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用于固体剂型包衣的水性胶体聚合物分散体制备的干、湿纤维素和丙烯酸薄膜的机械性能。

Mechanical properties of dry and wet cellulosic and acrylic films prepared from aqueous colloidal polymer dispersions used in the coating of solid dosage forms.

作者信息

Bodmeier R, Paeratakul O

机构信息

College of Pharmacy, University of Texas at Austin 78712.

出版信息

Pharm Res. 1994 Jun;11(6):882-8. doi: 10.1023/a:1018942127524.

Abstract

The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or water-insoluble), drying or curing conditions, method of film preparation (pseudolatex-vs solvent casting) and ratio of Eudragit RS/RL 30 D in mixed Eudragit RS/RL films. Dry and wet mechanical strengths of the polymeric films depended primarily on the types of the colloidal polymer dispersion and the plasticizer. Films prepared from ethylcellulose dispersions resulted in very weak and brittle films when compared to the acrylic films. Pseudolatex-cast ethylcellulose films showed lower puncture strength and elongation values when compared to those of the solvent-cast films. Curing of the pseudolatex-cast ethylcellulose films had minimal effects on their mechanical properties. Eudragit L 30D, an enteric polymer dispersion, resulted in brittle films in the dry state, but in very flexible films in the wet state because of the plasticization effect of water. Wet Eudragit RS 30 D polymer films plasticized with water-insoluble plasticizers were significantly more flexible than the corresponding wet films plasticized with water-soluble plasticizers. The water-soluble plasticizers leached from the films during exposure to the aqueous medium, while the water-insoluble plasticizers were almost completely retained within the wet films. The low permeability of a water-soluble drug, chlorpheniramine maleate, and the weak mechanical properties of Aquacoat films could suggest osmotic driven/rupturing effects as the release mechanisms from Aquacoat-coated dosage forms.

摘要

通过穿刺试验评估了由各种水性聚合物分散体制备的干、湿聚合物薄膜的机械性能。研究了聚合物分散体类型(纤维素类:Aquacoat和Surelease;丙烯酸类:Eudragit NE、L、RS和RL 30 D)、增塑剂类型(水溶性或水不溶性)、干燥或固化条件、薄膜制备方法(伪胶乳法与溶剂浇铸法)以及Eudragit RS/RL混合薄膜中Eudragit RS/RL 30 D的比例对其的影响。聚合物薄膜的干、湿机械强度主要取决于胶体聚合物分散体和增塑剂的类型。与丙烯酸类薄膜相比,由乙基纤维素分散体制备的薄膜非常脆弱且易碎。与溶剂浇铸薄膜相比,伪胶乳浇铸的乙基纤维素薄膜的穿刺强度和伸长率值较低。伪胶乳浇铸的乙基纤维素薄膜的固化对其机械性能影响极小。肠溶性聚合物分散体Eudragit L 30D在干燥状态下形成易碎薄膜,但在潮湿状态下由于水的增塑作用而形成非常柔韧的薄膜。用水不溶性增塑剂增塑的湿Eudragit RS 30 D聚合物薄膜比用水溶性增塑剂增塑的相应湿薄膜明显更柔韧。水溶性增塑剂在暴露于水性介质期间从薄膜中沥出,而水不溶性增塑剂几乎完全保留在湿薄膜中。水溶性药物马来酸氯苯那敏的低渗透性以及Aquacoat薄膜较弱的机械性能可能表明渗透驱动/破裂效应是Aquacoat包衣剂型的释放机制。

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