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阿昔洛韦与利多卡因透粘膜或透皮贴剂制备的初步研究

Preliminary Study for the Preparation of Transmucosal or Transdermal Patches with Acyclovir and Lidocaine.

作者信息

Marioane Cristina-Adela, Bunoiu Mădălin, Mateescu Mădălina, Sfîrloagă Paula, Vlase Gabriela, Vlase Titus

机构信息

Research Centre for Thermal Analysis in Environmental Problems, West University of Timisoara, Pestalozzi Street 16, 300115 Timisoara, Romania.

Faculty of Physics, West University of Timisoara, V. Parvan Ave., No. 4, 300223 Timisoara, Romania.

出版信息

Polymers (Basel). 2021 Oct 19;13(20):3596. doi: 10.3390/polym13203596.

DOI:10.3390/polym13203596
PMID:34685355
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8538249/
Abstract

The present study aimed to prepare and evaluate patches for the controlled release of lidocaine/acyclovir and the binary mixture between lidocaine: acyclovir in the oral cavity. Mucoside adhesive patches containing 12.5 mg/cm lidocaine/acyclovir or binary mixture base were developed by a solvent casting method using sodium alginate, polyvinylpyrrolidone (PVP), glycerol (Gly), polyvinyl alcohol (PVA), and Span 80 (S). Binary mixtures between all components were prepared before the patches' formulation in order to be able to check the substance compatibility. All formulated patches were analyzed by FT-IR spectroscopy, UV-Vis analysis, thermogravimetry (TGA), and scanning electron microscopy (SEM). FT-IR and TGA analyses were also used to check compatibility between binary mixtures. The study establishes which membranes are indicated in the controlled release of lidocaine/acyclovir and those membranes that contain both active principles. Membranes based on alginate, PVP, and PVA can be used to release the active substance. Simultaneously, membranes with SPAN used as a gelling agent were excluded due to the interaction with the active substance. The following membranes composition have been chosen for lidocaine release: Alginate:Gly and Alginate:Gly:PVP. At the same time, the following membrane compositions were chosen for acyclovir membranes: Alginate:Gly:PVP and Alginate:PVA:Gly. Both active substances could be included to obtain a homogeneous distribution only in the membrane based on alginate, PVA, and Gly.

摘要

本研究旨在制备并评估用于口腔局部释放利多卡因/阿昔洛韦以及利多卡因与阿昔洛韦二元混合物的贴剂。采用溶剂浇铸法,以海藻酸钠、聚乙烯吡咯烷酮(PVP)、甘油(Gly)、聚乙烯醇(PVA)和司盘80(S)为原料,制备了含12.5 mg/cm利多卡因/阿昔洛韦或二元混合物基质的黏膜黏附贴剂。在制备贴剂之前,先制备了所有组分之间的二元混合物,以便检查物质相容性。所有制备的贴剂均通过傅里叶变换红外光谱(FT-IR)、紫外-可见光谱分析(UV-Vis)、热重分析(TGA)和扫描电子显微镜(SEM)进行分析。FT-IR和TGA分析也用于检查二元混合物之间的相容性。该研究确定了哪些膜适用于利多卡因/阿昔洛韦的控释以及哪些膜含有两种活性成分。基于海藻酸盐、PVP和PVA的膜可用于释放活性物质。同时,由于与活性物质的相互作用,排除了以司盘作为凝胶剂的膜。以下膜组合物被选用于利多卡因释放:海藻酸盐:甘油和海藻酸盐:甘油:PVP。同时,以下膜组合物被选用于阿昔洛韦膜:海藻酸盐:甘油:PVP和海藻酸盐:PVA:甘油。只有在基于海藻酸盐、PVA和甘油的膜中,两种活性物质才能均匀分布。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/8eb8775eae2f/polymers-13-03596-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/73fb144b5b9d/polymers-13-03596-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/bdce68d208df/polymers-13-03596-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/e1a18e717a0d/polymers-13-03596-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/10c365c55f9a/polymers-13-03596-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/a64d542e1d9e/polymers-13-03596-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/a3ca70b39b75/polymers-13-03596-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/fc68b39bc164/polymers-13-03596-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/a25587665ef9/polymers-13-03596-g008a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/8eb8775eae2f/polymers-13-03596-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/73fb144b5b9d/polymers-13-03596-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/bdce68d208df/polymers-13-03596-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/e1a18e717a0d/polymers-13-03596-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/10c365c55f9a/polymers-13-03596-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/a64d542e1d9e/polymers-13-03596-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/a3ca70b39b75/polymers-13-03596-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/fc68b39bc164/polymers-13-03596-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/a25587665ef9/polymers-13-03596-g008a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf8d/8538249/8eb8775eae2f/polymers-13-03596-g009.jpg

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