依托昔布增强溶出的磺基丁醚-β-环糊精包合物的研制与评价

Q2 Pharmacology, Toxicology and Pharmaceutics
M. Nagpal, Vivekanand Vishvakarma, Malkiet Kaur, P. Maman
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引用次数: 0

摘要

Etoricoxib是BCS II类药物,水溶性差,具有镇痛和抗炎特性。环糊精络合是一种广泛使用的方法,用于提高药物的溶解度和生物利用度。在目前的研究工作中,使用捏合、蒸发和冷冻干燥方法制备了使用环糊精改性形式的依托里考昔包合物,即标题溶胶,以提高溶解度和溶解特性。Etoricoxib包合物(比例为1:1)采用捏合、蒸发和冷冻干燥方法配制。对所配制的包合物的相溶解度、平衡溶解度研究、傅立叶变换红外光谱、粉末X射线衍射、扫描电子显微镜、差示扫描量热法研究、体外药物释放、相似因子和体内研究进行了评估。冷冻干燥法产生的包合物具有最高的平衡溶解度(是纯药物的十倍)。傅立叶变换红外光谱研究显示没有药物-聚合物相互作用。差示扫描量热法和扫描电子显微镜研究表明,该药物被掺入环糊精的包合物中。捏合法、蒸发法和冻干法包合物的体外溶出度研究显示,在3h内药物释放率分别为66.53%、79.13%和88%,而纯药物在3h内释放率为61.77%。获得的f1值小于50,这表明捏合的释放特性存在显著差异,蒸发和冷冻干燥方法。体内研究表明,与揉捏和蒸发法制备的制剂相比,冷冻干燥法制备的包合物显示出更好的镇痛和抗炎作用。结果表明,与捏合法和蒸发法制备的制剂相比,冷冻干燥法制备出的制剂显著提高了依托里昔的溶出度和溶解度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and evaluation of sulfobutylether-β-cyclodextrin inclusion complexes of etoricoxib for enhancing dissolution
Etoricoxib is a BCS class II drug with poor aqueous solubility and analgesic and anti-inflammatory properties. Complexation with cyclodextrins is one of the widely used methods, amongst others, for enhancing the solubility and bioavailability of drugs. In current research work, inclusion complexes of etoricoxib using modified forms of cyclodextrin, i.e., captisol were prepared using kneading, evaporation, and freeze-drying methods to improve the solubility and dissolution characteristics. Etoricoxib inclusion complexes (ratio 1:1) were formulated using kneading, evaporation, and freeze-drying methods. The formulated inclusion complexes were evaluated for phase solubility, equilibrium solubility studies, Fourier transform infrared spectroscopy, powder X-ray diffraction, scanning electron microscopy, differential scanning calorimetry studies, in vitro drug release, similarity factor and in vivo studies. The freeze-drying method produced inclusion complexes with the highest equilibrium solubility (ten times that of the pure drug). Fourier transform infrared spectroscopy studies showed no drug-polymer interaction. Differential scanning calorimetry and scanning electron microscopy studies suggested the incorporation of the drug into inclusion complexes of cyclodextrin. In vitro dissolution studies of kneading, evaporation and freeze-drying method inclusion complexes showed 66.53%, 79.13% and 88% drug release, respectively, in 3h, whereas pure drug exhibited 61.77% drug release in 3 h. The f1 value obtained was less than 50, which is indicative of a significant difference in release characteristics of kneading, evaporation and freeze-drying methods with that of the marketed formulation. In vivo studies indicated that inclusion complexes formulated by the freeze-drying method showed better analgesic and anti-inflammatory effects in comparison to formulations prepared by kneading and evaporation methods. It is concluded that the formulation prepared by the freeze-drying method led to a significant enhancement of dissolution and solubility rate of etoricoxib in comparison to the formulation prepared by the kneading method and evaporation method.
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来源期刊
Current Bioactive Compounds
Current Bioactive Compounds Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.90
自引率
0.00%
发文量
112
期刊介绍: The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.
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