A new transdermal delivery system for pilocarpine in glaucoma treatment.
We studied the intraocular pressure (IOP)-lowering effect and the side effects of a new transdermal delivery system (TDS) containing pilocarpine. After giving their written informed consent, patients were randomly assigned to receive a pilocarpine TDS or a placebo TDS. Two patches, each containing 30 mg of pilocarpine or placebo, were applied to the supraclavicular skin of 24 patients. The IOP was recorded before and at +12, 16, and 20 h after application. Plasma samples were analyzed for pilocarpine before treatment and 12 and 20 h later via high-performance liquid chromatography. The amount of drug remaining on the dermal patches was analyzed at 20 h. The mean IOP recorded before application was 22.7 +/- 5.8 mmHg. As compared with the placebo TDS, the pilocarpine TDS did not significantly reduce IOP at 12, 16, or 20 h after application (P = 0.42). The mean plasma concentrations were 2.9 ng/ml at 12 h and 1.3 ng/ml at 20 h. The verum TDS showed a residual mean drug concentration of 35.3 mg pilocarpine on the TDS. A substantial amount of pilocarpine was released from the TDS to the dermis, causing detectable plasma levels of pilocarpine at 12 and 20 h after administration. The pilocarpine TDS is a new nonocular pharmaceutical device that should avoid the side effects well known in glaucoma treatment when conventional eye drops are used.
Department of Ophthalmology, University of Cologne, Germany.
S
S
Dinslage
M
M
Diestelhorst
T
T
Hille
K
K
Otto
D000042:Absorption; D000279:Administration, Cutaneous; D000287:Administration, Topical; D000368:Aged; D000369:Aged, 80 and over; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems / Q000379:methods*; D017889:Exfoliation Syndrome / Q000150:complications; D005260:Female; D005902:Glaucoma, Open-Angle / Q000150:complications / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D007429:Intraocular Pressure; D008297:Male; D008875:Middle Aged; D018721:Muscarinic Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D009883:Ophthalmic Solutions; D010862:Pilocarpine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012867:Skin / Q000378:metabolism*
D018721:Muscarinic Agonists; D009883:Ophthalmic Solutions; D010862:Pilocarpine