Preparation and in Vitro and in Vivo evaluation of freeze-dried alprostadil lipid microspheres
- Author:
Jun-Xia FU
1
Author Information
- Publication Type:Journal Article
- Keywords: Alprostadil; Freeze-dried; Lipid microsphere; Pharmacokinetics; Stability
- From: Chinese Pharmaceutical Journal 2015;50(19):1704-1708
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To prepare freeze-dried alprostadil lipid microspheres and investigate their stability and pharmacokinetic characteristics. METHODS: The alprostadil lipid microspheres were prepared by two-step emulsifying method and then freeze-dried. The physicochemical properties were characterized.The stability in vitro and pharmacokinetics in Beagle dogs were also studied. RESULTS: The freeze-dried alprostadil lipid microspheres presented a good appearance and the rehydrated time was short. The size after reconstruction was (164.1±3.9) nm, the encapsulation efficiency was (92.5±3.3)% and the content of PGA1 was (1.38±0.21)%. It showed good stability after storing for 6 months as indicated by the size and contents of alprostadil and PGA1. After intravenous injection in Beagle dogs, the half time and peak time were (7.5±3.7) and (7.6±2.9) min respectively, and the peak plasma concentration of PGE1 was (105±40.4) ng·L-1, which was similar to the reference formulation. CONCLUSION: The freeze-dried alprostadil lipid microspheres can significantly improve the stability of alprostadil lipid microspheres with good pharmacokinetic characteristics, which indicates a promising prospect in clinic use.
