摘要
目的研究美洛昔康纳米骨架胶囊的溶出行为与体内药代动力学特征,初步进行体内、体外相关性考察。方法以市售美洛昔康片(莫比可)作为对照品,采用《中国药典》2015年版溶出度测定第二法,测定2种制剂在不同pH介质中的溶出曲线;并以比格犬为实验动物,进行两者药代动力学对比研究,用DAS2.0软件计算药动学参数。结果美洛昔康纳米骨架胶囊在4种介质中30 min的溶出度均大于80%,高于莫比可;比格犬药代动力学研究表明,与莫比可相比,美洛昔康纳米骨架胶囊药物达峰浓度(C max)提高1.461倍,药时曲线下面积(AUC 0~t)提高1.319倍。结论美洛昔康纳米骨架胶囊体外溶出度与比格犬体内生物利用度均有显著提高,具有一定的体内外相关性,为未来将其开发为改良型新药提供依据。
Objective To study the in vitro dissolution and the pharmacokinetics of Nano-matrix Meloxicam Capsules and to preliminarily investigate the in vivo and in vitro correlation.Methods By taking commercially available Meloxicam Tablets as the reference product,the dissolution of the 2 preparations in different media was determined according to the second method of dissolution section in Chinese Pharmacopoeia(2015 edition).Then,Beagle dogs were used for comparative pharmacokinetic study,and DAS2.0 software was utilized for parameter calculation.Results The dissolution rate of Nano-matrix Meloxicam Capsules was higher than 80%in all of the 4 media in 30 minutes,higher than that of reference product.Compared with the reference product,the C max of the Nano-matrix Meloxicam Capsules in Beagle dogs was increased by 1.461 times and the AUC 0-t was increased by 1.319 times.Conclusion The in vitro dissolution and the bioavailability in Beagle dogs of the Nano-matrix Meloxicam Capsules was significantly improved,and there is a certain correlation between in vivo and in vitro,which provides support for the development of modified new drugs in future.
作者
张丹
王小旭
谢贺贺
吴翠栓
ZHANG Dan;WANG Xiaoxu;XIE Hehe;WU Cuishuan(Beijing Delivery Pharmaceutical Limited Company Technology,Beijing 102101,China)
出处
《西北药学杂志》
CAS
2021年第5期784-788,共5页
Northwest Pharmaceutical Journal
