• 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

将纤维素衍生物的特性粘数与溶胀亲水性基质片剂的机械敏感性相关联。

Correlating cellulose derivative intrinsic viscosity with mechanical susceptibility of swollen hydrophilic matrix tablets.

机构信息

Lek Pharmaceuticals d.d, Verovškova 57, 1526, Ljubljana, Slovenia.

出版信息

AAPS PharmSciTech. 2012 Sep;13(3):903-10. doi: 10.1208/s12249-012-9811-6. Epub 2012 Jun 19.

DOI:10.1208/s12249-012-9811-6
PMID:22711256
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3429674/
Abstract

Hydrophilic matrix tablets are prone to mechanical stress while passing through the gastrointestinal tract, which may result in inappropriate drug-release characteristics. Intrinsic viscosity is a physical polymer property that can be directly compared across various types and grades of polymers and correlated with the mechanical susceptibility of swollen matrix tablets. Five tablet formulations containing different HPMC and HPC polymers were prepared and analyzed using an in vitro glass bead manipulation test. The dissolution rate results were modeled using the Korsmeyer-Peppas equation and a correlation was found between the fit constants k and n, goodness-of-fit measure parameters, and intrinsic viscosity. Moreover, the dissolution profiles were used to calculate the degree of mechanical susceptibility for each formulation, defined as the ratio of the average dissolution rate after manipulation and the initial dissolution rate before manipulation. It was confirmed that an increased intrinsic viscosity polymer value resulted in a decrease in mechanical susceptibility. Considering this, two simple rules were defined for designing robust matrix tablets with respect to mechanical stresses.

摘要

亲水基质片剂在通过胃肠道时容易受到机械应力的影响,这可能导致药物释放特性不合适。特性黏度是一种物理聚合物性质,可以在不同类型和等级的聚合物之间直接比较,并与溶胀基质片剂的机械敏感性相关。制备了包含不同 HPMC 和 HPC 聚合物的五种片剂配方,并使用体外玻璃珠操作测试进行了分析。使用 Korsmeyer-Peppas 方程对溶出速率结果进行建模,并发现拟合常数 k 和 n、拟合度参数以及特性黏度之间存在相关性。此外,还使用溶出曲线计算了每个配方的机械敏感性程度,定义为操作后平均溶出速率与操作前初始溶出速率的比值。证实了聚合物特性黏度值的增加会导致机械敏感性降低。考虑到这一点,针对机械应力,定义了两个设计稳健基质片剂的简单规则。

