• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

一种新型天然聚合物罗勒(Ocicum)作为固体分散体中溶解度和溶出度增强剂的安全性和药学评价

Safety and Pharmaceutical Evaluation of a Novel Natural Polymer, Ocicum, as Solubility and Dissolution Enhancer in Solid Dispersion.

作者信息

Manzoor Mobina, Raza Syed Atif, Asim Mulazim Hussain, Bukhari Nadeem Irfan, Arshad Shumaila, Zafar Uzma

机构信息

Punjab University College of Pharmacy, University of the Punjab, Lahore 54000, Pakistan.

Institute of Pharmacy, Lahore College for Women University, Lahore 54000, Pakistan.

出版信息

Pharmaceuticals (Basel). 2022 Jul 14;15(7):869. doi: 10.3390/ph15070869.

DOI:10.3390/ph15070869
PMID:35890167
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9321241/
Abstract

Plant mucilages are commonly employed as excipients in pharmaceutical manufacturing. (Lamiaceae family), a source of hydrophilic mucilage referred herein as Ocicum, was evaluated for the solubility enhancer of a model drug, aceclofenac, in solid dispersions prepared using different methods. Polymer was extracted from and solid dispersions of aceclofenac were fabricated with Ocicum or Poloxamer 407 using polymer-to-drug ratios of 1:1, 1:2 and 1:3 utilizing solvent evaporation, lyophilization and melt methods. Ocicum was evaluated for its safety via acute toxicity study including different biochemical and hematological parameters including liver and kidney profiles. Moreover, different characterization studies including melting-point, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and differential thermal analysis (TGA) were used for evaluation of polymer and solid dispersions. Furthermore, solubility and dissolution studies were performed to confirm solubility enhancement. Ocicum was found to be safer, and different characterization studies confirmed the purity of the compounds. In addition, Ocicum exhibited up to 6.27-fold enhanced solubility as compared to pure aceclofenac; similarly, 4.51-fold increased solubility by the synthetic polymer in their respective solid dispersions was shown. Furthermore, Ocicum-based solid dispersions showed substantial improvement in dissolution of aceclofenac. Therefore, it can be concluded from the above-mentioned results that Ocicum might be used as an economical natural oral delivery carrier alternative to the synthetic polymers.

摘要

植物黏液在药物制造中通常用作辅料。对唇形科植物(本文中称为Ocicum,一种亲水性黏液的来源)作为模型药物醋氯芬酸在采用不同方法制备的固体分散体中的增溶剂进行了评估。从Ocicum中提取聚合物,并使用溶剂蒸发、冻干和熔融方法,以聚合物与药物的比例为1:1、1:2和1:3,用Ocicum或泊洛沙姆407制备醋氯芬酸的固体分散体。通过急性毒性研究评估Ocicum的安全性,包括不同的生化和血液学参数,如肝脏和肾脏指标。此外,还使用了不同的表征研究,包括熔点、傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)、扫描电子显微镜(SEM)、差示扫描量热法(DSC)和差热分析(TGA)来评估聚合物和固体分散体。此外,进行了溶解度和溶出度研究以确认溶解度的提高。发现Ocicum更安全,不同的表征研究证实了化合物的纯度。此外,与纯醋氯芬酸相比,Ocicum的溶解度提高了6.27倍;同样,合成聚合物在其各自的固体分散体中的溶解度提高了4.51倍。此外,基于Ocicum的固体分散体显示醋氯芬酸的溶出度有显著改善。因此,从上述结果可以得出结论,Ocicum可能用作合成聚合物的一种经济的天然口服给药载体替代品。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/e364b4663556/pharmaceuticals-15-00869-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/a8cd4c0ad46e/pharmaceuticals-15-00869-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/23f1c3f40504/pharmaceuticals-15-00869-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/255d52d58956/pharmaceuticals-15-00869-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/3749e95df7c4/pharmaceuticals-15-00869-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/897d589626be/pharmaceuticals-15-00869-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/f23b3fef8b44/pharmaceuticals-15-00869-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/e364b4663556/pharmaceuticals-15-00869-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/a8cd4c0ad46e/pharmaceuticals-15-00869-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/23f1c3f40504/pharmaceuticals-15-00869-g002a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/255d52d58956/pharmaceuticals-15-00869-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/3749e95df7c4/pharmaceuticals-15-00869-g004a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/897d589626be/pharmaceuticals-15-00869-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/f23b3fef8b44/pharmaceuticals-15-00869-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7bba/9321241/e364b4663556/pharmaceuticals-15-00869-g007.jpg

