Khalafalla N
Pharmazie. 1980;35(9):555-8.
An in vitro dissolution rate test was developed for possible use in formulation design and control of griseofulvin tablets. Dissolution profiles of five brands of griseofulvin tablets were obtained using a two-phase system consisting essentially of a 11 three-necked round-bottom flask. Appropriate sink conditions in the aqueous phase were maintained by means of an upper organic phase composed of a mixture of equal parts of benzene and chlorobenzene. The dissolution media tested were 0.02% polysorbate 80 in water (pH = 6--7), sodium desoxycholate (10 mmol/1) in water (pH = 7.2) and 0.02% polysorbate 80 in HCl (0.1 mol/l, pH = 2). Interbrand differences in dissolution were better seen in neutral medium containing the non-ionic surfactant. Reduced deaggregation tendencies of griseofulvin in acid medium and unfavourable partitioning conditions in the presence of bile salt masked the differences in dissolution in the other two media. Dissolution profiles obtained under sink conditions could be characterized by rate constants.
开发了一种体外溶出速率试验,可能用于灰黄霉素片的制剂设计和质量控制。使用一个主要由三颈圆底烧瓶组成的两相系统,获得了五个品牌灰黄霉素片的溶出曲线。通过由等份苯和氯苯混合物组成的上层有机相,在水相中维持适当的漏槽条件。所测试的溶出介质为水中0.02%聚山梨酯80(pH = 6 - 7)、水中脱氧胆酸钠(10 mmol/L,pH = 7.2)和HCl(0.1 mol/L,pH = 2)中的0.02%聚山梨酯80。在含有非离子表面活性剂的中性介质中,品牌间的溶出差异更明显。灰黄霉素在酸性介质中解聚趋势降低,以及在胆盐存在下不利的分配条件,掩盖了在其他两种介质中的溶出差异。在漏槽条件下获得的溶出曲线可用速率常数来表征。