相似文献

1
Correlating cellulose derivative intrinsic viscosity with mechanical susceptibility of swollen hydrophilic matrix tablets.将纤维素衍生物的特性粘数与溶胀亲水性基质片剂的机械敏感性相关联。
AAPS PharmSciTech. 2012 Sep;13(3):903-10. doi: 10.1208/s12249-012-9811-6. Epub 2012 Jun 19.
2
In vitro release of ketoprofen from hydrophilic matrix tablets containing cellulose polymer mixtures.含纤维素聚合物混合物的亲水基质片剂中酮洛芬的体外释放。
Drug Dev Ind Pharm. 2013 Nov;39(11):1651-62. doi: 10.3109/03639045.2012.729146. Epub 2012 Oct 24.
3
Determining the polymer threshold amount for achieving robust drug release from HPMC and HPC matrix tablets containing a high-dose BCS class I model drug: in vitro and in vivo studies.确定从含有高剂量BCS I类模型药物的羟丙基甲基纤维素(HPMC)和羟丙基纤维素(HPC)基质片剂中实现稳健药物释放的聚合物阈值量:体外和体内研究
AAPS PharmSciTech. 2015 Apr;16(2):398-406. doi: 10.1208/s12249-014-0234-4. Epub 2014 Oct 18.
4
Release Kinetics of Hydroxypropyl Methylcellulose Governing Drug Release and Hydrodynamic Changes of Matrix Tablet.羟丙基甲基纤维素的释放动力学及其对基质片剂药物释放和流体动力学变化的影响。
Curr Drug Deliv. 2022;19(5):520-533. doi: 10.2174/1567201818666210820101549.
5
The effect of substitution pattern of HPMC on polymer release from matrix tablets.HPMC 取代模式对骨架片中聚合物释放的影响。
Int J Pharm. 2010 Apr 15;389(1-2):147-56. doi: 10.1016/j.ijpharm.2010.01.029. Epub 2010 Jan 25.
6
Formulating Amorphous Solid Dispersions: Impact of Inorganic Salts on Drug Release from Tablets Containing Itraconazole-HPMC Extrudate.无定形固体分散体的制定:无机盐对含伊曲康唑-HPMC 挤出物片剂中药物释放的影响。
Mol Pharm. 2020 Aug 3;17(8):2768-2778. doi: 10.1021/acs.molpharmaceut.9b01109. Epub 2020 Jul 21.
7
Interaction between fed gastric media (Ensure Plus®) and different hypromellose based caffeine controlled release tablets: comparison and mechanistic study of caffeine release in fed and fasted media versus water using the USP dissolution apparatus 3.进食状态下胃内介质(安素益加®)与不同羟丙甲纤维素基咖啡因控释片之间的相互作用:使用美国药典溶出度仪3对进食和空腹状态下介质与水中咖啡因释放情况的比较及机理研究
Int J Pharm. 2014 Jan 30;461(1-2):419-26. doi: 10.1016/j.ijpharm.2013.12.003. Epub 2013 Dec 14.
8
FORMULATION, EVALUATION AND IN VITRO DISSOLUTION PERFORMANCE OF ENALAPRIL MALEATE SUSTAINED RELEASE MATRICES: EFFECT OF POLYMER COMPOSITION AND VISCOSITY GRADE.马来酸依那普利缓释基质的处方、评价及体外溶出性能:聚合物组成和黏度等级的影响
Acta Pol Pharm. 2016 Jul;73(4):1037-1043.
9
Study the effect of formulation variables on drug release from hydrophilic matrix tablets of milnacipran and prediction of in-vivo plasma profile.研究制剂变量对米那普仑亲水基质片药物释放的影响及体内血浆浓度预测。
Pharm Dev Technol. 2014 Sep;19(6):708-16. doi: 10.3109/10837450.2013.823993. Epub 2013 Aug 12.
10
Study of the critical points and the role of the pores and viscosity in carbamazepine hydrophilic matrix tablets.卡马西平亲水骨架片的关键点、孔和粘度的作用研究。
Eur J Pharm Biopharm. 2012 Jan;80(1):136-42. doi: 10.1016/j.ejpb.2011.09.007. Epub 2011 Sep 17.

引用本文的文献

1
A Rational Approach to Predicting Immediate Release Formulation Behavior in Multiple Gastric Motility Patterns: A Combination of a Biorelevant Apparatus, Design of Experiments, and Machine Learning.预测多种胃动力模式下速释制剂行为的合理方法:生物相关性装置、实验设计和机器学习的结合
Pharmaceutics. 2023 Jul 31;15(8):2056. doi: 10.3390/pharmaceutics15082056.
2
Improved functionality of Ligilactobacillus salivarius Li01 in alleviating colonic inflammation by layer-by-layer microencapsulation.通过层层微囊化提高唾液乳杆菌 Li01 缓解结肠炎症的功能。
NPJ Biofilms Microbiomes. 2021 Jul 9;7(1):58. doi: 10.1038/s41522-021-00228-1.
3
Gel Strength of Hydrophilic Matrix Tablets in Terms of In Vitro Robustness.水凝胶基质片剂的体外稳定性与凝胶强度的关系。
Pharm Res. 2021 Jul;38(7):1297-1306. doi: 10.1007/s11095-021-03068-y. Epub 2021 Jun 21.
4
Determining the polymer threshold amount for achieving robust drug release from HPMC and HPC matrix tablets containing a high-dose BCS class I model drug: in vitro and in vivo studies.确定从含有高剂量BCS I类模型药物的羟丙基甲基纤维素(HPMC)和羟丙基纤维素(HPC)基质片剂中实现稳健药物释放的聚合物阈值量:体外和体内研究
AAPS PharmSciTech. 2015 Apr;16(2):398-406. doi: 10.1208/s12249-014-0234-4. Epub 2014 Oct 18.
5
A novel beads-based dissolution method for the in vitro evaluation of extended release HPMC matrix tablets and the correlation with the in vivo data.一种基于新型珠体的溶出度方法,用于评估 HPMC 骨架片的体外释放度,并与体内数据相关联。
AAPS J. 2013 Jan;15(1):267-77. doi: 10.1208/s12248-012-9422-x. Epub 2012 Nov 28.

