title: The ophthalmic lyophilisate carrier system (OLCS): development of a novel dosage form, freeze-drying technique, and in vitro quality control tests.
abstract: The ophthalmic lyophilisate carrier system (OLCS) is a novel dosage form for delivery of pharmacologically active ingredients or other substances improving the structure of the tear film to the eye. A drop of lyophilisate containing the drug and bulk forming water-soluble or swelling excipients is attached to a flexible hydrophobic carrier. Placebo OLCS and OLCS containing several drugs commonly used in ophthalmology were compared to conventional eye drops containing the same ingredients. A novel lyophilization procedure for the production of this dosage form is described, which allows stricter control of the freezing and drying conditions and shortens the production cycle by at least an order of magnitude. In clinical studies it was found that OLCS are easy to administer and well tolerated if the force of adhesion between lyophilisates and carrier strips and the structural firmness of the lyophilisates themselves are well controlled. These parameters are critical for convenient administration and complete delivery of the dose of active ingredients incorporated, therefore suitable in vitro tests were developed with which their values can be determined for the purpose of process validation. A study of fluorescein OLCS in humans indicated that concentration profiles in the cornea and anterior chamber are significantly higher than after administration of equal doses of the diagnostic in conventional eye drops.
authors.affiliation: Pharmazeutisches Institut der Universität Bonn, Pharmazeutische Technologie, Bonn, Germany. sueverkruep@uni-bonn.de
authors.forename: Richard
authors.initials: R
authors.lastname: Süverkrüp
authors.forename: Sabine
authors.initials: S
authors.lastname: Grunthal
authors.forename: Olena
authors.initials: O
authors.lastname: Krasichkova
authors.forename: Stephan
authors.initials: S
authors.lastname: Maier
authors.forename: Anja
authors.initials: A
authors.lastname: Weichselbaum
authors.forename: Bernd
authors.initials: B
authors.lastname: Neff
authors.forename: Michael
authors.initials: M
authors.lastname: Diestelhorst
authors.forename: Sven
authors.initials: S
authors.lastname: Dinslage
authors.forename: Anja
authors.initials: A
authors.lastname: Lux
mesh_terms: D004304:Dosage Forms; D004337:Drug Carriers / Q000008:administration & dosage / Q000592:standards; D005123:Eye / Q000187:drug effects* / Q000378:metabolism; D005612:Freeze Drying / Q000379:methods; D006801:Humans; D009883:Ophthalmic Solutions / Q000008:administration & dosage* / Q000592:standards*; D011786:Quality Control
chemical_list: D004304:Dosage Forms; D004337:Drug Carriers; D009883:Ophthalmic Solutions