以聚苯乙烯和含羥基之苯乙烯共聚物為共膜材料製備乙基纖維素微膠囊及其制放行為研究

Preparation and Release Behaviour of Ethylcellulose Microcapsule by Using Polystyrene and Polystyrene Copolymer Containing Hydroxyl as the Co-wall Materials

陳暉(Hui Chen) ； 蔡燕鈴(Yen-Ling Tsai) ； 劉政常(Theng-Chang Liu)

《化學》 56卷3期 (1998/09) Pp. 147-155

https://doi.org/10.6623/chem.1998021

摘要

本實驗先合成聚苯乙烯(PS)及苯乙烯(St)與甲基丙烯酸- 2-羥基乙酯(HEMA)的共聚物(PSOH)，並利用PS與PS -OH作為乙基纖維素(EC)的共膜材料，以探討其對微膠囊制放特性之影響，微膠囊之粒徑大小、表面形態、藥物釋放速率及溶出行為皆加以討論。微膠囊的製備採用有機溶液添加非溶劑相分離法，以二氯甲院為溶劑、正己烷為非溶劑，並選用茶葉鹼(TH)為核物質。微膠囊之表面形態會受共膜材料之性質與析出時間影響，因PS與EC之材料結構有所差異，故對PS/EC系統而言，若PS添加量較多，則其析出時對未硬化完全的微膠囊表面的破壞較大，形成非常多的小球結塊，造成藥物之溶出速率加快。但在P S-OH/EC系統中，共膜材料PS -OH之羥基含量愈高將使PS -OH與EC沈析膜的分子間作用力增強，因而改善共膜材料性質，達到延緩藥物釋放速率之效果。本研究製備所得之微膠囊，當PS -OH( H) /EC比例為1/39w/w時，藥物之釋放速率可延長為純EC微膠囊的3.4倍。而PS/EC微膠囊最長可將藥物釋放連率延長為純EC微膠囊的1.6，最短可縮短為0.4倍。在溶出模式方面之探討，發現複合膜徵膠囊前40%的藥物溶出動力學特性皆能符合一階溶出模式及Higuchi圓球形間質化溶出模式。

關鍵字

微膠囊 ； 乙基纖維素 ； 聚苯乙烯 ； 甲基丙烯酸-2-羥基乙酯 ； 非溶劑添加相分離法 ； 制放速率 ； 動力學特性 ； 茶葉鹼

並列摘要

In order to be used as co-wall materials for the preparation of EC microcapsules, both polystyrene and styrene - 2-hydroxyethyl methacrylate copolymer (PS-OH) were synthesized at the beginning of this study. Subsequently, their effects on the drug release rate, the particle size, the surface morphology and the kinetic characteristics of EC microcapsules were investigated. The composite microcapsules used in this study were prepared by the non-solvent addition method in which theophylline was chosen as a core material and dichloromethane - n-hexane was treated as a solvent - non-solvent pair. The surface morphology of composite microcapsules was depended upon the properties and the precipitation time of the co-wall materials. However, the physical properties of PS and EC are somewhat different. Thus, for PS/EC microcapsules, an increase in PS additive showed evidence of an increasing rate of drug dissolution due to a positive tendency to form a numbers of ball-like aggregation on the surface of uncured microcapsules during precipitation. Nevertheless, for PS-OH/EC microcapsules, an increase in the hydroxyl content of PS-OH co-wall material could result in a modification of the property difference of co-wall materials possibly due to a strengthen interaction established between precipitated PS-OH and EC so that the drug release rate of microcapsules could be decreased. The drug release time of PS-OH/EC microcapsules with composition of a 1:39 (by weight) PS-OH to EC ratio, was extended by 3.4 times as long as that of EC microcapsule. However, the drug release time of PS/EC microcapsules, with some specific PS to EC ratios, could lengthen up to 1.6 times or shorten down to 0.4 time as long as that of Ee microcapsules. In dissolution studies in these composite microcapsules, it seemed that the kinetic characteristics of the former part by forty percent of total drug content were followed by the first order and Higuchi spherical matrix model.

並列關鍵字

Microcapsules ； Ethylcellulose ； Polystyrene ； 2-Hydroxyethyl methacrylate ； Non-solvent addition method ； Release rate ； Kinetic characteristics ； Theophylline