Preparation and evaluation of Eudragit gels. I: Eudragit organogels containing drugs as rectal sustained-release preparations.
New organogels containing salicylic acid, sodium salicylate, procaine, and ketoprofen were prepared by using Eudragit L and S, and propylene glycol. The physical properties (e.g., penetration and extensibility) of the organogels were affected considerably by the incorporation of a basic drug, such as procaine, rather than an acidic drug, such as salicylic acid. In in vivo evaluation using rabbits, it was found that 30% Eudragit L organogels containing 1.25% (w/w) salicylic acid or 2.5% (w/w) ketoprofen showed sustained plasma salicylic acid or ketoprofen levels and almost the same AUC as compared with Witepsol H-15 suppositories containing these drugs. Furthermore, the relative bioavailability for salicylic acid and ketoprofen released from 30% Eudragit L organogels, with 10% (w/w) linolic acid or oleic acid as absorption enhancer, increased to 1.55-1.75- and 1.46-1.85-fold, respectively, compared with 30% Eudragit L organogels without these unsaturated fatty acids.
Goto
S
S
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Kawata
M
M
Suzuki
T
T
Kim
N S
NS
Ito
C
C
D000180:Acrylic Resins / Q000008:administration & dosage*; D000285:Administration, Rectal; D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D005782:Gels; D007660:Ketoprofen / Q000008:administration & dosage / Q000493:pharmacokinetics; D008297:Male; D011109:Polymethacrylic Acids; D011817:Rabbits; D012459:Salicylates / Q000008:administration & dosage / Q000493:pharmacokinetics; D020156:Salicylic Acid
D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D005782:Gels; D011109:Polymethacrylic Acids; D012459:Salicylates; C038300:methylmethacrylate-methacrylic acid copolymer; D007660:Ketoprofen; D020156:Salicylic Acid