Influence of polyvinylpyrrolidone quantity on the solubility, crystallinity and oral bioavailability of fenofibrate in solvent-evaporated microspheres.
The objective of this study is to explore the influence of polyvinylpyrrolidone (PVP) quantity on the solubility, crystallinity and oral bioavailability of poorly water-soluble fenofibrate in solvent-evaporated microspheres. Numerous microspheres were prepared with fenofibrate, sodium lauryl sulphate (SLS) and PVP using the spray-drying technique. Their aqueous solubility, dissolution, physicochemical properties and pharmacokinetics in rats were assessed. The drug in the solvent-evaporated microspheres composed of fenofibrate, PVP and SLS at the weight ratio of 1:0.5:0.25 was not entirely changed to the amorphous form and partially in the microcrystalline state. However, the microspheres at the weight ratio of 1:4:0.25 provided the entire conversion to the amorphous form. The latter microspheres, with an improvement of about 115 000-fold in aqueous solubility and 5.6-fold improvement in oral bioavailability compared with the drug powder, gave higher aqueous solubility and oral bioavailability compared with the former. Thus, PVP quantity played an important role in these properties of fenofibrate in the solvent-evaporated microspheres.
a College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University , Ansan , South Korea ;|b Faculty of Pharmacy , University of Central Punjab , Johar , Lahore , Pakistan ;
Abid Mehmood
AM
Yousaf
a College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University , Ansan , South Korea ;
Dong Wuk
DW
Kim
a College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University , Ansan , South Korea ;
Dong Shik
DS
Kim
c College of Pharmacy, Yeungnam University , Gyongsan , South Korea ;
Jong Oh
JO
Kim
d School of Pharmacy, Sungkyunkwan University , Suwon , South Korea ;
Yu Seok
YS
Youn
e College of Pharmacy, Inje University , Gimhae , South Korea.
Kwan Hyung
KH
Cho
c College of Pharmacy, Yeungnam University , Gyongsan , South Korea ;
Chul Soon
CS
Yong
a College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University , Ansan , South Korea ;
Han-Gon
HG
Choi
D000284:Administration, Oral; D000818:Animals; D011345:Fenofibrate / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D008297:Male; D008863:Microspheres; D011205:Povidone / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012997:Solvents / Q000737:chemistry
D012997:Solvents; D011205:Povidone; D011345:Fenofibrate
Fenofibrate; aqueous solubility; crystallinity; oral bioavailability; polyvinylpyrrolidone; solvent-evaporated microsphere