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本文介绍将肠溶衣材料和固体分散技术应用于存有制剂问题的二个药物中。地高辛是一种难溶性并在酸性介质中不稳定的药物。制成固态分散体能降低药物在第一种释放介质(pH1.2)(日本药典第十版)中的溶出速率,并改善了化学稳定性,而在第二种释放介质(pH6.8)中加快溶出并达过饱和。这种技术能提供地高辛胃肠吸收的一种有效剂型。潘生丁是一种难溶性的有机碱,制成固态分散体在酸性介质中溶出受抑制,而在中性或碱性介质中达过饱和。这种剂型吸收缓慢而具有良好的生物利用度。
This article describes the application of enteric coating materials and solid dispersion techniques to two drugs that contain the formulation problem. Digoxin is a poorly soluble drug that is not stable in acidic media. The manufacture of a solid dispersion reduces the dissolution rate of the drug in the first release medium (pH 1.2) (Japanese Pharmacopoeia tenth edition) and improves the chemical stability whereas in the second release medium (pH 6.8) Accelerate dissolution and reach saturation. This technique provides an effective form of gastrointestinal absorption of digoxin. Dipyridamole is a poorly soluble organic base made from solid dispersions that are inhibited from dissolution in acidic media and supersaturated in neutral or alkaline media. This dosage form absorbs slowly and has good bioavailability.