Freie Universität Berlin, Berlin, Germany.
Drug Dev Ind Pharm. 2010 Feb;36(2):152-60. doi: 10.3109/03639040903410334.
To investigate the physical stability and drug release-related properties of the aqueous polymer dispersions Kollicoat((R)) SR 30 D and Aquacoat((R)) ECD (an ethylcellulose-based dispersion) in the presence water-soluble polymers (pore formers) with special attention to the potential flocculation of the polymer dispersions.
A precise characterization of the flocculation phenomena in undiluted samples was monitored with turbidimetric measurements using the Turbiscan Lab-Expert. Theophylline or propranolol HCl drug-layered pellets were coated with Kollicoat((R)) SR 30 D and Aquacoat((R)) ECD by the addition of water-soluble polymers polyvinyl pyrrolidone (Kollidon((R)) 30 and 90 F), polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat((R)) IR), and hydroxypropyl methylcellulose (Pharmacoat((R)) 603 or 606) in a fluidized bed coater Glatt GPCG-1 and drug release was performed according to UPS paddle method.
Stable dispersions were obtained with both Kollicoat((R)) SR 30 D (a polyvinyl acetate-based dispersion) and Aquacoat((R)) ECD with up to 50% hydrophilic pore formers polyvinyl alcohol-polyethylene glycol graft copolymer (Kollicoat((R)) IR) and polyvinyl pyrrolidone (Kollidon((R)) 30). In general, Kollicoat((R)) SR 30 D was more stable against flocculation than Aquacoat((R)) ECD. Stable dispersions were also obtained with higher amounts of water-soluble polymer or by reducing the concentration of the polymer dispersion. Flocculated dispersions resulted in porous films and, thus, in a sharp increase in drug release.
Kollicoat((R)) SR 30 D was more resistant to flocculation upon addition of water-soluble polymers than Aquacoat((R)) ECD. The continuous adjustment of drug release from Kollicoat((R)) SR 30-coated pellets was possible with Kollicoat((R)) IR amounts over a broad range.
研究水性聚合物分散体 Kollicoat((R)) SR 30 D 和 Aquacoat((R)) ECD（一种乙基纤维素分散体）在水溶性聚合物（成孔剂）存在下的物理稳定性和药物释放相关性质，并特别关注聚合物分散体的潜在絮凝。
使用 Turbiscan Lab-Expert 浊度测量法精确监测未稀释样品中絮凝现象。通过在流化床包衣机 Glatt GPCG-1 中添加水溶性聚合物聚乙烯吡咯烷酮（Kollidon((R)) 30 和 90 F）、聚乙烯醇-聚乙二醇接枝共聚物（Kollicoat((R)) IR）和羟丙基甲基纤维素（Pharmacoat((R)) 603 或 606），将茶碱或盐酸普萘洛尔层状丸剂包衣用 Kollicoat((R)) SR 30 D 和 Aquacoat((R)) ECD 包衣，并根据 UPS 桨法进行药物释放。
Kollicoat((R)) SR 30 D（一种醋酸乙烯酯基分散体）和 Aquacoat((R)) ECD 均可获得稳定的分散体，最高可添加 50%亲水性成孔剂聚乙烯醇-聚乙二醇接枝共聚物（Kollicoat((R)) IR）和聚乙烯吡咯烷酮（Kollidon((R)) 30）。一般来说，Kollicoat((R)) SR 30 D 比 Aquacoat((R)) ECD 更能抵抗絮凝。通过添加更多的水溶性聚合物或降低聚合物分散体的浓度，也可以获得稳定的分散体。絮凝的分散体导致多孔膜，从而导致药物释放急剧增加。
与 Aquacoat((R)) ECD 相比，添加水溶性聚合物时，Kollicoat((R)) SR 30 D 更能抵抗絮凝。通过在广泛的范围内添加 Kollicoat((R)) IR 量，可以对 Kollicoat((R)) SR 30 包衣丸剂的药物释放进行连续调整。
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