Marvola M, Hannula A M, Ojantakanen S, Westermarck E, Rajamäki M
Acta Pharm Nord. 1989;1(6):355-62.
The release of drugs from hard gelatin capsules is often limited by the disintegration rate of the capsule. We set out to determine whether it is possible to hasten the in vivo disintegration of hard gelatin capsules by adding disintegrants (sodium bicarbonate or sodium starch glycolate) to the formulation. This radiological study was carried out in six beagle dogs. We conclude that if rapid disintegration is desired for a hard gelatin capsule formulation, water-soluble diluents should primarily be selected. Sparingly water-soluble, gelforming diluents cause slow in vivo disintegration. Using swellable disintegrants such as sodium starch glycolate does not accelerate disintegration and may even retard it. With sodium bicarbonate it is possible to shorten the disintegration time of capsules containing water-insoluble ingredients, but not to the extent possible with water-soluble diluents.
硬明胶胶囊中药物的释放通常受胶囊崩解速率的限制。我们着手研究通过在制剂中添加崩解剂（碳酸氢钠或羟丙基淀粉钠）是否有可能加速硬明胶胶囊在体内的崩解。这项放射学研究在六只比格犬身上进行。我们得出结论，对于硬明胶胶囊制剂而言，如果希望快速崩解，应主要选择水溶性稀释剂。微溶性的成胶稀释剂会导致体内崩解缓慢。使用诸如羟丙基淀粉钠之类的可膨胀崩解剂不会加速崩解，甚至可能会延缓崩解。使用碳酸氢钠可以缩短含有水不溶性成分的胶囊的崩解时间，但无法达到使用水溶性稀释剂时可能达到的程度。
