title: Precorneal sampling techniques for ophthalmic gels.
abstract: Drug-cornea contact time is a critical issue in ocular drug delivery. Existing methods for its experimental determination are developed mainly for eye drops and ointments, and have not been reported for ophthalmic gels. The present study evaluated two tear film sampling techniques (capillary tubes and Schirmer strips) and one recovery technique (cotton swab) for their suitability for the determination of precorneal drug concentration as a function of time for ophthalmic gels. The study was conducted using the rabbit eye model, and the gel studied was a commercial polyacrylate-based gel containing pilocarpine HCl. The three techniques explored yield similar results with respect to drug-cornea contact time, about one hour for the gel studied. The strip method suffers from a gel-carry-over problem at the early time points; therefore it is not recommended for tear sampling until most of the gel is cleared from the cul-de-sac. Successful tear sampling was accomplished using capillary tubes. Drug concentration in the tear film as a function of time determined using this technique reveals not only the duration of contact between the drug and the cornea, but also demonstrates a nonuniform drug distribution in the tear film at the early time points (10 and 30 minutes). Finally the cotton swab technique is gentle, easy, and nondestructive. It recovers total drug remaining in the cul-de-sac but does not yield information for the tear film.
authors.affiliation: Allergan, Inc. Irvine, California.
authors.forename: S
authors.initials: S
authors.lastname: Ding
authors.forename: C C
authors.initials: CC
authors.lastname: Chen
authors.forename: R
authors.initials: R
authors.lastname: Salome-Kesslak
authors.forename: D D
authors.initials: DD
authors.lastname: Tang-Liu
authors.forename: K J
authors.initials: KJ
authors.lastname: Himmelstein
mesh_terms: D000818:Animals; D001082:Aqueous Humor / Q000737:chemistry / Q000378:metabolism; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003315:Cornea / Q000737:chemistry / Q000378:metabolism*; D004337:Drug Carriers; D005260:Female; D005782:Gels; D010862:Pilocarpine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D011817:Rabbits; D013048:Specimen Handling; D013666:Tears / Q000737:chemistry / Q000378:metabolism*
chemical_list: D004337:Drug Carriers; D005782:Gels; D010862:Pilocarpine