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      Hydrolysis of Prednisolone Succinate by Esterase in Rabbit Ocular Tissue

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          Abstract

          Prednisolone concentrations in serum after both subconjunctival and intravenous injections of prednisolone sodium succinate at a 1 mg/kg equivalent dose of prednisolone in rabbits were analyzed by regularly phased high-performance liquid chromatography. The systemic availability after subconjunctival injection was determined to be almost 1.0 by comparing areas under the serum concentration-time curves for both administration routes. The initial hydrolytic rate of prednisolone succinate ester was dependent on the amount of total protein in ocular tissue homogenates and fluids as well as that in serum. The rate followed Michaelis-Menten kinetics, with an almost consistent Michaelis constant. Although the maximum hydrolytic rate per unit amount of tissue protein was the highest in conjunctival tissue, followed by corneal tissue and serum, the esterase activity corrected by total protein in the whole rabbit body should be the highest in serum, followed by conjunctival tissue. These results indicate that prednisolone sodium succinate administered subconjunctivally is hydrolized rapidly by esterase and absorbed almost completely into the systemic circulation.

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          Author and article information

          Journal
          ORE
          Ophthalmic Res
          10.1159/issn.0030-3747
          Ophthalmic Research
          S. Karger AG
          0030-3747
          1423-0259
          1987
          1987
          04 December 2009
          : 19
          : 6
          : 322-329
          Affiliations
          aFaculty of Pharmaceutical Sciences, Kanazawa University, Kanazawa, Japan; bDepartment of Ophthalmology, Kanazawa Medical University, Uchinada, Ishikawa, Japan
          Article
          265516 Ophthalmic Res 1987;19:322–329
          10.1159/000265516
          3441354
          df9b81f7-15eb-4ef3-b0dd-738d1f6a14a9
          © 1987 S. Karger AG, Basel

          Copyright: All rights reserved. No part of this publication may be translated into other languages, reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording, microcopying, or by any information storage and retrieval system, without permission in writing from the publisher. Drug Dosage: The authors and the publisher have exerted every effort to ensure that drug selection and dosage set forth in this text are in accord with current recommendations and practice at the time of publication. However, in view of ongoing research, changes in government regulations, and the constant flow of information relating to drug therapy and drug reactions, the reader is urged to check the package insert for each drug for any changes in indications and dosage and for added warnings and precautions. This is particularly important when the recommended agent is a new and/or infrequently employed drug. Disclaimer: The statements, opinions and data contained in this publication are solely those of the individual authors and contributors and not of the publishers and the editor(s). The appearance of advertisements or/and product references in the publication is not a warranty, endorsement, or approval of the products or services advertised or of their effectiveness, quality or safety. The publisher and the editor(s) disclaim responsibility for any injury to persons or property resulting from any ideas, methods, instructions or products referred to in the content or advertisements.

          History
          : 12 February 1987
          : 03 June 1987
          Page count
          Pages: 8
          Categories
          Original Paper

          Vision sciences,Ophthalmology & Optometry,Pathology
          Subconjunctival administration,Ocular tissue,Prednisolone, prodrug,Systemic availability,Esterase activity,Enzymatic hydrolysis,Prednisolone sodium succinate

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