Kala H, Traue J, Moldenhauer H, Zessin G
Pharmazie. 1981;36(2):106-11.
Spray drying of phenobarbital-polyvinyl pyrrolidone (PVP), phenobarbital-polyvinyl alcohol (PVA) and digoxin-PVP solutions yielded embeddings in the form of very fine powders. Depending on the drug-adjuvant ratio, the form in which the drug was embedded in the indifferent carriers was microcrystalline to radio-amorphous. In vitro studies showed that the dissolution of all the spray products was more rapid than that of the corresponding physical mixtures, and that the resulting solutions of the respective drugs were always oversaturated. The oversaturated solutions obtained from embeddings containing the amorphous forms of the difficulty soluble drugs were relatively stable. PVP inhibited the crystallization of phenobarbital to a greater extent than PVA, and led to a higher oversaturation of the drug in the resulting solutions. The in vitro release of digoxin was significantly more rapid from PVP embeddings (and tablets made from them) than from products containing digoxin in crystalline form.
对苯巴比妥 - 聚乙烯吡咯烷酮(PVP)、苯巴比妥 - 聚乙烯醇(PVA)和地高辛 - PVP溶液进行喷雾干燥,得到了极细粉末形式的包埋物。根据药物 - 辅料比例,药物在惰性载体中的包埋形式从微晶态到无定形态不等。体外研究表明,所有喷雾产品的溶出速度均比相应物理混合物更快,且各药物的所得溶液始终处于过饱和状态。从含有难溶性药物无定形形式的包埋物中获得的过饱和溶液相对稳定。PVP比PVA更能抑制苯巴比妥的结晶,并导致所得溶液中药物的过饱和度更高。地高辛从PVP包埋物(以及由其制成的片剂)中的体外释放速度明显快于含有结晶形式地高辛的产品。