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| 題名: | Abiraterone acetate口服自發性微乳化劑型製備及特性評估
Development and Characterization of Oral Self-Microemulsifying Drug Delivery System for Abiraterone acetate |
| 作者: | 張泓軒
CHANG, HUNG-HSUAN |
| 貢獻者: | 藥學系碩士班
劉景平 |
| 關鍵詞: | 自發性微乳化
Abiraterone acetate |
| 日期: | 2024-01-17 |
| 上傳時間: | 2024-09-11 19:15:23 (UTC+8) |
| 摘要: | 自發性微乳化藥物傳輸系統(SMEDDSs)通常由藥物、水相、油相和界面活性劑?成，透過接觸胃腸道液體(水相)以及在消化管壁地蠕動後自發性微乳化，此一系統可以有效的作為載體幫助難溶性藥物進行傳輸。Abiraterone acetate是一種用於治療轉移性前列腺癌之口服藥物，然而根據美國FDA的BCS分類系統（生物製劑分類系統），Abiraterone acetate屬於Class IV類藥物，為了提高溶解度與生物地用度，在本研究中，利用油酸乙酯Ethyl oleate作為油相並使用非離子型界面活性劑Labrasol和Transcutol HP製備成自發性微乳化藥物傳輸系統，並構建由水相、油相和界面活性劑所組成的三相圖選擇配方之適當比例。為了做進一步的探討，利用高效能液相層析法（HPLC）測量Abiraterone acetate濃度之方法開發將選擇出的配方進行安定性試驗。此外也透過體外溶離實驗觀察在模擬胃腸道環境下的釋放情形，最後口服給藥於雄性Sprague - Dawley大鼠，進行藥物動力學試驗。結果顯示，自發性微乳化劑型在溶解度試驗的評估下確實能增加Abiraterone acetate的溶解度，但對於其生體可用率經體外溶離試驗以及藥物動力學試驗的評估後無顯著提高，未來可將改善藥物釋放作為之後的研究方向。
SMEDDSs (self-microemulsifying drug delivery systems) are typically composed of drug, oil phase, surfactant, and co-surfactant, which can spontaneously emulsify upon contact with gastrointestinal fluids and peristaltic movement of the intestinal wall. This system can effectively serve as a carrier to help transport poorly soluble drugs. Abiraterone acetate is an oral medication used to treat metastatic prostate cancer. However, according to the US FDA's BCS (biopharmaceutics classification system), Abiraterone acetate belongs to Class IV drugs, which are poorly soluble. In this study, ethyl oleate was used as the oil phase, and non-ionic surfactants Labrasol and Transcutol HP were used to prepare a self-microemulsifying drug delivery system to improve solubility and bioavailability. A pseudo ternary phase diagram composed of water phase, oil phase, and surfactant was constructed to select the appropriate ratio of the formulation. To further investigate, a high-performance liquid chromatography (HPLC) method was developed to measure the concentration of Abiraterone acetate and stability tests were performed on the selected formulation. In addition, in vitro dissolution experiments were conducted to observe the release profile in simulated gastrointestinal conditions, and finally, pharmacokinetic studies were carried out after oral administration to male Sprague-Dawley rats. The results show that the self-microemulsification dosage form can indeed increase the solubility of Abiraterone acetate when evaluated by the solubility test, but its bioavailability is not significantly improved after the evaluation of the in dissolution test and pharmacokinetics test. Therefore, to improve drug release is a feasible future research direction. |
| 描述: | 碩士
指導教授：劉景平
口試委員：劉景平
口試委員：黃偉展
口試委員：劉宜旻 |
| 資料類型: | thesis |
| 顯示於類別: | [藥學系] 博碩士論文
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