Effect of carvone on the permeation of nimodipine from a membrane-moderated transdermal therapeutic system.
The purpose of this investigation was to develop a membrane-moderated transdermal therapeutic system (TTS) of nimodipine using 2% w/w hydroxypropylmethylcellulose (HPMC) gel as a reservoir system containing 10% w/w of carvone (penetration enhancer) in 60% v/v ethanol. The flux of nimodipine through an ethylene vinyl acetate (EVA) copolymer membrane was found to increase with an increase in vinyl acetate content in the copolymer. The effect of a pressure-sensitive adhesive (TACKWHITE A 4MED) on the permeability of nimodipine through an EVA 2825 membrane (28% w/w vinyl acetate) or an EVA 2825 membrane/skin composite was also studied. An EVA 2825 membrane coated with TACKWHITE 4A MED was found to provide the required flux of nimodipine (117 +/- 5 microg/cm2/h) across rat abdominal skin. Thus a new transdermal therapeutic system for nimodipine was formulated using EVA 2825 membrane, coated with a pressure-sensitive adhesive TACKWHITE 4A MED, and 2% w/w HPMC gel as reservoir containing 10% w/w of carvone as a penetration enhancer. Studies in healthy human volunteers indicated that the TTS of nimodipine, designed in the present study, provided steady-state plasma concentration of the drug with minimal fluctuations.
Krishnaiah
Y S R
YS
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India. krishnaysr112@rediffmail.com
Bhaskar
P
P
Satyanarayana
V
V
D000279:Administration, Cutaneous; D000465:Algorithms; D000818:Animals; D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D000081005:Cyclohexane Monoterpenes; D005079:Excipients; D005782:Gels; D006801:Humans; D066298:In Vitro Techniques; D007785:Lactose / Q000031:analogs & derivatives*; D008297:Male; D008567:Membranes, Artificial; D008747:Methylcellulose / Q000031:analogs & derivatives*; D039821:Monoterpenes; D009553:Nimodipine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D010078:Oxazines; D010539:Permeability; D011145:Polyvinyls; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects*; D013056:Spectrophotometry, Ultraviolet; D013607:Tablets; D013729:Terpenes / Q000494:pharmacology*
D002121:Calcium Channel Blockers; D000081005:Cyclohexane Monoterpenes; D005079:Excipients; D005782:Gels; D008567:Membranes, Artificial; D039821:Monoterpenes; D010078:Oxazines; D011145:Polyvinyls; D013607:Tablets; D013729:Terpenes; C016438:ethylenevinylacetate copolymer; D009553:Nimodipine; C006923:carvone; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose