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In vitro Dissolution and Pharmacokinetics in Beagle Dogs of a Self-Emulsifying Formulation of Tretinoin

QUAN Dong-qin*, XU Gui-xia   

  1. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China
  • Received:2004-09-18 Revised:2005-05-10 Online:2005-06-15 Published:2005-06-15
  • Contact: QUAN Dong-qin*

Abstract: Aim In vitro dissolution test and pharmacokinetics in beagle dogs were conducted to assess the formulation of tretinoin in self-emulsifying systems. Methods The concentrations of tretinoin were determined by HPLC. A crossover study was performed in four fasting beagle dogs with the formulation of self-emulsifying systems and commercial capsules. Results The results showed that the dissolution rate in 15 min of tretinoin in self-emulsifying systems was higher than 80% while that of the commercial capsules was lower than 5%. The area under the plasma concentration-time curve (AUC) of the self-emulsifying formulation was significantly higher and Cmax was approximately two times greater than those of commercial capsule, respectively. In addition, the time taken to reach peak was shorter (2 h to 1.25 h) for self-emulsifying formulation of tretinoin. Conclusion The self-emulsifying drug delivery systems can significantly increase tretinoin in vitro dissolution and in vivo absorption.

Key words: self-emulsifying systems, self-emulsifying systems, tretinoin, tretinoin, bioavailability, bioavailability, dissolution, dissolution

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