吡罗昔康原料晶型对片剂溶出度的影响研究

Characterization of crystal form of piroxicam and its impacts on dissolution in tablets

目的:研究吡罗昔康原料及其在片剂中的晶型特征,并探讨不同晶型对吡罗昔康原料、片剂溶出度的影响。方法:通过差示扫描量热分析(DSC)、傅里叶红外光谱(FTIR)、粉末X射线衍射谱(PXRD)测定吡罗昔康原料的晶型;通过近红外光谱(NIR)使用相关系数模型快速筛查吡罗昔康片的原料晶型;使用光纤溶出仪测定不同晶型原料的固有溶出速率及不同晶型原料片剂的溶出度。结果:目前市场上吡罗昔康原料主要存在2种晶型;不同晶型的吡罗昔康原料固有溶出速率存在差异,不同原料晶型片剂溶出度亦有一定差异。结论:吡罗昔康PⅡ晶型与PⅠ晶型相比,溶出行为更优,晶型的测定为吡罗昔康的质量控制提供了科学依据。

Objective：To investigate the polymorphic forms of piroxicam and its influence of polymorphism on dissolution proflie in tablets.Methods：The crystal forms of piroxicam were measured and analyzed by differential scanning calorimeter（DSC）,Fourier transform infrared spectroscopy（FTIR）and X-ray powder diffractometer（PXRD）;the correlation coefficient model was applied for rapid screening of the crystal form of API in piroxicam tablets by near-infrared spectroscopy（NIR）;the intrinsic dissolution rates of different crystal forms of piroxicam as well as the dissolution rates of piroxicam tablets were investigated.Results：Two different crystal forms of piroxicam were observed;differences of intrinsic dissolution rate and dissolution rate of tablets between various polymorphic forms were confirmed.Conclusion：Piroxicam of polymorphic form P Ⅱ has better solubility compared with the from P Ⅰ,and crystal form investigation provide a scientific evidence for the specification setting of piroxicam and dosage forms.