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西罗莫司无定形纳米颗粒制剂及其片剂

Amorphous Nanoparticulate Formulation of Sirolimus and Its Tablets.

作者信息

Shen Yudong, Li Xingya, Le Yuan

机构信息

State Key Laboratory of Organic-Inorganic Composites, Beijing University of Chemical Technology, Beijing 100029, China.

出版信息

Pharmaceutics. 2018 Sep 11;10(3):155. doi: 10.3390/pharmaceutics10030155.

DOI:10.3390/pharmaceutics10030155
PMID:30208637
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6161202/
Abstract

Nanocrystallization and amorphization have proven to be two effective strategies to improve the bioavailability of water-insoluble drugs. The purpose of our work was to develop a nano-formulated tablet of sirolimus (SRL) for enhanced dissolution. Amorphous SRL nanocomposites were prepared using anti-solvent precipitation via a high-gravity rotating packed bed. Various factors that affect particle size and size distribution, such as excipients, rotating speed, antisolvent/solvent flow rate, were investigated. Structure, stability and in vitro dissolution of the as-prepared SRL were evaluated. Furthermore, the nanoparticulated SRL tablet formula was screened to control drug release. Importantly, SRL tablets exhibit different dissolution profile by adjusting HPMC (hydroxypropyl methyl cellulose) content, which makes them more suitable for various formulation developments.

摘要

纳米晶化和非晶化已被证明是提高水不溶性药物生物利用度的两种有效策略。我们工作的目的是开发一种用于增强溶出度的西罗莫司（SRL）纳米制剂片剂。通过高重力旋转填充床采用反溶剂沉淀法制备了非晶态SRL纳米复合材料。研究了各种影响粒径和粒径分布的因素，如辅料、转速、反溶剂/溶剂流速等。对所制备的SRL的结构、稳定性和体外溶出度进行了评估。此外，对纳米颗粒SRL片剂配方进行了筛选以控制药物释放。重要的是，通过调整羟丙基甲基纤维素（HPMC）含量，SRL片剂表现出不同的溶出曲线，这使其更适合各种制剂开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/629038cdf3c8/pharmaceutics-10-00155-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/1af2204066bc/pharmaceutics-10-00155-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/b8e27c763211/pharmaceutics-10-00155-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/61961207b443/pharmaceutics-10-00155-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/bc6df1442032/pharmaceutics-10-00155-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/ddfe1c35393e/pharmaceutics-10-00155-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/a0a8433aeaf1/pharmaceutics-10-00155-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/55f848e2e690/pharmaceutics-10-00155-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/2646c1baddca/pharmaceutics-10-00155-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/3747231cf613/pharmaceutics-10-00155-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/af0aa5f66bf1/pharmaceutics-10-00155-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/4fa5af569b59/pharmaceutics-10-00155-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/25c7b38ca26e/pharmaceutics-10-00155-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/629038cdf3c8/pharmaceutics-10-00155-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/1af2204066bc/pharmaceutics-10-00155-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/b8e27c763211/pharmaceutics-10-00155-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/61961207b443/pharmaceutics-10-00155-g003a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/bc6df1442032/pharmaceutics-10-00155-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/ddfe1c35393e/pharmaceutics-10-00155-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/a0a8433aeaf1/pharmaceutics-10-00155-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/55f848e2e690/pharmaceutics-10-00155-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/2646c1baddca/pharmaceutics-10-00155-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/3747231cf613/pharmaceutics-10-00155-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/af0aa5f66bf1/pharmaceutics-10-00155-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/4fa5af569b59/pharmaceutics-10-00155-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/25c7b38ca26e/pharmaceutics-10-00155-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26f8/6161202/629038cdf3c8/pharmaceutics-10-00155-g013.jpg

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