Impact of Swelling of Spray Dried Dispersions in Dissolution Media on their Dissolution: An Investigation Based on UV Imaging

溶解 肿胀 的 聚合物 羟丙基纤维素 化学 化学工程 溶解试验 溶解度 膨胀能力 色谱法 卵磷脂 材料科学 核化学 有机化学 生物制药分类系统 工程类
作者
Jinjiang Li,Christopher A. Zordan,Steven Ponce,Xujin Lu
出处
期刊:Journal of Pharmaceutical Sciences [Elsevier BV]
卷期号:111 (6): 1761-1769 被引量:1
标识
DOI:10.1016/j.xphs.2021.12.007
摘要

Impact of SDD-dissolution medium interactions on the swelling and dissolution of spray dried dispersions (SDDs) was investigated using UV imaging by monitoring SDD swelling in situ, along with correlating of the swelling with the micro-dissolution and intrinsic dissolution of SDDs. SDDs of ketoconazole or indomethacin with three polymers: polyvinylpyrrolidone (PVP), hydroxypropyl cellulose (HPC), and hydroxypropyl methylcellulose acetate succinate (HPMC-AS) were prepared for the study. Dissolution media employed for assessing swelling and dissolution include water, acetate buffer, phosphate buffer, fasted state simulated intestinal fluid (FaSSIF), and fed state simulated intestinal fluid (FeSSIF), in which influence of polymers and drugs together with the physical-chemical properties of dissolution media (pH, and the presence of sodium taurocholate and lecithin) on SDD swelling and dissolution was evaluated. It appears that hydrophilic and hydrophobic properties of polymers can significantly impact SDD swelling and thus the dissolution. Furthermore, properties of dissolution media such as pH as well as presence of bile salts and lecithin seems to affect SDD swelling and dissolution as well. Throughout the text, thermodynamic swelling of polymers was used to interpret SDD dissolution behavior. Finally, practical implication of polymer swelling on dissolution was discussed.

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