作者
Korbinian Löbmann, Holger Grohganz, Riikka Laitinen, Clare Strachan, Thomas Rades
发表日期
2013/11/1
期刊
European journal of pharmaceutics and biopharmaceutics
卷号
85
期号
3
页码范围
873-881
出版商
Elsevier
简介
Poor aqueous solubility of an active pharmaceutical ingredient (API) is one of the most pressing problems in pharmaceutical research and development because up to 90% of new API candidates under development are poorly water soluble. These drugs usually have a low and variable oral bioavailability, and therefore an unsatisfactory therapeutic effect. One of the most promising approaches to increase dissolution rate and solubility of these drugs is the conversion of a crystalline form of the drug into its respective amorphous form, usually by incorporation into hydrophilic polymers, forming glass solutions. However, this strategy only led to a small number of marketed products usually because of inadequate physical stability of the drug (crystallization). In this study, we investigated a fundamentally different approach to stabilize the amorphous form of drugs, namely the use of amino acids as small molecular weight …
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K Löbmann, H Grohganz, R Laitinen, C Strachan… - European journal of pharmaceutics and …, 2013