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Solubility parameters of hypromellose acetate succinate and plasticization in dry coating procedures

增塑剂 三醋酸甘油酯 溶解度 涂层 涂膜 聚乙二醇 聚乙烯醇 化学 甘油 材料科学 化学工程 肠衣 有机化学 工程类
作者
Fabian Klar,Nora Anne Urbanetz
出处
期刊:Drug Development and Industrial Pharmacy [Taylor & Francis]
卷期号:42 (10): 1621-1635 被引量:30
标识
DOI:10.3109/03639045.2016.1160106
摘要

Solubility parameters of HPMCAS have not yet been investigated intensively. On this account, total and three-dimensional solubility parameters of HPMCAS were determined by using different experimental as well as computational methods. In addition, solubility properties of HPMCAS in a huge number of solvents were tested and a Teas plot for HPMCAS was created. The total solubility parameter of about 24 MPa(0.5) was confirmed by various procedures and compared with values of plasticizers. Twenty common pharmaceutical plasticizers were evaluated in terms of their suitability for supporting film formation of HPMCAS under dry coating conditions. Therefore, glass transition temperatures of mixtures of polymer and plasticizers were inspected and film formation of potential ones was further investigated in dry coating of pellets. Contact angles of plasticizers on HPMCAS were determined in order to give a hint of achievable coating efficiencies in dry coating, but none was found to spread on HPMCAS. A few common substances, e.g. dimethyl phthalate, glycerol monocaprylate, and polyethylene glycol 400, enabled plasticization of HPMCAS; however, only triethyl citrate and triacetin were found to be suitable for use in dry coating. Addition of acetylated monoglycerides to triacetin increased coating efficiency, which was likewise previously demonstrated for triethyl citrate.
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