本文引用的文献

1
Thermo sensitive behavior of cellulose derivatives in dilute aqueous solutions: from macroscopic to mesoscopic scale.纤维素衍生物在稀水溶液中的热敏行为:从宏观到介观尺度。
J Colloid Interface Sci. 2011 May 15;357(2):372-8. doi: 10.1016/j.jcis.2011.02.041. Epub 2011 Feb 22.
2
Physiological parameters for oral delivery and in vitro testing.口服给药和体外测试的生理参数。
Mol Pharm. 2010 Oct 4;7(5):1388-405. doi: 10.1021/mp100149j. Epub 2010 Sep 7.
3
Magnetic marker monitoring: high resolution real-time tracking of oral solid dosage forms in the gastrointestinal tract.磁标记监测:胃肠道内口服固体制剂的高分辨率实时跟踪。
Eur J Pharm Biopharm. 2010 Jan;74(1):93-101. doi: 10.1016/j.ejpb.2009.07.007. Epub 2009 Jul 18.
4
Assessing gastrointestinal motility and disintegration profiles of magnetic tablets by a novel magnetic imaging device and gamma scintigraphy.用新型磁成像设备和γ闪烁成像评估磁性片剂的胃肠动力和崩解特性。
Eur J Pharm Biopharm. 2010 Jan;74(1):84-92. doi: 10.1016/j.ejpb.2009.01.004. Epub 2009 Jan 20.
5
Gut instincts: explorations in intestinal physiology and drug delivery.直觉:肠道生理学与药物递送探索
Int J Pharm. 2008 Dec 8;364(2):213-26. doi: 10.1016/j.ijpharm.2008.05.012. Epub 2008 May 20.
6
Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses.使用模拟体内物理应力的溶出度试验装置,可以预测双氯芬酸缓释片的不规则吸收曲线。
Eur J Pharm Biopharm. 2008 Oct;70(2):421-8. doi: 10.1016/j.ejpb.2008.05.029. Epub 2008 Jun 7.
7
Statistical evaluation of influence of viscosity and content of polymer on dipyridamole release from floating matrix tablets: a technical note.聚合物粘度和含量对双嘧达莫从漂浮型骨架片中释放影响的统计评估:技术说明
AAPS PharmSciTech. 2007 Aug 24;8(3):E69. doi: 10.1208/pt0803069.
8
A framework to investigate drug release variability arising from hypromellose viscosity specifications in controlled release matrix tablets.一种用于研究控释基质片剂中羟丙甲纤维素粘度规格引起的药物释放变异性的框架。
J Pharm Sci. 2008 Jun;97(6):2277-85. doi: 10.1002/jps.21145.
9
A novel in vitro and numerical analysis of shear-induced drug release from extended-release tablets in the fed stomach.进食状态下胃中缓释片中剪切诱导药物释放的新型体外及数值分析
Pharm Res. 2005 Aug;22(8):1215-26. doi: 10.1007/s11095-005-5272-x. Epub 2005 Aug 3.
10
Quantitative evaluation of polymer concentration profile during swelling of hydrophilic matrix tablets using 1H NMR and MRI methods.使用¹H NMR和MRI方法对亲水性基质片剂溶胀过程中聚合物浓度分布进行定量评估。
Eur J Pharm Biopharm. 2005 Feb;59(2):299-306. doi: 10.1016/j.ejpb.2004.08.010.