相似文献

1
Safety and Pharmaceutical Evaluation of a Novel Natural Polymer, Ocicum, as Solubility and Dissolution Enhancer in Solid Dispersion.一种新型天然聚合物罗勒(Ocicum)作为固体分散体中溶解度和溶出度增强剂的安全性和药学评价
Pharmaceuticals (Basel). 2022 Jul 14;15(7):869. doi: 10.3390/ph15070869.
2
Physicochemical characterization and dissolution study of solid dispersions of Lovastatin with polyethylene glycol 4000 and polyvinylpyrrolidone K30.洛伐他汀与聚乙二醇4000和聚乙烯吡咯烷酮K30固体分散体的物理化学表征及溶出度研究
Pharm Dev Technol. 2007;12(1):21-33. doi: 10.1080/10837450601166510.
3
Physicochemical characterization and in vitro dissolution studies of solid dispersions of ketoprofen with PVP K30 and d-mannitol.酮洛芬与 PVP K30 和 D-甘露醇固体分散体的理化性质表征及体外溶出度研究。
Saudi Pharm J. 2013 Jan;21(1):77-84. doi: 10.1016/j.jsps.2011.12.007. Epub 2011 Dec 24.
4
Determination of Alteration in Micromeritic Properties of a Solid Dispersion: Brunauer-Emmett-Teller Based Adsorption and Other Structured Approaches.测定固体分散体微粉性质的变化:基于 Brunauer-Emmett-Teller 的吸附和其他结构方法。
AAPS PharmSciTech. 2022 Jul 28;23(6):209. doi: 10.1208/s12249-022-02367-w.
5
Selection of the suitable polymer for supercritical fluid assisted preparation of carvedilol solid dispersions.选择合适的聚合物用于超临界流体辅助制备卡维地洛固体分散体。
Int J Pharm. 2019 Jan 10;554:190-200. doi: 10.1016/j.ijpharm.2018.11.015. Epub 2018 Nov 8.
6
Effect of excipients on dissolution enhancement of aceclofenac solid dispersions studied using response surface methodology: a technical note.采用响应面法研究辅料对醋氯芬酸固体分散体溶出度增强的影响:技术说明
Arch Pharm Res. 2014 Mar;37(3):340-51. doi: 10.1007/s12272-013-0146-y. Epub 2013 May 15.
7
Preparation, characterization and in vitro/vivo evaluation of tectorigenin solid dispersion with improved dissolution and bioavailability.具有改善溶出度和生物利用度的鸢尾黄素固体分散体的制备、表征及体内外评价
Eur J Drug Metab Pharmacokinet. 2016 Aug;41(4):413-22. doi: 10.1007/s13318-015-0265-6. Epub 2015 Feb 11.
8
Physicochemical characterization of solid dispersions of three antiepileptic drugs prepared by solvent evaporation method.采用溶剂蒸发法制备的三种抗癫痫药物固体分散体的物理化学表征
J Pharm Pharmacol. 2007 May;59(5):645-53. doi: 10.1211/jpp.59.5.0004.
9
Physicochemical properties of tadalafil solid dispersions - Impact of polymer on the apparent solubility and dissolution rate of tadalafil.他达拉非固体分散体的物理化学性质——聚合物对他达拉非表观溶解度和溶出速率的影响。
Eur J Pharm Biopharm. 2015 Aug;94:106-15. doi: 10.1016/j.ejpb.2015.04.031. Epub 2015 May 19.
10
Application of Solid Dispersion Technique to Improve Solubility and Sustain Release of Emamectin Benzoate.固体分散技术在提高甲氨基阿维菌素苯甲酸盐溶解度和持续释放中的应用。
Molecules. 2019 Nov 26;24(23):4315. doi: 10.3390/molecules24234315.

