Discriminatory Dissolution Test for Tablets Containing alpha- and beta-Thalidomide Polymorphs

作者：Cappra Silva Ana Paula; Meneghini Leonardo Zanchetti; Bajerski Lisiane; Carini Juliana Poglia; Fialho Silvia Ligorio; Mayorga Paulo; Froeehlich Pedro Eduardo

来源：Dissolution Technologies, 2013, 20(1): 19-25.

Over the years, thalidomide has been prescribed for an increasing number of diseases, including multiple myeloma and erythema nodosum leprosum. In Brazil and other countries, thalidomide is available in tablets, and there is no official dissolution testing available for this dosage form. Considering this, a dissolution method was developed and validated for tablets containing 100 mg of each polymorph using 1-L vessels to verify that it can differentiate between polymorphs, since drug product is supposed to be formulated with the alpha form. In addition, the possibility of using smaller volumes of dissolution medium was also explored.
This method was compared with the USP dissolution method for thalidomide capsules (4-L vessel) with independent models using difference and similarity factors as well as dissolution efficiency. Dissolution kinetics was evaluated using zero-order, first-order, Higuchi, and Korsmeyer-Peppas models. The kinetic parameters and the suitability of the models for experimental data were evaluated. The developed dissolution method was fully validated. It allowed a better discrimination of thalidomide polymorphs than the USP method for the formulations tested. Considering that it uses a conventional dissolution apparatus with 1-L vessels and there is no method described for tablets, it can be used for quality control of thalidomide in this dosage form.

• 出版日期2013-2