A New Multi-Component Solid of Atorvastatin Calcium with a Dipicolinic Acid Coformer for Improving the Water Solubility

IF 1.4 4区管理学 Q2 ENGINEERING, MULTIDISCIPLINARY International Journal of Technology Management Pub Date : 2023-05-09 DOI:10.14716/ijtech.v14i3.5088

Yudi Wicaksono, A. S. Nugraha, E. Irawan, Nadifa Nada, Sofyan Dimas Nurhansyah

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Abstract

. Atorvastatin calcium is a potent active pharmaceutical ingredient that reduces blood cholesterol levels. However, oral bioavailability is low because it is difficult to dissolve in water. Therefore, further research to increase the solubility of the drug is needed to improve its bioavailability properties. This research aimed to increase the solubility of atorvastatin calcium through the formation of a multi-component solid. Furthermore, the drug was formed into a multi-component solid with dipicolinic acid as a coformer using the solvent evaporation-quenching method. A powder X-ray diffractometer (PXRD), Fourier transform infrared (FTIR) spectrometer, differential scanning calorimeter (DSC), and scanning electron microscope (SEM) was used to characterize the solid. Also, the shake-flask method was used to analyze the solubility of the solid in distilled water. The results showed that atorvastatin calcium and dipicolinic acid formed a new multi-component solid of cocrystal type. The solubility of the atorvastatin calcium from the multi-component solid was 344.31 ± 37.09 mg/L, which was a significant increase of about 2.7-fold compared to the pure form.

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具有二吡啶酸共构象的新型阿托伐他汀钙多组分固体的水溶性改善

．阿托伐他汀钙是一种有效的活性药物成分，可以降低血液中的胆固醇水平。然而，口服生物利用度低，因为它很难溶于水。因此，需要进一步研究提高药物的溶解度，以提高其生物利用度。本研究旨在通过形成多组分固体来提高阿托伐他汀钙的溶解度。采用溶剂蒸发-猝灭法将药物以二吡啶酸为共体形成多组分固体。采用粉末x射线衍射仪(PXRD)、傅里叶变换红外光谱仪(FTIR)、差示扫描量热仪(DSC)和扫描电子显微镜(SEM)对固体进行了表征。用摇瓶法测定了固体在蒸馏水中的溶解度。结果表明，阿托伐他汀钙与二吡啶酸形成了一种新型的多组分共晶型固体。多组分固体中阿托伐他汀钙的溶解度为344.31±37.09 mg/L，较纯形式显著提高约2.7倍。

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来源期刊

International Journal of Technology Management 管理科学-工程：综合

CiteScore

2.70

自引率

3.60%

发文量

审稿时长

6-12 weeks

期刊介绍： The IJTM aims to provide a refereed and authoritative source of information in the field of managing with technology, and the management of engineering, science and technology. It seeks to establish channels of communication between government departments, technology executives in industry, commerce and related business, and academic experts in the field.