Abstract:
Well-controlled crystallization of the API�s (Active Pharmaceutical Ingredients) is often an important factor in pharmaceuticalindustries. The development of new crystallization methods to design the products with specific physico-chemical propertiesis a complex and challenging issue. This existing challenge impetus us to explore the possible ways to control thecrystallization of gefitinib. Gefitinib, [N-(3-chloro-4-fluro-phenyl)-7-methoxy-6-(3-morpholin-4-yl propoxy) quinazolin-4-amine] is an anticancer drug used in the treatment of non-small cell lung cancer. Gefitinib exists in five polymorphic forms (i)anhydrous (ii) solvate of MeOH (iii) solvate of DMSO, (iv) monohydrate and (v) trihydrate forms. Each polymorph hasdifferent physical properties and leads to large variation in the biopharmaceutical performance. The bioavailability of puregefitinib is low and there is a need to enhance the solubility. With this regard, our aim is to isolate the more specificcrystalline polymorph of gefitinib and to enhance the solubility of the preferred form. Here we present, the effect of selectiveamino acids used for co-crystallization with gefitinib and the results will be discussed in detail.