Department of Drug Sciences, University of Pavia, Viale Taramelli 12, Pavia 27100, Italy.
Department of Chemistry, Physical Chemistry Section, University of Pavia, Viale Taramelli 16, Pavia 27100, Italy.
J Pharm Sci. 2018 Jan;107(1):507-511. doi: 10.1016/j.xphs.2017.06.001. Epub 2017 Jun 15.
The purpose of this investigation is to determine how the dissolution media may influence the release rate of an insoluble drug in in vitro conditions. Some oral dosage forms containing ibuprofen, a molecule that shows pH-dependent solubility, are tested. They are evaluated in different media to simulate the gastrointestinal transit at paddle rotation speeds of 50 and 100 rpm. Moreover, the potential effect of different ethanol concentrations on drug release is tested. The dissolution profiles of the tablets show a similar behavior in water (pH 1.0) and phosphate buffer (pH 4.5) where the 2 doses are not completely dissolved. The soft capsules show a different behavior: a certain amount of ibuprofen, which is in solution inside the capsule, reprecipitates in water and in the pH 4.5 buffer. Instead, ibuprofen dissolves rapidly in the pH 6.8 buffer from all the formulations. In the water-ethanol solutions, the dissolution curves show a valuable increase in the drug dissolved at higher ethanol concentrations.
本研究旨在确定溶解介质如何影响难溶性药物在体外条件下的释放速率。本文对含有布洛芬的一些口服剂型进行了测试，布洛芬是一种具有 pH 依赖性溶解度的分子。这些剂型在不同的介质中进行评估，以模拟桨叶转速为 50 和 100 rpm 时的胃肠道转运。此外，还测试了不同乙醇浓度对药物释放的潜在影响。片剂的溶解曲线在水（pH 1.0）和磷酸盐缓冲液（pH 4.5）中表现出相似的行为，其中两种剂量都没有完全溶解。软胶囊表现出不同的行为：胶囊内处于溶液状态的一定量布洛芬在水和 pH 4.5 缓冲液中重新沉淀。相反，所有配方中的布洛芬在 pH 6.8 缓冲液中迅速溶解。在水-乙醇溶液中，随着乙醇浓度的升高，溶解的药物曲线显示出有价值的增加。
