Prolonged release of tegafur from S/O/W multiple emulsion.
To develop a prolonged and sustained release preparation, we prepared an albumin microsphere-in-oil-in-water emulsion (S/O/W) and examined sustained release from it in comparison with other control preparations such as water-in-oil (W/O) emulsions and microspheres in vitro and in vivo, respectively. Tegafur was used as a model drug. A microsphere-in-oil emulsion was prepared by adding albumin microspheres to soybean oil containing 20% Span 80. To prepare an S/O/W emulsion, the microsphere-in-oil emulsion was added into an aqueous solution of hydroxypropyl methylcellulose containing Pluronic F68. The mean particle size of the albumin microspheres was 3 microns, and the ratio of entrapment of tegafur into albumin microspheres was about 25%. In an in vitro release test, the t75 of the S/O/W emulsion was fourfold greater and in an in vivo release test the mean residence time of tegafur from the S/O/W emulsion was more than twofold that from a W/O emulsion or microsphere system. The mean residence time of 5-fluorouracil (5-FU) from an S/O/W emulsion was also greater than with other dosage forms. These results suggest the possible usefulness of an S/O/W emulsion for the sustained and prolonged release of tegafur.
Oh
I
I
College of Pharmacy, Chonnam National University, Kwangju, Korea.
Kang
Y G
YG
Lee
Y B
YB
Shin
S C
SC
Kim
C K
CK
D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000627:therapeutic use*; D003692:Delayed-Action Preparations; D004655:Emulsions; D008297:Male; D008863:Microspheres; D051381:Rats; D017207:Rats, Sprague-Dawley; D005641:Tegafur / Q000627:therapeutic use*
D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D004655:Emulsions; D005641:Tegafur