Abstract：The low aqueous solubility is the main reason that for most pharmacological active ingredients are challengeable to develop into oral solid formulation. Polymeric amorphous solid dispersion(PASD) can greatly improve the apparent solubility and dissolution rate of poorly soluble drugs, has become a common technology to improve the oral bioavailability of poorly soluble drugs. However, due to the amorphous form of the drug at a high surface free energy in PASD, crystallization would occur during storage and dissolution, thereby losing its formulation advantages. The review attempts to provide a structural development approach of PASD products from the aspects of formulation and technology, in order to guide the development of stable and commercially viable PASD formulations. And the trend analysis of marketed products and patents of PASD will be discussed to understand the prospects of PASD's application in improving the bioavailability of poorly soluble oral solid formulations.
李思佳, 王森怡, 李凌晖, 涂迎盈, 蒋曙光. 基于聚合物无定形固体分散体技术的难溶性药物口服固体制剂开发[J]. 中国药学杂志, 2020, 55(3): 169-176.
LI Si-jia, WANG Sen-yi, LI Ling-hui, TU Ying-ying, JIANG Shu-guang. Development of Oral Solid Formulation for Insoluble Drugs Based on PASD Technology. Chinese Pharmaceutical Journal, 2020, 55(3): 169-176.
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2020, Vol. 55 
