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采用超声间歇技术制备含阿昔洛韦的固体泡沫

Preparation of Acyclovir-Containing Solid Foam by Ultrasonic Batch Technology.

作者信息

Haimhoffer Ádám, Fenyvesi Ferenc, Lekli István, Béresová Mónika, Bak István, Czagány Máté, Vasvári Gábor, Bácskay Ildikó, Tóth Judit, Budai István

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary.

Doctoral School of Pharmaceutical Sciences, University of Debrecen, H-4032 Debrecen, Hungary.

出版信息

Pharmaceutics. 2021 Sep 27;13(10):1571. doi: 10.3390/pharmaceutics13101571.

Abstract

In recent years, the application of solid foams has become widespread. Solid foams are not only used in the aerospace field but also in everyday life. Although foams are promising dosage forms in the pharmaceutical industry, their usage is not prevalent due to decreased stability of the solid foam structure. These special dosage forms can result in increased bioavailability of drugs. Low-density floating formulations can also increase the gastric residence time of drugs; therefore, drug release will be sustained. Our aim was to produce a stable floating formula by foaming. Matrix components, PEG 4000 and stearic acid type 50, were selected with the criteria of low gastric irritation, a melting range below 70 °C, and well-known use in oral drug formulations. This matrix was melted at 54 °C in order to produce a dispersion of active substance and was foamed by different gases at atmospheric pressure using an ultrasonic homogenizer. The density of the molded solid foam was studied by the pycnometer method, and its structure was investigated by SEM and micro-CT. The prolonged drug release and mucoadhesive properties were proved in a pH 1.2 buffer. According to our experiments, a stable foam could be produced by rapid homogenization (less than 1 min) without any surfactant material.

摘要

近年来,固体泡沫的应用已变得十分广泛。固体泡沫不仅应用于航空航天领域,也应用于日常生活中。尽管泡沫在制药行业是很有前景的剂型,但由于固体泡沫结构稳定性降低,其应用并不普遍。这些特殊剂型可提高药物的生物利用度。低密度漂浮制剂还可延长药物在胃内的停留时间;因此,药物释放将得以持续。我们的目标是通过发泡制备一种稳定的漂浮制剂。基质成分聚乙二醇4000和50型硬脂酸是根据低胃刺激性、低于70℃的熔点范围以及在口服药物制剂中的广泛应用等标准选择的。该基质在54℃熔化以制备活性物质分散体,并在大气压下使用超声均质器用不同气体进行发泡。用比重瓶法研究模制固体泡沫的密度,并用扫描电子显微镜和微型计算机断层扫描研究其结构。在pH 1.2缓冲液中证明了其延长的药物释放和粘膜粘附特性。根据我们的实验,无需任何表面活性剂材料,通过快速均质化(少于1分钟)即可制备出稳定的泡沫。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d597/8541121/4865c8763aea/pharmaceutics-13-01571-g001.jpg

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