Summary of - Raloxifene HCl – Quercetin Co-amorphous System

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Article

Abstract

Study Background: The research titled "Raloxifene HCl–quercetin co-amorphous system: preparation, characterization, and investigation of its behavior in phosphate buffer" by Dr Bhat and team focuses on modifying the molecular structure of Raloxifene HCl (RLX), a drug used for treating osteoporosis in post-menopausal women, to enhance its solubility using co-amorphous technology.

Research Goals and Hypotheses: The primary aim is to improve the solubility and concentration of RLX through co-amorphization with Quercetin (QCT), utilizing various preparation techniques.

Methodological Approach:

  1. Preparation Techniques: RLX was co-amorphized with QCT using solvent evaporation (SE), quench cooling (QC), and ball milling (BM) techniques.
  2. Characterization: The co-amorphous systems (CAMs) were characterized using X-ray Diffraction (XRD), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FT-IR).
  3. Quantification: A Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) method was developed to quantify RLX and QCT in the prepared systems.
  4. Behavior Analysis: The behavior in aqueous media was analyzed by studying amorphous and equilibrium solubility, and drug release of RLX using USP phosphate buffer pH 6.8.

Results and Discoveries:

  1. Homogeneous System: Solvent evaporation (RQ(SE)) produced a homogeneous system, while quench cooling led to thermal degradation, and ball milling failed to amorphize the blend.
  2. Thermal Properties: DSC results indicated that RQ(SE) increased the glass transition temperature by 40°C.
  3. Solubility and Aggregation: Solubility of RLX reduced due to the formation of phosphate aggregates, which further complexed with QCT, as determined by residual particle analysis from solubility studies.
  4. Drug Release: Despite reduced solubility, the drug release study showed that RQ(SE) improved RLX concentration by 2.3 times.

Conclusions: The solvent evaporation method (RQ(SE)) successfully formed a stable co-amorphous system. Although the solubility of RLX in the presence of QCT was reduced, the co-amorphous technique significantly improved the concentration of RLX in drug release studies.

Citation to the base paper: K. S., N. S., Dengale, S. J., Mutalik, S., & Bhat, K. (2022). Raloxifene HCl – quercetin co-amorphous system: preparation, characterization, and investigation of its behavior in phosphate buffer. Drug Development and Industrial Pharmacy, 48(6), 227–238. https://doi.org/10.1080/03639045.2022.2104308

Publication Date: 2022

Publication Date

2022

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