塞来昔布负载羟丙基甲基纤维素(HPMC)微粒体内模型的配方开发及药动学评价。

IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Khuram Shahazad, Syed Umer Jan, Rahman Gul, Mahjabeen Tafazzul, Safia Mengal, Falsafa Jamal, Nayab Iqbal
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引用次数: 0

摘要

本研究旨在利用羟丙基甲基纤维素(HPMC)制备塞来昔布负载微颗粒,用于靶向递送到结肠。塞来昔布治疗结直肠癌(CRC)相关疼痛和炎症的有效性受到其低溶解度和胃肠道副作用的影响。采用乳化溶剂蒸发(ESE)油中油技术合成了17个配方。通过傅里叶变换红外光谱、x射线衍射、扫描电镜和差示扫描量热分析了配方的理化性质;以家兔为生物样本,在家兔血浆中进行体内药代动力学评价。将塞来昔布纯药F1和F2一次性给予家兔进行药代动力学评价。f1的平均粒径为497.93μm, f2的平均粒径为497.93μm。体外24h累积释放率F1为88.77%,F2为88.85%。FTIR分析证实了配方成分的相容性,XRD显示了塞来昔布从结晶到非晶的转变,DSC显示了配方的热稳定性,SEM图像显示了致密的球形微粒。考虑到这些因素,使用HPMC微颗粒携带塞来昔布可以增强药物在体内的传递和释放,可能获得有效的治疗,副作用更少。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation development and pharmacokinetic evaluation of celecoxib loaded hydroxyl propyl methyl cellulose (HPMC) microparticles in in-vivo model.

This investigation aimed to formulate Celecoxib-loaded microparticles for targeted delivery to the colon, employing Hydroxypropylmethylcellulose (HPMC). Celecoxib's effectiveness in managing colorectal cancer (CRC)-related pain and inflammation is compromised by its low solubility and gastrointestinal side effects. A total of seventeen formulations were synthesized through emulsion solvent evaporation (ESE) oil-in-oil technique. The physicochemical properties of the formulations were analyzed through Fourier Transform Infrared Spectroscopy, X-ray Diffraction, Scanning Electron Microscopy and Differential Scanning Calorimetry; however, rabbits served as the biological specimens in the in vivo pharmacokinetic evaluation in Rabbits plasma. Celecoxib pure drug, F1 and F2 were given to the rabbits one time dose to assess the pharmacokinetics evaluation. The average particle size for F 1 was 497.93μm and 497.93 μm for F 2. In vitro showed cumulative release rates of 88.77% for F1 and 88.85% F2 after 24 hours. FTIR analysis confirmed the compatibility of the formulation ingredients, XRD revealed a transition of Celecoxib from its crystalline to amorphous form, DSC indicated the formulations' thermal stability and SEM images showed dense, spherical microparticles. Given these factors, using HPMC micro particles to carry Celecoxib could enhance the drug delivery and released in the body and may result effective treatment with fewer side effects.

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来源期刊
CiteScore
1.40
自引率
12.50%
发文量
211
审稿时长
4.5 months
期刊介绍: Pakistan Journal of Pharmaceutical Sciences (PJPS) is a peer reviewed multi-disciplinary pharmaceutical sciences journal. The PJPS had its origin in 1988 from the Faculty of Pharmacy, University of Karachi as a biannual journal, frequency converted as quarterly in 2005, and now PJPS is being published as bi-monthly from January 2013. PJPS covers Biological, Pharmaceutical and Medicinal Research (Drug Delivery, Pharmacy Management, Molecular Biology, Biochemical, Pharmacology, Pharmacokinetics, Phytochemical, Bio-analytical, Therapeutics, Biotechnology and research on nano particles.
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