近年來,隨著現(xiàn)代化進程的不斷推進,生活節(jié)奏不斷加快,人們的生活壓力也不斷增加,失眠問題逐漸成為了炙手可熱的焦點問題。失眠癥是指在良好的睡眠條件下,不存在任何睡眠影響因素時,無法入睡或無法維持睡眠狀態(tài),導致日間疲勞、痛苦、日間功能障礙,降低生活質(zhì)量,并增加精神健康問題、濫用藥物和酒精的風險,同時增加醫(yī)療保健的占用率。研究顯示,失眠與高發(fā)的心血管系統(tǒng)疾病如高血壓等密切相關(guān)。失眠癥對于人們的身心健康和生命質(zhì)量危害極大,是造成意外事故和死亡的高危因素。右佐匹克隆是一種非苯二氮?類鎮(zhèn)靜催眠藥物,相比于苯二氮?類藥物,右佐匹克隆具有起效快、作用時間短、安全性高、成癮潛力低等優(yōu)勢。2004年美國食品藥物管理局(FDA)批準該藥用于治療失眠,為目前較為理想的一線助眠藥物,2007年由天士力集團首先在國內(nèi)上市。作為佐匹克隆的右旋異構(gòu)體,右佐匹克隆對苯二氮?受體的親和力是左旋體的50倍,具有縮短入睡時間、延長睡眠時間、減少覺醒次數(shù)、提高睡眠質(zhì)量等特點。由于是單一的光學異構(gòu)體給藥,可避免服用消旋佐匹克隆產(chǎn)生的副作用,如:由于唾液分泌藥物引起的口干、倦睡、早晨疲勞、頭痛、眩暈、神經(jīng)運動功能損傷等。右佐匹克隆的...

【文章頁數(shù)】：96 頁

【學位級別】：碩士

【文章目錄】：
摘要
abstract
Chapter1 Background
    1.1 Introduction
    1.2 Discovery and efficacy of eszopiclone
    1.3 Research progress in oral time controlled released preparations
    1.4 Clinical application and drawbacks of eszopiclone
    1.5 Proposing of the subject
Chapter2 Physical Properties of Eszopiclone
    2.1 Equipment and chemicals
        2.1.1 Equipment
        2.1.2 Chemicals
    2.2 Methods
        2.2.1 Determination of the solubility of eszopiclone
        2.2.2 Melting point
        2.2.3 Specific rotation
    2.3 Results and discussion
        2.3.1 Determination of the solubility of eszopiclone
        2.3.2 Melting point
        2.3.3 Specific rotation
    2.4 Conclusion
Chapter3 Preformulation Studies
    3.1 Equipment and chemicals
        3.1.1 Equipment
        3.1.2 Chemicals
    3.2 Methods
        3.2.1 Pretreatment of eszopiclone API via micronization
        3.2.2 Establishment of method for determination of the dissolution curve
        3.2.3 Establishment of method for determination of the content
        3.2.4 Establishment of method for chiral impurity detection
    3.3 Results and discussion
        3.3.1 Pretreatment of eszopiclone API via micronization
        3.3.2 Establishment of method for determination of the dissolution curve
        3.3.3 Establishment of method for determination of the content
        3.3.4 Establishment of method for chiral impurity detection
    3.4 Conclusion
Chapter4 Preparation of Eszopiclone Tablet Core
    4.1 Equipments and chemicals
        4.1.1 Equipment
        4.1.2 Chemicals
    4.2 Methods
        4.2.1 Evaluation indicators
        4.2.2 Preparation processes for the tablet core
        4.2.3 Screening of the tablet core formulation
        4.2.4 Investigation of preparation processes of the tablet core
    4.3 Results and discussion
        4.3.1 Screening of the tablet core formulation
        4.3.2 Determination of eszopiclone’s tablet core formulation
        4.3.3 Investigation of preparation processes of the tablet core
    4.4 Conclusion
Chapter5 Preparation of Eszopiclone Time-controlled Release Tablets
    5.1 Equipment and chemicals
        5.1.1 Equipment
        5.1.2 Chemicals
    5.2 Methods
        5.2.1 The preparation process of time-controlled release tablets
        5.2.2 The preparation of swelling layer and controlled release layer
        5.2.3 The influence of different conditions on the dissolution rate
    5.3 Results and discussion
        5.3.1 The preparation of swelling layer and controlled release layer
        5.3.2 Experimental verification
        5.3.3 The influence of different conditions on the dissolution rate
    5.4 Conclusion
Chapter6 Pharmacokinetic Study on Eszopiclone Time-controlled Release Tablets
    6.1 Equipment and chemicals
        6.1.1 Equipment
        6.1.2 Chemicals
    6.2 Methods
        6.2.1 Administration to animals and blood collection protocol
        6.2.2 Processing method for plasma samples
        6.2.3 LC-MS/MS chromatographic conditions
    6.3 Results and discussion
    6.4 Conclusion
Chapter7 Conclusions
References
Publications
Acknowledgements



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