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多奈哌齐/环糊精络合口腔崩解膜：基于动态过程和药物吸收的环糊精对掩味的影响

A donepezil/cyclodextrin complexation orodispersible film: Effect of cyclodextrin on taste-masking based on dynamic process and drug absorption.

作者信息

Liu Tingting, Wan Xiaocao, Luo Zheng, Liu Chao, Quan Peng, Cun Dongmei, Fang Liang

机构信息

Wuya college of Innovation, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.

School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China.

出版信息

Asian J Pharm Sci. 2019 Mar;14(2):183-192. doi: 10.1016/j.ajps.2018.05.001. Epub 2018 May 24.

DOI:10.1016/j.ajps.2018.05.001
PMID:32104450
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7032196/
Abstract

The aim of this study was to develop a palatable donepezil (DP) orodispersible film (ODF) to facilitate the swallowing process and investigate the effect of cyclodextrin on taste-masking based on dynamic process and drug absorption. Complexation of DP with hydroxypropyl-β-cyclodextrin (HP-β-CD) was applied to mask the bitter taste then the prepared complexes were incorporated into ODF using solvent casting method. The taste-masking efficiency was evaluated by e-tongue; meanwhile the pharmacokinetic behavior of DP/HP-β-CD ODF was investigated by study. Results showed the optimized film was more palatable than donepezil hydrochloride (DH) film and was bioequivalent with DH. The molecular mechanism was revealed by phase solubility study, Fourier-transform infrared spectrometer (FT-IR), Differential scanning calorimeter (DSC), X-ray diffraction (XRD) and molecular modeling. Taste-masking was attributed to the formation of DP/HP-β-CD which was due to moderate interaction between DP and HP-β-CD. The stability of DP/HP-β-CD was decreased because of the acid environment in stomach, which facilitated the absorption of DP. These results extended our understanding about the application of cyclodextrin complexation and provided guidance for the design of ODF especially for drugs with disgusting taste.

摘要

本研究的目的是开发一种可口的多奈哌齐（DP）口腔崩解膜（ODF）以促进吞咽过程，并基于动态过程和药物吸收研究环糊精对掩味的影响。将DP与羟丙基-β-环糊精（HP-β-CD）络合以掩盖苦味，然后使用溶剂浇铸法将制备的络合物掺入ODF中。通过电子舌评估掩味效率；同时通过研究考察DP/HP-β-CD ODF的药代动力学行为。结果表明，优化后的膜比盐酸多奈哌齐（DH）膜更可口，且与DH生物等效。通过相溶解度研究、傅里叶变换红外光谱仪（FT-IR）、差示扫描量热仪（DSC）、X射线衍射（XRD）和分子模拟揭示了分子机制。掩味归因于DP/HP-β-CD的形成，这是由于DP与HP-β-CD之间的适度相互作用。由于胃中的酸性环境，DP/HP-β-CD的稳定性降低，这有利于DP的吸收。这些结果扩展了我们对环糊精络合应用的理解，并为ODF的设计提供了指导，特别是对于有令人厌恶味道的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/bc077e0df7b0/gr9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/6f21d31b8081/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/2657286f7d7b/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/1cfb15cbe137/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/3f6c2c0ab120/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/b86e1a0b9582/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/28f3c27e42db/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/4e50d5098eaf/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/f2c09cf1a6b0/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/1b3296f49bb8/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/bc077e0df7b0/gr9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/6f21d31b8081/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/2657286f7d7b/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/1cfb15cbe137/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/3f6c2c0ab120/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/b86e1a0b9582/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/28f3c27e42db/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/4e50d5098eaf/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/f2c09cf1a6b0/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/1b3296f49bb8/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1643/7032196/bc077e0df7b0/gr9.jpg

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