摘要
目的:制备美洛昔康口腔速溶膜(meloxicam oral fast dissolving films,MLX-OFDF),并进行体外释放研究。方法:以葡甲胺(meglumine,MEG)作为助溶剂,通过溶剂浇铸法制备MLX-OFDF,用单因素试验法优选成膜材料和增塑剂;固定主药物含量,以羟丙甲纤维素E30(HPMC-E30)、聚乙二醇400(PEG-400)、磷酸二氢钾(KH_2PO_4)为考察因素,以百分伸长率、体外崩解时间、表面pH值为评价指标,用正交试验法优化处方;对以最优处方制备的MLX-OFDF进行崩解时间、含量均匀度及体外释放度考察。结果:以最优处方:1.50%(g·mL^(-1))MLX,1.10%(g·mL^(-1))MEG,3.00%(g·mL^(-1))HPMC-E30,4.00%(g·mL^(-1))PEG-400,0.15%(g·mL^(-1))KH_2PO_4制得的MLX-OFDF能够在30 s内崩解,含量均匀度符合规定(A+2.2S<15),药物在5 min时累积释放度达到(95.51±1.38)%。结论:通过单因素试验法与正交试验法优化得到的MLXOFDF处方有效可行,制备的MLX-OFDF外观平整透明、崩解迅速,体外释放良好,具有广阔的应用前景。
Objective： To prepare meloxicam oral fast dissolving films （MLX-OFDF） and evaluate its in vitro release characteristics.Methods： MLX-OFDF was prepared with meglumine （MEG） as cosolvent by solvent casting method.First,the film forming material and plasticizer of MLX-OFDF were selected by single factor experiment.Then the formulation of MLX-OFDF was optimized by employing orthogonal design with the amounts of hydroxypropyl methylcellulose E30 （HPMC-E30）,polyethylene glycol 400 （PEG-400） and potassium dihydrogen phosphate （KH2PO4） as investigation factors,and percent elongation,surface p H and disintegration time as evaluation indexes.Finally,the disintegration time,content uniformity and in vitro release of the optimized formulation were also evaluated.Results： MLX-OFDF prepared by the optimized formulation [1.50% （g·mL（-1））MLX,1.10% （g·mL（-1）） MEG,3.00% （g·mL（-1）） HPMC-E30,4.00% （g·mL（-1）） PEG-400,0.15% （g·mL（-1））KH2PO4]could disintegrate within 30 s,the cumulative release in vitro at 5 min reached （95.51 ± 1.38） %,and the conformity of drug content was up to the standard （A ＋ 2.2 S 15）.Conclusion： Using single factor test method and orthogonal design to prepare MLX-OFDF is effective and feasible.The optimized MLX-OFDF which has a good appearance and rapid disintegration and release is a new preparation for MLX with profound application prospect.
作者
连王权
申宝德
沈成英
刘肖
廖卫波
袁海龙
LIAN Wang-quan SHEN Bao-de SHEN Cheng-ying LIU Xiao LIAO Wei-bo YUAN Hai-long(Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China Department of Pharmacy, Air Force General Hospital, PLA, Beijing 100142, China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2017年第20期2478-2484,共7页
Chinese Journal of New Drugs
基金
军队后勤科研目录重点项目(BKJ16J011)
关键词
美洛昔康
口腔速溶膜
正交试验
溶剂浇铸法
体外释放度
meloxicam
oral fast dissolving films
orthogonal design
solvent casting method
in vitro release
