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Narcotic Antagonists: Naltrexone Pharmacochemistry and Sustained-Release Preparations

NIDA Research Monograph, Number 28 [Printed in 1981]

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Table of Contents

The Editors


Historical Perspective on the Chemistry and Development of Naltrexone-----3
Sydney Archer

Treatment of Heroin-Dependent Persons With Antagonists: Current Status-----11
Pierre Renault


An Electron-Capture Gas Chromatographic Assay for Naltrexone in Biological Fluids-----25
R. H. Reuning, S. B. Ashcraft, and B. E. Morrison

Quantitative Determination of Naltrexone, 6 β-Naltrexol and 2-Hydroxy-3-methoxy-6β-naltrexol (HMN) in Human Plasma, Red Blood Cells, Saliva and Urine by Gas Liquid Chromatography-----36
Karl Verebey

Analytical Methods for Quantitative and Qualitative Analysis of Naltrexone and Metabolites in Biological Fluids-----52
Monroe E. Wall and Dolores R. Brine


Background on Animal Testing in the Drug Delivery Systems Program-----69
William L. Dewey

Pharmacological Evaluation of Narcotic Antagonist Delivery Systems in Rhesus Monkeys-----77
Stephen E. Harrigan and David A. Dawns

A Comparative Study of the Oral, Intravenous, and Subcutaneous Administration of 3H Naltrexone to Normal Male Volunteers-----93
Mario Perez-Reyes and Monroe E. Wall


The Metabolism of Naltrexone in Man-----105
Monroe E. Wall, Dolores R. Brine, and Mario Perez-Reyes

Current Status of Preclinical Research on Disposition, Pharmacokinetics, and Metabolism of Naltrexone-----132
Anand L. Misra

The Clinical Pharmacology of Naltrexone: Pharmacology and Pharmacodynamics-----147
Karl Verebey


Overview of Human Pharmacokinetics of Naltrexone-----161
Vojtech Licko

Pharmacokinetic Quantitation of Naltrexone Release From Several Sustained-Release Delivery Systems-----172
R. H. Reuning, S.H.T. Liao, and A.E. Staubus


A Review of Parenteral Sustained-Release Naltrexone Systems-----187
James L. Olsen and Fred A. Kincl

Development of Drug Delivery Systems for use in Treatment of Narcotic Addiction-----194
A. Carl Sharon and Donald L. Wise

Use of Synthetic Polypeptides in the Preparation of Biodegradable Delivery Systems for Narcotic Antagonists-----214
Kenneth R. Sidman, Arthur D. Schwope, William D. Steber, and Stephen E. Rudolph

Biodegradable Drug Delivery Systems Based on Aliphatic Polyesters: Application to Contraceptives and Narcotic Antagonists-----232
Colin G. Pitt, Thomas A. Marks, and Anton Schindler

An Improved Long-Acting Delivery System for Narcotic Antagonists-----254
Anand L. Misra and Ronald B. Pontani

Solid Solutions as Long-Acting Naltrexone Delivery Systems-----265
James L. Olsen

Participants in Technical Review-----272

List of Monographs-----274

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