013923:Thromboembolism / Q000517:prevention & control
chemical_list: D000991:Antithrombins; D004655:Emulsions; D005079:Excipients; D014677:Pharmaceutical Vehicles; D013501:Surface-Active Agents; D000069604:Dabigatran
keywords: BCS class IIb drugs; bioavailability; enhanced dissolution; nanoemulsion; phase distribution; solid self-nanoemulsifying drug delivery system