| 摘要 | 第3-7页 |
| abstract | 第7-8页 |
| Chapter1 Background | 第12-20页 |
| 1.1 Introduction | 第12-13页 |
| 1.2 Discovery and efficacy of eszopiclone | 第13-14页 |
| 1.3 Research progress in oral time controlled released preparations | 第14-17页 |
| 1.4 Clinical application and drawbacks of eszopiclone | 第17页 |
| 1.5 Proposing of the subject | 第17-20页 |
| Chapter2 Physical Properties of Eszopiclone | 第20-26页 |
| 2.1 Equipment and chemicals | 第20-21页 |
| 2.1.1 Equipment | 第20-21页 |
| 2.1.2 Chemicals | 第21页 |
| 2.2 Methods | 第21-22页 |
| 2.2.1 Determination of the solubility of eszopiclone | 第21页 |
| 2.2.2 Melting point | 第21页 |
| 2.2.3 Specific rotation | 第21-22页 |
| 2.3 Results and discussion | 第22-23页 |
| 2.3.1 Determination of the solubility of eszopiclone | 第22页 |
| 2.3.2 Melting point | 第22-23页 |
| 2.3.3 Specific rotation | 第23页 |
| 2.4 Conclusion | 第23-26页 |
| Chapter3 Preformulation Studies | 第26-54页 |
| 3.1 Equipment and chemicals | 第26-27页 |
| 3.1.1 Equipment | 第26页 |
| 3.1.2 Chemicals | 第26-27页 |
| 3.2 Methods | 第27-36页 |
| 3.2.1 Pretreatment of eszopiclone API via micronization | 第27-28页 |
| 3.2.2 Establishment of method for determination of the dissolution curve | 第28-31页 |
| 3.2.3 Establishment of method for determination of the content | 第31-33页 |
| 3.2.4 Establishment of method for chiral impurity detection | 第33-36页 |
| 3.3 Results and discussion | 第36-51页 |
| 3.3.1 Pretreatment of eszopiclone API via micronization | 第36-39页 |
| 3.3.2 Establishment of method for determination of the dissolution curve | 第39-43页 |
| 3.3.3 Establishment of method for determination of the content | 第43-47页 |
| 3.3.4 Establishment of method for chiral impurity detection | 第47-51页 |
| 3.4 Conclusion | 第51-54页 |
| Chapter4 Preparation of Eszopiclone Tablet Core | 第54-70页 |
| 4.1 Equipments and chemicals | 第54-55页 |
| 4.1.1 Equipment | 第54-55页 |
| 4.1.2 Chemicals | 第55页 |
| 4.2 Methods | 第55-60页 |
| 4.2.1 Evaluation indicators | 第55-56页 |
| 4.2.2 Preparation processes for the tablet core | 第56-57页 |
| 4.2.3 Screening of the tablet core formulation | 第57-59页 |
| 4.2.4 Investigation of preparation processes of the tablet core | 第59-60页 |
| 4.3 Results and discussion | 第60-68页 |
| 4.3.1 Screening of the tablet core formulation | 第60-65页 |
| 4.3.2 Determination of eszopiclone’s tablet core formulation | 第65-66页 |
| 4.3.3 Investigation of preparation processes of the tablet core | 第66-68页 |
| 4.4 Conclusion | 第68-70页 |
| Chapter5 Preparation of Eszopiclone Time-controlled Release Tablets | 第70-80页 |
| 5.1 Equipment and chemicals | 第70页 |
| 5.1.1 Equipment | 第70页 |
| 5.1.2 Chemicals | 第70页 |
| 5.2 Methods | 第70-75页 |
| 5.2.1 The preparation process of time-controlled release tablets | 第70-71页 |
| 5.2.2 The preparation of swelling layer and controlled release layer | 第71-74页 |
| 5.2.3 The influence of different conditions on the dissolution rate | 第74-75页 |
| 5.3 Results and discussion | 第75-78页 |
| 5.3.1 The preparation of swelling layer and controlled release layer | 第75-76页 |
| 5.3.2 Experimental verification | 第76-77页 |
| 5.3.3 The influence of different conditions on the dissolution rate | 第77-78页 |
| 5.4 Conclusion | 第78-80页 |
| Chapter6 Pharmacokinetic Study on Eszopiclone Time-controlled Release Tablets | 第80-86页 |
| 6.1 Equipment and chemicals | 第80-81页 |
| 6.1.1 Equipment | 第80页 |
| 6.1.2 Chemicals | 第80-81页 |
| 6.2 Methods | 第81-82页 |
| 6.2.1 Administration to animals and blood collection protocol | 第81页 |
| 6.2.2 Processing method for plasma samples | 第81页 |
| 6.2.3 LC-MS/MS chromatographic conditions | 第81-82页 |
| 6.3 Results and discussion | 第82-84页 |
| 6.4 Conclusion | 第84-86页 |
| Chapter7 Conclusions | 第86-90页 |
| References | 第90-94页 |
| Publications | 第94-96页 |
| Acknowledgements | 第96页 |