引用本文的文献

1
Recent Patents on Solid Dispersions Emphasize Promising Benefits in Solubility Enhancement of Poorly Water-soluble Drugs.固体分散体的最新专利强调了在提高难溶性药物溶解度方面的显著优势。
Recent Pat Nanotechnol. 2025;19(2):216-240. doi: 10.2174/0118722105229356231030065938.
2
Effects of Larrea nitida nanodispersions on the growth inhibition of phytopathogens.亮叶拉瑞阿纳米分散体对植物病原体生长抑制的影响。
AMB Express. 2023 Sep 21;13(1):98. doi: 10.1186/s13568-023-01605-z.

本文引用的文献

1
Amelioration of physicochemical, pharmaceutical, and pharmacokinetic properties of lornoxicam by cocrystallization with a novel coformer.通过与新共晶形成剂共结晶改善洛索洛芬的物理化学、药物和药代动力学性质。
Drug Dev Ind Pharm. 2021 Mar;47(3):498-508. doi: 10.1080/03639045.2021.1892744. Epub 2021 Mar 1.
2
In-Vitro and In-Vivo Evaluation of Velpatasvir- Loaded Mesoporous Silica Scaffolds. A Prospective Carrier for Drug Bioavailability Enhancement.载有维帕他韦的介孔二氧化硅支架的体外和体内评价。一种提高药物生物利用度的潜在载体。
Pharmaceutics. 2020 Mar 28;12(4):307. doi: 10.3390/pharmaceutics12040307.
3
Spray-Dried Amorphous Solid Dispersions of Griseofulvin in HPC/Soluplus/SDS: Elucidating the Multifaceted Impact of SDS as a Minor Component.
灰黄霉素在羟丙基纤维素/聚乙烯己内酰胺/十二烷基硫酸钠中的喷雾干燥无定形固体分散体:阐明十二烷基硫酸钠作为次要成分的多方面影响
Pharmaceutics. 2020 Feb 25;12(3):197. doi: 10.3390/pharmaceutics12030197.
4
Silymarin-laden PVP-PEG polymeric composite for enhanced aqueous solubility and dissolution rate: Preparation and in vitro characterization.用于提高水溶性和溶解速率的载水飞蓟素PVP-PEG聚合物复合材料:制备与体外表征
J Pharm Anal. 2019 Feb;9(1):34-39. doi: 10.1016/j.jpha.2018.09.003. Epub 2018 Sep 19.
5
Applying Supercritical Fluid Technology to Prepare Ibuprofen Solid Dispersions with Improved Oral Bioavailability.应用超临界流体技术制备具有改善口服生物利用度的布洛芬固体分散体。
Pharmaceutics. 2019 Feb 3;11(2):67. doi: 10.3390/pharmaceutics11020067.
6
Electrospun amorphous solid dispersions of poorly water-soluble drugs: A review.静电纺丝技术制备的难溶性药物无定形固体分散体:综述
J Control Release. 2018 Dec 28;292:91-110. doi: 10.1016/j.jconrel.2018.08.016. Epub 2018 Aug 14.
7
Extraction optimization of mucilage from Basil ( L.) seeds using response surface methodology.采用响应面法优化罗勒籽黏液质的提取工艺
J Adv Res. 2017 May;8(3):235-244. doi: 10.1016/j.jare.2017.01.003. Epub 2017 Feb 2.
8
Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407.使用嵌段共聚物泊洛沙姆407提高布洛芬溶解度和溶解速率的融合方法
AAPS PharmSciTech. 2016 Dec;17(6):1428-1440. doi: 10.1208/s12249-016-0482-6. Epub 2016 Jan 27.
9
Formulation and Characterization of Solid Dispersion Prepared by Hot Melt Mixing: A Fast Screening Approach for Polymer Selection.热熔混合法制备固体分散体的处方设计与表征:聚合物选择的快速筛选方法
J Pharm (Cairo). 2014;2014:105382. doi: 10.1155/2014/105382. Epub 2014 Mar 12.
10
Practical murine hematopathology: a comparative review and implications for research.实用小鼠血液病理学:比较性综述及其对研究的启示
Comp Med. 2015 Apr;65(2):96-113.