吡罗昔康的晶型转变和溶出速率。
Crystal modifications and dissolution rate of piroxicam.
机构信息
School of Pharmacy and Health Sciences, International Medical University, Bukit Jalil, Kuala Lumpur, Malaysia.
出版信息
Acta Pharm. 2011 Dec;61(4):391-402. doi: 10.2478/v10007-011-0037-z.
Piroxicam is a nonsteroidal anti-inflammatory drug with low aqueous solubility which exhibits polymorphism. The present study was carried out to develop polymorphs of piroxicam with enhanced solubility and dissolution rate by the crystal modification technique using different solvent mixtures prepared with PEG 4000 and PVP K30. Physicochemical characteristics of the modified crystal forms of piroxicam were investigated by X-ray powder diffractometry, FT-IR spectrophotometry and differential scanning calorimetry. Dissolution and solubility profiles of each modified crystal form were studied and compared with pure piroxicam. Solvent evaporation method (method I) produced both needle and cubic shaped crystals. Slow crystallization from ethanol with addition of PEG 4000 or PVP K30 at room temperature (method II) produced cubic crystal forms. Needle forms produced by method I improved dissolution but not solubility. Cubic crystals produced by method I had a dissolution profile similar to that of untreated piroxicam but showed better solubility than untreated piroxicam. Cubic shaped crystals produced by method II showed improved dissolution, without a significant change in solubility. Based on the XRPD results, modified piroxicam crystals obtained by method I from acetone/benzene were cube shaped, which correlates well with the FTIR spectrum; modified needle forms obtained from ethanol/methanol and ethanol/acetone showed a slight shift of FTIR peak that may be attributed to differences in the internal structure or conformation.
吡罗昔康是非甾体抗炎药，水溶性低，存在多晶型现象。本研究采用 PEG4000 和 PVP K30 制备的不同溶剂混合物的晶体修饰技术，旨在开发具有增强溶解性和溶解速率的吡罗昔康多晶型物。采用 X 射线粉末衍射法、FT-IR 分光光度法和差示扫描量热法对修饰后的吡罗昔康晶体形式的物理化学特性进行了研究。对各修饰晶体形式的溶解和溶解度曲线进行了研究，并与纯吡罗昔康进行了比较。溶剂蒸发法（方法 I）产生了针状和立方状晶体。从室温下加入 PEG4000 或 PVP K30 的乙醇中缓慢结晶（方法 II）产生了立方晶型。方法 I 产生的针状形式改善了溶解度，但没有提高溶解度。方法 I 产生的立方晶体的溶解曲线与未处理的吡罗昔康相似，但溶解度优于未处理的吡罗昔康。方法 II 产生的立方状晶体的溶解度得到了改善，而溶解度没有明显变化。根据 X 射线粉末衍射结果，方法 I 从丙酮/苯中获得的修饰吡罗昔康晶体为立方形状，这与 FTIR 光谱很好地吻合；从乙醇/甲醇和乙醇/丙酮中获得的修饰针状形式显示出 FTIR 峰的轻微偏移，这可能归因于内部结构或构象的差异。
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