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Preparation and In Vitro/Vivo Evaluation of New Celecoxib Solid Dispersions with Co-Carrier Containing Aerosil and Poloxamer 188
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2021-01-01 , DOI: 10.1007/s11094-021-02316-0
Xiangjun Shi , Zejie Ding , Jiayin Bao , Chao Wang

Solid dispersions (SDs) containing co-carrier were developed to improve in vitro dissolution and in vivo pharmacokinetics of celecoxib (CXB). Various polymers, including PVP K30, PEG4000, PEG6000, Poloxamer 188, Eudragit E100 and colloidal SiO 2 , were studied in the preparation of CXB-containing SDs. Poloxamer 188 and Aerosil stood out in preliminary characterization. Further study was focused on the selection and characterization of optimum ratio of CXB and polymer in solid dispersions (CXB-Poloxamer 188-Aerosil, 1:5:1). Results exhibited remarkable enhancement of both the dissolution and bioavailability of CXB which retained an amorphous form in SD samples.

中文翻译:

含气硅和泊洛沙姆 188 共载体的新型塞来昔布固体分散体的制备和体外/体内评价

开发了含有共载体的固体分散体 (SD) 以改善塞来昔布 (CXB) 的体外溶出度和体内药代动力学。在制备含 CXB 的 SD 时,研究了各种聚合物,包括 PVP K30、PEG4000、PEG6000、泊洛沙姆 188、Eudragit E100 和胶体 SiO 2 。泊洛沙姆 188 和 Aerosil 在初步表征中脱颖而出。进一步的研究集中在固体分散体中 CXB 和聚合物最佳比例的选择和表征(CXB-泊洛沙姆 188-Aerosil,1:5:1)。结果显示 CXB 的溶解度和生物利用度均显着增强,其在 SD 样品中保留了无定形形式。
更新日期:2021-01-01
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