環狀糊精於Aripiprazole 之溶解度關係

The Solubility of Aripiprazole with Cyclodextrin

金來承(Lai-Cheng Chin)

指導教授 ： 芮祥鵬

國立臺北科技大學/工程學院/有機高分子研究所/碩士(2013年)

摘要

本實驗主要在於研究關於環狀糊精之應用，探討以不同種類的環狀糊精如Alpha、Beta、Gamma-Cyclodextrin與配合特定之難溶性藥物精神分裂症用藥(Aripiprazole)，隨時間觀察溶解度之變化。並Beta-Cyclodextrin為主，探討轉速不同的環境下溶解度是否也會隨之變化，以及Beta-Cyclodextrin濃度對於藥物溶解度的影響。最後，將所得之結果將藥物與環狀糊精乾燥成粉態，並模擬在胃中的溶離率變化。實驗結果得知，Beta-Cyclodextrin為幫助增加藥物溶解度最適化之環狀糊精，並且由數據結果得知不同轉速環境下，不會影Beta-Cyclodextrin之助溶效果，但隨時間變化助溶之安定性就呈一級反應方式漸漸降低。而實驗證明經過Beta-Cyclodextrin包覆之藥物相對未經加工之原料藥，在模擬胃酸之環境下，確實大大提升了藥物溶離率，期許研究結果對未來Aripiprazole臨床上，有提升人體吸收效率上的幫助。

關鍵字

溶離環狀糊精

並列摘要

This study focuses on the application of cyclodextrin in the drug release field. Different types of cyclodextrin including Alpha, Beta, Gamma types accompanied with a specific insoluble drug, the schizophrenia medication (Aripiprazole), have been used to study the improvement of drug solubility. Experimental results show that Beta-Cyclodextrin can effectively increase drug solubility. The rotational speed of the mixing blades, however,reveals an insignificant effect. The release kinetics was determined as a first order mode.Finally, experimental results demonstrate that the drug-coated with Beta-Cyclodextrin can
survive in a gastric acid environment and indeed can greatly enhance the drug dissolution rate of Aripiprazole. This study can help the clinical trial of Class 3 for the improvement of Aripiprazole release in the future.

並列關鍵字

Cyclodextrin ； drug dissolution

參考文獻

1. Qun Lu，Ｅnhancing oral bioavailability through enabled formulation，Developability of

Pharmaceutical Profiling for Drug Candidates(2012)

3. T.Loftsson, M.E. Brewster. Physicochemical properties of water and its effect on drug

4. C.Sweerman,Martindale ： The Complete Drug Reference.33rded., pharmaceutical

5. H.Kuhl, Pharmacology of estrogens and progestagens：influence of different routes of