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孟鲁司特和左西替利嗪固定剂量复方单层片中稳定性和相容性的增强

Enhanced Stability and Compatibility of Montelukast and Levocetirizine in a Fixed-Dose Combination Monolayer Tablet.

作者信息

Yun Tae Han, Kim Moon Jung, Lee Jung Gyun, Bang Kyu Ho, Kim Kyeong Soo

机构信息

Department of Pharmaceutical Engineering, Gyeongsang National University, 33 Dongjin-ro, Jinju 52725, Republic of Korea.

出版信息

Pharmaceutics. 2024 Jul 21;16(7):963. doi: 10.3390/pharmaceutics16070963.

DOI:10.3390/pharmaceutics16070963
PMID:39065660
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11279677/
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

本研究的目的是提高孟鲁司特和左西替利嗪的稳定性，以开发一种固定剂量复方（FDC）单层片剂。为了评估孟鲁司特和左西替利嗪的相容性，制备了两种药物的混合物，并在60°C的干燥箱中观察外观特征和杂质含量的变化。选择对杂质增加贡献最小的辅料以尽量减少药物相互作用。选择甘露醇、微晶纤维素、交联羧甲基纤维素钠、羟丙甲纤维素和柠檬酸钠作为辅料，并通过分别对两种药物进行湿法制粒来制备孟鲁司特-左西替利嗪FDC单层片剂。孟鲁司特和左西替利嗪分别制粒，并加入柠檬酸钠作为pH稳定剂，可最大限度地减少片剂外观和杂质水平的变化。在比较溶出度试验中，制备的片剂显示出与市售产品相当的释放曲线。随后在40±2°C和75±5%RH条件下进行6个月的稳定性试验，证实药物含量、溶出率和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单层片剂为市售产品提供了一种潜在的替代方案。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/7f5de235663f/pharmaceutics-16-00963-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/eba918736e48/pharmaceutics-16-00963-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/fc8ac87c7ca8/pharmaceutics-16-00963-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/a6c0ef1b7db9/pharmaceutics-16-00963-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/902b6dfdedc5/pharmaceutics-16-00963-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/7e739b8ba866/pharmaceutics-16-00963-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/0f1780feeaf8/pharmaceutics-16-00963-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/4d91aed15ba3/pharmaceutics-16-00963-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/90b87c61ab5b/pharmaceutics-16-00963-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/363e5b4a16f1/pharmaceutics-16-00963-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/7f5de235663f/pharmaceutics-16-00963-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/eba918736e48/pharmaceutics-16-00963-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/fc8ac87c7ca8/pharmaceutics-16-00963-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/a6c0ef1b7db9/pharmaceutics-16-00963-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/902b6dfdedc5/pharmaceutics-16-00963-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/7e739b8ba866/pharmaceutics-16-00963-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/0f1780feeaf8/pharmaceutics-16-00963-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/4d91aed15ba3/pharmaceutics-16-00963-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/90b87c61ab5b/pharmaceutics-16-00963-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/363e5b4a16f1/pharmaceutics-16-00963-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac72/11279677/7f5de235663f/pharmaceutics-16-00963-g010.jpg

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