Ketoprofen 控釋圓粒劑型之研究

A Study on the Controlled Release Pellets Dosage Form of Ketoprofen

黃曉鳳(Hsiao-Feng Huang)

指導教授 ： 詹道明

高雄醫學大學/藥學院/藥學研究所/碩士(2004年)

摘要

本實驗主要目的是利用田口直交表和23全因子試驗設計法評估以擠壓搓圓方式製備ketoprofen圓粒產品之可行性。 根據ANOVA試驗結果顯示，水含量和黏合劑含量會影響圓粒的產率，而搓圓速度則是影響圓粒圓度之重要改變因子。 以底部噴霧方式及Wurster筒流動床機器裝置使用，並且以乙基纖維素乳膠(Surelease®)作為包覆圓粒的控釋材質，可成功地得到最適宜化的圓粒處方。 由熱分析結果顯示，ketoprofen藥品粉末與本實驗中所使用的賦形劑並不會有交互作用產生。水不溶性藥品的溶解度變化對溶離評估是一個很重要的參數，在本實驗中，ketoprofen在不同pH值及不同界面活性劑(如SLS、PVP K30)之溶解度已全面性評估，實驗結果顯示，溶離媒液中含有SLS、PVP K30可以增加ketoprofen釋出情況。 所有處方與原廠藥品Oruvial 200®以f1和f2溶離曲線比對符合因子，實驗結果顯示，所製得之處方F-S 20所製備之圓粒相似於Oruvial 200® 在pH6.8溶離媒液之溶離曲線。 綜合實驗結果顯示，使用Wurster fluid bed 機器，並且以乙基纖維素乳膠(Surelease®)作為包覆圓粒的控釋材質來製備ketoprofen控釋圓粒劑型在本實驗中是可行的。

關鍵字

伍思特流動床 ； Ketoprofen ； 控釋圓粒劑型 ； 擠壓搓圓

並列摘要

The objective of this study was to evaluate the feasibility of the preparation of ketoprofen pellets by extrusion-spheronization method using Taguchi orthogonal and 23 full factorial experiment design. According to the ANOVA test, the results showed that amount of water content and amount of binder content have a significant effect on the yield, while the important variables which influence the roundness of pellets seem to the spheronization speed. Successively, the optimized pellets were coated with an ethylcellulose pseudolatex preparation (Surelease®) in a fluid bed coating machine using a bottom spray and a Wurster column. The thermograms showed that no interaction was occurring between ketoprofen powder and excipients. The solubility behavior of water insoluble drug is an important parameter for dissolution evaluation. In this study, the solubility of ketoprofen was well estimated by the sample additive model for the effect of various pH values and different surfactants (SLS, PVP K30). The results displayed that dissolution medium containing SLS and PVP K30 were increased condition for ketoprofen release. Dissolution profiles of all formulation including Oruvial 200® were compared by f1 and f2 fit factors. The results showed that dissolution profiles of F-S 20 formulation was the same as Ourvil 200® in the pH 6.8 dissolution medium. Therefore, the preparation of ketoprofen pellets coated with Surelease® by Wurster fluid bed were feasibile in this study.

並列關鍵字

Controlled Release Pellets Dosage Form ； Extrusion-Spheronization ； Ketoprofen ； Wurster fluided bed

參考文獻

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