PDF(Pubmed)
Abstract：
The purpose of this study was to enhance the stability of montelukast and levocetirizine for the development of a fixed-dose combination (FDC) monolayer tablet. To evaluate the compatibility of montelukast and levocetirizine, a mixture of the two drugs was prepared, and changes in the appearance characteristics and impurity content were observed in a dry oven at 60 °C. Excipients that contributed minimally to impurity increases were selected to minimize drug interactions. Mannitol, microcrystalline cellulose, croscarmellose sodium, hypromellose, and sodium citrate were chosen as excipients, and montelukast-levocetirizine FDC monolayer tablets were prepared by wet granulating the two drugs separately. A separate granulation of montelukast and levocetirizine, along with the addition of sodium citrate as a pH stabilizer, minimized the changes in tablet appearance and impurity levels. The prepared tablets demonstrated release profiles equivalent to those of commercial products in comparative dissolution tests. Subsequent stability testing at 40 ± 2 °C and 75 ± 5% RH for 6 months confirmed that the drug content, dissolution rate, and impurity content met the specified acceptance criteria. In conclusion, the montelukast-levocetirizine FDC monolayer tablet developed in this study offers a potential alternative to commercial products.
摘要：
这项研究的目的是增强孟鲁司特和左西替利嗪的稳定性，以开发固定剂量组合（FDC）单层片剂。评价孟鲁司特与左西替利嗪的相容性,制备了两种药物的混合物，在60°C的干燥烘箱中观察外观特性和杂质含量的变化。选择对杂质增加贡献最小的赋形剂以使药物相互作用最小化。甘露醇,微晶纤维素,交联羧甲基纤维素钠，羟丙甲纤维素,选择柠檬酸钠作为赋形剂，孟鲁司特-左西替利嗪FDC单层片是通过将两种药物分别湿法制粒制备的。孟鲁司特和左西替利嗪的单独造粒，加入柠檬酸钠作为pH稳定剂，最小化片剂外观和杂质水平的变化。所制备的片剂在比较溶出试验中显示出与市售产品相同的释放曲线。随后在40±2°C和75±5%RH下进行6个月的稳定性测试证实，药物含量，溶出度,杂质含量符合规定的验收标准。总之,本研究开发的孟鲁司特-左西替利嗪FDC单层片提供了商业产品的潜在替代品.
