A New Protocol To Determine the Solubility of Drugs into Polymer Matrixes
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- 作者：Aur茅lien Mahieu ; Jean-Fran莽ois Willart ; Emeline Dudognon ; Florence Dan猫de ; Marc Descamps
- 刊名：Molecular Pharmaceutics
- 出版年：2013
- 出版时间：February 4, 2013
- 年：2013
- 卷：10
- 期：2
- 页码：560-566
- 全文大小：317K
- 年卷期：v.10,no.2(February 4, 2013)
- ISSN：1543-8392
文摘
In this paper we present a new protocol to determine faster the solubility of drugs into polymer matrixes. The originality of the method lies in the fact that the equilibrium saturated states are reached by demixing of supersaturated amorphous solid solutions and not by dissolution of crystalline drug into the amorphous polymer matrix as for usual methods. The equilibrium saturated states are thus much faster to reach due to the extra molecular mobility resulting from the strong plasticizing effect associated with the supersaturation conditions. The method is validated using the indomethacin/polyvinylpyrrolidone mixture whose solubility diagram was previously determined by usual techniques. The supersaturated states have been directly obtained in the solid state by comilling, and the investigations have been performed by differential scanning calorimetry and powder X-ray diffraction.