Modelling ocular pharmacokinetics of fluorescein administered as lyophilisate or conventional eye drops.
OBJECTIVE: The objective of this evaluation was to model ocular pharmacokinetics of fluorescein administered as conventional eye drops and as lyophilisate to healthy volunteers in order to assess the relative bioavailability of the lyophilisate formulation. METHODS: A total of 44 healthy subjects re...
| Publicado en: | European Journal of Clinical Pharmacology Vol. 64; no. 5; pp. 521 - 530 |
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| Autores principales: | , , , , , , , |
| Formato: | clinical trial research Journal Article |
| Publicado: |
Springer Nature
May2008
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=105792095&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 105792095 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 00316970 NP9 jtl: European Journal of Clinical Pharmacology issn: 00316970 maglogo: N pubinfo: dt: May2008 vid: 64 iid: 5 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 105792095 2009880445 10.1007/s00228-007-0457-3 NLM18219479 105792095 ppf: 521 ppct: 9 formats: fmt: @attributes: type: P tig: atl: Modelling ocular pharmacokinetics of fluorescein administered as lyophilisate or conventional eye drops. aug: au: Abduljalil K Diestelhorst M Doroshyenko O Lux A Steinfeld A Dinslage S Süverkrüp R Fuhr U affil: Department of Pharmacology, Clinical Pharmacology Unit, University of Cologne, Gleueler Str. 24, D-50931, Köln, Germany. sug: subj: Fluorescent Dyes Administration and Dosage Fluorescent Dyes Pharmacokinetics Models, Biological Administration, Topical Adult Anterior Chamber Metabolism Biological Availability Clinical Trials Cornea Metabolism Drug Delivery Systems Female Freeze Drying Male Middle Age Ophthalmic Solutions Pharmacokinetics Human Adult: 19-44 years Middle Aged: 45-64 years Female Male ab: OBJECTIVE: The objective of this evaluation was to model ocular pharmacokinetics of fluorescein administered as conventional eye drops and as lyophilisate to healthy volunteers in order to assess the relative bioavailability of the lyophilisate formulation. METHODS: A total of 44 healthy subjects received equivalent doses of fluorescein as lyophilisate to one eye and as eye drops to the fellow eye in three individual studies. Fluorescein concentrations in the cornea and anterior chamber were measured by fluorophotometry. Data were analyzed by noncompartmental methods (WinNonlin software) and by compartmental population pharmacokinetic methods (NONMEM software). RESULTS: Compared to eye drops, both maximum fluorescein concentrations (C(max)) and the areas under the concentration-time curve (AUC(0-t )) values of fluorescein in the cornea and anterior chamber for lyophilisate were increased in the noncompartmental analysis: mean lyophilisate C(max) in the studies was 6.3- to 14.6-fold higher and mean AUC(0-t ) was 4.7- to 8.9-fold higher for ocular concentrations in the three studies. A three-compartment open model with first-order elimination from the anterior chamber adequately described population data. Estimated fluorescein systemic bioavailability (F) via the ocular route from lyophilisate relative to eye drops was 3.7-fold higher (95% CI 2.6-4.8). CONCLUSION: The data clearly show a considerably superior intraocular bioavailability of fluorescein when given as lyophilisate compared to conventional eye drops. There is a clear pharmacokinetic advantage of the lyophilisate preparation. pubtype: Academic Journal doctype: clinical trial research Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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