Oral self emulsifying powder of lercanidipine hydrochloride: Formulation and evaluation
Oral self emulsifying powder of lercanidipine hydrochloride: Formulation and evaluation
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DOI：
10.1016/j.powtec.2012.01.032
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发表时间：
2012-05-01
影响因子：
5.2
通讯作者：
Veerareddy, Prabhakar Reddy
中科院分区：
文献类型：
--
作者：
Kallakunta, Venkata Raman;Bandari, Suresh;Veerareddy, Prabhakar Reddy
对难溶性盐酸乐卡地平自乳化粉剂进行了增溶研究。筛选了各种载体，以Capmul MCM L 8为油，Tween（R）80为表面活性剂，PEG 400为助表面活性剂配制了LCH的液体SEDDS。对制备的处方进行了自乳化能力评价，并绘制了相图以优化体系。这些系统进一步表征了小球大小、pH值的影响和对稀释的稳健性、浊点、热力学稳定性、表面形态和药物释放。该系统对不同pH介质和稀释体积具有耐用性。优化的体系具有169 +/- 06 nm的平均球尺寸和76 ℃的浊点。以纽斯林为载体，将液体自乳化给药系统（SEDDS）吸附于载体上，制备自乳化粉末。所配制的SEP是自由流动的，具有与液体SEDDS相似的乳化特性。对SEP的X射线衍射、差示扫描量热分析表明，由于LCH在SEDDS中的溶解状态，使其晶体结构发生了变化。扫描电子显微镜进一步证实了这一点。与纯药物相比，SEP的高溶出效率值表明SEP中LCH的溶出特性增加。（c）2012 Elsevier B. V.保留所有权利。
The current investigation was aimed to improve the solubility of poorly soluble lercanidipine hydrochloride as self emulsifying powder (SEP). Liquid SEDDS of LCH was formulated with Capmul MCM L8 as oil, Tween (R) 80 as surfactant and PEG 400 as co surfactant after screening various vehicles. The prepared formulations were evaluated for self emulsifying ability and phase diagram was constructed to optimize the system. These systems were further characterized for globule size, effect of pH and robustness to dilution, cloud point, thermodynamic stability, surface morphology and drug release. The system was robust to different pH media and dilution volumes. The optimized system possessed a mean globule size of 169 +/- 06 nm and cloud point of 76 degrees C. The self emulsifying powder was prepared by adsorbing the liquid SEDDS on to neusilin as carrier. The SEP formulated was free flowing with similar emulsification characteristics as that of liquid SEDDS. The X-ray diffraction, Differential Scanning Calorimetric studies of SEP revealed transformation of crystalline structure of LCH because of its molecularly dissolved state in the liquid SEDDS. This was further confirmed by scanning electron microscopy. High dissolution efficiency value of SEP compared with pure drug indicated the increase in dissolution characteristics of LCH in SEP. (c) 2012 Elsevier B.V. All rights reserved.