Amelian Aleksandra, Wasilewska Katarzyna, Wesoły Małgorzata, Ciosek-Skibińska Patrycja, Winnicka Katarzyna
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2C, 15-222 Białystok, Poland.
Departmentof Clinical Pharmacy, Medical University of Białystok, Mickiewicza 2A, 15-222 Białystok, Poland.
Saudi Pharm J. 2017 Dec;25(8):1144-1150. doi: 10.1016/j.jsps.2017.06.001. Epub 2017 Jun 19.
Orally disintegrating tablets and oral lyophilisates are novel attractive dosage forms that disintegrate or dissolve in the buccal cavity within seconds without necessity of drinking. The major limitation in designing of these dosage forms is unpleasant taste of the drug substance. Cetirizine dihydrochloride is a H-antihistamine substance indicated for the treatment of allergy. It is characterized by extremely bitter taste, therefore in order to deliver cetirizine dihydrochloride using orodispersible formulations, effective taste-masking is required. The aim of this study was to investigate whether microparticles containing cetirizine dihydrochloride could be successfully used to formulate orally disintegrating tablets by direct compression method and oral lyophilisates by freeze-drying process. Taste masking of cetirizine dihydrochloride was achieved by the spray-drying technique using Eudragit E PO as the drug agent carrier. Based on the preliminary studies, optimal compositions of microparticles, tablets and lyophilisates were chosen. Obtained dosage forms were characterized for drug content, disintegration time and mechanical properties. In order to determine whether the microparticles subjected to direct compression and freeze-drying process effectively mask the bitter taste of cetirizine dihydrochloride, the and evaluation was performed. The results showed that designed formulates with microparticles containing cetirizine dihydrochloride were characterized by appropriate mechanical properties, uniformity of weight and thickness, short disintegration time, and the uniform content of the drug substance. Taste-masking assessment performed by three independent methods (e-tongue evaluation, human test panel and the drug release) revealed that microparticles with Eudragit E PO are effective taste - masking carriers of cetirizine dihydrochloride and might be used to formulate orally disintegrating tablets and oral lyophilisates.
口腔崩解片和口服冻干制剂是新型的、有吸引力的剂型，能在数秒内在口腔内崩解或溶解，无需用水冲服。设计这些剂型的主要限制是药物本身味道不佳。盐酸西替利嗪是一种用于治疗过敏的H1抗组胺药。其特点是味道极苦，因此，为了使用口腔崩解制剂递送盐酸西替利嗪，需要有效的掩味措施。本研究的目的是调查含盐酸西替利嗪的微粒是否能成功用于通过直接压片法制备口腔崩解片以及通过冷冻干燥法制备口服冻干制剂。使用Eudragit E PO作为药物载体，通过喷雾干燥技术实现了盐酸西替利嗪的掩味。基于初步研究，选择了微粒、片剂和冻干制剂的最佳组成。对所得剂型进行了药物含量、崩解时间和机械性能的表征。为了确定经过直接压片和冷冻干燥处理的微粒是否能有效掩盖盐酸西替利嗪的苦味，进行了 和 评估。结果表明，所设计的含盐酸西替利嗪微粒的制剂具有适当的机械性能、重量和厚度均匀性、较短的崩解时间以及药物物质含量均匀。通过三种独立方法（电子舌评估、人体测试小组和 药物释放）进行的掩味评估表明，含Eudragit E PO的微粒是盐酸西替利嗪有效的掩味载体，可用于制备口腔崩解片和口服冻干制剂。
