乙胺嘧啶药物的多晶型及性质研究

Study on the Polymorph and Properties of Pyrimethamine

摘要: 采用升华法和重结晶法制备乙胺嘧啶药物的A、B、C三种晶型，通过扫描电镜，XRD和红外光谱对三种多晶型进行表征，采用粉末直接压片法分别制得A、B晶型乙胺嘧啶片剂，对制备的片剂按《中国药典》2015版乙胺嘧啶片中规定的主要项目进行检测。结果表明，乙胺嘧啶药物存在ABC三种晶型。A晶型在280℃时升华转化成B晶型，B晶型乙醇重结晶得到C晶型，证实A和C为同一种晶型，B晶型为另一种晶型。AB晶型的溶解性是有差异的，A晶型略有引湿性，B晶型有引湿性，所制备片剂的重量差异、含量、含量均匀度、溶出度检测结果均符合《中国药典》2015版乙胺嘧啶片标准规定的范围。乙胺嘧啶药物AB两种晶型片剂的溶出曲线相似。

Abstract: In this paper, polymorph of pyrimethamine was studied by using the sublimation and recrystalli-zation of the drug to prepare form A, B and C three types of crystal, which were characterized by SEM, XRD and IR spectra. At the same time, the tablets of three crystals were prepared according to “Chinese Pharmacopoeia” 2015 version for testing, and focused on whether the tablets of the dissolution profile similarity. Form A converted to Form B after sublimation at 280˚C, Form B re-crystallized in ethanol to give crystal Form C. The solubility results show that A crystalline has slightly hygroscopic; B polymorph has hygroscopic. The prepared tablets of Form A and Form B pyrimethamine about content, content uniformity, dissolution test results are in line with the scope of the 2015 edition of Chinese Pharmacopoeia standards. The dissolution curves of Form A and Form B pyrimethamine are similar to each other.