Formulation of a reservoir-type testosterone transdermal delivery system.
A reservoir-type transdermal delivery system of testosterone (TS) was developed using an ethanol/water (70:30) cosolvent system as the vehicle. The maximum permeation rate achieved by 70% (v/v) of ethanol was further increased from 2.69 to 47.83 microg/cm(2)/h with the addition of 1.0% dodecylamine as the skin permeation enhancer. The permeation rate of TS through the ethylene vinyl acetate (EVA) membrane was observed to increase as the vinyl acetate content in the copolymer increased. Addition of 1.0% (w/w) gelling agent, hydroxypropyl methlycellulose (HPMC), in the reservoir formulation resulted in desirable rheological properties with an insignificant effect on the skin permeation rate of TS. Thus, a new transdermal delivery system for TS was formulated using EVA membrane coated with a pressure-sensitive adhesive (Duro-Tak 87-2510) and HPMC as a gelling agent. This experimental patch showed comparable plasma concentration profiles in the in vivo study when compared with a commercial product, Androderm(R). Moreover, the results suggested the possibility of further enhancing the permeation rate of TS by controlling the composition of the reservoir formulation.
Kim
M K
MK
College of Pharmacy, Pusan National University, 609-735, Pusan, South Korea.
Zhao
H
H
Lee
C H
CH
Kim
D D
DD
D000279:Administration, Cutaneous; D000818:Animals; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D005079:Excipients; D005782:Gels; D066298:In Vitro Techniques; D007785:Lactose / Q000031:analogs & derivatives*; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives*; D010078:Oxazines; D011863:Radioimmunoassay; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption; D012995:Solubility; D013739:Testosterone / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D014783:Viscosity
D003692:Delayed-Action Preparations; D005079:Excipients; D005782:Gels; D010078:Oxazines; D013739:Testosterone; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose