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奋乃静/羟丙基-β-环糊精包合物口腔崩解片的研制。

Development of orally disintegrating tablets of Perphenazine/hydroxypropyl-β-cyclodextrin inclusion complex.

机构信息

Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, PR China.

出版信息

Pharm Dev Technol. 2013 Sep-Oct;18(5):1101-10. doi: 10.3109/10837450.2012.700932. Epub 2012 Jul 3.

Abstract

The aim of the present work was to prepare perphenazine (PPZ) orally disintegrating tablets (ODTs) based on the use of hydroxypropyl-β-cyclodextrin (HP-β-CD) forming inclusion complex with PPZ to improve the solubility and dissolution of this practically insoluble drug. Phase solubility studies were performed to evaluate the complexation of PPZ with HP-β-CD in three aqueous systems. The inclusion complex prepared by evaporation method was characterized by different physicochemical techniques, including the dissolution studies. The prepared complex was incorporated into ODTs containing different fillers and disintegrants. The ODTs prepared by direct compression were evaluated for drug content, hardness, porosity, friability, in vitro disintegration time (DT), wetting time (WT) and dissolution profiles. The solubility and dissolution rate were substantially improved compared with that of PPZ. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR) analyses suggested that PPZ could form true inclusion complex with HP-β-CD. The optimized formulation F6 exhibited short DT (15.5 ± 1.9 s) and WT (34.2 ± 2.3 s), sufficient hardness (30.4 ± 1.6 N/mm) and rapid drug dissolution. The developed tablet formulation could be a promising drug delivery system with improvements in PPZ bioavailability and patient compliance.

摘要

本工作旨在制备盐酸苯海拉明(PPZ)口崩片(ODTs),方法是使用羟丙基-β-环糊精(HP-β-CD)与 PPZ 形成包合络合物,以提高该实际难溶性药物的溶解度和溶出度。通过相溶解度研究评估了 PPZ 在三种水体系中与 HP-β-CD 的络合作用。通过蒸发法制备的包合物采用不同的物理化学技术进行了表征,包括溶解研究。将制备的包合物掺入含有不同赋形剂和崩解剂的 ODT 中。通过直接压片制备的 ODT 进行了药物含量、硬度、孔隙率、脆碎度、体外崩解时间(DT)、润湿时间(WT)和溶解曲线评价。与 PPZ 相比,溶解度和溶解速率得到了显著提高。差示扫描量热法(DSC)、X 射线粉末衍射(XRD)和傅里叶变换红外光谱(FTIR)分析表明,PPZ 可以与 HP-β-CD 形成真正的包合络合物。优化的配方 F6 表现出较短的 DT(15.5±1.9 s)和 WT(34.2±2.3 s)、足够的硬度(30.4±1.6 N/mm)和快速的药物溶解。所开发的片剂制剂可能是一种有前途的药物传递系统,可提高 PPZ 的生物利用度和患者顺应性。

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