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Preformulation and metabolic studies on novel aminoalkylpyridine anticonvulsants.

Tse Kai Kong. / Thesis submitted in: August 1998. / Thesis (M.Phil.)--Chinese University of Hong Kong, 1999. / Includes bibliographical references (leaves 116-122). / Abstract also in Chinese. / ABSTRACT --- p.ii / 摘要 --- p.v / ACKNOWLEDGEMENTS --- p.viii / CONTENTS --- p.ix / LIST OF FIGURES --- p.xiii / LIST OF TABLES --- p.xvii / ABBREVIATIONS --- p.xix / Chapter CHAPTER ONE --- Introduction --- p.1 / Chapter 1 --- Introduction --- p.2 / Chapter 1.1 --- Definition and Prevalence of Epilepsy --- p.2 / Chapter 1.2 --- Neurophysiology and Pathophysiology of Epilepsy --- p.3 / Chapter 1.3 --- Drugs Currently Used in the Treatment of Epilepsy --- p.5 / Chapter 1.4 --- Triazolines Aminoalkylpyridines as a New Class of Potential Antiepileptic Drugs --- p.9 / Chapter 1.5 --- Chemical Synthesis of Aminoalkylpyridines --- p.14 / Chapter 1.6 --- Metabolism of Aminoalkylpyridines --- p.15 / Chapter 1.7 --- Anticonvulsant Activities of Aminoalkylpyridines --- p.16 / Chapter 1.8 --- Aim and Scope of the Present Study --- p.18 / Chapter CHAPTER TWO --- Experimental --- p.19 / Chapter 2.1 --- MATERIALS --- p.20 / Chapter 2.2 --- PREFORMULATION STUDIES ON AMINOALKYLPYRIDINES --- p.22 / Chapter 2.2.1 --- Determination of Partition Coefficient --- p.22 / Chapter 2.2.2 --- Determination of Aqueous Solubilities --- p.22 / Chapter 2.2.3 --- Determination of Thermal Properties --- p.23 / Chapter 2.3 --- DEVELOPMENT OF A HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC ASSAY FORp-C1 AMINOALKYLPYRIDINES --- p.24 / Chapter 2.3.1 --- HPLC Apparatus and Conditions --- p.24 / Chapter 2.3.2 --- Animal Treatments and Biological Fluid Collection --- p.24 / Chapter 2.3.3 --- Solid Phase Extraction --- p.25 / Chapter 2.3.4 --- Construction of Calibration Curves for p-Cl AAP in Rat Blood --- p.25 / Chapter 2.3.5 --- Construction of Calibration Curves for p-Cl AAP in Rat Urine --- p.26 / Chapter 2.3.6 --- Accuracy and Precision in the Quantitation of p-C1 AAP in Biological Fluids --- p.26 / Chapter 2.4 --- PRELIMINARY PHARMACOKINETICS OF p-C1 AAP FOLLOWING INTRAVENOUS ADMINISTRATION --- p.27 / Chapter 2.4.1 --- Cannulae Preparation --- p.27 / Chapter 2.4.2 --- Dosage --- p.27 / Chapter 2.4.3 --- Animal Surgery and Sample Collection --- p.28 / Chapter 2.4.4 --- Pharmacokinetic Calculations --- p.29 / Chapter 2.5 --- URINARY METABOLIC STUDIES OF p-C1 AAP --- p.30 / Chapter 2.5.1 --- Animal Treatment and Urine Collection --- p.30 / Chapter 2.5.2 --- Deconjugation Assay --- p.30 / Chapter 2.5.3 --- Non-deconjugated Urine Sample Treatment --- p.31 / Chapter 2.5.4 --- Separation of Metabolites by HPLC --- p.31 / Chapter 2.5.5 --- Identification of Metabolites by LC/MS --- p.31 / Chapter 2.5.6 --- Quantitative Analysis --- p.32 / Chapter 2.5.7 --- Preparation of the authentic β-amino alcohol --- p.34 / Chapter 2.6 --- STATISTICAL ANALYSIS --- p.34 / Chapter CHAPTER THREE --- Results and Discussion --- p.35 / Chapter 3.1 --- PREFORMULATION STUDIES ON AMINOALKYLPYRIDINES --- p.36 / Chapter 3.1.1 --- PARTITION COEFFICIENT (K°W) --- p.36 / Chapter 3.1.2 --- AQUEOUS SOLUBILITY --- p.37 / Chapter 3.1.3 --- THERMAL ANALYSIS --- p.41 / Chapter 3.2 --- DEVELOPMENT OF A HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC ASSAY FOR p-C1 AMINOALKYLPYRIDINES --- p.49 / Chapter 3.2.1 --- SOLID PHASE EXTRACTION --- p.49 / Chapter 3.2.2 --- CONSTRUCTION OF CALIBRATION CURVES FOR p-C1 AAP IN THE RAT BLOOD --- p.49 / Chapter 3.2.3 --- CONSTRUCTION OF CALIBRATION CURVES FOR p-C1 AAP IN THE RAT URINE --- p.52 / Chapter 3.2.4 --- ACCURACY AND PRECISION IN THE QUANTITATION OF p-Cl IN THE BIOLOGICAL FLUIDS --- p.54 / Chapter 3.3 --- PRELIMINARY PHARMACOKINETICS OF p-C1 AAP FOLLOWING INTRAVENOUS ADMINISTRATION --- p.57 / Chapter 3.4 --- URINARY METABOLIC STUDIES OF p-C1AAP --- p.61 / Chapter 3.4.1 --- QUALITATIVE STUDIES : IDENTIFICATION OF METABOLITES --- p.61 / Chapter 3.4.2 --- QUANTITATIVE STUDIES --- p.94 / Chapter CHAPTER FOUR --- Conclusion --- p.111 / REFERENCES --- p.115 / APPENDIX Published Papers --- p.121

Identiferoai:union.ndltd.org:cuhk.edu.hk/oai:cuhk-dr:cuhk_322539
Date January 1999
ContributorsTse, Kai Kong., Chinese University of Hong Kong Graduate School. Division of Pharmacy.
Source SetsThe Chinese University of Hong Kong
LanguageEnglish, Chinese
Detected LanguageEnglish
TypeText, bibliography
Formatprint, xix, 122 leaves : ill. ; 30 cm.
RightsUse of this resource is governed by the terms and conditions of the Creative Commons “Attribution-NonCommercial-NoDerivatives 4.0 International” License (http://creativecommons.org/licenses/by-nc-nd/4.0/)

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