新型固体自乳化给药系统,提高乳香和没药超临界流体提取物的物理性能和生物利用度

IF 4.5 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Wansi Li , Panwen Huang , Xianghuan Sun , Yongtai Zhang , Ying Liu , Nianping Feng , Zhi Wang
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引用次数: 0

摘要

乳香和没药是常用的中药,临床研究表明,两者联合应用对炎症和肿瘤有很好的治疗效果。本研究将乳香没药超临界流体萃取物(SFE-FM)制备成乳香没药固体自乳化给药系统(FM - sedds)微型片剂。以SFE-FM为主油相,采用拟三元相图和中心复合设计筛选自微乳。以Neusilin为载体和包衣材料,HPMC K100M为基质材料制备缓释微型片剂。采用扫描电镜(SEM)、差示扫描量热法(DSC)、傅里叶变换红外(FTIR)等表征技术对其进行表征,并对其抗拉强度(TS)、含量均匀性、体外释放度和体内药代动力学进行评价。sem - sedds的平均粒径为22.36 nm,多分散性指数(PDI)为0.23,zeta电位为- 1.66 mV,室温下性能稳定30 d。它表现出合适的压片性能,包括流动性、压缩性和相容性,同时保留了其自微乳化能力。体外实验证实,与空白片相比,乙酰-11-酮-β-乳香酸(AKBA)、β-乳香酸(β-BA)和β-柠檬酸(β-EA)完全释放。Beagle犬的药代动力学结果表明,三种活性成分具有显著的缓释作用,且具有较强的体内外相关性(IVIVC)。SEDDS技术可提高SFE-FM等脂溶性药物的口服生物利用度,具有广阔的工业应用潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel solid self-emulsifying drug delivery system to improve the physical performance and bioavailability of supercritical fluid extracts of frankincense and myrrh
Frankincense and myrrh are commonly used in traditional Chinese medicines, and clinical studies have shown that their combined application has a good therapeutic effect on inflammation and tumors. In this study, the supercritical fluid extract of frankincense and myrrh (SFE-FM) was prepared into frankincense and myrrh solid self-emulsifying drug delivery system (FM S-SEDDS) mini-tablets. SFE-FM was used as the main oil phase, and the self-microemulsion was screened using a pseudo-ternary phase diagram and a central composite design. Neusilin was used as the carrier and coating material, with HPMC K100M serving as the matrix material to prepare the sustained-release mini-tablets. Characterization techniques, including scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared (FTIR) analysis, assessed the FM-SEDDS powders, with evaluations of tensile strength (TS), content uniformity, in vitro release, and in vivo pharmacokinetic conducted on the tablets. The FM-SEDDS had an average particle size of 22.36 nm, a polydispersity index (PDI) of 0.23, and a zeta potential of −1.66 mV, with stable properties for 30 d room temperature. It demonstrated suitable tableting properties, including flow, compressibility, and compatibility, while retaining its self-microemulsifying capabilities. In vitro testing confirmed complete release of acetyl-11-keto-β-boswellic acid (AKBA), β-boswellic acid (β-BA), and β-elemonic acid (β-EA) compared to blank tablets. Pharmacokinetic results in Beagle dogs indicated a significant sustained-release effect for the three active ingredients with a strong in vitroin vivo correlation (IVIVC). SEDDS technology can improve the oral bioavailability of liposoluble drugs like SFE-FM, offering promising industrial application potential.
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来源期刊
CiteScore
8.00
自引率
8.00%
发文量
879
审稿时长
94 days
期刊介绍: The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.
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