水溶性聚合物对水性聚合物分散体物理稳定性的影响及其对包衣丸剂药物释放的影响。
Effect of water-soluble polymers on the physical stability of aqueous polymeric dispersions and their implications on the drug release from coated pellets.
机构信息
Freie Universität Berlin, Berlin, Germany.
出版信息
Drug Dev Ind Pharm. 2010 Feb;36(2):152-60. doi: 10.3109/03639040903410334.
PURPOSE
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.
METHODS
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.
RESULTS
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.
CONCLUSIONS
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.
目的
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。
方法
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。
结果
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。
结论
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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