The present study explored the effect of co-amorphous technology in improving the dissolution rate and stability of silybin based on the puerarin-silybin co-amorphous system prepared by the spray-drying method. Solid-state characterization was carried out by powder X-ray diffraction(PXRD), polarizing microscopy(PLM), Fourier transform infrared spectroscopy(FT-IR), differential scanning calorimetry(DSC), etc. Saturated powder dissolution, intrinsic dissolution rate, moisture absorption, and stability were further investigated. The results showed that puerarin and silybin formed a co-amorphous system at a single glass transition temperature which was higher than that of any crude drug. The intrinsic dissolution rate and supersaturated powder dissolution of silybin in the co-amorphous system were higher than those of the crude drug and amorphous system. The co-amorphous system kept stable for as long as three months under the condition of 40 ℃, 75% relative humidity, which was longer than that of the single amorphous silybin. Therefore, the co-amorphous technology could significantly improve the dissolution and stability of silybin.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.19540/j.cnki.cjcmm.20210511.301 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
A drug-drug co-amorphous system for highly improved solubility of breviscapine: an experimental and computational study.
Sci Rep
December 2024
College of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming, 650500, China.
Drug-drug co-amorphous systems are a promising approach to improve the aqueous solubility of poorly water-soluble drugs. This study explores the combination of breviscapine (BRE) and matrine (MAT) form an amorphous salt, aiming to synergistically enhance the solubility and dissolution of BRE. In silico analysis of electrostatic potential and local ionization energy were conducted on BRE-MAT complex to predict the intermolecular interactions, and solvent-free energies were calculated using thermodynamic integration and density functional theory.
View Article and Find Full Text PDFBreaking barriers: enhancing solubility and dissolution of efonidipine using co-amorphous formulations.
Naunyn Schmiedebergs Arch Pharmacol
November 2024
School of Pharmacy, RK University, Kasturbadham, Rajkot, Gujarat, 360020, India.
The study aims to enhance the solubility and dissolution characteristics of efonidipine hydrochloride ethanolate (EFD), an antihypertensive drug, through the co-amorphous approach. Hypertension is a prevalent chronic condition characterized by consistently elevated blood pressure. Efonidipine, a BCS class II drug, has high permeability but low solubility, limiting its therapeutic effectiveness.
View Article and Find Full Text PDFValsartan/2-Aminopyridine Co-Amorphous System: Preparation, Characterization, and Supramolecular Structure Simulation by Density Functional Theory Calculation.
Molecules
November 2024
School of Chemical Engineering, Shandong Institute of Petroleum and Chemical Technology, Dongying 257061, China.
The objective of this work was to improve the solubility and discover a stable co-amorphous form of valsartan (VAL), a BCS class-II drug, by utilizing small molecule 2-Aminopyridine (2-AP) in varying molar ratios (2:1, 1:1, and 1:2), employing a solvent evaporation technique. Additionally, by way of a density functional theory (DFT)-based computational method with commercially available software, a new approach for determining the intermolecular connectivity of multi-molecular hydrogen bonding systems was proposed. The binary systems' features were characterized by PXRD, DSC, FTIR, and Raman spectroscopy, while the equilibrium solubility and dissolution was determined in 0.
View Article and Find Full Text PDF"Aging" in co-amorphous systems: Dissolution decrease and non-negligible dissolution increase during storage without recrystallization.
Int J Pharm
December 2024
Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, Zhejiang, China; Wenzhou Institute, University of Chinese Academy of Science, Wenzhou 325024, Zhejiang, China. Electronic address:
Developing co-amorphous systems is a promising strategy to improve the water solubility of poorly water-soluble drugs. Most of the studies focused on the initial dissolution rate of the fresh co-amorphous systems, and only physical stability was investigated after storage. However, the maintenance of the enhanced dissolution rate of co-amorphous systems after storage is necessary for further product development.
View Article and Find Full Text PDFEvaluation of aspartame as a co-former in the preparation of co-amorphous formulations of dipyridamole using spray drying.
Int J Pharm
December 2024
Pharmaceutical and Molecular Biotechnology Research Centre, South East Technological University, Waterford, Ireland; SSPC, The Research Ireland Centre for Pharmaceuticals, South East Technological University, Waterford, Ireland. Electronic address:
Article Synopsis
- Co-amorphous systems (CAMs) can improve the solubility of poorly water-soluble drugs, but challenges like a limited number of co-formers and lab-scale preparation techniques exist.
- This study uses aspartame and dipyridamole to create CAMs through spray drying, showing that AspPhe has better solid-state properties and physical stability than individual amino acids.
- Molecular interactions analyzed by Hirshfeld Surface analysis and FT-IR spectroscopy demonstrate that hydrogen bond interactions significantly enhance the stability of the DPM-AspPhe co-amorphous system, while crystallization rates are affected by temperature and humidity.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!