Synergetic taste masking of lipid coating and beta-cyclodextrin inclusion

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物制剂研究中心

	Synergetic taste masking of lipid coating and beta-cyclodextrin inclusion
	Li Xue 3; Guo Zhen 1; Hao Jiebing 2; Li Biao 2; Liu Congbiao 1; Guo Tao 1; Li Haiyan1 ; Shi Senlin 3; Wang Liuyi 2; Zhang Jiwen3
刊名	Acta Pharmaceutica Sinica
	2014
卷号	49 期号:3 页码:392-398
关键词	taste masking lipid microsphere beta-cyclodextrin electronic tongue paracetamol
ISSN号	0513-4870
其他题名	脂质包裹与环糊精包合的协同矫味研究
文献子类	Article
英文摘要	Paracetamol was used as a model drug in this study to investigate the synergetic effects of lipid coating and beta-cyclodextrin (beta-CD) inclusion for masking the bitter taste of poorly soluble drugs. To control the concentration as low as possible of the free drug which produced a bitter taste, a kinetic model was established to calculate the drug distribution theoretically among the free drug in medium, lipid coated particles and molecular inclusion on the basis of the preparation and characterization of the lipid microspheres, so as to select the proper amount of beta-CD. Finally, the synergetic drug delivery systems were prepared and characterized by ~1H nuclear magnetic resonance (~1H NMR), molecular simulation and the electronic tongue. As a result, the drug release rate constant (k) of the lipid microspheres coated with octadecanol was determined as 0.001 270 s~(?1). Then, the synergetic drug delivery systems were prepared with the ratio of 6.74∶1 (w/w) for beta-CD and paracetamol. The chemical shift values for the fingerprint peaks of paracetamol all increased and hydrogen bonds were formed between the oxygen on the phenolic hydroxyl group, the nitrogen on the imino in paracetamol and the hydrogens on the hydroxyl groups in beta-CD. The results tested by the electronic tongue indicated that the paracetamol, lipid microspheres, beta-CD inclusion and their mixture showed different taste characteristics, with the bitterness order of the synergetic drug delivery systems lipid microspheres < beta-CD inclusion < paracetamol, which confirmed the synergetic taste masking effects of lipid coating and beta-CD molecular inclusion. In summary, the synergetic taste masking was jointly achieved through the retard of the drug release by the lipid coating and the inclusion of the free paracetamol by beta-CD through hydrogen bonds.
资助项目	国家自然科学基金资助项目[00000000]
WOS研究方向	Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种	中文
CSCD记录号	CSCD:5080605
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/269349]
专题	药物制剂研究中心
作者单位	1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.; 2.Hainan Weikang Pharmaceutical Co., LTD, Anqing, Anhui 246000, China. 3.Zhejiang Chinese Medical University, Hangzhou, Zhejiang 310000, China.;
推荐引用方式 GB/T 7714	Li Xue,Guo Zhen,Hao Jiebing,et al. Synergetic taste masking of lipid coating and beta-cyclodextrin inclusion[J]. Acta Pharmaceutica Sinica,2014,49(3):392-398.
APA	Li Xue.,Guo Zhen.,Hao Jiebing.,Li Biao.,Liu Congbiao.,...&Zhang Jiwen.(2014).Synergetic taste masking of lipid coating and beta-cyclodextrin inclusion.Acta Pharmaceutica Sinica,49(3),392-398.
MLA	Li Xue,et al."Synergetic taste masking of lipid coating and beta-cyclodextrin inclusion".Acta Pharmaceutica Sinica 49.3(2014):392-398.