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尤特奇NE 30D/尤特奇L 30D-55共混物在延迟药物释放应用中作为功能性包衣材料的新用途。

Novel use of Eudragit NE 30D/Eudragit L 30D-55 blends as functional coating materials in time-delayed drug release applications.

作者信息

El-Malah Yasser, Nazzal Sami

机构信息

Department of Basic Pharmaceutical Sciences, College of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71209-0497, USA.

出版信息

Int J Pharm. 2008 Jun 5;357(1-2):219-27. doi: 10.1016/j.ijpharm.2008.02.003. Epub 2008 Feb 13.

Abstract

The objectives of this study were to evaluate the mechanical and thermal properties of films prepared from Eudragit NE 30D/Eudragit L 30D-55 blends and to examine the dissolution behavior of beads coated with the polymer blends up to 120% weight gain. Eudragit NE 30D and L 30D-55 dispersions were blended at 50:50, 67:33, 75:25, and 80:20 ratios. Cast films were evaluated by texture analysis and differential scanning calorimetry. Increasing Eudragit NE 30D concentration increased miscibility, softness, and decreased stiffness of the films. At 80:20 ratio, the polymer blend was completely miscible whereby Eudragit L 30D-55 was molecularly distributed in the mixture. This was confirmed by SEM analysis. The surface morphology of films and beads was evaluated before and after dissolution by scanning electron microscopy. SEM analysis demonstrated that the size of the pores formed after the dissolution of Eudragit L 30D-55 at pH 6.8 was dependent on the miscibility of the Eudragit blend. The implications of this effect were apparent in dissolution studies. For the 75:25 and 80:20 blends, a linear increase in lag time up to 7 h was observed with an increase in coat weight gain from 15 to 120%. At 60% weight gain, the 80:20 blend delayed drug release by approximately 7 h whereas the less miscible 75:25 blend delayed drug release by only 3.5 h. A lag time could therefore be controlled by manipulating both the theoretical weight gain of the beads and the concentration of Eudragit NE 30D in the blend.

摘要

本研究的目的是评估由尤特奇NE 30D/尤特奇L 30D-55共混物制备的薄膜的机械性能和热性能,并研究涂覆有聚合物共混物且增重高达120%的微丸的溶出行为。尤特奇NE 30D和L 30D-55分散体按50:50、67:33、75:25和80:20的比例混合。通过质地分析和差示扫描量热法对流延薄膜进行评估。增加尤特奇NE 30D的浓度会提高共混物的混溶性、薄膜的柔软度并降低其硬度。在80:20的比例下,聚合物共混物完全互溶,尤特奇L 30D-55以分子形式分布在混合物中。扫描电子显微镜分析证实了这一点。通过扫描电子显微镜对薄膜和微丸在溶出前后的表面形态进行评估。扫描电子显微镜分析表明,在pH 6.8条件下尤特奇L 30D-55溶解后形成的孔隙大小取决于尤特奇共混物的混溶性。这种效应在溶出研究中的影响很明显。对于75:25和80:20的共混物,随着包衣增重从15%增加到120%,滞后时间线性增加至7小时。在增重60%时,80:20的共混物使药物释放延迟约7小时,而混溶性较差的75:25共混物仅使药物释放延迟3.5小时。因此,可以通过控制微丸的理论增重和共混物中尤特奇NE 30D的浓度来控制滞后时间。

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