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本文介绍Difenoxin盐酸盐{1-(3-氰基-3,3-二苯基-丙基)-4-苯基异哌啶酸-[3]盐酸盐}的多晶型研究的实验方法。经红外光谱测定,晶型I的含量与透光率呈直线关系。又经溶解度试验表明,晶型I的溶解度比晶型II大,而该药的游离碱基的溶解度比其盐的两种晶型的溶解度都小。晶型I的含量增加,最大溶解度也增加。从溶出结果表明,该法能灵敏地区分多晶型含量的较大差异,但其关系是非线性的。晶粒的微粉化可增加片剂的溶出量。实验将Difenoxin盐酸盐用不同的结晶方法分别制得晶型I和晶型II的纯品,用X-线衍射法来鉴别。
This article describes the experimental study of the polymorphism of Difenoxin hydrochloride {1- (3-cyano-3,3-diphenyl-propyl) -4-phenylpipipronoic acid- [3] hydrochloride} method. After the determination by infrared spectroscopy, the content of crystal form I has a linear relationship with the light transmittance. Solubility tests show that the solubility of Form I is greater than that of Form II, and the free base of the drug has a lower solubility than both of its salt forms. Form I increased, the maximum solubility also increased. From the dissolution results show that this method can be sensitive to distinguish between the larger differences in polymorph content, but the relationship is non-linear. Micronization of the grains increases the dissolution of the tablets. Difenoxin hydrochloride was prepared by different crystallization methods to obtain the pure products of Form I and Form II, respectively, and identified by X-ray diffraction.