Mj. Habib et R. Mesue, DEVELOPMENT OF CONTROLLED-RELEASE FORMULATIONS OF KETOPROFEN FOR ORALUSE, Drug development and industrial pharmacy, 21(12), 1995, pp. 1463-1472
Microencapsulated forms of ketoprofen were formulated using polymers a
nd polymer combinations and their in-vitro release characteristics wer
e evaluated against pure ketoprofen using Vanderkamp 600 dissolution t
est apparatus. Suspensions of cellulose acetate phthalate were prepare
d and various quantities of drug, glycerin, tween 80, span 80, methoce
l and avicel were added and the resulting solution was passed through
a peristaltic pump into a hardening solution. Beads were formed, dried
and the release of the drug was studied at various time intervals in
a dissolution medium of simulated intestinal pH. The dissolution studi
es of the ketoprofen demonstrated differences in drug release properti
es depending on composition and method of preparation. A formulation o
f Methocel beads with equal proportions of the two surfactants release
d its drug content over a period of 12 hours in a zero-order fashion.
Rapid drug dissolution was seen when the formulations contained Tween
80 as a surfactant. Varying the drug to CAP ratio in the suspension fr
om 0.1 to 0.4 did not appear to alter dissolution. It is concluded tha
t proper control of the formulation can give any desirable release fro
m ketoprofen formulations.