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采用 Kollicoat(®) Smartseal 30 D 制备掩味奥硝唑颗粒并对其进行口腔干混悬剂的处方前研究与开发。

Formulation and development of oral dry suspension using taste masked Ornidazole particles prepared using Kollicoat(®) Smartseal 30 D.

机构信息

BASF India Ltd, Pharma Ingredients and Services, Turbhe, Navi Mumbai, India.

出版信息

Drug Dev Ind Pharm. 2013 Jul;39(7):1091-7. doi: 10.3109/03639045.2012.709250. Epub 2012 Aug 20.

DOI:10.3109/03639045.2012.709250
PMID:22900982
Abstract

The purpose of this work was to taste mask highly bitter active, Ornidazole by means of particle coating. The aim of the work was further extended into formulating these coated particles into an acceptable oral dosage form such as dry suspension. Ornidazole drug particles were coated using Kollicoat(®) Smartseal 30 D as a taste masking polymer. Kollicoat(®) Smartseal 30 D is a methyl methacrylate - diethylaminoethyl methacrylate copolymer (6:4). Successful taste masking was achieved for Ornidazole with both top spray and bottom spray techniques using fluid bed processor. Effective taste masking was achieved at a weight gain of 50% w/w and 40% w/w for bottom and top spray techniques respectively without having a significant effect on the release pattern. A taste masked dry suspension was prepared with around 80% w/w coated Ornidazole particles and pH was maintained around 7-8. The suspension prepared with these coated Ornidazole particles, which were maintained in the alkaline pH was found to be stable for 7 days without affecting the taste. The bitter taste intensity was evaluated using volunteers by comparison of test samples with standard solutions containing Ornidazole at various concentrations. Thus, Kollicoat(®) Smartseal 30 D was found to be an effective polymer for taste masking of a bitter active like Ornidazole. The formulation development of taste masked dry suspensions was only possible due to unique properties possessed by Kollicoat(®) Smartseal 30 D.

摘要

这项工作的目的是通过颗粒包衣来掩盖奥硝唑的强烈苦味。工作的目的进一步扩展到将这些包衣颗粒制成可接受的口服剂型,如干混悬剂。奥硝唑药物颗粒采用 Kollicoat(®) Smartseal 30 D 作为掩味聚合物进行包衣。Kollicoat(®) Smartseal 30 D 是甲基丙烯酸甲酯-二乙氨基乙基甲基丙烯酸酯共聚物(6:4)。使用流化床处理器,通过顶喷和底喷技术均成功实现了奥硝唑的掩味。在底喷和顶喷技术中,分别在增重 50%w/w 和 40%w/w 时即可实现有效的掩味,而对释放模式没有显著影响。使用约 80%w/w 包衣奥硝唑颗粒制备了掩味干混悬剂,并将 pH 值维持在 7-8 左右。用这些包衣奥硝唑颗粒制备的混悬剂在碱性 pH 值下保持稳定 7 天,而不会影响味道。苦味强度通过志愿者比较含有不同浓度奥硝唑的标准溶液与测试样品来评估。因此,Kollicoat(®) Smartseal 30 D 被发现是一种有效用于掩蔽苦味活性物质如奥硝唑的聚合物。由于 Kollicoat(®) Smartseal 30 D 所具有的独特性质,才有可能开发出掩味干混悬剂的配方。

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