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体外和体内评估含有胶凝多糖车前子的粘膜粘附贴片用于氯己定碱的颊部给药。

Ex-vivoand in-vitro assessment of mucoadhesive patches containing the gel-forming polysaccharide psyllium for buccal delivery of chlorhexidine base.

机构信息

Department FABIT, University of Bologna, Via San Donato 15, 40127 Bologna, Italy.

Department FABIT, University of Bologna, Via Belmeloro 6, 40127 Bologna, Italy.

出版信息

Int J Pharm. 2015 Dec 30;496(2):593-600. doi: 10.1016/j.ijpharm.2015.10.077. Epub 2015 Nov 2.

Abstract

The aim of the present study was to evaluate the gel-forming polysaccharide psyllium in the preparation of mucoadhesive patches for the controlled release of chlorhexidine (CHX) to treat pathologies in the oral cavity, using the casting-solvent evaporation technique. A number of different film-forming semi-synthetic polymers, such as sodium carboxymethyl cellulose (SCMC) and hydroxypropylmethyl cellulose (HPMC) were evaluated for comparison. The patch formulations were characterized in terms of drug content, morphology surface, swelling and mucoadhesive properties, microbiology inhibition assay and in vitro release tests. Three ex-vivo testswere carried out using porcine mucosa: an alternative dissolution test using artificial saliva that allows contemporary measurement of dissolution and mucoadhesion, a permeation test through the mucosa and the measurement of mucoadhesion using a Nouy tensile tester, as the maximum force required for the separation of the patch from the mucosa surface. The patches were also examined for determination of the minimum inhibitory concentration in cultures of Escherichia coli and Staphylococcus aureus. All the patches incorporating psyllium were found suitable in terms of external morphology, mucoadhesion and controlled release of the drug: in the presence of psyllium the drug displays prolonged zero-order release related to slower swelling rate of the system.

摘要

本研究旨在评估胶凝多糖车前子壳在制备具有控制释放性能的口腔黏附贴片中的应用,以治疗口腔病理,采用浇铸-溶剂蒸发技术。此外,还评估了多种不同的膜形成半合成聚合物,如羧甲基纤维素钠(SCMC)和羟丙基甲基纤维素(HPMC),作为比较。根据药物含量、形态表面、溶胀和黏附性能、微生物抑制试验和体外释放试验对贴片配方进行了表征。使用猪黏膜进行了三项离体测试:替代溶解试验使用人工唾液,允许同时测量溶解和黏附;通过黏膜的渗透试验以及使用努伊拉伸试验机测量黏膜的黏附,即分离贴片和黏膜表面所需的最大力。还通过测定大肠杆菌和金黄色葡萄球菌的最小抑菌浓度来检查贴片。所有包含车前子壳的贴片在外貌、黏附性和药物的控制释放方面均表现良好:车前子壳的存在使药物表现出与系统较慢溶胀速率相关的延长零级释放。

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