使用親水瓊脂膠體奈米微粒系統來促進Indomethacin對水之溶解速率

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標題:	使用親水瓊脂膠體奈米微粒系統來促進Indomethacin對水之溶解速率 Application of Agar Hydrogel Based Nanoparticulate System for Enhancing the Dissolution Rates of Indomethacin
作者:	李國豪 Guo-hao Li
貢獻者:	林恆弘嘉南藥理科技大學：生物科技研究所
關鍵字:	奈米粒子親水膠體吲哚美洒辛水難溶性 Indomethacin Water-insoluble Nanoparticles Hydrogel
日期:	2006
上傳時間:	2008-11-24 17:02:38 (UTC+8)
摘要:	水難溶性藥物一般有生體可用率不佳的特性。此實驗的研究目的，是設計含有奈米粒子的膠體包埋系統來包埋Indomethacin，以增進其水溶性。親水膠體奈米微粒懸浮劑包埋Indomethacin的製作，藉由將藥物溶於固化凝膠以機械粉碎法，研磨成奈米微粒，再利用凍晶乾燥將懸浮劑凍乾。凍晶乾燥製程中，親水膠體因水的含量及溫度的變化，最後可能產生水難溶性的聚集，藉由pH值的調整及抗凍劑加入來防止聚集，在凍晶乾燥後儲存。藉由凍晶乾燥後的乾粉及加水復原的懸浮劑，進行物理性質的檢測。粒子大小是經由表面電位及粒徑大小分佈分析儀進行測定；除外，藥物－聚合膠體的交互作用則使用卡式熱分析儀(DSC)分析，藥物溶解度的測定是用濁度計來檢測。結果顯示，固化凝膠機械粉碎法可得到粒徑在 40 nm到 400 nm的Indomethacin－親水膠體奈米粒子。在凍晶乾燥前將奈米粒子鹼化及加入抗凍劑，也顯示對包埋的奈米粒子產生更好的安定性。由DSC的結果也顯示在凍晶乾燥的製造過程中，並無明顯的化學交互作用。由凍晶乾粉製程的奈米粒子，能迅速的在水中分散，形成清澈且穩定的狀態。此結果將有助於發展其他水難溶性藥物助溶系統。 The bioavailability of water-insoluble drug is poor. The aim of the present study was to design a suspension composed of numberless nanoparticles to improve the solubility of indomethacin. Hydrogel based nanoparticles encapsulating indomethacin were prepared by using the solid jelly pulverization technique, and then freeze-dry to lyophilized powder. In the freeze-drying process, hydrogel based nanoparticles undergo change of temperature and water content, eventually forming water-insoluble aggregates. The pH value adjusted as well as the cryoprotectants was added to stable the dispersion system during formulation, lyophilization, and storage. The physical studies of hydrogel based nanoparticles were performed in a freeze-drying or resuspended form. The size of the indomethacin- hydrogel nanoparticles was assessed using a LS particle size analyzer. In addition, any drug-polymer interactions were assessed using a differential scanning calorimeter (DSC). The dissolution was determined by the apparatus of Franz diffusion and analyzed by turbidimeter. The results show that solid jelly pulverization technique yielded indomethacin hydrogel nanoparticles with a mean diameter of 40 nm to 400 nm. Alkalization of suspension containing nanoparticles or blending of cryoprotectants in suspension before the freeze-drying process showed better stabilization of encapsulated drug. The DSC measurements indicated that the chemical interaction does not occur among the components during manufacturing processes and lyophilized powder. The lyophilized powder of nanoparticles reconstitutes rapidly, the resulting product has remarkable clarity, and stability. The above results will be helpful to possible development of the other water-insoluble drug delivery systems.
關聯:	校內馬上公開，校外一年後公開
顯示於類別:	[生物科技系(所)] 博碩士論文

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