Suppr超能文献

弱碱性药物与酸性共形成物的共晶体如何调节溶解度和稳定性。

How cocrystals of weakly basic drugs and acidic coformers might modulate solubility and stability.

作者信息

Kuminek G, Rodríguez-Hornedo N, Siedler S, Rocha H V A, Cuffini S L, Cardoso S G

机构信息

Department of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI, USA.

出版信息

Chem Commun (Camb). 2016 Apr 30;52(34):5832-5. doi: 10.1039/c6cc00898d. Epub 2016 Apr 4.

Abstract

Cocrystals of a weakly basic drug (nevirapine) with acidic coformers are shown to alter the solubility dependence on pH, and to exhibit a pHmax above which a less soluble cocrystal becomes more soluble than the drug. The cocrystal solubility advantage can be dialed up or down by solution pH.

摘要

一种弱碱性药物(奈韦拉平)与酸性共形成物的共晶体被证明会改变溶解度对pH值的依赖性,并表现出一个pH最大值,高于该值时,溶解度较低的共晶体比药物更易溶解。共晶体的溶解度优势可通过溶液pH值进行调节。

相似文献

1
How cocrystals of weakly basic drugs and acidic coformers might modulate solubility and stability.
Chem Commun (Camb). 2016 Apr 30;52(34):5832-5. doi: 10.1039/c6cc00898d. Epub 2016 Apr 4.
2
Mechanistic Basis of Cocrystal Dissolution Advantage.
J Pharm Sci. 2018 Jan;107(1):380-389. doi: 10.1016/j.xphs.2017.09.014. Epub 2017 Oct 6.
3
Mechanistic Analysis of Cocrystal Dissolution as a Function of pH and Micellar Solubilization.
Mol Pharm. 2016 Mar 7;13(3):1030-46. doi: 10.1021/acs.molpharmaceut.5b00862. Epub 2016 Feb 15.
4
pH-dependent solubility of indomethacin-saccharin and carbamazepine-saccharin cocrystals in aqueous media.
Mol Pharm. 2012 Sep 4;9(9):2605-12. doi: 10.1021/mp300189b. Epub 2012 Aug 23.
5
Cocrystal solubility product analysis - Dual concentration-pH mass action model not dependent on explicit solubility equations.
Eur J Pharm Sci. 2017 Dec 15;110:2-18. doi: 10.1016/j.ejps.2017.03.049. Epub 2017 Apr 6.
6
Understanding the Differences Between Cocrystal and Salt Aqueous Solubilities.
J Pharm Sci. 2018 Jan;107(1):113-120. doi: 10.1016/j.xphs.2017.10.033. Epub 2017 Oct 31.
7
Cocrystals Mitigate Negative Effects of High pH on Solubility and Dissolution of a Basic Drug.
Cryst Growth Des. 2018 Mar 7;18(3):1358-1366. doi: 10.1021/acs.cgd.7b01206. Epub 2018 Feb 14.
9
Design of nevirapine derivatives insensitive to the K103N and Y181C HIV-1 reverse transcriptase mutants.
SAR QSAR Environ Res. 2006 Apr;17(2):183-94. doi: 10.1080/10659360600636147.
10
Crystal engineering of stable temozolomide cocrystals.
Chem Asian J. 2012 Oct;7(10):2274-85. doi: 10.1002/asia.201200205. Epub 2012 May 21.

引用本文的文献

1
Discovery of Cilnidipine Cocrystals with Enhanced Dissolution by the Use of Computational Tools and Semiautomatic High-Throughput Screening.
Cryst Growth Des. 2025 Apr 29;25(10):3374-3385. doi: 10.1021/acs.cgd.5c00184. eCollection 2025 May 21.
2
Virtual Screening, Structural Analysis, and Formation Thermodynamics of Carbamazepine Cocrystals.
Pharmaceutics. 2023 Mar 3;15(3):836. doi: 10.3390/pharmaceutics15030836.
4
Continuous Manufacture and Scale-Up of Theophylline-Nicotinamide Cocrystals.
Pharmaceutics. 2021 Mar 20;13(3):419. doi: 10.3390/pharmaceutics13030419.
5
Potential Anti-Tumor Drug: Co-Crystal 5-Fluorouracil-nicotinamide.
ACS Omega. 2020 Jun 24;5(26):15777-15782. doi: 10.1021/acsomega.9b03574. eCollection 2020 Jul 7.
6
Multidrug Cocrystal of Anticonvulsants: Influence of Strong Intermolecular Interactions on Physiochemical Properties.
Cryst Growth Des. 2017 Oct 4;17(10):5012-5016. doi: 10.1021/acs.cgd.7b00741. Epub 2017 Sep 8.
7
Cocrystals Mitigate Negative Effects of High pH on Solubility and Dissolution of a Basic Drug.
Cryst Growth Des. 2018 Mar 7;18(3):1358-1366. doi: 10.1021/acs.cgd.7b01206. Epub 2018 Feb 14.
9
Understanding the Differences Between Cocrystal and Salt Aqueous Solubilities.
J Pharm Sci. 2018 Jan;107(1):113-120. doi: 10.1016/j.xphs.2017.10.033. Epub 2017 Oct 31.
10
Mechanistic Basis of Cocrystal Dissolution Advantage.
J Pharm Sci. 2018 Jan;107(1):380-389. doi: 10.1016/j.xphs.2017.09.014. Epub 2017 Oct 6.

本文引用的文献

1
Cocrystal Solubilization in Biorelevant Media and its Prediction from Drug Solubilization.
J Pharm Sci. 2015 Dec;104(12):4153-4163. doi: 10.1002/jps.24640. Epub 2015 Sep 21.
2
Cocrystal Transition Points: Role of Cocrystal Solubility, Drug Solubility, and Solubilizing Agents.
Mol Pharm. 2015 Oct 5;12(10):3535-46. doi: 10.1021/acs.molpharmaceut.5b00111. Epub 2015 Aug 28.
3
Thermodynamic Solubility Profile of Carbamazepine-Cinnamic Acid Cocrystal at Different pH.
J Pharm Sci. 2015 Aug;104(8):2559-65. doi: 10.1002/jps.24525. Epub 2015 Jun 10.
4
pH-dependent solubility of indomethacin-saccharin and carbamazepine-saccharin cocrystals in aqueous media.
Mol Pharm. 2012 Sep 4;9(9):2605-12. doi: 10.1021/mp300189b. Epub 2012 Aug 23.
5
Engineering cocrystal solubility, stability, and pH(max) by micellar solubilization.
J Pharm Sci. 2011 Dec;100(12):5219-34. doi: 10.1002/jps.22725. Epub 2011 Sep 9.
6
Solid-state characterization of nevirapine.
Indian J Pharm Sci. 2008 Sep;70(5):619-30. doi: 10.4103/0250-474X.45401.
7
Solubility of sparingly-soluble ionizable drugs.
Adv Drug Deliv Rev. 2007 Jul 30;59(7):568-90. doi: 10.1016/j.addr.2007.05.008. Epub 2007 May 29.
8
Salt formation to improve drug solubility.
Adv Drug Deliv Rev. 2007 Jul 30;59(7):603-16. doi: 10.1016/j.addr.2007.05.010. Epub 2007 May 29.
9
Nonnucleoside inhibitors of HIV-1 reverse transcriptase: nevirapine as a prototype drug.
AIDS Res Hum Retroviruses. 1992 Feb;8(2):145-52. doi: 10.1089/aid.1992.8.145.

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验