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载有布洛芬的离心纺微纤维,可快速缓解大鼠炎症。

Ibuprofen-loaded centrifugally spun microfibers for quick relief of inflammation in rats.

机构信息

University College of Pharmacy, University of the Punjab, Lahore, Pakistan.

Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.

出版信息

Drug Dev Ind Pharm. 2021 Nov;47(11):1786-1793. doi: 10.1080/03639045.2022.2059500. Epub 2022 Apr 8.

DOI:10.1080/03639045.2022.2059500
PMID:35343341
Abstract

The conventional dosage forms (tablets, capsules) of ibuprofen have less potential in the suppression of pain and inflammation due to their slow dissolution rates and lower bioavailability. The aim of this study was to fabricate fibrous solid dispersion of ibuprofen for improved dissolution rate and quick therapeutic action. Drug-loaded microfibers were fabricated using centrifugal melt spinning (CMS) technique from the physical mixture of sucrose, ibuprofen and a hydrophilic polymer, PVP. These fibers were characterized by SEM, PXRD, DSC, and FTIR spectroscopy. The selected formulation was also pressed into tablets by direct compression method followed by its and characterization. The production yield of fibers was 75 ± 2% with an average diameter of 15 ± 5 µm. The drug loading efficiency (DLE) was 85 ± 5%. The tablets dissolved rapidly (<40 s). dissolution studies have shown >85% of ibuprofen dissolved from tablet within first 2 min which was ∼5 times quicker than drug alone. Dissolution efficiency has improved from 0.63 of ibuprofen to 0.95 of that in fibers with ∼7 times reduction in mean dissolution time. PXRD, and DSC have shown the amorphous state of ibuprofen in the formulation and FTIR spectra demonstrated no interaction of drug with excipients. anti-inflammatory studies using rabbits revealed a significant ( < 0.05) reduction in paw volume (mm) in the groups treated with fibrous formulation. This study concludes that microfibers produced by centrifugal melt spinning have improved dissolution rates and bioavailability of ibuprofen. Incorporation of polymer in the formulations improves the production yield and drug loading efficiency of microfibers.

摘要

由于布洛芬的溶解速度较慢且生物利用度较低,传统的剂型(片剂、胶囊)在抑制疼痛和炎症方面的潜力较小。本研究旨在制备布洛芬纤维状固体分散体,以提高其溶解速率和快速治疗作用。采用离心熔融纺丝(CMS)技术,从蔗糖、布洛芬和亲水性聚合物 PVP 的物理混合物中制备载药微纤维。通过 SEM、PXRD、DSC 和 FTIR 光谱对这些纤维进行了表征。还通过直接压缩法将选定的配方压制成片剂,并对其进行了 和 表征。纤维的产率为 75±2%,平均直径为 15±5μm。药物载量效率(DLE)为 85±5%。片剂迅速溶解(<40s)。溶解研究表明,在最初的 2 分钟内,有超过 85%的布洛芬从片剂中溶解,这比单独使用药物快约 5 倍。溶解效率从布洛芬的 0.63 提高到纤维的 0.95,平均溶解时间减少了约 7 倍。PXRD 和 DSC 表明制剂中布洛芬呈无定形态,FTIR 光谱表明药物与赋形剂之间没有相互作用。用兔子进行的抗炎研究表明,用纤维制剂治疗的组的爪体积(mm)显著减少(<0.05)。本研究得出结论,离心熔融纺丝制备的微纤维提高了布洛芬的溶解速率和生物利用度。在制剂中加入聚合物可提高微纤维的产率和载药效率。

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