Parmar Komal R, Satapara Vijay P, Shah Sunny R, Sheth Navin R
Department of Pharmaceutical Sciences, Saurashtra University, Rajkot, Gujarat, India.
Pharmazie. 2011 Feb;66(2):119-23.
The aim of the present work was to improve the dissolution characteristics of the poorly water soluble antiepileptic drug lamotrigine (LMN) by inclusion complexation using hydroxy propyl beta-cyclodextrin (HP beta-CD) by co-evaporation technique and by, solid dispersion, prepared by the melt method using poloxamer 407 (L 127). Phase solubility studies showed AL type curves with both the carriers. Dissolution of LMN was significantly improved (p < 0.05) by inclusion complexation and solid dispersion preparation. Results of solid state characterization performed by Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry and Powder X-ray Diffractrometry techniques revealed a decrease in the crystallinity of LMN that might be accounting for improvement in the dissolution properties as seen from dissolution studies.
本研究的目的是通过共蒸发技术使用羟丙基-β-环糊精（HPβ-CD）以及通过采用泊洛沙姆407（L127）的熔融法制备固体分散体，通过包合络合来改善难溶性抗癫痫药物拉莫三嗪（LMN）的溶出特性。相溶解度研究表明两种载体均呈现AL型曲线。通过包合络合和固体分散体制备，LMN的溶出度得到显著提高（p<0.05）。通过傅里叶变换红外光谱、差示扫描量热法和粉末X射线衍射技术进行的固态表征结果显示，LMN的结晶度降低，这可能是从溶出度研究中观察到的溶出性能改善的原因。
