Transdermal delivery of theophylline using an ethanol/panasate 800-ethylcellulose gel preparation.
A novel ethylcellulose gel preparation using an ethanol/panasate 800 (tricaprylin) (40/60) binary lipophilic vehicle was developed and applied to the transdermal delivery of theophylline. The in vitro skin permeability of theophylline across excised hairless mouse skin was improved by the use of this ethanol/panasate 800 (40/60) binary vehicle compared with either ethanol or panasate 800 as a single vehicle, and the addition of lauric acid as a permeation enhancer to the binary vehicle shortened the lag time and increased the permeated amount of theophylline up to 6 h (initial permeation amount). The in vitro permeability of theophylline from the ethanol/panasate 800 (40/60)-ethylcellulose gels decreased with an increase in the content of ethylcellulose in the gels. In the in vivo evaluation using abdominal rat skin, the ethanol/panasate 800 (40/60)-7% (w/w) ethylcellulose gel produced a good feature as a sustained-release preparation, with a relatively high bioavailability (BA) of theophylline, and dose dependency was observed.
Lee
C K
CK
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Kitagawa
K
K
Uchida
T
T
Kim
N S
NS
Goto
S
S
D000279:Administration, Cutaneous; D000818:Animals; D001682:Biological Availability; D002210:Caprylates; D002482:Cellulose / Q000031:analogs & derivatives; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004058:Diffusion; D000431:Ethanol; D005079:Excipients; D005782:Gels; D066298:In Vitro Techniques; D007850:Lauric Acids / Q000494:pharmacology; D051379:Mice; D008819:Mice, Nude; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption; D013806:Theophylline / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D014280:Triglycerides
D002210:Caprylates; D003692:Delayed-Action Preparations; D005079:Excipients; D005782:Gels; D007850:Lauric Acids; D014280:Triglycerides; C030358:lauric acid; D000431:Ethanol; C003637:tricaprylin; C013517:ethyl cellulose; D002482:Cellulose; D013806:Theophylline