A mesoporous molecular sieve-based oral taste-masking agent with efficient shielding effect for oral administration of cetirizine

Mesoporous molecular sieve is a kind of porous material with pore size of 2-50 nm. It has ordered pore structure, high surface area, uniform pore structure, excellent thermal stability and mechanical stability, strong adsorption capacity, and no pharmacological activity and toxicity, which conforms to the basic conditions of drug carrier. The current reports mainly focus on the synthesis and characterization of materials and drug sustained release and controlled release. The application of mesoporous molecular sieves in the field of drug taste masking has not been reported. Taste masking technique ( API ) refers to the use of various methods and techniques to mask or reduce the bad taste of active pharmaceutical ingredients in drugs. Cetirizine ( CTZ ) is a second-generation antihistamine drug with a strong bitter taste. Cetirizine binds to membrane receptors on tongue sensory cells, causing bitterness and leading to swallowing suffering. Orally disintegrating tablets and dispersible tablets are usually used in patients with dysphagia such as coma and infants. Orally disintegrating tablets are required to be significantly smaller ( ≤ 60 mg ) and need to be rapidly disintegrated in the mouth to prevent oral disintegrating tablets from sticking to the patient 's throat, causing danger. Therefore, it is of great clinical significance to find an efficient new taste masking agent with high drug loading, good taste masking effect and low dosage.

The Gaobo team of Jilin University used the bitter drug cetirizine as a model drug, MCM-41, MCM-48, HMSS molecular sieve, aspartame ( APM ) and β-cyclodextrin ( β-CD ) as carriers, optimized the drug loading ratio, and compared the performance of each material in drug loading and taste masking. The drug-loaded composites were characterized by XRD, FT-IR and TEM, and the new role of mesoporous molecular sieves as a new and efficient drug masking agent was explored. The results showed that except aspartame was only physically mixed, the other four materials were successfully adsorbed or included in the drug ; among them, HMSS hollow mesoporous molecular sieve has a drug loading of up to 50 %, and the bitterness of the drug after drug loading is not obvious. Its taste masking effect is significantly better than other materials, and it is expected to become a new type of high-efficiency taste masking agent.

About the Authors

Gao Bo, Professor of Jilin University, Director of Department of Biopharmaceutics, College of Life Sciences, Jilin University, Director of Biochemistry and Molecular Biology Association of Jilin Province, and Supervisor of Rana chensinensis Association of Jilin Province. The research direction is mainly the application of porous materials in biology and pharmacy, and the modernization of traditional Chinese medicine. It has undertaken more than ten scientific research projects, and has published more than 50 academic papers, including more than 20 SCI papers. Apply for or authorize 32 invention patents. He participated in the compilation of more than ten teaching monographs and textbooks, and undertook one teaching reform project. He has presided over and participated in the national major new drug creation, the National Natural Science Foundation, the national major public welfare project ( State Forestry Administration ), the Jilin Provincial Science and Technology Department, the Jilin Provincial Development and Reform Commission, the Jilin Provincial Administration of Traditional Chinese Medicine, and enterprise cooperation projects. For more information, please pay attention to his research homepage https://life.jlu.edu.cn/info/1026/1190.htm

About Nano Research

Nano Research is a peer-reviewed, open access, international and interdisciplinary research journal, sponsored by Tsinghua University and the Chinese Chemical Society, published by Tsinghua University Press on the platform SciOpen. It publishes original high-quality research and significant review articles on all aspects of nanoscience and nanotechnology, ranging from basic aspects of the science of nanoscale materials to practical applications of such materials. After 18 years of development, it has become one of the most influential academic journals in the nano field. Nano Research has published more than 1,000 papers every year from 2022, with its cumulative count surpassing 7,000 articles. In 2024 InCites Journal Citation Reports, its 2024 IF is 9.0 (8.7, 5 years), and it continues to be the Q1 area among the four subject classifications. Nano Research Award, established by Nano Research together with TUP and Springer Nature in 2013, and Nano Research Young Innovators (NR45) Awards, established by Nano Research in 2018, have become international academic awards with global influence.