Amorphous solid dispersion formulation of pimobendan for bioavailability enhancement: A comprehensive study on miscibility, interactions, and in vitro dissolution behavior

IF 4.5 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology Pub Date : 2025-04-03 DOI:10.1016/j.jddst.2025.106884

Beibei Qu , Hengqian Wu , Zhuang Ding , Rupeng Bu , Heng Zhang , Jun Han , Mingzhong Li , Zhengping Wang

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引用次数: 0

Abstract

Amorphous solid dispersions (ASDs) of poorly soluble pimobendan (PIMO) in cellulose matrices, including hydroxypropyl methylcellulose acetate succinate (HPMCAS-HG, HPMCAS-MG, HPMCAS-LG), polyvinylpyrrolidone-vinyl acetate (PVPVA64), and polyvinylpyrrolidone (PVPK30), were investigated, aiming to identify the optimal polymer to enhance its solubility and stability of the drug product. The results indicated that the miscibility between PIMO and the selected polymers can be predicted by Hansen solubility parameters and Flory-Huggins interaction parameters, with the ranking order of PVPVA64 > PVPK30 > HPMCAS. Fourier transform infrared (FTIR) spectroscopy analysis revealed significant interactions between PIMO and these polymers. Recrystallization inhibition and dissolution performance were ranked as HPMCAS-HG > HPMCAS-MG > HPMCAS-LG > PVPK30 > PVPVA64. Additionally, the results also indicated that HPMCAS-HG had superior stability compared to PVPVA64 and PVPK30 under elevated humidity, as confirmed by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) analysis. These findings provide a theoretical basis for selection of the optimal polymer for design of PIMO ASDs.

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来源期刊

Journal of Drug Delivery Science and Technology 医学-药学

CiteScore

8.00

自引率

8.00%

发文量

879

审稿时长

94 days

期刊介绍： The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.